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21. 发明申请

WO1994022829A2 DIHYDROPYRIDINES AND NEW USES THEREOF 审中-公开
标题翻译：二氢吡啶类及其新用途
公开(公告)号：WO1994022829A2
公开(公告)日：1994-10-13
申请号：PCT/US1994003852
申请日：1994-04-05
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GLUCHOWSKI, Charles , WETZEL, John, M. , CHIU, George , MARZABADI, Mohammad, R. , WONG, Wai, C. , NAGARATHNAM, Dhanapalan
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C07D211/90
CPC分类号： C07D401/12 , C07D211/90 , C07D401/14 , C07D405/14 , C07D471/04 , C07D471/10 , C07F7/0812
摘要： The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having structure (I) wherein Y is -(CH2)n-, where n is 1, 2, 3, 4 or 5; -(CH2)h-O-(CH2)k-, where h and k are independently the same or different and are 2, 3 or 4; -(CH2)h-CH=CH-(CH2)k-; or -(CH2)h-CC-(CH2)k-, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is 0, NH, or CH2; wherein R is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R and R are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R and R are independently the same or different and are H, OH, Cl, Br, F, No2, CN, CF3, or NH2, or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressure.
摘要翻译：本发明提供一种治疗受试者的良性前列腺增生的方法，其包括向受试者施用治疗有效量的具有结构（I）的化合物，其中Y为 - （CH 2）n - ，其中n为1,2,3， 4或5; - （CH 2）h -O-（CH 2）k - ，其中h和k独立地相同或不同，为2,3或4; - （CH 2）H-CH = CH-（CH 2）K-; 或 - （CH 2）h-CC-（CH 2）k - ，其中h和k独立地相同或不同，并且是1,2,3或4; 其中Z为0，NH或CH 2; 其中R 1是直链或支链烷基，烷氧基烷基或芳基烷基; 其中R 2和R 4独立地相同或不同，为H或直链或支链烷基; 其中R 3是H，直链或支链烷基，烷氧基，烷氧基烷基或酰基; 并且其中R 5和R 6独立地相同或不同，为H，OH，Cl，Br，F，No2，CN，CF3或NH2，或直链或支链烷基，烷氧基，烷氧基羰基，酰基，烷基亚砜，烷基砜或单或二烷基氨基。还公开了含有一个，两个或三个环的其它活性化合物以及由其制备的药物组合物和用于治疗BPH，抑制胆固醇合成和降低眼内压的方法。

22. 发明申请

WO1994014957A3 DNA ENCODING 5-HT4 SEROTONIN RECEPTORS AND USES THEREOF 审中-公开
公开(公告)号：WO1994014957A3
公开(公告)日：1994-07-07
申请号：PCT/US1993012586
申请日：1993-12-22
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , GERALD, Christophe , HARTIG, Paul , BRANCHEK, Theresa, A. , WEINSHANK, Richard, L.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C12N01/15

23. 发明申请

WO1993010228A1 DNA ENCODING A GLYCINE TRANSPORTER AND USES THEREOF 审中-公开
标题翻译：编码糖蛋白转运蛋白的DNA及其用途
公开(公告)号：WO1993010228A1
公开(公告)日：1993-05-27
申请号：PCT/US1992009662
申请日：1992-11-12
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , SMITH, Kelli , BORDEN, Laurence, A. , BRANCHEK, Theresa , HARTIG, Paul, R. , WEINSHANK, Richard, L.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： C12N15/00
CPC分类号： C07K14/47 , A01K2217/05 , A61K38/00
摘要： This invention provides isolated nucleic acid molecules encoding a mammalian or human glycine transporter, vectors comprising the isolated nucleic acid molecules, mammalian cells comprising such vectors, nucleic acid probes, antisense oligonucleotides complementary to any sequence of a nucleic acid molecule which encodes a mammalian glycine transporter, and non-human transgenic animals which express DNA encoding a normal or a mutant mammalian glycine transporter. The invention also provides the mammalian or human glycine transporter proteins, antibodies directed to them, and pharmaceutical compounds related to the human glycine transporter. The invention further provides methods for determining ligand binding, detecting expression, drug screening, as well as treatments for alleviating abnormalities associated with mammalian or human glycine transporters.
摘要翻译：本发明提供编码哺乳动物或人甘氨酸转运蛋白的分离的核酸分子，包含分离的核酸分子的载体，包含此类载体的哺乳动物细胞，核酸探针，与编码哺乳动物甘氨酸转运蛋白的核酸分子的任何序列互补的反义寡核苷酸，以及表达编码正常或突变型哺乳动物甘氨酸转运蛋白的DNA的非人转基因动物。本发明还提供哺乳动物或人甘氨酸转运蛋白，针对它们的抗体和与人甘氨酸转运蛋白相关的药物化合物。本发明还提供了用于确定配体结合，检测表达，药物筛选以及用于减轻与哺乳动物或人甘氨酸转运蛋白相关的异常的治疗的方法。

24. 发明申请

WO2005059550A1 DNA ENCODING SNORF138 AND USES THEREOF 审中-公开
标题翻译： DNA编码SNORF138及其用途
公开(公告)号：WO2005059550A1
公开(公告)日：2005-06-30
申请号：PCT/US2003/031659
申请日：2003-10-06
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION
发明人： ARTYMYSHYN, Roman , DELGADO, Liliana , VAYSSE, Pierre , ZHANG, Hong , GUO, Weinong
IPC分类号： G01N33/53
CPC分类号： G01N33/5041 , A61K38/00 , A61K49/0004 , C07K14/705 , G01N33/5008 , G01N33/566 , G01N33/567
摘要： This invention provides methods of treating an abnormality that is linked to the activity of the mammalian SNORF138 receptor, as well as methods of determining binding of compounds to the mammalian SNORF138 receptor, methods of identifying agonists and antagonists of the SNORF138 receptor, and agonists and antagonists so identified.
摘要翻译：本发明提供了治疗与哺乳动物SNORF138受体的活性相关的异常的方法，以及确定化合物与哺乳动物SNORF138受体的结合的方法，鉴定SNORF138受体的激动剂和拮抗剂的方法，以及激动剂和拮抗剂如此确定。

25. 发明申请

WO2004093789A2 USE OF GALR3 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF DEPRESSION AND/OR ANXIETY AND COMPOUNDS USEFUL IN SUCH METHODS 审中-公开
标题翻译：使用GALR3受体拮抗剂治疗抑郁症和/或抗生素和化合物在这些方法中有用
公开(公告)号：WO2004093789A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/011698
申请日：2004-04-15
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION
发明人： KONKEL, Michael , WETZEL, John, M. , TALISMAN, Jamie
IPC分类号： A61K
CPC分类号： C07D401/06 , A61K31/404 , A61K31/405 , A61K31/407 , A61K31/4709 , A61K31/4745 , A61K31/497 , A61K31/498 , A61K31/52 , A61K31/53 , C07D209/40 , C07D401/12 , C07D403/02 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D417/12
摘要： This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及作为GALR3受体的拮抗剂的吲哚酮衍生物。本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。本发明还提供通过将治疗有效量的本发明化合物和药学上可接受的载体组合而制备的药物组合物。本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。

26. 发明申请

WO2004060282A3 USES OF THE SNORF207 RECEPTOR 审中-公开
公开(公告)号：WO2004060282A3
公开(公告)日：2004-07-22
申请号：PCT/US2003/039465
申请日：2003-12-10
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION
发明人： DELGADO, Liliana , BERRADA, Karim , ARTYMYSHYN, Roman
IPC分类号： G01N33/53
摘要： The invention provides methods of treating an abnormality that is linked to the activity of the mammalian SNORF207 receptor, as well as methods of determining binding of compounds to the mammalian SNORF207 receptor, methods of identifying agonists and antagonists of the SNORF207 receptor, and agonists and antagonists so identified.

27. 发明申请

WO2003054540A1 DNA ENCODING A HUMAN RECEPTOR (HP15A) AND USES THEREOF 审中-公开
标题翻译：编码人类受体（HP15A）的DNA及其用途
公开(公告)号：WO2003054540A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/040612
申请日：2002-12-19
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION
发明人： SMITH, Kelli, E. , WEINSHANK, Richard
IPC分类号： G01N33/50
CPC分类号： C07K14/705
摘要： This invention provides an isolated nucleic acid encoding a human hp15a receptor, a purified human hp15a receptor, vectors comprising isolated nucleic acid encoding a human hp15a receptor, cells comprising such vectors, antibodies directed to a human hp15a receptor, nucleic acid probes useful for detecting nucleic acid encoding a human hp15a receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a human hp15a receptor, transgenic, nonhuman animals which express DNA encoding a normal or mutant human hp15a receptor, methods of isolating a human hp15a receptor, methods of treating an abnormality that is linked to the activity of the human hpl5a receptor, as well as methods of determining binding of compounds to human hp15a receptors.
摘要翻译：本发明提供编码人hp15a受体的分离的核酸，纯化的人hp15a受体，包含编码人hp15a受体的分离的核酸的载体，包含此类载体的细胞，针对人hp15a受体的抗体，用于检测核酸的核酸探针编码人hp15a受体的酸，与编码人hp15a受体的核酸的独特序列互补的反义寡核苷酸，表达编码正常或突变型人hp15a受体的DNA的转基因非人动物，分离人hp15a受体的方法，与人hpl5a受体的活性相关的异常，以及确定化合物与人hp15a受体结合的方法。

28. 发明申请

WO2003026667A1 QUINAZOLINO- AND QUINOLINO- GUANIDINES AS LIGANDS FOR THE NEUROP EPTIDE FF (NPFF) RECEPTORS 审中-公开
标题翻译：喹诺酮类和喹诺酮类作为神经病毒（NPFF）受体的配体
公开(公告)号：WO2003026667A1
公开(公告)日：2003-04-03
申请号：PCT/US2002/030259
申请日：2002-09-24
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION
发明人： KAWAKAMI, Joel, K. , KONKEL, Michael, J. , BOTEJU, Lakmal, W. , WETZEL, John, M. , NOBLE, Stewart, A. , WAN, Honghe
IPC分类号： A61K31/517
CPC分类号： C07D215/38 , A61K31/47 , A61K31/517 , A61K31/519 , C07D239/70 , C07D239/84 , C07D491/04
摘要： This invention provides compounds having the structure formula (I); wherein X= CH, C(CH 3 ) or N; each of R 1 , R 2 , R 3 , R 4 and R 5 is independently H, C 1 -C 10 straight chained or branched alkyl, C 2 -C 10 straight chained or branched alkenyl, C 2 -C 10 straight chained or branched alkynyl, C 3 -C 10 cycloalkyl, substituted or unsubstituted aryl, hydroxy, halogenated ether, nitro, amino, halogen, -CN, -C(=Z)R 6 , -C(=Z)OR 6 , -C(=Z)N(R 6 ) 2' -N(R 6 )-C(=Z)R 6 , -N(R 6 )-C(=Z)N(R) 2 , -OC(=Z)R 6 , -C(=Z)OR 6 OR 6 or SR 6 ; wherein Z is O or S; and wherein R 6 is C 1 -C 10 straight chained or branched alkyl, aryl, (CH 2 ) n Q, C 2 -C 10 alkenyl, C 3 -C 10 cycloalkyl, C 3 -C 10 cycloalkyl, c 5 -c 10 cycloalkenyl, wherein Q is OR 7 , SR 7 , N(R 7 ) 2 or aryl, wherein R 7 is H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, wherein R 2 and R 3 and the carbons to which they are attached form a fused aryl, heteroaryl, C 5 -C 10 cyclic alkyl or heterocyclic alkyl ring; or wherein R 3 and R 4 and the carbons to which they are attached form a fused aryl, heteroaryl, cyclic alkyl or heterocyclic alkyl ring; and wherein each alkyl, alkenyl, alkynyl and alkoxy group is optionally substituted with a substituent independently selected from R a , where R a is 1) hydroxy, 2) C 1 -C 10 a1koxy, 3) halogen, 4) nitro, 5) amino, 6) CF 3 , or 7) carboxy, and each cycloa1kyl group is optionally substituted with a substituent independently selected from R b , where R b is 1) a group selected from R a , 2) C 1 -C 7 alkyl, 3) C 2 -C 7 alkenyl, 4) C 2 -C 7 alkynyl or 5) cyclic C 1 -C 10 alkyl, and each aryl is optionally substituted with R 1 . This invention also provides methods of treating pain, urge incontinence; as well as methods of preparing the compounds.
摘要翻译：本发明提供具有结构式（I）的化合物; 其中X = CH，C（CH 3）或N; R 1，R 2，R 3，R 4和R 5各自独立地为H，C 1 -C 10直链或支链烷基，C 2 -C 10直链或支链烯基，C 2 -C 10直链或支链炔基，C 3 -C 10环烷基，取代或未取代的芳基，羟基，卤代醚，硝基，氨基，卤素，-CN，-C（= Z）R6，-C（= Z）OR6，-C（= Z）N（R6） C（= Z）R6，-N（R6）-C（= Z）N（R）2，-OC（= Z）R6，-C（= Z）OR6 OR6或SR6; 其中Z是O或S; 其中R 6是C 1 -C 10直链或支链烷基，芳基，（CH 2）nQ，C 2 -C 10烯基，C 3 -C 10环烷基，C 3 -C 10环烷基，C 5 -C 10环烯基，其中Q是OR 7，SR 7，N ）2或芳基，其中R 7为H，烷基，烯基，炔基，环烷基，环烯基，芳基，其中R 2和R 3及其连接的碳形成稠合芳基，杂芳基，C 5 -C 10环烷基或杂环烷基环 ; 或其中R 3和R 4及其连接的碳原子形成稠合的芳基，杂芳基，环烷基或杂环烷基环; 并且其中每个烷基，烯基，炔基和烷氧基任选地被独立地选自Ra的取代基取代，其中R a是1）羟基，2）C 1 -C 10亚烷氧基，3）卤素，4）硝基，5）氨基，6） CF 3或7）羧基，并且每个环烷基任选被独立地选自Rb的取代基取代，其中Rb是1）选自Ra的基团，2）C 1 -C 7烷基，3）C 2 -C 7烯基，4）C 2 -C 7炔基或5）环状C 1 -C 10烷基，并且每个芳基任选被R 1取代。本发明还提供了治疗疼痛，急迫性尿失禁的方法; 以及制备化合物的方法。

29. 发明申请

WO1997026853A2 DNA ENCODING GALANIN GALR2 RECEPTORS AND USES THEREOF 审中-公开
标题翻译： DNA编码GALANIN GALR2受体及其用途
公开(公告)号：WO1997026853A2
公开(公告)日：1997-07-31
申请号：PCT/US1997001301
申请日：1997-01-24
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , SMITH, Kelli, E. , GERALD, Christophe, P., G. , WEINSHANK, Richard, L. , LINEMEYER, David , BRANCHEK, Theresa , FORRAY, Carlos
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K00/00
CPC分类号： C12P21/02 , A01K2217/05 , A61K38/00 , A61K39/00 , A61K48/00 , C07K14/72
摘要： This invention provides isolated nucleic acids encoding mammalian galanin receptors, isolated galanin receptor proteins, vectors comprising isolated nucleic acid encoding a mammalian galanin receptor, cells comprising such vectors, antibodies directed to a mammalian galanin receptor, nucleic acid probes useful for detecting nucleic acid encoding a mammalian galanin receptor, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding a mammalian galanin receptor, nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian galanin receptor, as well as methods of determining binding of compounds to mammalian galanin receptors.
摘要翻译：本发明提供了编码哺乳动物甘丙肽受体的分离的核酸，分离的甘丙肽受体蛋白，包含编码哺乳动物甘丙肽受体的分离的核酸的载体，包含这种载体的细胞，针对哺乳动物甘丙肽受体的抗体，用于检测编码哺乳动物甘丙肽受体，与编码哺乳动物甘丙肽受体的核酸的唯一序列互补的反义寡核苷酸，表达编码正常或突变型哺乳动物甘丙肽受体的DNA的非人转基因动物，以及确定化合物与哺乳动物甘丙肽受体结合的方法。

30. 发明申请

WO1997019682A1 ARYL SULFONAMIDE AND SULFAMIDE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： ARYL SULFONAMIDE和SULFAMIDE衍生物及其用途
公开(公告)号：WO1997019682A1
公开(公告)日：1997-06-05
申请号：PCT/US1996019085
申请日：1996-11-27
申请人： SYNAPTIC PHARMACEUTICAL CORPORATION , ISLAM, Imadul , DHANOA, Daljit, S. , FINN, John, M. , DU, Ping , GLUCHOWSKI, Charles , JEON, Yoon, T.
发明人： SYNAPTIC PHARMACEUTICAL CORPORATION
IPC分类号： A61K31/18
CPC分类号： C07D405/12 , C07C311/18 , C07C311/29 , C07C311/39 , C07C2601/14 , C07C2602/10 , C07D207/48 , C07D211/96 , C07D215/06 , C07D215/54 , C07D217/26 , C07D241/44
摘要： This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
摘要翻译：本发明涉及新的芳基磺酰胺和磺酰胺化合物，它们选择性地结合并抑制人Y5受体的活性。本发明还涉及这些化合物用于治疗哺乳障碍如肥胖症，神经性厌食症，神经性贪食症和异常病症如性/生殖障碍，抑郁症，癫痫发作，高血压，脑出血，充血性心力衰竭或睡眠障碍和用于治疗任何可能使用Y5受体拮抗作用的疾病。

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