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公开(公告)号：EP2137149A2
公开(公告)日：2009-12-30
申请号：EP08746183.6
申请日：2008-04-18
发明人： GOUGOUTAS, Jack Z. , MALLEY, Mary F. , DIMARCO, John D. , YIN, Xiaotian S. , WEI, Chenkou , YU, Jurong , VU, Truc Chi , JONES, Gregory Scott , SAVAGE, Scott A.
IPC分类号： C07D209/52 , A61K31/403 , A61P3/00
CPC分类号： C07D209/52 , A61K31/403 , A61K45/06 , A61K2300/00
摘要： Physical crystal structures of a compound of the formula (I): are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
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12.发明公开CRYSTALLINE FORMS OF (3R,4R)-4-AMINO-1-[[4-[(3-METHOXYPHENYL)AMINO]PYRROLO[2,1-F][1,2,4]TRIAZIN-5-YL]METHOL]PIPERIDIN-3-OL 有权（3R，4R）-4-氨基-1 - [[4 - [（3-甲氧基苯基）氨基]吡咯并[2,1-f] [1,2,4]三嗪-5-基]甲基] - 哌啶-3-醇
公开(公告)号：EP1989207A1
公开(公告)日：2008-11-12
申请号：EP07757088.5
申请日：2007-02-16
发明人： WEI, Chenkou , NORRIS, Derek, J.
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
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公开(公告)号：EP1039890A1
公开(公告)日：2000-10-04
申请号：EP98960437.6
申请日：1998-12-01
发明人： TIMMINS, Peter , WINTER, William, J. , SRIVASTAVA, Sushil, K. , BRETNALL, Alison , WEI, Chenkou , POWERS, Gerald, L.
IPC分类号： A61K31/155
CPC分类号： C07C279/26
摘要： Novel salts of the antidiabetic agent metformin are provided which are metformin salts of dibasic acids (2:1 molar ratio), preferably metformin (2:1) fumarate and metformin (2:1) succinate, which may be employed alone or in combination with another antihyperglycemic agent such as glyburide, for treating diabetes. A method for treating diabetes employing the novel metformin salt by itself or in combination with another antidiabetic agent is also provided.
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公开(公告)号：EP4387968A1
公开(公告)日：2024-06-26
申请号：EP22769445.2
申请日：2022-08-19
IPC分类号： C07D403/12 , A61K31/501 , A61P29/00 , A61P37/00
CPC分类号： C07D403/12
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公开(公告)号：EP2688871B1
公开(公告)日：2015-08-26
申请号：EP12711739.8
申请日：2012-03-26
发明人： KICK, Ellen, K. , HAGEMAN, Michael, J. , GUARINO, Victor, R. , SU, Ching-Chiang , WEI, Chenkou , WARRIER, Jayakumar Sankara , NAIR, Satheesh Kesavan
IPC分类号： C07D233/64 , A61K31/4164 , A61P3/00 , C07F9/141 , C07F9/145
CPC分类号： C07D233/64 , A61K31/4174 , A61K31/675 , A61K45/06 , C07F9/12 , C07F9/65061
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公开(公告)号：EP2688871A1
公开(公告)日：2014-01-29
申请号：EP12711739.8
申请日：2012-03-26
发明人： KICK, Ellen, K. , HAGEMAN, Michael, J. , GUARINO, Victor, R. , SU, Ching-Chiang , WEI, Chenkou , WARRIER, Jayakumar Sankara , NAIR, Satheesh Kesavan
IPC分类号： C07D233/64 , A61K31/4164 , A61P3/00 , C07F9/141 , C07F9/145
CPC分类号： C07D233/64 , A61K31/4174 , A61K31/675 , A61K45/06 , C07F9/12 , C07F9/65061
摘要： Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
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17.发明公开CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3- YLAMINO)PYRROLO [1,2-F][1,2,4]TRIAZIN-2-YL)-N-(6-FLUOROPYRIDIN- 3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE 审中-公开（S）-1-（4-（5-环丙基-1H-吡唑-3-基）氨基]吡咯并[1,2-F] [1,2,4]三嗪-2-基）-N-（ 6-氟吡啶-3-基）-2-甲基吡啶-2-羰基氧化物
公开(公告)号：EP2531507A1
公开(公告)日：2012-12-12
申请号：EP11703551.9
申请日：2011-02-03
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I)are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
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18.发明公开PROCESS EMPLOYING CONTROLLED CRYSTALLIZATION IN FORMING CRYSTALS OF A PHARMACEUTICAL 审中-公开与控制结晶晶体中医药的形成过程
公开(公告)号：EP1758664A2
公开(公告)日：2007-03-07
申请号：EP05745530.5
申请日：2005-05-03
发明人： KIM, Soojin , WEI, Chenkou , LINDRUD, Mark , CHUNG, Hyei-Jha
IPC分类号： B01D9/00
CPC分类号： C07D213/42 , C07D263/32
摘要： A process is provided which employs reactive controlled crystallization to produce drug substance having desirable crystal properties which process involves providing reactants A and B in liquid or solution form and adding reactant B to reactant A using a cubic or incremental addition technique to control extent of reaction and thus crystallization kinetics, including supersaturation and nucleation, to produce crystals of drug substance which are generally larger, better quality and with few fines and narrow particle size distribution than normally obtainable employing prior art crystallization techniques. In addition, crystals of drug substance produced by the above process is also provided.
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公开(公告)号：EP1390011A2
公开(公告)日：2004-02-25
申请号：EP02728982.6
申请日：2002-04-23
发明人： SPROCKEL, Omar, Leopold , LAI, Chiajen , DISCORDIA, Robert, Paul , WEI, Chenkou , KOTHARI, Sanjeev, H. , KIM, Soojin
CPC分类号： A61K9/2009 , A61K9/2054 , A61K9/2059 , A61K31/16 , A61K31/40 , A61K31/44 , A61K38/05
摘要： The invention is directed toward a method for increasing the compactability of an active ingredient by determining the crystallization parameters of the active ingredient that affect compactablility; and controlling the crystallization parameters to achieve increased compactability (Figure 1).
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公开(公告)号：EP3983086A1
公开(公告)日：2022-04-20
申请号：EP20750493.7
申请日：2020-06-09
IPC分类号： A61P37/00 , C07D403/12 , A61K31/501
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