Class / Patent application number | Description | Number of patent applications / Date published |
514263220 | The additional hetero ring is six-membered consisting of one nitrogen and five carbons | 70 |
20080207648 | Organic Compounds - Compounds of formula I | 08-28-2008 |
20080242683 | Organic Compounds - Compounds of (I) | 10-02-2008 |
20080255159 | 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula | 10-16-2008 |
20080262001 | AGONISTS OF A2A ADENOSINE RECEPTORS FOR TREATING RECURRENT TUMOR GROWTH IN THE LIVER FOLLOWING RESECTION - The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A | 10-23-2008 |
20090099213 | Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR | 04-16-2009 |
20090099214 | Organic Compounds - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 04-16-2009 |
20090118309 | Selective antagonists of A2A adenosine receptors - The present invention provides compounds of formulae Ia and Ib: | 05-07-2009 |
20090143413 | Thiazole Derivatives as CXCR3 Receptor Modulators - The invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, which are antagonist of the CXCR3 chemokine receptor useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed. | 06-04-2009 |
20090149480 | METHODS OF USING PDE V INHIBITORS FOR THE TREATMENT OF CONGESTIVE HEART FAILURE - The uses of PDE V inhibitors in methods for the treatment of congestive heart failure and other physiological disorders, as a monotherapy and in combination with other active agents are disclosed. Such PDE V inhibitors include those having the formula (I), with the variables defined herein: | 06-11-2009 |
20090209561 | Xanthine Derivatives with HM74A Receptor Activity - The present invention relates to therapeutically active xanthine compound derivatives, corresponding pharmaceutical formulations containing, processes for making or manufacture and the use of the aforementioned compounds in therapy, particularly in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial. | 08-20-2009 |
20090253718 | Pharmaceutical Compounds - The invention provides a compound having the formula (I): | 10-08-2009 |
20090270427 | PURINE DERIVATIVES - The present invention relates to compounds of formula 1 | 10-29-2009 |
20090318476 | Azacycloalkane Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I). | 12-24-2009 |
20090325983 | NEW PURINE DERIVATIVES - The present invention relates to compounds of formula 1 | 12-31-2009 |
20100016340 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds of the formula (I): | 01-21-2010 |
20100075995 | COMPOUNDS - Compounds of formula (I): | 03-25-2010 |
20100093769 | COMPOUNDS - The present invention relates to compounds of formula (I) | 04-15-2010 |
20100105705 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 04-29-2010 |
20100105706 | METHOD OF PREVENTING AND TREATING AIRWAY REMODELING AND PULMONARY INFLAMMATION USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The present invention relates to methods of preventing airway remodeling using A | 04-29-2010 |
20100120798 | SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY - The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R)x N * (GP1) (2) GP is a group GP2: 10 (R)r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims | 05-13-2010 |
20100173916 | Xanthine Derivatives, the Preparation Thereof and Their Use as Pharmaceutical Compositions - The present invention relates to substituted xanthines of general formula | 07-08-2010 |
20100204249 | SECRETORY PHOSPHOLIPASE A2 (SPLA2) INHIBITOR AND NIACIN DRUG COMPOSITIONS AND METHODS FOR TREATING CARDIOVASCULAR DISEASE AND DYSLIPIDEMIA - Niacin drugs are frequently utilized as a therapeutic to treat CVD, increase HDL levels, and/or decrease TG levels. As disclosed herein, it has been found that administration of one or more sPLA | 08-12-2010 |
20100204250 | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula | 08-12-2010 |
20100240680 | Purine derivatives as a2a agonists - Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R | 09-23-2010 |
20100292255 | Therapeutic Compounds and Their Use in Treating Diseases and Disorders - The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders, such as cancer. | 11-18-2010 |
20100311768 | USE OF PURINE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT - The invention relates to the use of purine derivatives in the manufacture of a medicament for treating pathological conditions in which an imbalance between cell division and apoptosis is involved, and more particularly in which excessive apoptosis is responsible for the pathological condition. According to the invention, a purine derivative of formula I is used. The invention finds use in the pharmaceutical field. | 12-09-2010 |
20110086868 | SPECIFIC INHIBITORS FOR VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTORS - The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR. | 04-14-2011 |
20110144136 | NOVEL ADENINE DERIVATIVES - The present invention relates to compounds of formula (I): | 06-16-2011 |
20110152296 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 06-23-2011 |
20110190319 | SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused derivatives of Formula I: | 08-04-2011 |
20110201629 | CYCLOHEXYL AMIDE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS - There are described cyclohexyl amide derivatives of Formula I, | 08-18-2011 |
20110201630 | Fused Pyridine Derivatives as Kinase Inhibitors - A series of heteroaryl-substituted fused pyridine derivatives, in particular heteroaryl-substituted thieno[3,2-6]pyridine derivatives, being selective inhibitors of PO kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. | 08-18-2011 |
20110312979 | FUSED PYRROLE DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused pyrrole derivatives of Formula I: | 12-22-2011 |
20110319433 | FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREATMENT OF INFLAMMATION - Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists. | 12-29-2011 |
20120004247 | ORGANIC COMPOUNDS - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 01-05-2012 |
20120035192 | SELECTIVE ANTAGONISTS OF A2A ADENOSINE RECEPTORS - The present invention provides compounds of formulae Ia and Ib: | 02-09-2012 |
20120035193 | 6-AMINO-PURIN-8-ONE COMPOUNDS - Compounds of formula (I): | 02-09-2012 |
20120142712 | 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES, THEIR PREPARATION, AND THEIR USE AS PHARMACEUTICALS - The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof. | 06-07-2012 |
20120184568 | PROCESSES FOR PREPARING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES - Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof. | 07-19-2012 |
20120184569 | A3 ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS - Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V): | 07-19-2012 |
20120258974 | USE OF A2B ADENOSINE RECEPTOR ANTAGONISTS FOR TREATING HEART FAILURE AND ARRHYTHMIA IN POST-MYOCARDIAL INFARCTION PATIENTS - Provided are methods of improving the cardiac condition of post-myocardial infarction (MI) patients and reducing cardiovascular death and hospitalization due to heart failure or arrhythmias, by administering a therapeutically effective amount of an A | 10-11-2012 |
20120277257 | Methods of Treating Diseases, Pharmaceutical Compositions, and Pharmaceutical Dosage Forms - Disclosed herein are methods of treating diseases and disorders responsive to inhibition of Hsp90, pharmaceutical compositions, pharmaceutical dosage forms and medicaments useful for the treatment of diseases responsive to inhibition of Hsp90, and methods of making the pharmaceutical compositions, pharmaceutical dosage forms and medicaments. | 11-01-2012 |
20120309774 | SELECTIVE ANTAGONISTS OF A2A ADENOSINE RECEPTORS - The present invention provides compounds of formulae Ia and Ib: | 12-06-2012 |
20130005748 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof. | 01-03-2013 |
20130012526 | OXAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH - The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease. | 01-10-2013 |
20130053406 | THERAPEUTIC COMPOUNDS AND USES THEREOF - The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer. | 02-28-2013 |
20130059869 | METHODS AND COMPOSITIONS FOR TREATING DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 03-07-2013 |
20130072504 | CRYSTALLINE FORMS OF A PURINE DERIVATIVE - The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. | 03-21-2013 |
20130085151 | HETEROCYCLIC COMPOUNDS AND THEIR USES - Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 04-04-2013 |
20130109704 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS | 05-02-2013 |
20130197014 | PURINONE 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. | 08-01-2013 |
20130324562 | FUSED BICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS - The present invention is directed to novel bicyclic heterocycles 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. | 12-05-2013 |
20130338174 | PURINE DERIVATIVES - The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy. | 12-19-2013 |
20140024664 | NOVEL ADENINE DERIVATIVES - Compounds of formula (I): | 01-23-2014 |
20140100237 | FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREATMENT OF INFLAMMATION - Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists. | 04-10-2014 |
20140275127 | SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS - The present invention provides fused derivatives of Formula I: | 09-18-2014 |
20140288099 | COMPOSITION - Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma. | 09-25-2014 |
20140296261 | KINASE MODULATING COMPOUNDS, COMPOSITIONS CONTAINING THE SAME AND USE THEREOF - The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition. | 10-02-2014 |
20150011569 | NOVEL P13K p110 INHIBITORS AND METHODS OF USE THEREOF - The invention includes compositions that regulated PI3K p110 delta and are useful as an anti-viral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-viral therapeutic approach for treating a viral infection, for example influenza. The invention includes a method of modulating PI3K p110 delta in a cell infected with a virus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta. | 01-08-2015 |
20150025090 | SUBSTITUTED AZABICYCLES AND USE THEREOF - The present application relates to novel substituted azabicycles, 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. | 01-22-2015 |
20150087660 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF CHRONIC DISEASES AND INFLAMMATORY DISORDERS - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of chronic diseases and inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of intermittent claudication, obstructed arteries in the limbs, vascular dementia, Peyronie's disease, neuropathic injuries, sickle cell disease, nausea and headaches in the mountains (altitude sickness), acute alcoholic and non-alcoholic steatohepatitis, alcoholic liver disease, fibrotic lesions induced by radiation therapy for cancer, cytokine release syndrome, endometriosis, venous disease, inflammation, cancer, stroke, thrombosis, sepsis, gangrene, infection, type 1 diabetes, type 2 diabetes, pancreatic beta cell degeneration, beta cell dysfunction, respiratory diseases, rheumatoid arthritis, arthritis, osteoarthritis and vascular disease. | 03-26-2015 |
20150148354 | CRYSTALLINE FORMS OF A PURINE DERIVATIVE - The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms. | 05-28-2015 |
20150291627 | 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted xanthines of general formula | 10-15-2015 |
20150368247 | 2,6,7 SUBSTITUTED PURINES AS HDM2 INHIBITORS - The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt 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. | 12-24-2015 |
20150368248 | 2-SUBSTITUTED-6-BIARYLMETHYLAMINO-9-CYCLOPENTYL-9H-PURINE DERIVATIVES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS - This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines. | 12-24-2015 |
20160000798 | USES OF DPP IV INHIBITORS - The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments. | 01-07-2016 |
20160031886 | CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein. | 02-04-2016 |
20160096841 | SUBSTITUTED AMINOPURINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are Aminopurine Compounds having the following structures: | 04-07-2016 |
20160152619 | PROCESSES FOR PREPARING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES | 06-02-2016 |
20160194327 | 8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS | 07-07-2016 |