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1. 发明申请

WO2008060998A1 INDOLE SULFONAMIDES AS SFRP-1 MODULATORS 审中-公开
标题翻译：作为SFRP-1调节剂的单磺酰亚胺
公开(公告)号：WO2008060998A1
公开(公告)日：2008-05-22
申请号：PCT/US2007/084245
申请日：2007-11-09
申请人： WYETH , WELMAKER, Gregory, Scott , WILSON, Matthew, Alan , MOORE, William, Jay , KERN, Jeffrey, Curtis , TRYBULSKI, Eugene, John
发明人： WELMAKER, Gregory, Scott , WILSON, Matthew, Alan , MOORE, William, Jay , KERN, Jeffrey, Curtis , TRYBULSKI, Eugene, John
IPC分类号： C07D209/30 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/404 , A61P19/00 , A61P19/02 , A61P19/10
CPC分类号： C07D401/12 , C07D209/30 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Indole sulfonamide compounds or pharmaceutically acceptable salts thereof, are provided, which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis. (I) R 1 is alkyl, perfluoroalkyl, halo, cyano, or CO 2 alkyl; R 2 is optionally substituted alkyl, cycloalkyl, heterocycloalkyl, or spiroheterocycloalkyl; R 3 is optionally substituted aryl. R 4 is optionally substituted alkyl, cycloalkyl, or heterocycloalkyl; R 5 is hydrogen or alkyl; R 6 is optionally substituted aryl or heteroaryl; R 7 is alkyl, perfluoroalkyl, halo, cyano, or alkoxycarbonyl; and X is absent or SO 2 .
摘要翻译：提供了吲哚磺酰胺化合物或其药学上可接受的盐，其是分泌的卷曲相关蛋白-1的调节剂。化合物和含有这些化合物的组合物可用于治疗多种疾病，包括骨质疏松症。（I）R 1是烷基，全氟烷基，卤素，氰基或CO 2烷基; R 2是任选取代的烷基，环烷基，杂环烷基或螺杂环烷基; R 3是任选取代的芳基。 R 4是任选取代的烷基，环烷基或杂环烷基; R 5是氢或烷基; R 6是任选取代的芳基或杂芳基; R 7是烷基，全氟烷基，卤素，氰基或烷氧基羰基; 并且X不存在或者是SO 2。

2. 发明申请

WO2005037809A1 SUBSTITUTED ARYL CYCLOALKANOL DERIVATIVES AND METHODS OF THEIR USE 审中-公开
标题翻译：取代的芳基环烷醇衍生物及其使用方法
公开(公告)号：WO2005037809A1
公开(公告)日：2005-04-28
申请号：PCT/US2004/033990
申请日：2004-10-13
申请人： WYETH , TRYBULSKI, Eugene, John , SABATUCCI, Joseph, Peter , VU, An, Thien , SANTILLI, Arthur, Attilio , KRIM. Lori, Danielle , YE, Fei , MAHANEY, Paige, Erin , COHN, Stephen, Todd
发明人： TRYBULSKI, Eugene, John , SABATUCCI, Joseph, Peter , VU, An, Thien , SANTILLI, Arthur, Attilio , KRIM. Lori, Danielle , YE, Fei , MAHANEY, Paige, Erin , COHN, Stephen, Todd
IPC分类号： C07D295/092
CPC分类号： C07D295/088 , C07D207/14 , C07D209/14 , C07D211/44 , C07D211/46 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D241/04 , C07D243/08 , C07D295/03 , C07D307/14 , C07D307/81 , C07D309/12 , C07D317/58 , C07D333/28 , C07D333/58
摘要： The present invention is directed to substituted aryl cycloalkanoyl derivatives, 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.
摘要翻译：本发明涉及取代的芳基环烷酰基衍生物，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，其中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，糖尿病性神经病变及其组合的那些病症，慢性疲劳综合征，纤维肉瘤病综合征，神经系统疾病及其组合。

3. 发明申请

WO2003000649A1 6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1) 审中-公开
标题翻译： 6-（ARYL-AMIDO或芳基 - 氨基甲酰基） - 磷酸-2-乙酯酸衍生物作为PLASMINOGENA激活剂抑制剂类型1（PAI-1）的抑制剂
公开(公告)号：WO2003000649A1
公开(公告)日：2003-01-03
申请号：PCT/US2002/019193
申请日：2002-06-18
申请人： WYETH
发明人： COMMONS, Thomas, Joseph , CROCE, Susan, Christman , WOODWORTH, Richard, Page , TRYBULSKI, Eugene, John , ELOKDAH, Hassan, Mahmoud , CRANDALL, David, LeRoy
IPC分类号： C07C233/75
CPC分类号： C07D403/12 , C07C233/73 , C07C235/48 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D231/14 , C07D307/68 , C07D307/84 , C07D307/85 , C07D405/12
摘要： This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula (I), wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by one or more groups selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxy, phenyl-(CH 2 ) 0-6 -, phenyl-(CH 2 ) 0-6 O-,C 3 -C 6 cycloalkyl, -(CH 2 )-C 3 -C 6 cycloalkyl, halogen, C 1 -C 3 perflouroalkyl and C 1 -C 3 perfluoroalkoxy where phenyl can be substituted with from one or more groups selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, phenyl, halogen, trifluoromethyl and trifluoromethoxy; R 1 is hydrogen, C 1 -C 6 alkyl or phenyl-(CH 2 ) 1-6 - where phenyl can be substituted with C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R 2 and R 3 are H, C 1 -C 6 alkyl, phenyl-(CH 2 ) 0-3 -, halo and C 1 -C 3 perfluoroalkyl where phenyl can be substituted with C 1 -C 6 alkyl, C 1 -C 6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R 4 is -CHR 5 CO 2 H or -CH 2 -tetrazole where R 5 is H or benzyl; and n = 0 or 1; or a pharmaceutically acceptable salt or ester form thereof.
摘要翻译：本发明提供新的化合物，药物组合物和治疗哺乳动物血栓形成障碍的方法，具有式（I）的化合物，其中：Ar是苯基，萘基，呋喃基，苯并呋喃基，吲哚基，吡唑基，恶唑基，芴基，苯基环烷烃，其中环烷可以是环丙基，环丁基，环戊基或环己基，Ar可任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，苯基 - （CH 0-6 < - ，苯基 - （CH> 2 <）> 0-6 ）-C 3 -C 6环烷基，卤素，C 1 -C 3全氟烷基和C 1 -C 3全氟烷氧基，其中苯基可以被一个或多个选自C 1 -C 3烷基的基团取代， C 1-6烷基，C 1 -C 6烷氧基，苯基，卤素，三氟甲基和三氟甲氧基; R 1是氢，C 1 -C 6烷基或苯基 - （CH 2）1-6 - ，其中苯基可被C 1 -C 6烷基取代，C 卤代，三氟甲基和三氟甲氧基; R 2和R 3是H，C 1 -C 6烷基，苯基 - （CH 2）0-3 - ，卤素和C 1 -C 3全氟烷基其中苯基可被C 1 -C 6烷基取代，C 1 -C 6烷氧基，卤素，三氟甲基和三氟甲氧基; R> 4 <= -CHR> 5 2 - 四唑，其中R 5是H或苄基; 并且n = 0或1; 或其药学上可接受的盐或酯形式。

4. 发明公开

EP1732887A1 1-(1H-INDOL-1-YL)-3-(4-METHYLPIPERAZIN-1-YL)-1-PHENYL PROPAN-2-OL DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF THE NOREPINEPHRINE (NE) AND THE SEROTONINE (5-HT) ACTIVITY AND THE MONOAMINE REUPTAKE FOR THE TREATMENT OF VASOMOTOR SYMPTOMS (VMS) 有权
标题翻译： 1-（1H-吲哚-1-基）-3-（4-甲基哌嗪-1-基）-1-苯基丙-2- OLDERIVATE和去甲肾上腺素（NE）和血清素的调节剂相关的化合物（5- HT）活性和单阿明回收用于治疗血管舒缩症状（VMS）
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.

5. 发明公开

EP1385849A1 NOVEL HYDROXY CYCLOHEXENYL PHENYL CARBOXAMIDES TOCOLYTIC OXYTOCIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：新型羟基环己烯基苯基甲酰胺类药物催产素受体拮抗剂
公开(公告)号：EP1385849A1
公开(公告)日：2004-02-04
申请号：EP02721727.2
申请日：2002-04-11
申请人： Wyeth
发明人： FAILLI, Amedeo, Arturo , SANDERS, William, Jennings , TRYBULSKI, Eugene, John
IPC分类号： C07D487/04 , A61P15/06
CPC分类号： C07D487/04
摘要： The present invention provides substituted 10, 11-Dihydro-5H-benzo[e]-pyrrolo-[1,2-a][1,4]diazepine and 9,10-Dihydro-4H-3a,5,9-triaza-benzo[f]azulene compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and/or prevention and/or supression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression labor at term prior to caesarean deliver, and for the treatmet of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals.
摘要翻译：本发明提供了取代的10,11-二氢-5H-苯并[e] - 吡咯并[1,2-a] [1,4]二氮杂and和9,10-二氢-4H-3a，5,9-三氮杂 - 苯并[f]甘菊环化合物以及使用这些化合物治疗和/或预防和/或抑制可通过催产素拮抗剂活性来补救或缓解的疾病的方法和药物组合物，包括预防和/或抑制早产，抑制分娩前的分娩，以及痛经治疗。这些化合物还可用于提高生育率，提高存活率并使农场动物同步发情。

6. 发明公开

EP1377584A1 NOVEL CYCLOHEXENYL PHENYL DIAZEPINES AS VASOPRESSIN AND OXYTOCIN RECEPTOR MODULATORS 有权
标题翻译： NEW环己烯基 - 苯基二氮杂ALS加压素和催产素受体调节剂
公开(公告)号：EP1377584A1
公开(公告)日：2004-01-07
申请号：EP02728749.9
申请日：2002-04-11
申请人： Wyeth
发明人： FAILLI, Amedeo, Arturo , SANDERS, William, Jennings , TRYBULSKI, Eugene, John
IPC分类号： C07D487/04 , A61K31/5517 , A61P5/10 , A61P5/06
CPC分类号： C07D487/04
摘要： The present invention provides novel tricyclic diazepine compounds and methods and pharmaceutical compositions utilizing them for the treating or preventing disorders including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, congestive heart failure or for inducing temporary delay of urination, and in conditions with increased vascular resistance and coronary vasoconstriction; and for the treating or preventing disorders remedied or alleviated by oxytocin antagonist activity, including suppression of preterm labor, dysmenorrhea, endometritis, and for suppressing labor at term prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronising estrus in farm animals; and treatment of disfunction of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

7. 发明授权

EP1021444B1 3-CARBOXAMIDE DERIVATIVES OF 5H-PYRROLO[2,1-c][1,4]-BENZODIAZEPINES 失效
标题翻译： 5H PYRROO [2,1-c] [1,4]苯甲酸酯-3-羧酰胺衍生物
公开(公告)号：EP1021444B1
公开(公告)日：2003-09-24
申请号：EP97911809.8
申请日：1997-10-22
申请人： Wyeth
发明人： TRYBULSKI, Eugene, John , MOLINARI, Albert, John , BAGLI, Jehan, Framroz , ASHWELL, Mark, Anthony , CAGGIANO, Thomas, Joseph
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D487/04

8. 发明公开

EP1673059A2 ALKANOL AND CYCLOALKANOL-AMINE DERIVATIVES AND METHODS OF THEIR USE 审中-公开
标题翻译：芳基烷基哌嗪衍生物和其用于疾病的治疗，其由单胺再摄取改善使用，和血管舒缩症状
公开(公告)号：EP1673059A2
公开(公告)日：2006-06-28
申请号：EP04794957.3
申请日：2004-10-13
申请人： Wyeth
发明人： TRYBULSKI, Eugene, John , MAHANEY, Paige, Erin , KRIM, Lori, Danielle , MOORE, William, Jay , SABATUCCI, Joseph, Peter
IPC分类号： A61K8/18
CPC分类号： C07D295/073 , C07D207/14 , C07D209/14 , C07D211/46 , C07D211/48 , C07D211/56 , C07D211/58 , C07D213/38 , C07D215/12 , C07D215/14 , C07D243/08 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/155 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/20 , C07D333/38 , C07D333/58 , C07D409/06 , C07D471/04
摘要： The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, 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, nc 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, fibrornyalgia, pain, diabetic neuropathy, and combinations thereof.

9. 发明授权

EP1000062B1 TRICYCLIC VASOPRESSIN AGONISTS 失效
标题翻译：三环加压素激动剂
公开(公告)号：EP1000062B1
公开(公告)日：2004-09-22
申请号：EP98938017.5
申请日：1998-07-24
申请人： Wyeth
发明人： DUSZA, John, Paul , CHAN, Peter, Sinchun , ALBRIGHT, Jay, Donald , BAGLI, Jehan, Framroz , FAILLI, Amedeo, Arturo , ASHWELL, Mark, Anthony , MOLINARI, Albert, John , CAGGIANO, Thomas, Joseph , TRYBULSKI, Eugene, John
IPC分类号： C07D487/04 , A61K31/55
CPC分类号： C07D487/04
摘要： This invention relates to new compounds selected from those of general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof, wherein D, E, and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
摘要翻译：本发明涉及选自通式（I）的那些化合物或其药学上可接受的盐，酯或前药形式的新化合物，其中D，E和G是N或CH，它们用作加压素激动剂并用于治疗诸如尿崩症，夜间遗尿症，夜尿症，尿失禁，出血和凝血障碍以及不能暂时延缓排尿的药物组合物及其使用方法。

10. 发明公开

EP1377581A1 NOVEL TRICYCLIC PYRIDYL BENZAZEPINE CARBOXAMIDES AND DERIVATIVES THEREOF AS TOCOLYTIC OXYTOCIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：三环吡啶基苯并氮杂甲酰胺及其衍生物的AS宫缩催产素受体拮抗剂
公开(公告)号：EP1377581A1
公开(公告)日：2004-01-07
申请号：EP02723834.4
申请日：2002-04-11
申请人： Wyeth
发明人： FAILLI, Amedeo, Arturo , SHUMSKY, Jay, Scott , CAGGIANO, Thomas, Joseph , SABATUCCI, Joseph, Peter , MEMOLI, Kevin, Anthony , TRYBULSKI, Eugene, John
IPC分类号： C07D487/04 , A61K31/5517 , C07D487/14 , A61K31/495 , C07D491/14 , A61P25/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The invention provides novel substituted tricyclic pyridyl carboxamides selected from those of Formula (I) which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

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