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公开(公告)号：EP1746999B1
公开(公告)日：2011-11-16
申请号：EP05732761.1
申请日：2005-04-25
发明人： FAKHOURY, Stephen, Alan , LEE, Helen, Tsenwhei , REED, Jessica, Elizabeth , SCHLOSSER, Kevin, Matthew , SEXTON, Karen, Elaine , TECLE, Haile , WINTERS, Roy, Thomas
IPC分类号： A61K31/505 , C07D239/94 , A61P43/00 , A61P35/00
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12
摘要： This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
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2.发明授权
公开(公告)号：EP1368323B1
公开(公告)日：2010-06-30
申请号：EP02740096.9
申请日：2002-01-18
IPC分类号： C07D239/28 , A61K31/505 , C07D405/12 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61P19/02
CPC分类号： C07D239/28 , A61K31/505 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen, halo, hydroxy, C¿1?-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR?4 R5¿, CN, or CF¿3?; E is independently O or S; A and B independently are OR?4 or NR4R5; R4 and R5¿ independently are H, C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R?4 and R5¿ when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6.
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公开(公告)号：EP1485081B1
公开(公告)日：2010-05-05
申请号：EP03743950.2
申请日：2003-02-28
IPC分类号： A61K31/192 , A61K9/48 , A61K47/44
CPC分类号： A61K31/192 , A61K9/4858 , A61K47/02 , A61K47/44 , Y02A50/465
摘要： The present invention relates to pharmaceutically acceptable solutions for filling hard gelatin capsules, hard gelatin capsules containing these solutions.
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4.发明公开Octanoic acid derivative to treat fibromyalgia and other pains 审中-公开OctansäureDerivat zur Behandlung von Fibromyalgia und anderen Schmerzen
公开(公告)号：EP2172197A1
公开(公告)日：2010-04-07
申请号：EP09175270.9
申请日：2003-12-03
IPC分类号： A61K31/195 , A61P43/00
CPC分类号： A61K45/06 , A61K31/195
摘要： The invention relates to the use of (3S,5R)-3-aminomethyl-5-methyloctanoic acid, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment of a mammal for a disorder selected from fibromyalgia, abdominal or gynaecological pain, and pain caused by increased bladder contractions.
摘要翻译： 本发明涉及（3S，5R）-3-氨基甲基-5-甲基辛酸或其药学上可接受的盐在制备用于治疗哺乳动物的药物中的用途，所述疾病选自纤维肌痛，腹部或 妇科疼痛和膀胱收缩增加引起的疼痛。
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5.发明授权2-AMINOPYRIDINE SUBSTITUTED HETEROCYCLES AS INHIBITORS OF CELLULAR PROLIFERATION 有权2-氨基吡啶SUBSTITUIERTEHETEROCYCLEN AS细胞增殖的抑制剂的
公开(公告)号：EP1590341B1
公开(公告)日：2009-06-17
申请号：EP04701058.2
申请日：2004-01-09
发明人： FLAMME, Cathlin M., Pfizer Global R & D , McNAMARA, Dennis J., Pfizer Global R & D , REPINE, Joseph T., Pfizer Global R & D , TOOGOOD, Peter L., Pfizer Global R & D , VANDERWEL, Scott N., Pfizer Global R & D , WARMUS, Joseph S., Pfizer Global R & D
IPC分类号： C07D401/12 , C07D213/75
CPC分类号： C07D213/75 , C07D401/12 , C07D475/04
摘要： The present invention provides substituted 2-aminopyridines of formula (I), wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (Cdk4).
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6.发明公开Combinations for diabetes which contain a sulfonylurea, a glitazone and a biguanide 审中-公开含有包含磺酰脲类，格列酮和双胍类糖尿病的治疗组合
公开(公告)号：EP1514550A3
公开(公告)日：2009-04-29
申请号：EP04029821.8
申请日：1999-08-11
发明人： Whitcomb, Randall W.
IPC分类号： A61K31/155 , A61K31/427 , A61K31/4439 , A61K31/64 , A61K45/06 , A61P3/10 , A61K31/426
CPC分类号： A61K31/427 , A61K31/155 , A61K31/426 , A61K31/4439 , A61K31/64 , A61K45/06 , Y10S514/866 , A61K31/44 , A61K31/425 , A61K2300/00
摘要： Combinations of a glitazone antidiabetic agent, a biguanide antidiabetic agent, and a sulfonylurea antidiabetic agent, are useful for treating diabetes mellitus and improving glycemic control.
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7.发明授权GAMMA-AMINOBUTYRIC ACID DERIVATIVES CONTAINING, SOLID COMPOSITIONS AND PROCESS FOR PREPARING THE SAME 有权GAMMAAMINOBUTTERSÄUREDERIVATE含PRODUCING固态制剂和方法
公开(公告)号：EP1077691B1
公开(公告)日：2008-09-10
申请号：EP99924164.9
申请日：1999-05-10
发明人： AOMATSU, Akira
IPC分类号： A61K31/195 , A61K9/16 , A61K47/18
CPC分类号： A61K9/1688 , A61K9/1617 , A61K9/2013 , A61K9/282 , A61K9/284 , A61K31/565 , A61K2300/00
摘要： The present invention provides a stabilized solid composition containing a 4-amino 3-substituted-butanoic acid derivative which can be obtained by incorporating a humectant as a stabilizer.
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公开(公告)号：EP1117736B2
公开(公告)日：2008-08-13
申请号：EP99939129.5
申请日：1999-08-11
IPC分类号： C08L3/08 , C08L3/18 , C09D103/08 , C08L3/10 , C09D103/10 , A61K9/48 , A61K9/50
CPC分类号： A61K9/4816 , A61K9/4883 , A61K47/32 , A61K47/36
摘要： The invention concerns compositions from modified starches, such as starch ethers or oxidized starch, more particularly hydroxypropylated starch (HPS) or hydroxylethylated starch (HES) for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules. The hard capsules obtained by the present invention with a conventional dipping molding process are similar to hard gelatine capsules (HGC).
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公开(公告)号：EP1912937A1
公开(公告)日：2008-04-23
申请号：EP06779928.8
申请日：2006-07-20
发明人： PFEFFERKORN, Jeffrey Allen, Pfizer Global R. & D. , TRIVEDI, Bharat Kalidas, Pfizer Global R. & D.
IPC分类号： C07D205/08 , A61K31/397 , A61P3/06
CPC分类号： C07D205/08
摘要： Novel azetidinones and pharmaceutical compositions are described, as are the methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis.
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10.发明授权PYRIDO 2,3-D PYRIMIDINES AND 4-AMINOPYRIMIDINES AS INHIBITORS OF CELLULAR PROLIFERATION 失效吡啶并（2,3-D）嘧啶和4-氨基PRIMIDINE AS细胞增殖的抑制剂的
公开(公告)号：EP0964864B1
公开(公告)日：2008-04-09
申请号：EP98908442.1
申请日：1998-01-26
发明人： BOSCHELLI, Diane, Harris , DOBRUSIN, Ellen, Myra , DOHERTY, Annette, Marian , FATTAEY, Ali , FRY, David, W. , BARVIAN, Mark, R. , TRUMPP-KALLMEYER, Susanne, A , WU, Zhipei
IPC分类号： C07D471/00
CPC分类号： C07D239/47 , C07D239/48 , C07D471/04
摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 4-aminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II), where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R?8 and R9¿ include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
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