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1. 发明公开

EP2571353A4 MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF 有权
标题翻译： 5-HT受体调节剂及其使用方法
公开(公告)号：EP2571353A4
公开(公告)日：2014-01-22
申请号：EP10851903
申请日：2010-11-19
申请人： ABBVIE INC , ABBOTT GMBH & CO KG
发明人： AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , DJURIC STEVAN W , WILSON NOEL S , TURNER SEAN C , KRUGER ALBERT W , RELO ANA-LUCIA , SHEKHAR SHASHANK , WELCH DENNIE S , ZHAO HONGYU , GANDARILLA JORGE , GASIECKI ALAN F , LI HUANQIU , THOMPSON CHRISTINA M , ZHANG MIN
IPC分类号： A01N43/00 , A01N43/46 , A61K31/55
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04

2. 发明公开

EP2576564A4 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：大环内酯类C蛋白酶抑制剂
公开(公告)号：EP2576564A4
公开(公告)日：2014-01-22
申请号：EP11792997
申请日：2011-06-07
申请人： ABBVIE INC , ENANTA PHARM INC
发明人： CHEN HUI-JU , MCDANIEL KEITH F , GREEN BRIAN E , SHANLEY JASON P , KRUGER ALBERT W , GANDARILLA JORGE , WELCH DENNIE S , CINK RUSSELL D , GAI YONGHUA , WANG GUOQIANG , OR YAT SUN
IPC分类号： A61K31/498 , A61K31/407 , A61P31/14 , C07D487/04
CPC分类号： C07K5/081 , C07D487/04

4. 发明专利

AU2015224388B2 Modulators of 5-HT receptors and methods of use thereof 未知
公开(公告)号：AU2015224388B2
公开(公告)日：2017-02-02
申请号：AU2015224388
申请日：2015-09-08
申请人： ABBVIE DEUTSCHLAND , ABBVIE INC
发明人： WELCH DENNIE S , ZHAO HONGYU , GANDARILLA JORGE , GASIECKI ALAN F , LI HUANQIU , THOMPSON CHRISTINA M , ZHANG MIN , AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , DJURIC STEVAN W , WILSON NOEL S , TURNER SEAN C , KRUGER ALBERT W , RELO ANA-LUCIA , SHEKHAR SHASHANK
IPC分类号： C07D487/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/00 , C07D491/04 , C07D495/04
摘要： Modulators of 5-HT Receptors and Methods of Use Thereof The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) A R 4 R5 y3 Y1--Y2 (1) wherein R , R 2, R', R4, R , A, Y , Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds. (10d';n172 11-IP

5. 发明专利

ES2535490T3 Preparación de moduladores de receptores 5-HT 未知
公开(公告)号：ES2535490T3
公开(公告)日：2015-05-12
申请号：ES13161013
申请日：2010-05-20
申请人： ABBVIE INC , ABBVIE DEUTSCHLAND
发明人： WELCH DENNIE S , AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , DJURIC STEVAN W , WILSON NOEL S , TURNER SEAN C , KRUGER ALBERT W , RELO ANA-LUCIA , SHEKAR SHASHANK , ZHAO HONGYU , GANDARILLA JORGE , GASIECKI ALAN F , LI HUANQIU , THOMPSON CHRISTINA M , ZHANG MIN
IPC分类号： C07D487/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/00 , C07D491/04 , C07D495/04
摘要： Un proceso para preparar un compuesto de fórmula (1-5):**Fórmula** o una sal farmacéuticamente aceptable del mismo, donde A se selecciona entre el grupo que consiste en**Fórmula** X1 es N o CR9; X2 es N o CR10; X3 es N o CR11; X4 es N o CR12; con la condición de que solamente uno o dos de X1, X2, X3, o X4 pueden ser N; R9, R10, R11, R12, R13, R14, R15 y R16 cada uno es independientemente hidrógeno, alquilo, alquenilo, alquinilo, halógeno, ciano, -G1, -G2, -NO2, -OR1a, -OC(O)R1a, -OC(O)N(Rb)(R3a), -SR1a, -S(O)R2a, -S(O)2R2a, - S(O)2N(Rb)(R3a), -C(O)R1a, -C(O)G3, -C(O)OR1a, -C(O)N(Rb)(R3a), -N(Rb)(R3a), -N(RaC(O)R1a, -N(Ra)C(O)O(R1a), - N(Ra)C(O)N(Rb)(R3a), -N(Ra)S(O)2(R2a), -(CR4aR5a)m-NO2-(CR4aR5a)m-OR1a, -(CR4aR5a)m-OC(O)R1a, -(CR4aR5a)m- OC(O)N(Rb)(R3a), -(CR4aR5a)m-SR1a, -(CR4aR5a)m-S(O)R2a, -(CR4aR5a)m-S(O)2R2a, -(CR4R5a)S(O)2N(Rb)(R3a), -(CR4aR5a)m(O)R1a, -(CR4aR5a)m-C(O)OR1a, -(CR4aR5a)m-C(O)N(Rb)(R3a), -(CR4aR5a)m-N(Rb)(R3a), -(CR4aR5a)m- N(Ra) C(O)R1a, -(CR4aR5a)m-N(Ra)C(O)O(R1a), -(CR4aR5a)m-N(Ra)C(O)N(Rb)(R3a), -(CR4aR5a)m-G1, -CR4a>=CR5a-G1, -(CR4aR5a)m-G2, -CR4a>=CR5a-G2, -CR6a-C(R7a)2, cianoalquilo, haloalquilo, (v), (vi), (vii) o (viii); donde**Fórmula** R1a y R3a, en cada caso, cada uno es independientemente hidrógeno, alquilo, haloalquilo G1, -(CR4aR5a)m-G1, G2, o -(CR4aR5a)m-G2; R2a, en cada caso, es independientemente alquilo, haloalquilo, G1, o -(CR4aR5a)m-G1; R6a es alquilo o haloalquilo; R7a en cada caso, es independientemente hidrógeno, alquilo, o haloalquilo; R4a y R5a, en cada caso, cada uno es independientemente hidrógeno, halógeno, alquilo, o haloalquilo; G1, en cada caso, es independientemente arilo o heteroarilo, donde cada G1 está independientemente sin sustituir o sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados entre el grupo que consiste en alquilo, alquenilo, alquinilo, halógeno, ciano, -NO2, -OR1b, -OC(O)R1b, -OC(O)N(Rb)(R3b), -SR1b, -S(O)R2b, -S(O)2R2b, - S(O)2N(Rb)(R3b), -C(O)R1b, -C(O)OR1b, -C(O)N(Rb)(R3b), -N(Rb)(R3b), -N(Ra)C(O)R1b, -N(Ra)C(O)O(R1b), - N(Ra)C(O)N(Rb(R3b), -(CR4bR5b)m-NO2, -N(Rb)S(O)2(R2b), -(CR4bR5b)m-OR1b, -C(OH)[CR4bR5b)m-R4b]2, -(CR4bR5b)m- OCCO)R1b, -(CR4bR5b)m-OC(O)N(Rb)(R3b), -(CR4bR5b)m-SR1b, -(CR4bR5b)m-S(O)R2b, -(CR4bR5b)m-S(O)2R2b, - (CR4bR5b)m-S(O)2N(Rb)(R3b), -(CR4bR5b)m-C(O)R1b, -(CR4bR5b)m-C(O)OR1b, -(CR4bR5b)m-C(O)N(Rb)(R3b), - (CR4bR5b)m-N(Rb)(R3b), -(CR4bR5b)m-(Ra)C(O)R1b, -(CR4bR5b)m-N(Ra)C(O)O(R1b), -(CR4bR5b)m- N(Ra)C(O)N(Rb)(R3b), -(CR4bR5b)m-N(Rb)S(O)2(R2b), cianoalquilo, y haloalquilo; G2 es cicloalquilo, cicloalquenilo, o heterociclo sin sustituir o sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados entre el grupo que consiste en alquilo, alquenilo, alquinilo, halógeno, ciano, oxo, -SR1b, -S(O)R2b- S(O)2R2b, -S(O)2N(Rb)(R3b), -C(O)R1b, -C(O)OR1b, -C(O)N(Rb)(R3b), -N(Rb)(R3b), -N(Ra)C(O)R1b, - N(Ra)C(O)O(R1b), -N(Ra)C(O)N(Rb)(R3b), -(CR4bR5b)m-NO2, -N(Rb)S(O)2(R2b), -(CR4bR5b)m-OR1b, -(CR4bR5b)m- OC(O)R1b, -(CR4bR5b)m-OC(O)N(Rb)(R3b), -(CR4bR5b)m-SR1b, -(CR4bR5b)m-S(O)R2b, -(CR4bR5b)m-S(O)2R2b, - (CR4bR5b)m-S(O)2N(Rb)(R3b), -(CR4bR5b)m-C(O)R1b, -(CR4bR5b)m-C(O)OR1b, -(CR4bR5b)m-C(O)N(Rb)(R3b), - (CR4bR5b)m-(Rb)(R3b), -(CR4bR5b)m-(Ra)C(O)R1b, -(CR4bR5b)m-N(Ra)C(O)O(R1b), -(CR4bR5b)m-N(Ra)C(O)N(Rb)(R3b), -(CR4bR5b)m-N(Rb)S(O)2(R2b), cianoalquilo, y haloalquilo; Ra y Rb, en cada caso, cada uno es independientemente hidrógeno, alquilo, o haloalquilo; R1b y R3b, en cada caso, cada uno es independientemente hidrógeno, alquilo, o haloalquilo; R2b, en cada caso, es independientemente alquilo o haloalquilo; R4b y R5b, en cada caso, cada uno es independientemente hidrógeno, halógeno, alquilo, o haloalquilo; m, en cada caso, es independientemente 1, 2, 3, 4 o 5; G3 es un anillo heterocíclico unido al resto carbonilo adyacente a través de un átomo de nitrógeno contenido dentro del heterociclo; q es 1 o 2; o R9 y R10, R10 y R11, R11 y R12 o R13 y R14 tomados en conjunto con los átomos de carbono a los que están unidos forman un anillo de fenilo, cicloalquilo, heterociclo, o heteroarilo sustituido o sin sustituir.

6. 发明专利

CA2801584A1 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 未知
公开(公告)号：CA2801584A1
公开(公告)日：2011-12-15
申请号：CA2801584
申请日：2011-06-07
申请人： ABBVIE INC , ENANTA PHARM INC
发明人： CHEN HUI-JU , MCDANIEL KEITH F , GREEN BRIAN E , SHANLEY JASON P , KRUGER ALBERT W , GANDARILLA JORGE , WELCH DENNIE S , CINK RUSSELL D , GAI YONGHUA , WANG GUOQIANG , OR YAT SUN
IPC分类号： C07D487/04 , A61K31/407 , A61K31/498 , A61P31/14
摘要： The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.

7. 发明专利

CA2800161C MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF 未知
公开(公告)号：CA2800161C
公开(公告)日：2017-12-12
申请号：CA2800161
申请日：2010-11-19
申请人： ABBVIE INC , ABBOTT GMBH & CO KG
发明人： AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , DJURIC STEVAN W , WILSON NOEL S , TURNER SEAN C , KRUGER ALBERT W , RELO ANA-LUCIA , SHEKHAR SHASHANK , WELCH DENNIE S , ZHAO HONGYU , GANDARILLA JORGE , GASIECKI ALAN F , LI HUANQIU , THOMPSON CHRISTINA M , ZHANG MIN
IPC分类号： C07D487/04 , A61K31/407 , A61K31/55 , A61P3/00 , A61P25/00 , C07D471/14 , C07D491/044 , C07D491/147 , C07D495/14 , C07D513/04
摘要： The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

8. 发明专利

NZ618902A Modulators of 5-ht receptors and methods of use thereof 未知
公开(公告)号：NZ618902A
公开(公告)日：2015-06-26
申请号：NZ61890210
申请日：2010-05-20
申请人： ABBVIE INC , ABBVIE DEUTSCHLAND
发明人： WELCH DENNIE S , SHEKHAR SHASHANK , AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , RELO ANA-LUCIA , TURNER SEAN C , GANDARILLA JORGE , WILSON NOEL S , GASIECKI ALAN F , ZHANG MIN , DJURIC STEVAN W , ZHAO HONGYU , KRUGER ALBERT W , THOMPSON CHRISTINA M , LI HUANQIU
IPC分类号： C07D487/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/00 , C07D225/00 , C07D491/04 , C07D495/04
摘要： Disclosed is a compound of formula I, such as (3aS,10bS)-8-chloro-2-methyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo[3,4-c]azepin-6(10bH)-one and (3aS,10bS)-8-chloro-2-methyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo[3,4-c]azepin-6(10bH)-one, which is useful for treating disorders associated with 5HT receptors. Also disclosed is a process for making such compounds. Also disclosed is a process for the preparation of the compounds.

9. 发明专利

ES2423668T3 Moduladores de receptores 5-HT y métodos de uso de los mismos 未知
公开(公告)号：ES2423668T3
公开(公告)日：2013-09-23
申请号：ES10720502
申请日：2010-05-20
申请人： ABBOTT LAB , ABBOTT GMBH & CO KG , ABBVIE INC
发明人： WELCH DENNIE S , AKRITOPOULOU-ZANZE IRINI , BRAJE WILFRIED , DJURIC STEVAN W , WILSON NOEL S , TURNER SEAN C , KRUGER ALBERT W , RELO ANA-LUCIA , SHEKHAR SHASHANK , ZHAO HONGYU , GANDARILLA JORGE , GASIECKI ALAN F , LI HUANQIU , THOMPSON CHRISTINA M , ZHANG MIN
IPC分类号： C07D487/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/00 , C07D491/04 , C07D495/04
摘要： Un compuesto de fórmula (I):**Fórmula** o una sal farmacéuticamente aceptable del mismo,donde A está seleccionado entre el grupo que consiste en R1, R3, R4, y R5 están seleccionados independientemente entre el grupo que consiste en hidrógeno, alquenilo, alquilo, haloalquilo, G1, G2, -(CR4aR5a)m-G1, y -(CR4aR5a)m-G2; R4a y R5a, en cada caso, cada uno es independientemente hidrógeno, halógeno, alquilo, o haloalquilo; G1, en cada caso, es independientemente arilo o heteroarilo, donde cada G1 está independientemente sin sustituir osustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados entre el grupo que consiste en alquilo, alquenilo, alquinilo,halógeno, ciano, -NO2, -OR1b, -OC(O)R1b, -OC(O)N(Rb)(R3b), -SR1b, -S(O)R2b, -S(O)2R2b, -S(O)2N(Rb)(R3b), -C(O)R1b,-C(O)OR1b, -C(O)N(Rb)(R3b), -N(Rb)(R3b), -N(Ra)C(O)R1b, -N(Ra)C(O)O(R1b), -N(Ra)C(O)N(Rb)(R3b), -(CR4bR5b)m-NO2,-N(Rb)S(O)2(R2b), -(CR4bR5b)m-OR1b, -C(OH)[(CR4bR5b)m-R4b]2, -(CR4bR5b)m-OC(O)R1b, -(CR4bR5b)m-OC(O)N(Rb)(R3b), -(CR4bR5b)m-SR1b, -(CR4bR5b)m-S(O)R2b, -(CR4bR5b)m-S(O)2R2b, -(CR4bR5b)m-S(O)2N(Rb)(R3b),-(CR4bR5b)m-C(O)R1b, -(CR4bR5b)m-C(O)OR1b, -(CR4bR5b)m-C(O)N(Rb)(R3b), -(CR4bR5b)m-N(Rb)(R3b), -(CR4bR5b)m-N(Ra)C(O)R1b, -(CR4bR5b)m-N(Ra)C(O)O(R1b), -(CR4bR5b)m-N(Ra)C(O)N(Rb)(R3b), -(CR4bR5b)m-N(Rb)S(O)2(R2b),cianoalquilo, y haloalquilo.

10. 发明专利

NZ603792A Modulators of 5-ht receptors and methods of use thereof 未知
公开(公告)号：NZ603792A
公开(公告)日：2015-07-31
申请号：NZ60379210
申请日：2010-11-19
申请人： ABBVIE INC , ABBVIE DEUTSCHLAND
发明人： KRUGER ALBERT W , GASIECKI ALAN F , TURNER SEAN C , ZHANG MIN , LI HUANQIU , SHEKHAR SHASHANK , DJURIC STEVAN W , AKRITOPOULOU-ZANZE IRINI , WELCH DENNIE S , ZHAO HONGYU , RELO ANA-LUCIA , GANDARILLA JORGE , BRAJE WILFRIED , THOMPSON CHRISTINA M , WILSON NOEL S
IPC分类号： A01N43/00 , A01N43/46 , A61K31/55
摘要： Disclosed herein are aryl- and heteroaryl-fused decahydropyrroloazepine, octahydro-oxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds. Specific embodiments of the derivatives of formula (I) include the following: trans-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[c]pyrrolo[3,4-e]azepin-6(10bH)-one; trans-2-benzyl-5-(naphthalen-1-ylsulfonyl)-1,2,3,3a,4,5,6,10b-octahydrobenzo[c]pyrrolo[3,4-e]azepine; and cis-8-amino-2-benzyl-1,2,3,3a,4,5-hexahydrobenzo[e]pyrrolo[3,4-c]azepin-6(10bH)-one.

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