Entries |
Document | Title | Date |
20080214583 | 7H-Pyrrolo[2,3-D]Pyrimidine Derivatives, As Well As Their Therapeutically Acceptable Salts, Pharmaceutical Preparations Containing Them And Process For Production The Active Agent - The invention relates to new 7H-pyrrolo[2,3-d]pyrimidine derivatives, as well as their therapeutically acceptable salts, pharmaceutical preparations containing them and process for producing the active agent. The pharmaceutical preparation is adventageously antiphlogistic and analgetic one, a preparation reducing neuropathic hyperalgesia and rheumatic arthritis, a preparation for hindering destruction of bones chondrus, being applicable for treatment of other diseases, which may be connected with other inflammatory processes e.g. asthma, eczema or psoriasis. | 09-04-2008 |
20080214584 | Method for treating cancer - The present invention provides a method for treating cancer, which includes selecting a patient coexpressing HER2 and HER3, and administering an effective amount of a HER2 inhibitor to the patient. | 09-04-2008 |
20080214585 | NEW CLASSICAL ANTIFOLATES - The present invention is directed to antifolate compounds having the structure | 09-04-2008 |
20080221135 | COMBINATION THERAPY - This invention relates to a combination of anti-cancer compounds which comprises a) an orally effective taxane, and b) a thymidylate synthase inhibitor, and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use. | 09-11-2008 |
20080221136 | Novel Pyrrolo [3,2-D]Pyrimidin-4-One Derivatives And Their Use In Therapy - There are disclosed novel compounds of formula (I) wherein R | 09-11-2008 |
20080234298 | ANTIFOLATE AGENT COMBINATIONS IN THE TREATMENT OF CANCER - Compositions and methods useful in the treatment of certain cancers. The methods include administering, to a patient receiving an antifolate anticancer agent, methoxyamine administered in an amount sufficient to enhance or increase the effect of the antifolate anticancer agent. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents. | 09-25-2008 |
20080242685 | Chemical Compounds - The invention is directed to novel azaindole and azaindazole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): | 10-02-2008 |
20080262004 | Tgf-Beta Inhibitors - The present invention is directed to inhibitors of TGF-β of Formula I: | 10-23-2008 |
20080269261 | Combination of Zd6474 and Pemetrexed - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with pemetrexed; to a pharmaceutical composition comprising ZD6474 and pemetrexed; to a combination product comprising ZD6474 and pemetrexed for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and pemetrexed; to the use of ZD6474 and pemetrexed in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 10-30-2008 |
20080280928 | Pyrrolopyrimidine and Pyrrolopyridine Derivatives Substituted with a Cyclic Amino Group As Crf Antagonists - [PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc.
| 11-13-2008 |
20080306094 | Combination of Azd2171 and Pemetrexed - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with pemetrexed; to a pharmaceutical composition comprising AZD2171 and pemetrexed; to a combination product comprising AZD2171 and pemetrexed for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and pemetrexed; to the use of AZD2171 and pemetrexed in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 12-11-2008 |
20080312258 | METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides active metablites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-18-2008 |
20080312259 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-18-2008 |
20090012104 | Inhibitors of 5'-Methylthioadenosine Phosphorylase and 5'-Methylthioadenosine/S-Adenosylhomocysteine Nucleosidase - Described are compounds of the general formula (I), VI and (VII). Also described are pharmaceutical compositions comprising the compounds identified. The compounds and pharmaceutical compositions described are inhibitors of 5′-methylthioadenosine/S-adenosylhomocystein nucleosidase (MTAN) and/or 5′-methylthioadenosine phosphorylase (MTAP). Methods of treatment using the compounds and pharmaceutical compositions described are also provided for preventing and/or treating disease states and/or conditions by inhibiting MTAN and/or MTAP in patients. | 01-08-2009 |
20090012105 | Combination of Mtor Inhibitor and Antipolate Compound - Use of a combination of an mTOR inhibitor and an antifolate compound. | 01-08-2009 |
20090023757 | PROCESS FOR PREPARING BICYCLIC COMPOUNDS - The present invention relates to a novel process for preparing compounds of formula (IA), which are potent and specific antagonists of corticotropin-releasing factor (CRF) receptors, from intermediate compounds of formula (I), by a coupling reaction catalysed by copper. | 01-22-2009 |
20090069349 | DEUTERIUM-ENRICHED PEMETREXED - The present application describes deuterium-enriched pemetrexed, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090082369 | Pyrrolo[2,3d]pyrimidine compositions and their use - This invention pertains to compounds having the structure: | 03-26-2009 |
20090082370 | Pharmaceutical Combinations of PK Inhibitors and Other Active Agents - The invention provides a combination for use as a protein kinase B inhibitor, the combination comprising (or consisting essentially of) an ancillary compound and: (I) a compound of the formula: or salts, solvates, tautomers or N-oxides thereof, wherein R | 03-26-2009 |
20090088445 | Deazapurines useful as inhibitors of Janus kinases - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 04-02-2009 |
20090105284 | Aminocyclohexanes as Dipeptidyl Peptidase-IV for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 04-23-2009 |
20090124640 | Pyrrolo[3,2-D]Pyrimidin-4-One Derivative as Myeloperoxidase Inhibitor - The present invention relates to a new compound A: [Chemical formula should be inserted here. Please see paper copy] a process for its preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said active compound in therapy. The compound is an inhibitor of the enzyme MPO and is thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardiovascular disorders and respiratory disorders. | 05-14-2009 |
20090149483 | BICYCLIC PYRROLE DERIVATIVES - Compounds represented by the general formula (I), prodrugs thereof, or pharmaceutically acceptable salts of both are provided as compounds which have high DPP-IV inhibiting activity and are improved in safety, toxicity and so on: (I) | 06-11-2009 |
20090163523 | Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor - The invention provides a pharmaceutical combination comprising: a) at least one S1P receptor agonist, and b) at least one JAK3 kinase inhibitor and a method for treating or preventing autoimmune diseases or cell, tissue or organ graft rejection using such a combination. | 06-25-2009 |
20090163524 | Novel Protein Kinase B Inhibitors - 060 - The invention relates to a novel group of compounds of Formula (I) or salts thereof: | 06-25-2009 |
20090192177 | 2-ARYL pyrrologpyrimidines for A1 and A3 receptors - This invention pertains to compounds which specifically inhibit the adenosine A | 07-30-2009 |
20090203717 | FUSED HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula: | 08-13-2009 |
20090221614 | SELECTIVE SERINE/THREONINE KINASE INHIBITORS - Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue. | 09-03-2009 |
20090221615 | COMBINATION ANTI-CANCER AGENTS - The present disclosure relates to methods of treating cancer in mammals by administration of Lucanthone and at least one anti-metabolite. Pharmaceutical compositions and kits comprising Lucanthone and at least one anti-metabolite also are disclosed. | 09-03-2009 |
20090233948 | Inhibitors of nucleoside phosphorylases and nucleosidases - The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 09-17-2009 |
20090247558 | USE OF THE CRH (CORTICOTROPIN RELEASING HORMONE) - UCN (UROCORTIN) SYSTEM IN THE TREATMENT OF INFLAMMATORY DISEASES - The invention relates to the use of corticotropin-releasing hormone (CRH) receptor-1 (R1) antagonists and/or CRH-R2 receptor agonists for the treatment of inflammatory diseases via regulation of monocyte/macrophage cell activation, proliferation, differentiation, apoptosis, and inflammatory cytokine production. As CRH system we define natural and synthetic CRH and urocortin (UCN) agonists and antagonists for the CRH-R1 and CRH-R2 receptors and their subtypes as well as the CRH-binding protein (BP), a CRH pseudo-receptor. The invention is directed towards pharmacological intervention for the amelioration or treatment of inflammatory diseases using the CRH system-mediated control of monocyte/macrophage cells which play a key role in initiating and maintaining the inflammatory response via production of pro-inflammatory cytokines such as is the interleukin (IL)-1, IL-6 and tumor necrosis factor (TNF)-alpha. By the term inflammation we define the response of an organism to noxious endogenous or exogenous stimuli causing tissue injury. Inflammation is a host defence mechanism, which might harm the defending organism. The invention also provides methods for the in vitro and in vivo evaluation of natural and synthetic CRH system modulators for the control of the monocyte/macrophage system. | 10-01-2009 |
20090264450 | LIMK2 INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE - Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use. Particular compounds are of the formula: | 10-22-2009 |
20090270431 | Cyclopentenol Nucleoside Compounds Intermediates for their Synthesis and Methods of Treating Viral Infections - The present invention relates to compounds according to the structure (I), Where B is formula (Ia), formula (Ib) or formula (Ic); A is H, OR | 10-29-2009 |
20090306100 | METHODS OF TREATING SCHIZOPHRENIA - This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia. | 12-10-2009 |
20090318477 | CHEMICAL COMPOUNDS - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly Type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds. | 12-24-2009 |
20090325986 | Deazapurine Analogs of 1'-Aza-L-Nucleosides - The invention relates to compounds of the formula (I), which are L-enantiomeric forms of nucleoside analogues, and to pharmaceutical compositions containing the compounds, methods of treating certain diseases, including cancer, bacterial infection, parasitic infection, and T-cell mediated diseases, using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds. | 12-31-2009 |
20100022564 | PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS - The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR | 01-28-2010 |
20100035903 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - A compound of the formula | 02-11-2010 |
20100041681 | 2-AMINO PYRIMIDINE COMPOUNDS AS POTENT HSP-90 INHIBITORS - The present invention is directed to compounds of formula (I), | 02-18-2010 |
20100063072 | SOLID FORMS OF PEMETREXED - Duplex coating schemes and associated methods of formation, including a siloxane-based soft coating and a plasma-based SiO | 03-11-2010 |
20100069411 | CANCER TREATMENT METHOD - The present invention relates to a method of treating cancer in a mammal by administration of 4-quinazolinamines and at least one additional anti-neoplastic compound. In particular, the method relates to a methods of treating cancers by administration of N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine and salts and solvates thereof in combination with at least one additional anti-neoplastic compound. | 03-18-2010 |
20100075996 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein is pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 03-25-2010 |
20100081676 | SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME - Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: | 04-01-2010 |
20100093772 | QUINAZOLINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOCYTHEMIA - A method for the treatment of thrombocythemia in a subject comprising administering a therapeutically effective amount of compounds having the formulas (I) through (III) or equilibrating forms thereof. | 04-15-2010 |
20100105708 | PYRROLOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS - The present invention relates to novel pyrrolopyrimidine compounds of the general formula (1) and pharmaceutical compositions comprising said pyrrolopyrimidine compounds. Moreover, the present invention relates to the use of the pyrrolopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof. | 04-29-2010 |
20100120801 | AKT AND P70 S6 KINASE INHIBITORS - The present invention provides AKT and p70 S6 kinase inhibitors of the formula: | 05-13-2010 |
20100144765 | 5,6-TRIMETHYLENEPYRIMIDIN-4-ONE COMPOUNDS - Pyrimidone compounds of formula (I): | 06-10-2010 |
20100160356 | NOVEL CYCLOBUTYL COMPOUNDS AS KINASE INHIBITORS - The invention relates to compounds of the formula I, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the formation or course of which protein kinases are involved. | 06-24-2010 |
20100168141 | AZETIDINE ANALOGUES NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS - Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH | 07-01-2010 |
20100222370 | Methods of Treating Cancer - The invention relates to the treatment of cancer using an inhibitor of 5′-methylthioadenosine phosphorylase (MTAP). The invention particularly relates to the treatment of prostate cancer and head and neck cancer. | 09-02-2010 |
20100234403 | Aminotetrahydropyrans as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 09-16-2010 |
20100267751 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS - Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. Jak3 inhibitors useful for treating eye disorders include the compound 3-{(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile. | 10-21-2010 |
20100280053 | CyclopropylmethYl-[7-(5,7-dimethyl-benzo[1,2,5]thiodiazol-4-yl)-2,5,6-trim- ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-4-propyl-amine as a CRF Antagonist - The present invention relates to a novel benzothiadiazole of formula (A) in free base or acid addition salt form, its preparation, its use as pharmaceutical and pharmaceutical compositions containing the compound. | 11-04-2010 |
20100298355 | 3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANE-NITRILE AS JAK INHIBITORS - The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases. | 11-25-2010 |
20100305143 | PYRROLOPYRIMIDINE COMPOUNDS - Compounds of formula (I) are A | 12-02-2010 |
20100331350 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 12-30-2010 |
20110009433 | BICYCLIC PYRROLE COMPOUND - Disclosed is a compound composed of an easily-handleable crystal form and having storage stability that is practical enough to be used as an active ingredient of a pharmaceutical product. Specifically disclosed is 6-[(3R)-3-aminopiperidin-1-yl]-5-(2-chloro-5-fluorobenzyl)-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione monohydro chloride hemihydrate. | 01-13-2011 |
20110021543 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS PESTICIDES - Novel N-aryl substituted heteroindole compounds, processes for their manufacture, veterinary compositions containing such compounds, and methods of controlling ectoparasites are provided. The compounds are believed effective in the control of ectoparasites on warm-blooded productive livestock and domestic animals. | 01-27-2011 |
20110021544 | HYDROCHLORIDE SALT OF ((1S,2S,4R)-4--2-HYDROXYCYCLOPENTYL)METHYL SULFAMATE - Disclosed is a compound of formula (I): | 01-27-2011 |
20110046167 | ACYCLIC AMINE INHIBITORS OF 5-METHYTIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE - The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds. | 02-24-2011 |
20110053962 | AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYL-CHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION - Azaindole derivatives of formula (I): | 03-03-2011 |
20110059996 | NOVEL PYRROLO [3, 2-D] PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE IN THERAPY - There are disclosed novel compounds of formula (I) | 03-10-2011 |
20110082159 | METABOLITES OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYL- PROPANENITRILE - The present invention provides active metabolites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 04-07-2011 |
20110130412 | Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases - The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 06-02-2011 |
20110166167 | BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I). | 07-07-2011 |
20110172255 | Condensed N-Heterocyclic Compounds and their Use as CRF Receptor Antagonists - The present invention provides compounds of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF). | 07-14-2011 |
20110190320 | Compositions for Treating or Delaying the Onset of Hair Loss - Disclosed herein are novel methods and compositions for treating and/or preventing hair loss in patients. Specifically exemplified herein are compositions containing a modified pyrimidine that are topically applied to a scalp of an patient. Typically, the patient has androgenic alopecia, alopecia greata, postpartum alopecia or telogen effluvium. | 08-04-2011 |
20110201631 | PHARMACEUTICAL FORMULATIONS COMPRISING PEMETREXED - Pharmaceutical formulations comprising amorphous pemetrexed or its salts, and processes to prepare the formulations. | 08-18-2011 |
20110207754 | CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS - The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders. | 08-25-2011 |
20110207755 | USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection. | 08-25-2011 |
20110212978 | Combination of ZD6474 and Pemetrexed - The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with pemetrexed; to a pharmaceutical composition comprising ZD6474 and pemetrexed; to a combination product comprising ZD6474 and pemetrexed for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and pemetrexed; to the use of ZD6474 and pemetrexed in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation. | 09-01-2011 |
20110218210 | COMPOUNDS FOR TREATING ABNORMAL CELLULAR PROLIFERATION - Provided herein are compounds, compositions and methods for treating disorders mediated by abnormal cellular proliferation and processes for identifying such compounds. | 09-08-2011 |
20110218211 | AZAINDOLE INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: I wherein X | 09-08-2011 |
20110224239 | Combinations Comprising a S1P Receptor Agonist and a JAK3 Kinase Inhibitor - The invention provides a pharmaceutical combination comprising: a) at least one S1P receptor agonist, and b) at least one JAK3 kinase inhibitor and a method for treating or preventing autoimmune diseases or cell, tissue or organ graft rejection using such a combination. | 09-15-2011 |
20110251219 | TREATMENT FOR GLOMERULONEPHRITIS WITH 2-[4-(7-ETHYL-5H-PYRROLO[2,3-B]PYRAZIN-6-YL)PHENYL]PROPAN-2-OL - A treatment for glomerulonephritis, and other renal dysfunctions using a compound of Formula I is disclosed. | 10-13-2011 |
20110257208 | COMPOUNDS USEFUL AS FAAH MODULATORS AND USES THEREOF - Compounds are disclosed that have formula I: where A, B, L | 10-20-2011 |
20110288107 | TOPICAL FORMULATION FOR A JAK INHIBITOR - This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders. | 11-24-2011 |
20120046306 | Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists - There are provided compounds of the general formula | 02-23-2012 |
20120077828 | CHEMICAL COMPOUNDS - The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: | 03-29-2012 |
20120115892 | ADMINISTRATION OF NEDD8-ACTIVATING ENZYME INHIBITOR - Disclosed are methods for the treatment of patients with diseases, disorders or conditions responsive to the inhibition of NAE (Nedd8-activating enzyme), e.g., cancer. The methods comprise administering a clinically effective amount of the NAE-inhibitor ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) according to an intermittent dosing regimen in which there is a rest period of at least two days between each administration. | 05-10-2012 |
20120122898 | SOLID FORMS OF 3-(4-(AMINOMETHYL)-1-(5-METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PIPERIDINE- -4-CARBOXAMIDO)PHENYL DIMETHYLCARBAMATE - Solid forms of 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate and salts thereof are disclosed. Methods of its use to treat diseases and disorders of the eye are also disclosed. | 05-17-2012 |
20120122899 | PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 05-17-2012 |
20120122900 | PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 05-17-2012 |
20120122901 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein is pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 05-17-2012 |
20120136013 | ORGANIC COMPOUNDS - Optionally substituted (5- or 7-amino)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(6H)-ones, Compounds of Formula I, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. | 05-31-2012 |
20120149721 | METHYLPYRROLOPYRIMIDINECARBOXAMIDES - The compounds of Formula (I), | 06-14-2012 |
20120157479 | 3-HYDROXYPYRROLIDINE INHIBITORS OF 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE - The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds. | 06-21-2012 |
20120252825 | BENEFICIAL EFFECTS OF COMBINATION THERAPY ON CHOLESTEROL - The present invention discloses pharmaceutical combination therapies for the treatment or prevention of diseases in a mammal comprising a Janus Kinase inhibitor or a pharmaceutically acceptable salt thereof and a HMG-CoA reductase inhibitor or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions containing the same and kits for achieving a therapeutic effect in a mammal comprising pharmaceutical combination therapies are further described. | 10-04-2012 |
20120258976 | CRYSTALLINE PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - The present invention discloses novel crystalline and non-crystalline forms of 3-((3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-pip-eridin-1-yl)-3-oxopropionitrile, pharmaceutical composition containing the same, preparations thereof and the uses thereof. | 10-11-2012 |
20120258977 | INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 10-11-2012 |
20120295925 | SUBSTITUTED DERIVATIVES OF BICYCLIC [4.3.0] HETEROARYL COMPOUNDS - This invention relates to novel compounds of the Formula A, B, or C, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier. | 11-22-2012 |
20120295926 | SELECTIVE PROTON COUPLED FOLATE TRANSPORTER AND FOLATE RECEPTOR, AND GARFTASE INHIBITOR COMPOUNDS AND METHODS OF USING THE SAME - Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: | 11-22-2012 |
20120295927 | METHODS OF USING SELECTIVE CHEMOTHERAPEUTIC AGENTS FOR TARGETING TUMOR CELLS - A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor. | 11-22-2012 |
20120309776 | PYRROLO[2,3-D]PYRIMIDINE UREA COMPOUNDS AS JAK INHIBITORS - The present invention provides pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 12-06-2012 |
20120316186 | DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 12-13-2012 |
20120329818 | LIMK2 INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE - Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use. Particular compounds are of the formula: | 12-27-2012 |
20120329819 | NEW CRYSTALLINE FORM OF PEMETREXED DISODIUM - The present invention relates to a new polymorphic or crystalline form of Pemetrexed Disodium, processes for its preparation and its use, in particular for the preparation of medicaments. | 12-27-2012 |
20130012527 | PREQ1 RIBOSWITCHES AND METHODS AND COMPOSITIONS FOR USE OF AND WITH PREQ1 RIBOSWITCHES | 01-10-2013 |
20130040973 | JAK PI3K/mTOR COMBINATION THERAPY - Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy. | 02-14-2013 |
20130040974 | PIPERIDINE INHIBITORS OF JANUS KINASE 3 - The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof. | 02-14-2013 |
20130053407 | PYRROLO [3,2-D] PYRIMIDIN-3-YL DERIVATIVES USED AS ACTIVATORS OF AMPK - Pyrrolopyrimidones compounds of the formula (I), salts thereof, and pharmaceutical compositions containing them are disclosed herein, as well as methods for their use in medicine, for instance as activators of AMPK. | 02-28-2013 |
20130059870 | USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection. | 03-07-2013 |
20130096144 | ISOINDOLINONE AND PYRROLOPYRIDINONE DERIVATIVES AS AKT INHIBITORS - The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases. | 04-18-2013 |
20130116268 | USE OF MODIFIED PYRIMIDINE COMPOUNDS TO PROMOTE STEM CELL MIGRATION AND PROLIFERATION - Disclosed herein are methods and materials for improving vision. Particularly exemplified herein are pyrimidine compounds that serve to proliferate retinal stem cells. | 05-09-2013 |
20130123284 | HETEROCYCLIC COMPOUNDS USEFUL FOR KINASE INHIBITION - Provided herein are compounds useful for kinase inhibition. | 05-16-2013 |
20130165457 | INHIBITORS OF E1 ACTIVATING ENZYMES - This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia. | 06-27-2013 |
20130178486 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein A, R | 07-11-2013 |
20130190334 | N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS - The invention provides a compound of Formula (I) Z N N O N O A1R2 R1 R3R 3 L A2 (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3,Z, A1, L and A 5 2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal. | 07-25-2013 |
20130231357 | PHARMACEUTICAL COMPOSITIONS CONTAINING PEMETREXED HAVING EXTENDED STORAGE STABILITY - Long term storage stable pemetrexed-containing liquid pharmaceutical compositions are disclosed. The compositions can include pemetrexed or pharmaceutically acceptable salts thereof; an antioxidant selected from lipoic acid, dihydrolipoic acid, methionine and mixtures thereof; a chelating agent selected from lactobionic acid, sodium citrate, tribasic and mixtures thereof; and a pharmaceutically acceptable fluid. The pH of the compositions is in a range of about 8 to about 9.5. The pemetrexed-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 227 nm, after at least about 18 months of storage at a temperature of from about 5° C. to about 25° C. Methods of preparing the formulation as well as methods of treatment of pemetrexed-susceptible diseases using the same are also disclosed. | 09-05-2013 |
20130231358 | PIPERIDINONE CARBOXAMIDE INDANE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 09-05-2013 |
20130261138 | FUSED HETEROCYCLIC INDANE CARBOXAMIDE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to fused heterocyclic indane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 10-03-2013 |
20130267541 | FUSED HETEROCYCLIC AZAINDANE CARBOXAMIDE CGRP RECEPTOR ANTAGONISTS - The present invention is directed to fused heterocyclic azaindane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved. | 10-10-2013 |
20130303557 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS - Ophthalmic compositions comprising Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. | 11-14-2013 |
20130324565 | ORGANIC COMPOUNDS - The present invention relates to optionally substituted (5- or 7-oxy)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(3H,6H)-ones, e.g., Compounds of Formula II-A′ or II-B′ as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. | 12-05-2013 |
20130331404 | Methods and Compositions for Inhibition of Polymerase - The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents. | 12-12-2013 |
20130338175 | Multi-Arm Polymeric Prodrug Conjugates of Pemetrexed-Based Compounds - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved. | 12-19-2013 |
20130345243 | 1H-PYROLLO[3,2-D]PYRIMIDINEDIONE DERIVATIVES - The present invention relates to pyrimidinedione compounds of formula (I), | 12-26-2013 |
20140005209 | Methods of Using Selective Chemotherapeutic Agents for Targeting Tumor Cells | 01-02-2014 |
20140005210 | Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors | 01-02-2014 |
20140018374 | Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 01-16-2014 |
20140066463 | SOLID FORMS OF PEMETREXED - There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof. | 03-06-2014 |
20140066464 | METHODS OF DIAGNOSING AND TREATING CANCER - A method of determining the susceptibility of a cancer in a subject to treatment with an antimetabolite includes obtaining a sample of cancer cells from the subject, measuring the level of UDG expression in the cancer cells, and comparing the measured levels of UDG expression in the cancer cells to a control level. | 03-06-2014 |
20140073657 | 3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANE-NITRILE AS JAK INHIBITORS - The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases. | 03-13-2014 |
20140088123 | TREATMENT OF LUNG CANCER - Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed. | 03-27-2014 |
20140094476 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYL- PROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 04-03-2014 |
20140094477 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYL- PROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 04-03-2014 |
20140107137 | Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR | 04-17-2014 |
20140113919 | COMBINATION OF PANOBINOSTAT AND RUXOLITINIB IN THE TREATMENT OF CANCER SUCH AS A MYELOPROLIFERATIVE NEOPLASM - The invention relates to a combination which comprises:
| 04-24-2014 |
20140121227 | THERAPEUTIC TREATMENT - The present invention relates to a combination comprising (5)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, or a pharmaceutically acceptable salt thereof, hereafter “Compound (I)”, and a taxane. Taxanes include established cancer drugs such as docetaxel (Taxotere™) and paclitaxel (Taxol™). Such combinations may be useful in the treatment or prophylaxis of cancer. The invention also relates to a pharmaceutical composition comprising such Compound (I) and a taxane. The invention further relates to a method of treatment comprising the simultaneous, sequential or separate administration of Compound (I) and a taxane, to warm-blooded animal, such as man. The invention also relates to a kit comprising Compound (I) and a taxane, optionally with instructions for use. | 05-01-2014 |
20140135350 | SUSTAINED-RELEASE DOSAGE FORMS OF RUXOLITINIB - The present invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders. | 05-15-2014 |
20140142125 | Synthetic Rigidin Analogues as Anticancer Agents, Salts, Solvates and Prodrugs Thereof, and Method of Producing Same - A compound having the Formula I as follows: | 05-22-2014 |
20140142126 | PYRROLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 05-22-2014 |
20140163049 | Antimicrobial Compounds and Methods of Making and Using the Same - The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals. | 06-12-2014 |
20140171454 | Substituted Pyrrolo[2,3-d]pyrimidines as Inhibitors of Protein Kinases - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 06-19-2014 |
20140243360 | Heteroaryl Substituted Pyrrolo[2,3-B] Pyridines And Pyrrolo[2,3-B] Pyrimidines As Janus Kinase Inhibitors - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 08-28-2014 |
20140249167 | Administration of NEDD8-Activating Enzyme Inhibitor - Disclosed are methods for the treatment of patients with diseases, disorders or conditions responsive to the inhibition of NAE (Nedd8-activating enzyme), e.g., cancer. The methods comprise administering a clinically effective amount of the NAE-inhibitor ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) according to an intermittent dosing regimen in which there is a rest period of at least two days between each administration. | 09-04-2014 |
20140249168 | Trifluoromethyl-substituted fused pyrimidines and their use - The present application relates to novel trifluoromethyl-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 09-04-2014 |
20140303196 | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYL- PROPANENITRILE - The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 10-09-2014 |
20140315931 | DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. | 10-23-2014 |
20140336207 | PYRROLE SIX-MEMBERED HETEROARYL RING DERIVATIVE, PREPARATION METHOD THEREOF, AND MEDICINAL USES THEREOF - The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered herteroaryl ring derivative as represented by formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic method using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in the description. | 11-13-2014 |
20140378482 | Compositions and methods for potentiating immune response for the treatment of infectious diseases and cancer - Compositions and methods including at least one PNP inhibitor or at least one PNP inhibitor in combination with one or more agents identified as endogenous adjuvants useful in the treatment of pathogen infection and cancer are disclosed. The compositions may be formulated as pharmaceutical dosage forms and components may be assembled as kits. Methods for increasing levels of endogenous adjuvants to enhance an immune response and to potentiate/augment antiviral, antibacterial or anticancer effects of therapeutic agents are also disclosed. | 12-25-2014 |
20150051230 | Methods and Compositions for Inhibition of Polymerase - The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents. | 02-19-2015 |
20150073000 | STABLE READY-TO-USE PHARMACEUTICAL COMPOSITION OF PEMETREXED - A stable ready-to-use pharmaceutical composition comprising pemetrexed or pharmaceutically acceptable salts thereof, wherein the composition is free from antioxidants, amino acids and chelating agents. Also provided is a process for preparing a stable ready-to-use pharmaceutical composition comprising the steps: i) purging inert gas into a parenterally acceptable aqueous solvent until the dissolved oxygen content of the solvent comes to less than 7 mg/L, preferably less than 3 mg/L; ii) adding pemetrexed disodium under stirring; iii) adjusting the pH of the resulting solution to between 4 to 9; iv) optionally adding additional aqueous solvent; wherein the composition is purged with inert gas throughout the entire process. | 03-12-2015 |
20150073001 | METHYLPYRROLOPYRIMIDINECARBOXAMIDES - The compounds of Formula (I), | 03-12-2015 |
20150087661 | Crystalline Forms of (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]py- rimidin-4-yl) piperidine-4-carboxamide - The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy. | 03-26-2015 |
20150087662 | CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS - The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders. | 03-26-2015 |
20150099769 | PYRROLO[3,2-D]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE IN THERAPY - There are disclosed novel compounds of formula (I) | 04-09-2015 |
20150105411 | BIOMARKERS OF RESPONSE TO NAE INHIBITORS - Disclosed herein are markers whose mutational status is associated with sensitivity to treatment with NAE inhibitors. Mutational status is determined by measurement of characteristics of markers associated with the marker genes. Compositions and methods are provided to assess markers of marker genes to predict response to NAE inhibition treatment. | 04-16-2015 |
20150111905 | PHARMACEUTICAL COMPOSITIONS OF PEMETREXED - A pharmaceutical composition of Pemetrexed represented by formula (I), which is a liquid ready to use solution formulation or a lyophilized pharmaceutical composition for parenteral administration comprising a pharmaceutically acceptable organic amine, an inert gas and optionally containing at least one or more pharmaceutically acceptable excipients. Also provided are processes for preparation of the ready to use solution formulation or lyophilized pharmaceutical composition of the present invention. | 04-23-2015 |
20150111906 | Synthetic Rigidin Analogues as Anticancer Agents, Salts, Solvates and Prodrugs Thereof, and Method of Producing Same - A compound having the Formula as follows: | 04-23-2015 |
20150119410 | BIOMARKERS OF RESPONSE TO NAE INHIBITORS - Disclosed herein are markers whose mutational status is associated with sensitivity to treatment with NAE inhibitors. Mutational status is determined by measurement of characteristics of markers associated with the marker genes. Compositions and methods are provided to assess markers of marker genes to predict response to NAE inhibition treatment. | 04-30-2015 |
20150126535 | DOSING REGIMEN FOR JANUS KINASE (JAK) INHIBITORS - The present invention provides a method for treating allergic dermatitis, atopic dermatitis, or one or more symptoms thereof in a mammal in need, which method comprises administering to the mammal a first therapeutically effective dose of a Janus Kinase (JAK) inhibitor twice a day for a number of days sufficient to ease or eliminate one or more clinical signs in the mammal, followed by a second therapeutically effective dose of the JAK inhibitor at a reduced frequency. | 05-07-2015 |
20150126536 | Methods of Using Selective Chemotherapeutic Agents for Targeting Tumor Cells - A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor. | 05-07-2015 |
20150148357 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein is pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 05-28-2015 |
20150292022 | NATURAL-KILLER/T-CELL LYMPHOMA (NKTCL) SUSCEPTIBILITY PREDICTION, DIAGNOSIS AND THERAPY - Natural-Killer T-Cell Lymphoma (NKTCL) susceptibility prediction, diagnosis and therapy. The invention relates to a method for predicting Natural Killer T-cell Lymphoma (NKTCL) susceptibility and/or diagnosing NKTCL in a subject comprising testing for JAK mutations. The invention also relates to a method of screening for candidate agents capable of treating NKTCL using a cell line comprising at least one JAK mutation. The invention includes an NKTCL animal model comprising at least one JAK mutation. The invention also includes JAK inhibitors for treating NKTCL. | 10-15-2015 |
20150297598 | METHODS FOR TREATING RENAL DISEASE - The invention features methods for treating or reducing the likelihood of developing a renal disease by administering to a subject in need thereof an agent that decreases expression of a pathogenic APOL1. The agents of the method target various signaling pathways and decrease the level of the pathogenic APOL1 polypeptide. | 10-22-2015 |
20150297724 | STABILIZED PEMETREXED FORMULATION - The present invention relates to a stabilized pemetrexed formulation, and more particularly to a stabilized pemetrexed formulation comprising acetylcysteine as antioxidant and a citrate salt as buffer. | 10-22-2015 |
20150299796 | PREDICTION OF TREATMENT RESPONSE TO JAK/STAT INHIBITOR - The invention includes, in part, a method of selecting a subject having cancer for treatment with a JAK/STAT inhibitor and a method of determining if a therapeutically effective dose of a JAK/STAT inhibitor has been administered. | 10-22-2015 |
20150307497 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula | 10-29-2015 |
20150329548 | SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS - The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 11-19-2015 |
20150374701 | PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS - Described herein is pyrrolo {2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds. | 12-31-2015 |
20150376190 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein. | 12-31-2015 |
20160002267 | BENZYL-SUBSTITUTED PYRAZOLOPYRIDINES AND USE THEREOF - The present application relates to novel benzyl-substituted pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 01-07-2016 |
20160009722 | AMORPHOUS FORM OF 4-((4-(CYCLOPENTYLOXY)-5-(2-METHYLBENZO[D]OXAZOL-6-YL)-7H-PYRROLO[2,3-D]P- YRIMIDIN-2-YL)AMINO)-3-METHOXY-N-METHYLBENZAMIDE, COMPOSITIONS THEREOF AND METHODS OF THEIR USE | 01-14-2016 |
20160030432 | HYDROCHLORIDE SALT OF((1S,2S,4R)-4--2-HYDROXYCYCLOPENTYL) METHYL SULFAMATE - Disclosed is a compound of formula (I): | 02-04-2016 |
20160039830 | Substituted Pyrimidine Compounds and Methods of Use and Manufacture - This invention provides substituted pyrimidine compounds having the formula: | 02-11-2016 |
20160039831 | PYRROLO[3,2-d]PYRIMIDINE-2,4(3H,5H)-DIONE DERIVATIVES - This invention relates to novel Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione derivatives of Formula (I): | 02-11-2016 |
20160039840 | Pyrimidine Compounds and Pyrimido Indole Compounds and Methods of Use - The present invention discloses a compound comprising the formula: | 02-11-2016 |
20160051679 | Pemetrexed Formulation - The invention provides stable formulations of pemetrexed for infusion. The formulations are based on using pemetrexed diacid and certain selected suitable stabilising basic amine compounds that provide counter ions to the pemetrexed diacid, forming base addition salts. The formulations can be dried powder formulations to be reconstituted as liquid concentrate formulations or directly in ready-to-use infusion solutions, or they can be liquid formulations, most suitably concentrates to be diluted in infusion solution prior to use. The suitable basic amine addition compounds according to the invention are one or more of diethanolamine, tris-(hydroxymethyl)aminomethane and meglumine. | 02-25-2016 |
20160058767 | COMPOSITIONS AND METHODS OF INHIBITING IL-17 EXPRESSION OF NEUTROPHILS - A method of inhibiting IL-17 expression in neutrophils of a subject in need thereof includes administering to neutrophils of the subject a therapeutically effective amount of agent that inhibits STAT3 mediated IL-17 expression in the neutrophils of the subject. | 03-03-2016 |
20160060269 | DOT1L Inhibitors - Provided herein are inhibitors of DOT1L useful for treating diseases or disorders associated with DOT1L. An exemplary DOT1L inhibitor provided herein exhibits a biological half-life of 12.6 h. Methods for treating diseases associated with DOT1L are also provided. | 03-03-2016 |
20160067253 | 3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANE-NITRILE AS JAK INHIBITORS - The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases. | 03-10-2016 |
20160096824 | Heterocyclic Compounds Useful for Kinase Inhibition - Provided herein are compounds useful for kinase inhibition. | 04-07-2016 |
20160096842 | ANTI-INFLUENZA COMPOSITIONS AND METHODS - Disclosed are novel compounds comprising an imino-ribose derivative covalently linked to a carbocycle or heterocycle. Pharmaceutical compositions comprising the compounds of the invention are also described. Methods of inhibition, treatment and/or suppression of viral infections with the compounds of the invention are also described. The compositions or methods may optionally comprise one or more additional anti-viral agents. | 04-07-2016 |
20160102098 | BISULFATE OF JANUS KINASE (JAK) INHIBITOR AND PREPARATION METHOD THEREFOR - The present invention relates to a bisulfate of a Janus kinase (JAK) inhibitor and a preparation method therefor. More specifically, the present invention relates to a (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazole-5-group)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-group)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate shown in the formula (I), a preparation method therefor, and an application thereof. The bisulfate shown in the formula (I) can be well suitable as a Janus kinase (JAK) inhibitor in clinical work for treating rheumatism or rheumatoid arthritis. | 04-14-2016 |
20160120867 | STABILIZED PEMETREXED FORMULATION - The present invention relates to a stabilized pemetrexed formulation, and more specifically, to a stabilized pemetrexed formulation comprising acetylcysteine as an antioxidant and sodium citrate as a buffering agent. Additionally, the present invention relates to a pemetrexed formulation filled in a sealed container, comprising pemetrexed or a pharmaceutically acceptable salt thereof as an active ingredient, wherein the oxygen gas content within the headspace of the container is 3 v/v % or less. | 05-05-2016 |
20160143911 | STABLE AND WATER SOLUBLE PHARMACEUTICAL COMPOSITIONS COMPRISING PEMETREXED - The present invention relates to a solid pharmaceutical composition comprising pemetrexed and a solubilizing amount of meglumine or tromethamine. The composition is sufficiently stable for purpose of making pharmaceutical formulations, particularly lyophilized formulations, and is sufficiently soluble in water for purposes of using in parenteral administration. | 05-26-2016 |
20160145260 | STABLE PEMETREXED ARGININE SALT AND COMPOSITIONS COMPRISING IT - The present invention relates to arginine salt of pemetrexed of formula (1), particularly to a stable solid form thereof, and to pharmaceutical compositions comprising such salt. | 05-26-2016 |
20160151373 | COMBINATION TREATMENT OF CANCER | 06-02-2016 |
20160152623 | 1-[2-(AMINOMETHYL)BENZYL]-2-THIOXO-1,2,3,5-TETRAHYDRO-4H-PYRROLO[3,2-d]PYR- IMIDIN-4-ONES AS INHIBITORS OF MYELOPEROXIDASE | 06-02-2016 |
20160168150 | PYRROLO[3,2-D]PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND OTHER DISEASES | 06-16-2016 |
20160168153 | NOVEL CRYSTALLINE FORMS OF PEMETREXED TROMETHAMINE SALTS | 06-16-2016 |
20160375026 | PYRROLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS - Disclosed herein are methods of using pyrrolo[2,3-d]pyrimidine Btk inhibitors, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, and inflammatory diseases or conditions. | 12-29-2016 |
20190144448 | PIPERIDINYL DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | 05-16-2019 |