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1. 发明申请

WO2008021338A3 TRICYCLIC OXAZOLIDONE DERIVATIVES USEFUL AS PR MODULATORS 审中-公开
标题翻译：作为PR调节剂的TRICYCLIC OXAZOLIDONE衍生物有用
公开(公告)号：WO2008021338A3
公开(公告)日：2008-04-03
申请号：PCT/US2007017940
申请日：2007-08-13
申请人： WYETH CORP , COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE JR , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE , BERNOTAS RONALD CHARLES
发明人： COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE JR , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE , BERNOTAS RONALD CHARLES
IPC分类号： A61K31/428 , A61P5/36 , A61P15/02 , A61P15/18 , A61P35/00 , C07D417/04
CPC分类号： C07D417/04
摘要： Compounds of the following structure are described (I), wherein R 1 -R 6 , R 16 , m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
摘要翻译：以下结构的化合物描述为（I），其中R 1 -R 6，R 16，m，V，W，X， Y和Q在本文中描述，或其药学上可接受的盐，互变异构体，代谢物或前药。这些化合物可用于治疗各种激素相关病症，包括避孕，治疗或预防子宫肌瘤，子宫内膜异位症，功能障碍性出血，子宫平滑肌瘤，多囊卵巢综合征或激素依赖性癌症，提供激素替代疗法，刺激食物摄入或同步发情。

2. 发明申请

WO2004080170A3 AMINO SUBSTITUTED BENZO(HETERO)CYCLIC DERIVATIVES 审中-公开
标题翻译：氨基取代的苯并（杂环）环状衍生物
公开(公告)号：WO2004080170A3
公开(公告)日：2004-11-04
申请号：PCT/EP2004001677
申请日：2004-02-20
申请人： BASF AG , STEINER GERD , SCHMIDT THOMAS , KORDES MARKUS , DEYN WOLFGANG VON , HOFMANN MICHAEL , BAUMANN ERNEST , PUHL MICHAEL , HEFFERNAN GAVIN , CULBERTSON DEBORAH L , TREACY MICHAEL F
发明人： STEINER GERD , SCHMIDT THOMAS , KORDES MARKUS , VON DEYN WOLFGANG , HOFMANN MICHAEL , BAUMANN ERNEST , PUHL MICHAEL , HEFFERNAN GAVIN , CULBERTSON DEBORAH L , TREACY MICHAEL F
IPC分类号： A01N43/60 , A01N43/72
CPC分类号： A01N43/72 , A01N43/60
摘要： Use of compounds Formula (I), A = a 5- to 7-membered ring which may contain 1-3 heteroatoms and which may be saturated or partially or completely unsaturated; R = OH, SH, NH2, CN, NO2, halogen, C1-C6-alkyl, C1-C6-haloalkyl; C1-C6- alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-haloalkylthio, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkenylthio, C2-C6-alkynyl, C2-C6alkynyloxy, C2-C6-alkynylthio, C1-C6-alkylsulfonyl, C1-C6-alkylsulfoxyl, C2-C6-alkenylsulfonyl, C2-C6-alkynylsulfoxyl, C1-C6-alkylcarbonyl, C1-C6- alkoxycarbonyl, C1-C6-alkylcarbonyloxy; R = C1-C6-alkyl or a mono- or bicyclic 5- to 10-membered aromatic ringsystem which may contain 1 to 4 heteroatoms and which is either bonded directly or through an O, S, C1-C6-alkylene or C1-C6-alkyleneoxy linkage to A or fused to A and which may be substituted; R , R = H, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkylamino, C1-C6-alkoxy, C3-C6 cycloalkyl, or R and R together with the nitrogen atom to which they are attached form a saturated or partially saturated mono- or bicyclic 5- to 10-membered ring system con-taining 1 to 3 heteroatoms or a 5-membered hetaryl containing 1 to 4 nitro-gen atoms, wherein the carbon and/or nitrogen atoms in the ring systems may be substituted or phenyl or benzyl which may be substituted; or R and R together form the chains -(CH2)2N (O-)(CH2)2- or -(CH2)3N (O )(CH2)2 ; m = 0 to 4; n is 0 to 4; and the enantiomers, diastereomers, cis/trans isomers or salts thereof for combatting insects, arachnids or nematodes, methods for the control of these pests and of protecting growing plants attack or infestation by these pests by applying a pesticidally effective amount of a compound of formula (I), processes for preparing them, and compositions comprising them.
摘要翻译：式（I）化合物的用途，A =可含有1-3个杂原子且可以是饱和或部分或完全不饱和的5至7元环; R 1 = OH，SH，NH 2，CN，NO 2，卤素，C 1 -C 6烷基，C 1 -C 6卤代烷基; C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷硫基，C 1 -C 6卤代烷硫基，C 2 -C 6烯基，C 2 -C 6烯氧基，C 2 -C 6烯硫基， C 1 -C 6烷基磺酰基，C 1 -C 6烷基亚磺酰基，C 2 -C 6烯基磺酰基，C 2 -C 6炔基亚磺酰基，C 1 -C 6烷基羰基，C 1 -C 6烷氧基羰基， R 2 = C 1 -C 6烷基或可含有1至4个杂原子并且直接键合或通过O，S，C 1 -C 6亚烷基键合的单环或双环5至10元芳环体系或与A相连的C1-C6-亚烷氧基键或者与A相连并可以被取代的; R 3，R 4 = H，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基氨基，C 1 -C 6烷氧基，C 3 -C 6环烷基或R 3和 R 4与它们所连接的氮原子一起形成饱和或部分饱和的含有1至3个杂原子的5至10元环系统或含有1至4个硝基的5元杂芳基其中环系统中的碳和/或氮原子可以被取代或者可以被取代的苯基或苄基; 或者R 3和R 4一起形成链 - （CH 2）2 N +（O-）（CH 2）2 - 或 - （CH 2）3 N +（O-）（CH 2）2 < - >; m = 0至4; n是0至4; 以及用于防治昆虫，蛛形纲动物或线虫的对映异构体，非对映异构体，顺式/反式异构体或其盐，控制这些害虫的方法以及通过施用农药有效量的式（I）化合物来保护生长中的植物对这些害虫的侵袭或侵染（I），制备它们的方法以及包含它们的组合物。

3. 发明申请

WO2008021339A3 PYRROLIDINE AND RELATED DERIVATIVES USEFUL AS PR MODULATORS 审中-公开
标题翻译：吡咯烷和相关衍生物作为PR调节剂有用
公开(公告)号：WO2008021339A3
公开(公告)日：2008-05-15
申请号：PCT/US2007017941
申请日：2007-08-13
申请人： WYETH CORP , COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE
发明人： COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE
IPC分类号： C07D417/04 , A61K31/427 , A61K31/4748 , A61P15/00 , C07D453/06
CPC分类号： C07D417/04 , C07D453/06
摘要： Compounds of the structure (I) are described, wherein R 1 -R 6 , R 11 , R 12 , m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
摘要翻译：描述了结构（I）的化合物，其中R 1 -R 6，R 11，R 12，，m，V，X，Y，Z和Q，或其药学上可接受的盐，互变异构体，代谢物或前药。这些化合物可用于治疗各种激素相关病症，包括避孕，治疗或预防子宫肌瘤，子宫内膜异位症，功能障碍性出血，子宫平滑肌瘤，多囊卵巢综合征或激素依赖性癌症，提供激素替代疗法，刺激食物摄入或同步发情。

4. 发明申请

WO2008021337A1 OXAZINAN-2-ONE DERIVATIVES USEFUL AS PR MODULATORS 审中-公开
标题翻译： OXAZINAN-2-ONE衍生物作为PR调节剂有用
公开(公告)号：WO2008021337A1
公开(公告)日：2008-02-21
申请号：PCT/US2007/017939
申请日：2007-08-13
申请人： WYETH , COMMONS, Thomas, Joseph , FENSOME, Andrew , HEFFERNAN, Gavin, David , MCCOMAS, Casey, Cameron , WOODWORTH, Richard, Page , WEBB, Michael, Byron , MARELLA, Michael, Anthony , MELENSKI, Edward, George , BERNOTAS, Ronald, Charles
发明人： COMMONS, Thomas, Joseph , FENSOME, Andrew , HEFFERNAN, Gavin, David , MCCOMAS, Casey, Cameron , WOODWORTH, Richard, Page , WEBB, Michael, Byron , MARELLA, Michael, Anthony , MELENSKI, Edward, George , BERNOTAS, Ronald, Charles
IPC分类号： C07D417/04 , A61K31/5355 , A61K31/427 , A61P5/24
CPC分类号： C07D417/04
摘要： Compounds of the following structure are described (I), wherein R 1 -R 6 , m, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
摘要翻译：描述了以下结构的化合物（I），其中R 1至R 6，m，V，X，Y，Z和Q在本文中描述，或药学上可接受的盐，互变异构体，代谢物或前药。这些化合物可用于治疗各种激素相关病症，包括避孕，治疗或预防子宫肌瘤，子宫内膜异位症，功能障碍性出血，子宫平滑肌瘤，多囊卵巢综合征或激素依赖性癌症，提供激素替代疗法，刺激食物摄入或同步发情。

5. 发明申请

WO2008021331A3 OXAZOLIDONE DERIVATIVES AS PR MODULATORS 审中-公开
公开(公告)号：WO2008021331A3
公开(公告)日：2008-02-21
申请号：PCT/US2007/017931
申请日：2007-08-13
申请人： WYETH , COMMONS, Thomas, Joseph , FENSOME, Andrew , HEFFERNAN, Gavin, David , MCCOMAS, Casey, Cameron , WOODWORTH, Richard, Page, Jr. , WEBB, Michael, Byron , MARELLA, Michael, Anthony , MELENSKI, Edward, George , BERNOTAS, Ronald, Charles
发明人： COMMONS, Thomas, Joseph , FENSOME, Andrew , HEFFERNAN, Gavin, David , MCCOMAS, Casey, Cameron , WOODWORTH, Richard, Page, Jr. , WEBB, Michael, Byron , MARELLA, Michael, Anthony , MELENSKI, Edward, George , BERNOTAS, Ronald, Charles
IPC分类号： C07D417/04 , C07D417/14 , C07D413/04 , C07D263/48 , A61K31/427 , A61K31/422 , A61K31/433 , A61P15/00
摘要： Compounds of the structure (I) are described, wherein R 1 , R 2 , R 5 , R 6 , V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.

6. 发明申请

WO2006124581A3 PYRROLOBENZODIAZEPINES AND HETEROCYCLIC CARBOXAMIDE DERIVATIVES AS FOLLICLE STIMULATING HORMONE RECEPTOR (FSH-R) ANTAGONISTS 审中-公开
标题翻译：作为激素激素受体（FSH-R）拮抗剂的吡咯烷酮和杂环酰胺衍生物
公开(公告)号：WO2006124581A3
公开(公告)日：2007-01-18
申请号：PCT/US2006018420
申请日：2006-05-11
申请人： WYETH CORP , FAILLI AMEDEO A , QUAGLIATO DOMINICK A , HEFFERNAN GAVIN , COGHLAN RICHARD , SHEN EMILY S
发明人： FAILLI AMEDEO A , QUAGLIATO DOMINICK A , HEFFERNAN GAVIN , COGHLAN RICHARD , SHEN EMILY S
IPC分类号： C07D487/04 , A61K31/5517 , A61P15/16 , A61P15/18
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 , R 3 , and B are as defined in the accompanying specification. Methods of making such compounds are also provided.
摘要翻译：本发明提供了式（I）化合物或其药学上可接受的盐，其中R 1，R 1，R 2，R 3，和 B如所附说明书中所定义。还提供了制备这些化合物的方法。

7. 发明申请

WO2006116165A1 CHROMANE AND CHROMENE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： CHROMANE和CHROMENE DORIVATIVES及其用途
公开(公告)号：WO2006116165A1
公开(公告)日：2006-11-02
申请号：PCT/US2006/015208
申请日：2006-04-21
申请人： WYETH , HEFFERNAN, Gavin, David , STACK, Gary, Paul , GROSS, Jonathan, Laird , ZHOU, Dahui , GAO, Hong
发明人： HEFFERNAN, Gavin, David , STACK, Gary, Paul , GROSS, Jonathan, Laird , ZHOU, Dahui , GAO, Hong
IPC分类号： C07D401/04 , C07D311/04 , C07D311/20 , C07D313/08 , A61K31/353 , A61P25/24
CPC分类号： C07D311/04 , C07D311/20 , C07D311/58 , C07D313/08 , C07D401/04 , C07D405/04
摘要： Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R 1 , R 2 , R 3 , R 4 , y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
摘要翻译：提供式I化合物或其药学上可接受的盐：其中R 1，R 2，R 3，R 4， y，m，n和Ar如上所定义，并在本文的类别和亚类中描述，它们是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。

8. 发明申请

WO2008021331A2 OXAZOLIDONE DERIVATIVES AS PR MODULATORS 审中-公开
标题翻译：恶唑酮衍生物作为调节剂
公开(公告)号：WO2008021331A2
公开(公告)日：2008-02-21
申请号：PCT/US2007017931
申请日：2007-08-13
申请人： WYETH CORP , COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE JR , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE , BERNOTAS RONALD CHARLES
发明人： COMMONS THOMAS JOSEPH , FENSOME ANDREW , HEFFERNAN GAVIN DAVID , MCCOMAS CASEY CAMERON , WOODWORTH RICHARD PAGE JR , WEBB MICHAEL BYRON , MARELLA MICHAEL ANTHONY , MELENSKI EDWARD GEORGE , BERNOTAS RONALD CHARLES
CPC分类号： C07D417/04 , C07D263/48 , C07D413/04 , C07D417/14 , C07D453/06
摘要： Compounds of the structure (I) are described, wherein R 1 , R 2 , R 5 , R 6 , V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
摘要翻译：描述了结构（I）的化合物，其中R 1，R 2，R 5，R 6，，V，X，Y，Z和Q在本文中描述，或其药学上可接受的盐，互变异构体，代谢产物或前药。这些化合物可用于治疗各种激素相关病症，包括避孕，治疗或预防肌瘤，子宫内膜异位，功能失调性出血，子宫平滑肌瘤，多囊卵巢综合征或激素依赖性癌症，提供激素替代疗法，刺激食物摄入或同步发情。

9. 发明申请

WO2007041023A1 1- (1H- INDOL- 1-YL) -3- (METHYLAMINO) -1- PHENYLPROPAN-2-OL DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF THE MONOAMINE REUPTAKE FOR THE TREATMENT OF VASOMOTOR SYMPTOMS (VMS) 审中-公开
标题翻译： 1-（1H-INDOL-1-YL）-3-（甲基氨基）-1-苯基丙-2-醇衍生物及相关化合物作为用于治疗血管运动症状（VMS）的单胺类复发的调节剂
公开(公告)号：WO2007041023A1
公开(公告)日：2007-04-12
申请号：PCT/US2006/036965
申请日：2006-09-27
申请人： WYETH , MAHANEY, Paige, Erin , HEFFERNAN, Gavin, David , COGHLAN, Richard, D. , COHN, Stephen, Todd , KIM, Callain, Younghee , JENKINS, Douglas, John , MARELLA, Michael, Anthony , MCCOMAS, Casey, Cameron , SABATUCCI, Joseph, Peter , TEREFENKO, Eugene, Anthony , TRYBULSKI, Eugene, John , VU, An, Thien , YE, Fei , ZHANG, Puwen
发明人： MAHANEY, Paige, Erin , HEFFERNAN, Gavin, David , COGHLAN, Richard, D. , COHN, Stephen, Todd , KIM, Callain, Younghee , JENKINS, Douglas, John , MARELLA, Michael, Anthony , MCCOMAS, Casey, Cameron , SABATUCCI, Joseph, Peter , TEREFENKO, Eugene, Anthony , TRYBULSKI, Eugene, John , VU, An, Thien , YE, Fei , ZHANG, Puwen
IPC分类号： C07D209/08 , C07D209/96 , C07D209/12 , C07D471/04 , C07D241/42 , C07D209/34 , C07D235/26 , A61K31/4045 , A61K31/437 , A61K31/517 , A61P15/10 , A61P1/04 , A61P13/02 , A61P25/04
CPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D209/34 , C07D209/96 , C07D235/26 , C07D241/42 , C07D401/12 , C07D471/04
摘要： The present invention is directed to phenylaminopropanol derivatives of formulae (I), (II), and (III); 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, schizophrenia, and combinations thereof.
摘要翻译：本发明涉及式（I），（II）和（III）的苯基氨基丙醇衍生物; 或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS），性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病，精神分裂症及其组合的那些病症，纤维瘤病综合征，神经系统疾病及其组合。

10. 发明申请

WO2006124581A2 PYRROLOBENZODIAZEPINES AND HETEROCYCLIC CARBOXAMIDE DERIVATIVES AS FOLLICLE STIMULATING HORMONE RECEPTOR (FSH-R) ANTAGONISTS 审中-公开
标题翻译：作为激素激素受体（FSH-R）拮抗剂的吡咯烷酮和杂环酰胺衍生物
公开(公告)号：WO2006124581A2
公开(公告)日：2006-11-23
申请号：PCT/US2006/018420
申请日：2006-05-11
申请人： WYETH , FAILLI, Amedeo, A. , QUAGLIATO, Dominick, A. , HEFFERNAN, Gavin , COGHLAN, Richard , SHEN, Emily, S.
发明人： FAILLI, Amedeo, A. , QUAGLIATO, Dominick, A. , HEFFERNAN, Gavin , COGHLAN, Richard , SHEN, Emily, S.
IPC分类号： C07D487/04 , A61K31/5517 , A61P15/16 , A61P15/18
CPC分类号： C07D487/04
摘要： The invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 , R 3 , and B are as defined in the accompanying specification. Methods of making such compounds are also provided.
摘要翻译：本发明提供了式（I）化合物或其药学上可接受的盐，其中R 1，R 1，R 2，R 3，和 B如所附说明书中所定义。还提供了制备这些化合物的方法。

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