公开(公告)号：EP1732887A1

公开(公告)日：2006-12-20

申请号：EP05730271.3

申请日：2005-03-29

申请人： Wyeth

发明人： KIM, Callain, Younghee ,  MAHANEY, Paige, Erin ,  TRYBULSKI, Eugene, John ,  ZHANG, Puwen ,  TEREFENKO, Eugene, Anthony ,  MCCOMAS, Casey, Cameron ,  MARELLA, Michael, Anthony ,  COGHLAN, Richard, Dale ,  HEFFERNAN, Gavin, David ,  COHN, Stephen, Todd ,  VU, An, Thien ,  SABATUCCI, Joseph, Peter ,  YE, Fei

IPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D265/36 ,  C07D241/42 ,  C07D235/06 ,  C07D471/04 ,  A61K31/4045 ,  A61P15/10

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

摘要： The present invention is directed to phenylaminopropanol derivatives of formula (I): or a pharmaceutically acceptable salt thereof; wherein: the dotted line between Y and Z represents an optional double bond; the dotted line between the two R4 groups represents an optional heterocyclic ring of 4 to 6 ring atoms that may be formed between the two R4 groups, together with the nitrogen through which they are attached; Y is N, CR6, or C=O; Z is N, CR7, CR5, or C(R5)2; R2 is aryl substituted with 0-3 R1 or heteroaryl substituted with 0-3 R1; R3 is H or C1-C4 alkyl; n is an integer form 0 to 4; x is an integer from 1 to 2; and the other substituents are defined in the claims; compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected form the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

公开(公告)号：EP2091933A1

公开(公告)日：2009-08-26

申请号：EP07865518.0

申请日：2007-12-12

申请人： Wyeth

发明人： ZHANG, Puwen ,  SABATUCCI, Joseph P. ,  TEREFENKO, Eugene Anthony ,  TRYBULSKI, Eugene John

IPC分类号： C07D307/83 ,  C07D405/04 ,  A61K31/343 ,  A61P25/00

CPC分类号： C07D307/83 ,  C07D405/04

摘要： The present invention is directed to dihydrobenzofuranyl derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorder, cognitive disorder, diabetic neuropathy, pain, and Other diseases or disorders.

摘要翻译： 本发明涉及式（I）的二氢苯并呋喃基衍生物或其药学上可接受的盐，它们是单胺再摄取抑制剂，含有这些衍生物的组合物，以及它们用于预防和治疗病症的方法，特别包括， 血管舒缩症状，性功能障碍，胃肠疾病和泌尿生殖系统疾病，抑郁症，内源性行为障碍，认知障碍，糖尿病性神经病，疼痛和其他疾病或病症。

公开(公告)号：EP1515725A2

公开(公告)日：2005-03-23

申请号：EP03761263.7

申请日：2003-06-23

申请人： Wyeth

发明人： FENSOME, Andrew ,  GRUBB, Gary ,  HARRISON, Diane, Deborah ,  WINNEKER, Richard, Craig ,  ZHANG, Puwen ,  KERN, Jeffrey, Curtis ,  TEREFENKO, Eugene, Anthony

IPC分类号： A61K31/535 ,  A61K31/265 ,  A61K31/16

CPC分类号： A61K31/426 ,  A61K31/536 ,  A61K31/54 ,  A61K31/554 ,  A61K31/565 ,  A61K2300/00

摘要： The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: (I) and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I or formula II and a selective estrogen receptor modulator are also described.

摘要翻译： 本发明提供诱导避孕的方法，其包括在包括递送一种或多种选择性雌激素受体调节剂的方案中向女性递送含有式I，式II或其互变异构体的化合物的组合物，其中式I是 ：（I）并且其中R 1 -R 5和Q 1如本文所述定义。 还提供了提供激素替代疗法和用于治疗癌症，功能失调性出血，子宫平滑肌瘤，子宫内膜异位和多囊卵巢综合征的方法，其包括递送式I或式II化合物和选择性雌激素受体调节剂。

公开(公告)号：EP1934178A2

公开(公告)日：2008-06-25

申请号：EP06815743.7

申请日：2006-09-27

申请人： Wyeth

发明人： MCCOMAS, Casey, Cameron ,  ZHANG, Puwen ,  TEREFENKO, Eugene, Anthony ,  VU, An, Thien ,  COHN, Stephen, Todd

IPC分类号： C07D209/34 ,  C07D209/96 ,  C07D235/26 ,  C07D235/30 ,  C07D277/68 ,  A61P25/00

CPC分类号： C07D209/96 ,  C07D209/08 ,  C07D209/34 ,  C07D235/26 ,  C07D235/30 ,  C07D277/68

摘要： The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

公开(公告)号：EP1175411B1

公开(公告)日：2008-02-20

申请号：EP00930266.2

申请日：2000-05-01

申请人： Wyeth

发明人： ZHANG, Puwen ,  FENSOME, Andrew ,  TEREFENKO, Eugene, A. ,  ZHI, Lin ,  JONES, Todd, K. ,  COLLINS, MARK, A. ,  TEGLEY, Christopher, M. ,  WROBEL, Jay, E. ,  EDWARDS, James, P.

IPC分类号： C07D265/18 ,  C07D413/04 ,  A61K31/536 ,  A61P15/00 ,  A61P35/00

CPC分类号： C07D265/18 ,  C07D413/04

摘要： The present invention provides compounds which are agonists of the progesterone receptor and have structures (I) or (II) wherein R1 and R2 are independent substituents selected from the group of H, optionally substituted C1 to C6 alkyl, alkenyl, alkynyl, or alkynyl groups C3 to C8 cycloalkyl, aryl, substituted aryl, or heterocyclic groups, or COR?A or NRBCORA; or R1 and R2¿ are fused to form an optionally substituted 3 to 8 membered Spiro cyclic alkyl or alkenyl ring or a Spiro cyclic ring containing one to three heteroatoms selected from O, S and N; RA is selected from H, amino, or optionally substituted C¿1? to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; R?B¿ is H, C¿1? to C3 alkyl, or substituted C1 to C3 alkyl; R?3¿ is H, OH, NH¿2 COR?C, or optionally substituted C¿1? to C6 alkyl, C3 to C6 alkenyl, or alkynyl groups; R?C¿ is selected from H or optionally substituted C¿1? to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl groups; Q?1¿ is S, NR?7; or CR8R9, R5¿ is an optionally trisubstituted benzene ring or an optionally substituted five or six membered heterocyclic ring with 1, 2, or 3 ring heteroatoms selected from the group of O, S, SO, SO¿2? or NR?6¿; or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds for contraception and the treatment of progesterone-related maladies.

公开(公告)号：EP1732887B1

公开(公告)日：2008-01-09

申请号：EP05730271.3

申请日：2005-03-29

申请人： Wyeth

发明人： KIM, Callain, Younghee ,  MAHANEY, Paige, Erin ,  TRYBULSKI, Eugene, John ,  ZHANG, Puwen ,  TEREFENKO, Eugene, Anthony ,  MCCOMAS, Casey, Cameron ,  MARELLA, Michael, Anthony ,  COGHLAN, Richard, Dale ,  HEFFERNAN, Gavin, David ,  COHN, Stephen, Todd ,  VU, An, Thien ,  SABATUCCI, Joseph, Peter ,  YE, Fei

IPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D265/36 ,  C07D241/42 ,  C07D235/06 ,  C07D471/04 ,  A61K31/4045 ,  A61P15/10

CPC分类号： C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D235/06 ,  C07D241/42 ,  C07D265/36 ,  C07D471/04

摘要： The present invention is directed to phenylaminopropanol derivatives of formula (I): or a pharmaceutically acceptable salt thereof; wherein: the dotted line between Y and Z represents an optional double bond; the dotted line between the two R4 groups represents an optional heterocyclic ring of 4 to 6 ring atoms that may be formed between the two R4 groups, together with the nitrogen through which they are attached; Y is N, CR6, or C=O; Z is N, CR7, CR5, or C(R5)2; R2 is aryl substituted with 0-3 R1 or heteroaryl substituted with 0-3 R1; R3 is H or C1-C4 alkyl; n is an integer form 0 to 4; x is an integer from 1 to 2; and the other substituents are defined in the claims; compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected form the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

公开(公告)号：EP1175398B1

公开(公告)日：2007-07-11

申请号：EP00930289.4

申请日：2000-05-01

申请人： Wyeth

发明人： FENSOME, Andrew ,  MILLER, Lori, L. ,  ULLRICH, John, W. ,  BENDER, Reinhold, H., W. ,  ZHANG, Puwen ,  WROBEL, Jay, E. ,  ZHI, Lin ,  JONES, Todd, K. ,  TEGLEY, Christopher, M. ,  EDWARDS, James, P.

IPC分类号： C07D209/34 ,  A61K31/40 ,  A61P5/00 ,  C07D491/10 ,  C07D209/96 ,  C07D401/04 ,  C07D409/04 ,  C07D405/04 ,  C07D403/04 ,  C07D317/00 ,  C07D319/00 ,  C07D311/00 ,  C07D209/00

CPC分类号： C07D209/34 ,  C07D209/96 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

摘要： This invention comprises compounds of formula (I), which are antagonists of the progesterone receptor, their preparation and utility.

公开(公告)号：EP1173210B1

公开(公告)日：2004-09-15

申请号：EP00928611.3

申请日：2000-05-01

申请人： Wyeth ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： GRUBB, Gary, S. ,  ZHI, Lin ,  JONES, Todd, K. ,  TEGLEY,Christopher, M ,  EDWARDS, James, P. ,  FLETCHER, Horace, A. ,  WROBEL, Jay, E. ,  FENSOME, Andrew ,  ZHANG, Puwen ,  TEREFENKO, Eugene, A.

IPC分类号： A61K45/06 ,  A61K31/57 ,  A61K31/565 ,  A61P15/18

CPC分类号： A61K45/06 ,  A61K31/565 ,  A61K31/57 ,  A61K31/535 ,  A61K2300/00

摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (I): wherein R?1 and R2¿ may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, COR?C; RC¿ is H, C¿1? to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R?4¿ is H, halogen, CN, NO¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R?5¿ is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO¿2? or NR?6¿ and containing one or two independent substituents from the group including H, halogen, CN, NO¿2? , amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, COR?F, or NRGCORF¿; or pharmaceutically acceptable salt thereof. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endormetrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention inlcude stimulation of food intake.

公开(公告)号：EP2061776A1

公开(公告)日：2009-05-27

申请号：EP07862811.2

申请日：2007-12-12

申请人： Wyeth

发明人： MC COMAS, Casey Cameron ,  COHN, Stephen Todd ,  CRAWLEY, Matthew L. ,  FENSOME, Andrew ,  GOLDBERG, Joel Adam ,  JENKINS, Douglas John ,  KIM, Callain Younghee ,  MAHANEY, Paige Erin ,  MANN, Charles William ,  MARELLA, Michael Anthony ,  O'NEILL, David John ,  SABATUCCI, Joseph P. ,  TEREFENKO, Eugene Anthony ,  TRYBULSKI, Eugene John ,  VU, An Thien ,  WOODWORTH, Richard Page Jr. ,  ZHANG, Puwen

IPC分类号： C07D285/14 ,  C07D417/04 ,  C07D417/06

CPC分类号： C07D417/04 ,  C07D285/14 ,  C07D417/06

摘要： The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

公开(公告)号：EP1934193A1

公开(公告)日：2008-06-25

申请号：EP06815744.5

申请日：2006-09-27

申请人： Wyeth

发明人： MCCOMAS, Casey, Cameron ,  ZHANG, Puwen ,  TRYBULSKI, Eugene, John ,  TEREFENKO, Eugene, Anthony ,  VU, An, Thien

IPC分类号： C07D285/14 ,  A61K31/428

CPC分类号： C07D285/14

摘要： The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula (I): or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.