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1. 发明申请

WO2012129491A1 TRPV3 MODULATORS 审中-公开
标题翻译： TRPV3调制器
公开(公告)号：WO2012129491A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/030317
申请日：2012-03-23
申请人： ABBOTT LABORATORIES , CLAPHAM, Bruce , COX, Philip, B. , DART, Michael, J. , GOMTSYAN, Arthur , JINKERSON, Tammie, K. , KEDDY, Ryan, G. , KORT, Michael, E. , KYM, Philip, R. , MATULENKO, Mark , SCHMIDT, Robert, G., Jr. , VILLAMIL, Clara, I. , VOIGHT, Eric, A. , WOLLER, Kevin, R.
发明人： CLAPHAM, Bruce , COX, Philip, B. , DART, Michael, J. , GOMTSYAN, Arthur , JINKERSON, Tammie, K. , KEDDY, Ryan, G. , KORT, Michael, E. , KYM, Philip, R. , MATULENKO, Mark , SCHMIDT, Robert, G., Jr. , VILLAMIL, Clara, I. , VOIGHT, Eric, A. , WOLLER, Kevin, R.
IPC分类号： C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/44 , A61K31/505 , C07D211/06 , C07D239/28 , C07D239/30 , A61P25/00
CPC分类号： C07D213/61 , A61K31/44 , A61K31/505 , C07D211/06 , C07D213/38 , C07D213/64 , C07D213/643 , C07D213/74 , C07D239/26 , C07D239/28 , C07D239/30 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要： Disclosed herein are modulators of TRPV3 of formula (I) wherein X 1 , X 2 , R 1 , R 2 , R x , and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
摘要翻译：本文公开了式（I）的TRPV3的调节剂，其中X1，X2，R1，R2，Rx和n如说明书中所定义。还提出了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和障碍的方法。

2. 发明申请

WO2010045402A1 TRPV1 ANTAGONISTS 审中-公开
标题翻译： TRPV1拮抗剂
公开(公告)号：WO2010045402A1
公开(公告)日：2010-04-22
申请号：PCT/US2009/060734
申请日：2009-10-15
申请人： ABBOTT LABORATORIES , GOMTSYAN, Arthur R. , VOIGHT, Eric A. , BAYBURT, Erol K. , CHEN, Jun , DAANEN, Jerome F. , DIDOMENICO, Stanley, Jr. , KORT, Michael E. , KYM, Philip R. , MCDONALD, Heath A. , PERNER, Richard J. , SCHMIDT, Robert G.
发明人： GOMTSYAN, Arthur R. , VOIGHT, Eric A. , BAYBURT, Erol K. , CHEN, Jun , DAANEN, Jerome F. , DIDOMENICO, Stanley, Jr. , KORT, Michael E. , KYM, Philip R. , MCDONALD, Heath A. , PERNER, Richard J. , SCHMIDT, Robert G.
IPC分类号： C07D311/74 , C07D405/12 , A61K31/33 , A61P19/02
CPC分类号： C07D405/12 , C07D311/74
摘要： Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：本文公开了式（I）化合物或其药学上可接受的盐，溶剂合物，前药，前药盐或其组合，其中R1，R2，R3，R4和m在说明书中定义。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

3. 发明申请

WO2007137107A3 INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME 审中-公开
标题翻译：二乙酰胆碱酯酶1型酶的抑制剂
公开(公告)号：WO2007137107A3
公开(公告)日：2008-01-10
申请号：PCT/US2007069112
申请日：2007-05-17
申请人： ABBOTT LAB , IYENGAR RAJESH R , ZHAO GANG , FREEMAN JENNIFER C , GAO JU , JUDD ANDREW S , KYM PHILIP R , LYNCH JOHN K , MULHERN MATHEW M , SOUERS ANDREW J
发明人： IYENGAR RAJESH R , ZHAO GANG , FREEMAN JENNIFER C , GAO JU , JUDD ANDREW S , KYM PHILIP R , LYNCH JOHN K , MULHERN MATHEW M , SOUERS ANDREW J
IPC分类号： C07C211/22 , A61K31/155 , A61K31/17 , A61K31/381 , A61K31/4164 , A61K31/435 , A61P3/04 , C07C275/30 , C07C279/18 , C07C335/16 , C07D213/55 , C07D213/75 , C07D277/28 , C07D333/36
CPC分类号： C07C335/22 , C07C229/46 , C07C275/30 , C07C275/32 , C07C275/38 , C07C279/28 , C07C2601/08 , C07C2601/14 , C07D213/55 , C07D213/75 , C07D277/30 , C07D333/22 , C07D333/36 , C07D401/04 , C07D401/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 3 , X, Q, Z, A, D, m, and n are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 3，X，Q，Z，A，D，m和n如本文所定义。还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。

4. 发明申请

WO2008134693A1 INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME 审中-公开
标题翻译：二乙酰胆碱酯酶1型酶的抑制剂
公开(公告)号：WO2008134693A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061951
申请日：2008-04-30
申请人： ABBOTT LABORATORIES , JUDD, Andrew S , MULHERN, Mathew M , IYENGAR, Rajesh R , KYM, Philip R , SOUERS, Andrew J
发明人： JUDD, Andrew S , MULHERN, Mathew M , IYENGAR, Rajesh R , KYM, Philip R , SOUERS, Andrew J
IPC分类号： C07D277/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D493/08 , A61K31/427 , A61K31/44 , A61P3/04 , A61P3/10
CPC分类号： C07D417/04 , C07D213/40 , C07D213/75 , C07D277/28 , C07D277/82 , C07D405/04 , C07D417/12 , C07D417/14 , C07D498/08
摘要： The present invention relates to compounds of formula (I): wherein Q, G 1 , G 2 , and G 3 , are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译：本发明涉及式（I）的化合物：其中Q，G 1，G 2和G 3在本文中定义。还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。

5. 发明申请

WO2008067257A8 INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME 审中-公开
公开(公告)号：WO2008067257A8
公开(公告)日：2008-06-05
申请号：PCT/US2007/085543
申请日：2007-11-26
申请人： ABBOTT LABORATORIES , SOUERS, Andrew J. , GAO, Ju , HANSEN, Todd Matthew , IYENGAR, Rajesh R. , KYM, Philip R. , LIU, Bo X , PEI, Zhonghua , YEH, Vince , ZHAO, Gang
发明人： SOUERS, Andrew J. , GAO, Ju , HANSEN, Todd Matthew , IYENGAR, Rajesh R. , KYM, Philip R. , LIU, Bo X , PEI, Zhonghua , YEH, Vince , ZHAO, Gang
IPC分类号： A61K31/17 , C07C229/40 , A61P1/16 , A61P3/00
摘要： Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.

6. 发明申请

WO2007137103A3 INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME 审中-公开
标题翻译：二乙酰胆碱酯酶1型酶的抑制剂
公开(公告)号：WO2007137103A3
公开(公告)日：2008-01-24
申请号：PCT/US2007069104
申请日：2007-05-17
申请人： ABBOTT LAB , KYM PHILIP R , ZHAO GANG
发明人： KYM PHILIP R , ZHAO GANG
IPC分类号： C07C275/26 , A61K31/17 , A61K31/381 , A61K31/4164 , A61K31/4406 , A61P3/04 , C07C275/30 , C07C275/34 , C07C275/40 , C07D213/75 , C07D317/66 , C07D333/36
CPC分类号： C07C275/42 , C07C2601/08 , C07C2601/14 , C07D213/75 , C07D317/66 , C07D333/36
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, n, p and q are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， >，R 5，R 6，m，n，p和q在本文中定义。还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。

7. 发明申请

WO0243648A2 COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR II 审中-公开
标题翻译：化合物在GLUCOCORTICOID受体II中有活性
公开(公告)号：WO0243648A2
公开(公告)日：2002-06-06
申请号：PCT/IB0102302
申请日：2001-11-28
申请人： KAROBIO AB , ABBOTT LAB , PELCMAN BENJAMIN , GUSTAFSSON ANNIKA , KYM PHILIP R
发明人： PELCMAN BENJAMIN , GUSTAFSSON ANNIKA , KYM PHILIP R
IPC分类号： C07D295/08 , A61K31/192 , A61K31/36 , A61K31/426 , A61K31/4409 , A61K31/4453 , A61K31/5375 , A61P1/04 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/46 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/02 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/00 , A61P27/06 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07C59/90 , C07C69/76 , C07C205/34 , C07C205/35 , C07C323/12 , C07D213/30 , C07D277/24 , C07D295/092 , C07D317/62 , A61K
CPC分类号： C07D213/30 , C07C59/90 , C07C69/76 , C07C205/35 , C07C323/12 , C07D277/24 , C07D295/088 , C07D317/62
摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein X is selected from: CH2, CHYR , CHYC(O)R , C=O, C=S, and C=NOR ,; Y is selected from: O, S, and NR ; R is selected from: COOH and heteroaryl; R and R are independently of each other selected from: hydrogen, halogen, and C1-6 alkyl, provided that one of R or R is other than hydrogen; R is selected from: C1-6-alkyl, C2-6 alkenyl, C2-6-alkynyl, halogen, (R )(R )N, R C(Z)N(R ), R OC(Z)N(R ), (R )(R )NC(Z)N(R ),R S(O)2N(R ), (R )(R )NS(O)2N(R ), and R SC (Z)N(R );R is selected from: (i) C1-6-alkyl which is substituted by a group selected from A, provided that A is not halogen; (ii) C7-12-alkyl, C2-12-alkenyl and C2-12-alkynyl; (iii) C1-12-alkyl, where one or more carbon atoms are replaced by Y, and where one or more carbons are optionally substituted by a group selected from A, provided that if more than one carbon is replaced by Y, the said Y groups are not directly connected to each other; R is selected from: C1-12-alkyl, C3-8-cycloalkyl, C3-8-heterocycloalkyl, C2-6-alkenyl, and C2-6-alkynyl, aryl, and heteroaryl; R is optionally selected from hydrogen; R , R , R and R are independently of each other selected from: hydrogen, C1-6-alkyl, C3-8-cycloalkyl, C2-6-alkenyl, C2-6-alkynyl, and C3-8-heterocycloalkyl, aryl and heteroaryl; or where any pair of R , R , R and R together with the atom or atoms to which they are bound form a ring having 3-7 ring members; or pharmaceutically acceptable salts, stereoisomers or prodrugs thereof.
摘要翻译：本发明涉及作为肝选择性糖皮质激素受体拮抗剂的新型化合物，制备这些化合物的方法，以及在治疗和调节代谢中尤其是降低血糖水平使用这些化合物的方法。所谓的化合物是根据式1的化合物：其中X选自：CH 2，CHYR 7，CHYC（O）R 7，C = O，C = S和C = NOR 8， ; Y选自：O，S和NR 8; R 1选自：COOH和杂芳基; R 2和R 3彼此独立地选自：氢，卤素和C 1-6烷基，条件是R 2或R 3中的一个不是氢; R 4选自：C 1-6 - 烷基，C 2-6烯基，C 2-6炔基，卤素，（R 9）（R 10）N，R 8 C（Z）N （R 11），R 8 OC（Z）N（R 11），（R 9）（R 10）NC（Z）N（R 11） S（O）2 N（R 11），（R 9）（R 10）NS（O）2 N（R 11）和R 8 SC（Z） 11））; R 5选自：（i）被选自A的基团取代的C 1-6 - 烷基，条件是A不是卤素; （ii）C 7-12 - 烷基，C 2-12 - 烯基和C 2-12 - 炔基; （iii）C 1-12 - 烷基，其中一个或多个碳原子被Y代替，并且其中一个或多个碳任选地被选自A的基团取代，条件是如果多于一个碳被Y替代，则所述 Y组不直接相连; R 6选自：C 1-12 - 烷基，C 3-8 - 环烷基，C 3-8 - 杂环烷基，C 2-6 - 烯基和C 2-6 - 炔基，芳基和杂芳基; R 7任选地选自氢; R 8，R 9，R 10和R 11彼此独立地选自：氢，C 1-6 - 烷基，C 3-8 - 环烷基，C 2-6烯基，C 2-6 - 炔基和C 3-8 - 杂环烷基，芳基和杂芳基; 或者其中任何一对R 8，R 9，R 10和R 11与它们所连接的原子或原子一起形成具有3-7个环成员的环; 或其药学上可接受的盐，立体异构体或前药。

8. 发明申请

WO2012019315A1 NOVEL TRPV3 MODULATORS 审中-公开
标题翻译：新型TRPV3调制器
公开(公告)号：WO2012019315A1
公开(公告)日：2012-02-16
申请号：PCT/CN2010/001213
申请日：2010-08-10
申请人： ABBOTT LABORATORIES , ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD , BAYBURT, Erol, K. , CLAPHAM, Bruce , COX, Phil, B. , DAANEN, Jerome, F. , GOMTSYAN, Arthur , KORT, Michael, E. , KYM, Philip, R. , VOIGHT, Eric, A.
发明人： BAYBURT, Erol, K. , CLAPHAM, Bruce , COX, Phil, B. , DAANEN, Jerome, F. , GOMTSYAN, Arthur , KORT, Michael, E. , KYM, Philip, R. , VOIGHT, Eric, A.
IPC分类号： C07D213/30 , C07D239/26 , C07D405/06 , C07D405/08 , A61K31/4402 , A61K31/4433 , A61K31/505 , A61P25/00 , A61P29/00
CPC分类号： C07D213/30 , C07D213/50 , C07D239/26 , C07D401/12 , C07D405/12
摘要： Disclosed herein are modulators of TRPV3 of formula (I), wherein G 1 , X 1 , X 2 , X 3 , X 4 , X 5 , G 2 , Z 1 , R a , R b , u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
摘要翻译：本文公开了式（I）的TRPV3的调节剂，其中G1，X1，X2，X3，X4，X5，G2，Z1，Ra，Rb，u和p如说明书中所定义。还提出了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和障碍的方法。

9. 发明申请

WO2009055749A1 2-AMINOOXAZOLE DERIVATIVES AS TRPVL ANTAGONISTS USEFUL FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的TRPVL拮抗剂的2-氨基苯并噻唑衍生物
公开(公告)号：WO2009055749A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/081229
申请日：2008-10-25
申请人： ABBOTT LABORATORIES , PERNER, Richard J. , KOENIG, John R. , DIDOMENICO, Stanley, Jr. , BAYBURT, Erol, K. , DAANEN, Jerome, F. , GOMTSYAN, Arthur, R. , KORT, Michael E. , KYM, Philip R. , VASUDEVAN, Anil , SCHMIDT, Robert, G. , VOIGHT, Eric
发明人： PERNER, Richard J. , KOENIG, John R. , DIDOMENICO, Stanley, Jr. , BAYBURT, Erol, K. , DAANEN, Jerome, F. , GOMTSYAN, Arthur, R. , KORT, Michael E. , KYM, Philip R. , VASUDEVAN, Anil , SCHMIDT, Robert, G. , VOIGHT, Eric
IPC分类号： C07D263/48 , C07D413/04 , C07D413/12 , A61K31/421 , A61P29/00
CPC分类号： C07D413/12 , C07D263/48 , C07D413/04
摘要： Compounds of formula (I) wherein R 1 , R 2 , R 4 , and W are defined in the description are TRPV1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：在描述中定义R1，R2，R4和W的式（I）化合物是具有CNS穿透的TRPV1拮抗剂。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

10. 发明申请

WO2009023539A2 AMIDE DERIVATIVES AS TRPV1 ANTAGONISTS 审中-公开
标题翻译：酰胺衍生物作为TRPV1拮抗剂
公开(公告)号：WO2009023539A2
公开(公告)日：2009-02-19
申请号：PCT/US2008/072560
申请日：2008-08-08
申请人： ABBOTT LABORATORIES , KYM, Philip R , BROWN, Brian S , DAANEN, Jerome F , GOMTSYAN, Arthur R , KEDDY, Ryan G , KORT, Michael , MATULENKO, Mark A , VASUDEVAN, Anil
发明人： KYM, Philip R , BROWN, Brian S , DAANEN, Jerome F , GOMTSYAN, Arthur R , KEDDY, Ryan G , KORT, Michael , MATULENKO, Mark A , VASUDEVAN, Anil
IPC分类号： C07D401/04 , A61K31/4545
CPC分类号： C07D401/04
摘要： The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，前药，前药盐或其组合，其中R1，R2和R3在本说明书中定义。还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

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