Class / Patent application number | Description | Number of patent applications / Date published |
544293000 | Nitrogen bonded directly at 4-position | 46 |
20090012295 | Amorphous Erlotinib, processes for the preparation thereof, and processes to prepare additional forms of Erlotinib - The present invention provides amorphous erlotinib, processes for the preparation thereof, and processes to prepare additional forms of erlotinib. | 01-08-2009 |
20090131665 | Process for the preparation of crystalline forms A, B and pure crystalline form a of erlotinib HCI - The invention provides processes for preparing crystalline Forms A, B and pure crystalline Form A of Erlotinib hydrochloride. | 05-21-2009 |
20090131666 | ACYLAMINOPIPERIDINE COMPOUND - [Problem] To provide a compound which has an excellent activity to modulate the functions of CCR4 or TARC and/or MDC and can be used for the prevention and/or treatment of various inflammatory diseases, allergic diseases, autoimmune diseases and the like.
| 05-21-2009 |
20090171083 | PROCESS FOR PRODUCING 4-AMINOQUINAZOLINE COMPOUND - A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R | 07-02-2009 |
20090203905 | CHEMICAL PROCESS - The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline. | 08-13-2009 |
20090209758 | QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 08-20-2009 |
20090281315 | FORMS OF LAPATINIB DITOSYLATE AND PROCESSES FOR PREPARATION THEREOF - The present invention provides novel polymorphs of lapatinib ditosylate, processes for preparing them, and pharmaceutical compositions comprising one or more of these polymorphs. | 11-12-2009 |
20090286982 | NOVEL SALT-554 - 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described. | 11-19-2009 |
20090306377 | NOVEL PROCESS FOR THE PREPARTION OF ERLOTINIB - The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1 | 12-10-2009 |
20090306378 | PROCESS FOR PREPARING AMINOCROTONYLAMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES - The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups R | 12-10-2009 |
20100004449 | CRYSTALLINE FORMS OF ERLOTINIB BASE AND ERLOTINIB HCL - The preparation of crystalline Erlotinib base form G2 is described. This crystalline form can be converted to an Erlotinib salt, such as Erlotinib HCl, which can be used in the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC). | 01-07-2010 |
20100094004 | Process for Preparation of Erlotinib and its Pharmaceutically Acceptable Salts - A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4˜halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. | 04-15-2010 |
20100130741 | PROCESS FOR ERLOTINIB HYDROCHLORIDE - The present invention provides an improved and commercially viable process for preparation of erlotinib substantially free of N-methoxyethyl impurity, namely N-[(3-ethynylphenyl)-(2-methoxyethyl)]-6,7-bis(2-methoxyethoxy)-4-quinazolinamine, and its pharmaceutically acceptable acid addition salts thereof in High purity and in high yield. According to the present invention, erlotinib or a pharmaceutically acceptable acid addition salt of erlotinib substantially free of N-methoxyethyl impurity is prepared by isolating erlotinib or a pharmaceutically acceptable salt of erlotinib from a solvent medium comprising dimethyl sulfoxide and an alcoholic solvent. | 05-27-2010 |
20100174074 | NOVEL BENZOPHENONE HYBRIDS AS POTENTIAL ANTICANCER AGENTS AND A PROCESS FOR THE PREPARATION THEREOF - Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same. | 07-08-2010 |
20100197915 | LAPATINIB INTERMEDIATES - The invention provides lapatinib intermediates and improved processes for preparing lapatinib intermediates. The invention also provides processes for preparing lapatinib base and lapatinib ditosylate. | 08-05-2010 |
20110207932 | Process for preparing aminocrotonylamino-substituted quinazoline derivatives - The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) | 08-25-2011 |
20110245496 | Quinazoline Salt Compounds - Salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity. | 10-06-2011 |
20110263852 | NOVEL PROCESS FOR THE PREPARATION OF LAPATINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS - The present invention relates to an improved and novel process for the preparation of high purity crystalline base of Lapatinib of formula-(1) having chemical name N-{3-chloro-4-[(3-fluorobenzyloxy]phenyl}-6-[5-({[2-(methanesulfonyl)ethyl]amino}methyl]-2-furyl]-4-quin-azolinamine and its pharmaceutically acceptable salts. The present invention further relates to intermediates according to formula (8) and formula (9) used in this process | 10-27-2011 |
20110295004 | QUINAZOLINE BASED EGFR INHIBITORS - The present invention relates to quinazoline containing zinc-binding moiety based derivatives of formula I that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. | 12-01-2011 |
20120022256 | Novel Hydrated Form of Erlotinib Free Base and a Process For Preparation Of Erlotinib Hydrochloride Polymorph Form A Substantially Free of Polymorph Form B - The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D | 01-26-2012 |
20120035363 | CRYSTALLINE 4-(3-CHLORO-2-FLUOROANILINO)-7 METHOXY-6-... - 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline difumarate, pharmaceutical compositions containing the difumarate, the use of the difumarate in the treatment of hyperproliferative disorders such as cancer and processes for the manufacture of the difumarate are described. | 02-09-2012 |
20120095228 | METHOD FOR THE PREPARATION OF ERLOTINIB - An alternative method for the preparation of Erlotinib through a new chemical reaction for the preparation of the 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol key intermediate of formula (IV) according to the following scheme. | 04-19-2012 |
20120095229 | CHEMICAL PROCESS - The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline. | 04-19-2012 |
20120108814 | PROCESS 738 - Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described. | 05-03-2012 |
20120245350 | METHODS FOR THE PREPARATION OF LAPATINIB AND THE SALTS THEREOF - Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents. | 09-27-2012 |
20120245351 | PROCESS FOR THE PREPARATION OF LAPATINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS - The present invention relates to an improved and new process for the preparation of high purity crystalline base of Lapatinib of formula (1) having chemical name N-{3-chloro-4-[(3-fluorobenzyloxy]phenyl}-6-[5-({[2-(methanesulfonyl)ethyl]amino}methyl]-2-furyl]-4-quip-azolinamine and its pharmaceutically acceptable salts. | 09-27-2012 |
20120289701 | FORMS OF LAPATINIB DITOSYLATE AND PROCESSES FOR PREPARATION THEREOF - The present invention provides novel polymorphs of lapatinib ditosylate, processes for preparing them, and pharmaceutical compositions comprising one or more of these polymorphs. | 11-15-2012 |
20120302749 | PROCESSES FOR THE PREPARATION OF ERLOTINIB HYDROCHLORIDE FORM A AND ERLOTINIB HYDROCHLORIDE FORM B - The present invention relates to processes for the preparation of erlotinib hydrochloride Form A and erlotinib hydrochloride Form B. (I). | 11-29-2012 |
20130123497 | POLYMORPHIC FORMS OF LAPATINIB DITOSYLATE AND PROCESSES FOR THEIR PREPARATION - There is provided a crystalline form of Lapatinib, termed APO-I, and methods for making APO-I. There is also provided a crystalline solvate form of Lapatinib, termed APO-II, and methods for making APO-II. | 05-16-2013 |
20130131341 | NOVEL POLYMORPHS OF ERLOTINIB HYDROCHLORIDE AND METHOD OF PREPARATION - The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans. | 05-23-2013 |
20130137867 | NOVEL CRYSTAL OF ERLOTINIB BASE AND THE PREPARATION METHOD THEREOF - A novel crystal of antitumor drug erlotinib base and its preparation method are provided in the present invention. A preparation method of erlotinib hydrochloride with high-purity is also provided in the present invention. | 05-30-2013 |
20130178624 | QUINAZOLINE DERIVATIVES - The present invention concerns the compounds of formula | 07-11-2013 |
20130310562 | Bicyclic Heteroaromatic Compounds As Protein Tyrosine Kinase Inhibitors - A pharmaceutical formulation comprising the compound of formula | 11-21-2013 |
20140005391 | QUINAZOLINE BASED EGFR INHIBITORS | 01-02-2014 |
20140018535 | PROCESS FOR THE PREPARATION OF LAPATINIB AND ITS DITOSYLATE SALT - There is provided processes for preparing Lapatinib and pharmaceutically acceptable salts thereof by the reductive amination of the aldehyde of Formula II by treatment with 2-methanesulphonylethylamine followed by catalytic hydrogenation in the presence of a suitable hydrogenation catalyst. | 01-16-2014 |
20140024829 | PROCESS AND INTERMEDIATES FOR PREPARING LAPATINIB - A compound of formula (X): | 01-23-2014 |
20140121373 | PROCESS FOR PREPARING STABLE POLYMORPHIC FORM OF ERLOTINIB HYDROCHLORIDE - The present invention discloses an improved and efficient process for preparing Erlotinib hydrochloride suitable as a cancer drug. | 05-01-2014 |
20140155606 | QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (I) below. | 06-05-2014 |
20140194624 | Process for Preparation of Erlotinib and its Pharmaceutically Acceptable Salts - A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4-halo-6,7-bis(2-methoxyethoxy)quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. | 07-10-2014 |
20140275534 | METHOD FOR PREPARING 1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY) PIPERIDIN-1-YL)-PROP-2-EN-1-ONE HYDROCHLORIDE AND INTERMEDIATES USED THEREIN - The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase, and intermediates used therein. | 09-18-2014 |
20140378684 | Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)qu- inazoline - The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline. | 12-25-2014 |
20150299141 | Crystalline Erlotinib Hydrochloride Process - The present invention provides process for preparation of Crystalline Erlotinib HCl (I) Form-SE | 10-22-2015 |
20150344458 | Method For Preparing 1-(4-(4-(3,4-Dichloro-2-Fluorophenylamino)-7-Methoxyquinazolin-6-Yloxy)Pi- peridin-1-Yl)Prop-2-En-1-One - The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base. | 12-03-2015 |
20160083373 | METHOD FOR PREPARING AFATINIB AND INTERMEDIATE THEREOF - Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino)-I-oxo-2-buten-I-yl]amino-5-[(S)-(tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethyl acetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry. | 03-24-2016 |
20160115137 | PROCESS FOR THE PREPARATION OF ERLOTINIB - A process for the preparation of Erlotinib is disclosed in which the compound of formula (II) | 04-28-2016 |
20160185754 | Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)qu- inazoline - The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline. | 06-30-2016 |