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1. 发明申请

WO2011087713A3 SUBSTITUTED HEXAHYDROCHROMENO [3, 4 - B] PYRROLES WITH AFFINITY FOR THE SEROTONIN RECEPTOR (5-HT) FAMILY 审中-公开
标题翻译：取代四氢呋喃并[3，4-B]吡咯烷酮受体（5-HT）家族的亲和力
公开(公告)号：WO2011087713A3
公开(公告)日：2011-10-27
申请号：PCT/US2010060938
申请日：2010-12-17
申请人： CEPHALON INC , ALLWEIN SHAWN P , MORTON GEORGE C , ROSSE GERARD C , WANG YI
发明人： ALLWEIN SHAWN P , MORTON GEORGE C , ROSSE GERARD C , WANG YI
IPC分类号： C07D491/052 , A61K31/4439 , A61P1/00 , A61P3/00 , A61P25/00
CPC分类号： C07D491/052
摘要： This application relates to tricyclic compounds of Formula (I), including all stereoisomeric forms, all mixtures of stereoisomeric forms, and salts of these compounds. This application also relates to compositions comprising compounds of Formula (I), stereoisomeric forms, all mixtures of stereoisomeric forms, and salts thereof and uses therefor.
摘要翻译：本申请涉及式（I）的三环化合物，包括所有立体异构形式，立体异构形式的所有混合物和这些化合物的盐。本申请还涉及包含式（I）的化合物，立体异构形式，立体异构形式的所有混合物及其盐的组合物和用途。

2. 发明申请

WO2011087712A3 TRICYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译： TRICYCLIC衍生物及其药物用途和组合物
公开(公告)号：WO2011087712A3
公开(公告)日：2011-09-29
申请号：PCT/US2010060937
申请日：2010-12-17
申请人： CEPHALON INC , BACON EDWARD R , BAILEY THOMAS R , DUNN DEREK D , HOSTETLER GREG A , MCHUGH ROBERT J , MORTON GEORGE C , ROSSE GERARD C , SALVINO JOSEPH M , SUNDAR BABU G , TRIPATHY RABINDRANATH
发明人： BACON EDWARD R , BAILEY THOMAS R , DUNN DEREK D , HOSTETLER GREG A , MCHUGH ROBERT J , MORTON GEORGE C , ROSSE GERARD C , SALVINO JOSEPH M , SUNDAR BABU G , TRIPATHY RABINDRANATH
IPC分类号： C07D491/048 , A61K31/4355 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , C07D491/153 , C07D491/20 , C07D513/04
CPC分类号： C07D491/153 , C07D491/048 , C07D491/20 , C07D513/04
摘要： This application relates to tricyclic compounds of Formula (I), including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula (I) and uses therefore.
摘要翻译：本申请涉及式（I）的三环化合物，包括所有立体异构体，立体异构体的混合物及其盐。本申请还涉及包含式（I）化合物的组合物及其用途。

3. 发明申请

WO2004072102A3 BENZENE ACETAMIDE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：苯乙烯类化合物可用作丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004072102A3
公开(公告)日：2005-02-03
申请号：PCT/US2004003962
申请日：2004-02-10
申请人： SQUIBB BRISTOL MYERS CO , BISACCHI GREGORY S , TREUNER UWE D , MORTON GEORGE C
发明人： BISACCHI GREGORY S , TREUNER UWE D , MORTON GEORGE C
IPC分类号： A61K31/47 , A61K31/497 , A61K31/501 , A61K31/53 , C07C237/20 , C07C271/20 , C07D217/06 , C07D217/12 , C07D217/22 , C07D401/12 , C07K20060101
CPC分类号： C07D217/22 , C07C237/20 , C07C271/20 , C07D217/06 , C07D401/12
摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, or prodrugs thereof, are useful as serine protease inhibitors, wherein X is OH, O(alkyl), O(aryl), O(arylalkyl), NR5(aryl), or NR5(arylalkyl); W is hydrogen or (CR7R8)q-W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R5, R6, R7, and R16 are as defined in the specification.
摘要翻译：具有式（I）化合物及其药学上可接受的盐，水合物或前药可用作丝氨酸蛋白酶抑制剂，其中X是OH，O（烷基），O（芳基），O（芳基烷基），NR 5 ）或NR 5（芳基烷基）; W是氢或（CR7R8）q-W1; W1是氢或与R6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，以及R1，R2，R3，R5，R6，R7，和R 16如说明书中所定义。

4. 发明申请

WO2004072101A3 PHENYLGLYCINE DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：苯乙烯衍生物有效用作丝氨酸蛋白酶抑制剂
公开(公告)号：WO2004072101A3
公开(公告)日：2005-03-24
申请号：PCT/US2004003961
申请日：2004-02-10
申请人： SQUIBB BRISTOL MYERS CO , GLUNZ PETER W , BISACCHI GREGORY S , MORTON GEORGE C , HOLUBEC ALEXANDRA A , PRIESTLEY E SCOTT , ZHANG XIAOJUN , TREUNER UWE D
发明人： GLUNZ PETER W , BISACCHI GREGORY S , MORTON GEORGE C , HOLUBEC ALEXANDRA A , PRIESTLEY E SCOTT , ZHANG XIAOJUN , TREUNER UWE D
IPC分类号： A61K31/416 , A61K31/4184 , A61K31/42 , A61K31/472 , A61K31/4725 , A61K31/517 , C07C311/51 , C07D217/02 , C07D217/06 , C07D217/22 , C07D231/56 , C07D233/36 , C07D235/04 , C07D235/30 , C07D239/72 , C07D239/94 , C07D261/20 , C07D277/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07K20060101
CPC分类号： C07D231/56 , C07C311/51 , C07D217/02 , C07D217/06 , C07D217/22 , C07D233/36 , C07D235/30 , C07D239/94 , C07D261/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is NR6S(O)pR16; W is hydrogen or (CR7R8)q- W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3 , R6, R7, and R16 are as defined in the specification.
摘要翻译：具有式（I）化合物或其立体异构体或药学上可接受的盐或其水合物可用作因子VIIa抑制剂，其中X为NR 6 S（O）p R 16; W是氢或（CR7R8）q-W1; W1是氢或与R6的键; Z是5元杂芳基，5至6元杂环基或环烷基，9至10元双环芳基或杂芳基，或6元芳基或杂芳基，以及R1，R2，R3，R6，R7和R16 如本说明书中所定义。

5. 发明申请

WO02079146A3 COMPOUNDS USEFUL AS MODULATORS OF MELANOCORTIN RECEPTORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 审中-公开
标题翻译：有用的化合物作为MELANOCORTIN受体的调节剂和包含其的药物组合物
公开(公告)号：WO02079146A3
公开(公告)日：2003-02-06
申请号：PCT/US0206581
申请日：2002-03-02
申请人： SQUIBB BRISTOL MYERS CO , YU GUIXUE , MACOR JOHN , HERPIN TIMOTHY , LAWRENCE R MICHAEL , MORTON GEORGE C , RUEL REJEAN , POINDEXTER GRAHAM S , RUEDIGER EDWARD H , THIBAULT CARL
发明人： YU GUIXUE , MACOR JOHN , HERPIN TIMOTHY , LAWRENCE R MICHAEL , MORTON GEORGE C , RUEL REJEAN , POINDEXTER GRAHAM S , RUEDIGER EDWARD H , THIBAULT CARL
IPC分类号： C07D233/64 , A61K31/4178 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4747 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/527 , A61K31/537 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K38/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/14 , A61P5/16 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/14 , A61P17/16 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/06 , A61P31/18 , A61P31/20 , A61P33/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07D498/10 , C07K5/06 , C07K5/078 , A61K31/44 , A61K31/445 , A61K31/505 , C07D403/14
CPC分类号： C07D401/12 , A61K38/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07K5/06139 , C07K5/06191
摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is formula (II), X is N or CH, W is -NR16R17, -NR16C(=O)R22, -NR16CO2R22, -OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulators of melanocortin receptors, particularly MC-1R and MC-4R.
摘要翻译：式（I）化合物及其药学上可接受的盐，水合物和前药，其中E为式（II），X为N或CH，W为-NR16R17，-NR16C（= O）R22，-NR16CO2R22， -OR23或说明书中定义的杂芳基或杂环基，R1至R12，R16，R17，R22，R23，x，y和z如说明书中所定义，可用作黑皮质素受体的调节剂，特别是 MC-1R和MC-4R。

6. 发明申请

WO9967192A3 PROCESS FOR THE SOLID PHASE SYNTHESIS OF ALDEHYDE, KETONE, OXIME, AMINE, HYDROXAMIC ACID AND alpha , beta -UNSATURATED CARBOXYLIC ACID AND ALDEHYDE COMPOUNDS 审中-公开
标题翻译：醛，酮，OXIME，胺，羟基酸和α，β-受体羧酸和醛类化合物的固相合成方法
公开(公告)号：WO9967192A3
公开(公告)日：2000-04-06
申请号：PCT/US9914251
申请日：1999-06-23
申请人： AVENTIS PHARM PROD INC , SALVINO JOSEPH M , MORTON GEORGE C , MASON HELEN J , LABAUDINIERE RICHARD F
发明人： SALVINO JOSEPH M , MORTON GEORGE C , MASON HELEN J , LABAUDINIERE RICHARD F
IPC分类号： C07C45/61 , C07C45/00 , C07C45/41 , C07C45/45 , C07C45/51 , C07C45/65 , C07C47/228 , C07C47/277 , C07C47/546 , C07C47/55 , C07C49/213 , C07C49/807 , C07C51/353 , C07C57/42 , C07C209/00 , C07C209/30 , C07C209/40 , C07C209/42 , C07C209/66 , C07C211/03 , C07C231/10 , C07C231/12 , C07C233/33 , C07C233/87 , C07C239/08 , C07C239/20 , C07C249/08 , C07C251/54 , C07C259/06 , C07C259/08 , C07C259/10 , C07C269/06 , C07C271/18 , C07C315/04 , C07C317/44 , C07C317/46 , C07D307/33 , C07D311/68 , C07D311/82 , C07D313/12 , C08F8/00 , C08F12/26 , C40B40/14 , C40B50/00 , G01N24/00 , C08G63/44
CPC分类号： C07D307/33 , C07B2200/11 , C07C45/00 , C07C45/004 , C07C45/41 , C07C45/45 , C07C45/516 , C07C51/09 , C07C209/00 , C07C209/40 , C07C209/42 , C07C209/66 , C07C239/08 , C07C259/06 , C07C259/08 , C07C259/10 , C07C315/04 , C07D311/68 , C07D311/82 , C07D313/12 , C08F8/00 , C08F8/30 , C08F2810/30 , C08J7/12 , G01N24/00 , C07C49/213 , C07C49/807 , C07C47/228 , C07C47/277 , C07C47/55 , C07C47/23 , C07C317/44 , C07C57/42 , C08F212/08 , C08F8/34 , C08F8/10 , C08F8/18 , C08F8/06 , C08F112/14 , C08F8/02
摘要： This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
摘要翻译：本发明涉及用于固相合成醛，酮，肟，胺，异羟肟酸和α，β-不饱和羧酸和醛化合物的方法以及用于其的聚合羟胺树脂化合物。

7. 发明专利

HK1174919A1 TRICYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 未知
公开(公告)号：HK1174919A1
公开(公告)日：2013-06-21
申请号：HK13102198
申请日：2013-02-21
申请人： CEPHALON INC
发明人： BACON EDWARD R , BAILEY THOMAS R , DUNN DEREK D , HOSTETLER GREG A , MCHUGH ROBERT J , MORTON GEORGE C , ROSSE GERARD C , SALVINO JOSEPH M , SUNDAR BABU G , TRIPATHY RABINDRANATH
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.

8. 发明专利

MX2012007339A DERIVADOS TRICICLICOS Y SU USO FARMACEUTICO Y COMPOSICIONES. 未知
公开(公告)号：MX2012007339A
公开(公告)日：2012-07-20
申请号：MX2012007339
申请日：2010-12-17
申请人： CEPHALON INC
发明人： MORTON GEORGE C , ROSSE GERARD C , ALLWEIN SHAWN P , WANG YI
IPC分类号： C07D491/052 , A61K31/4439 , A61P1/00 , A61P3/00 , A61P25/00
摘要： Esta solicitud se refiere a compuestos tricíclicos de la Fórmula I: (Ver Formula) incluyendo todas las formas estereoisoméricas, todas las mezclas de formas estereoisoméricas y sales de estos compuestos. Esta aplicación también se refiere a composiciones que comprenden compuestos de la Fórmula 1, formas estereoisoméricas, todas las mezclas de formas estereoisoméricas y sus sales y sus usos.

9. 发明专利

ES2523766T3 Hexahidrocromeno[3,4-b]pirroles sustituidos con afinidad por la familia de los receptores de serotonina (5-HT) 未知
公开(公告)号：ES2523766T3
公开(公告)日：2014-12-01
申请号：ES10801042
申请日：2010-12-17
申请人： CEPHALON INC
发明人： ALLWEIN SHAWN P , MORTON GEORGE C , ROSSE GERARD C , WANG YI
IPC分类号： C07D491/052 , A61K31/4439 , A61P1/00 , A61P3/00 , A61P25/00
摘要： Un compuesto que tiene la estructura de fórmula II**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que: R3 está seleccionado de H, alquilo (C1-C6), hidroxialquilo (C1-C6), haloalquilo (C1-C6), alquil (C1-C6)alcoxi (C1- C6), CO-alquilo (C1-C6), CONH-alquilo (C1-C6), CO2-alquilo (C1-C6), SO2-alquilo (C1-C6), SO2NH-alquilo (C1-C6), CO-arilo (C6-C10), CONH-arilo (C6-C10), CO2-arilo (C6-C10), SO2-arilo (C6-C10), SO2NH-arilo (C6-C10), arilo (C6- C10), alquil (C1-C6)arilo (C6-C10), cicloalquilo (C3-C10), CO-cicloalquilo (C3-C10), CONH-cicloalquilo (C3-C10), CO2- cicloalquilo (C3-C10), SO2-cicloalquilo (C3-C10), SO2NH-cicloalquilo (C3-C10), alquil (C1-C6)cicloalquilo (C3-C10), CO-alquil (C1-C6)cicloalquilo (C3-C10), CONH-alquil (C1-C6)cicloalquilo (C3-C10), CO2-alquil (C1-C6)-cicloalquilo (C3-C10), SO2-alquil (C1-C6)-cicloalquilo (C3-C10), SO2NH-alquil (C1-C6)cicloalquilo (C3-C10), heterocicloalquilo (C2-C9), alquil (C1-C6)heterocicloalquilo (C2-C9), CONH-alquil (C1-C6)heterocicloalquilo (C2-C9), CO-alquil (C1- C6)heterocicloalquilo (C2-C9), CO2-alquil (C1-C6)heterocicloalquilo (C2-C9), SO2-alquil (C1-C6)heterocicloalquilo (C2-C9), SO2NH-alquil (C1-C6)heterocicloalquilo (C2-C9), heteroarilo (C5-C9), CO-heteroarilo (C5-C9), CONH30 heteroarilo (C5-C9), CO2-heteroarilo (C5-C9), SO2-heteroarilo (C5-C9), SO2NH-heteroarilo (C5-C9), alquil (C1- C6)heteroarilo (C5-C9), CO-alquil (C1-C6)-heteroarilo (C5-C9), CONH-alquil (C1-C6)-heteroarilo (C5-C9), SO2-alquil (C1-C6)-heteroarilo (C5-C9), SO2NH-alquil (C1-C6)heteroarilo (C5-C9) y CO2-alquil (C1-C6)heteroarilo (C5-C9), en el que cualquiera de los anteriores, excepto H, está opcionalmente sustituido con uno o más sustituyentes y a condición de que heteroarilo (C5-C9) no sea 1,3,4-triazol opcionalmente sustituido en cualquiera de alquil (C1- C6)heteroarilo (C5-C9), CO-alquil (C1-C6)-heteroarilo (C5-C9), CONH-alquil (C1-C6)heteroarilo (C5-C9) y CO2- alquil (C1-C6)heteroarilo (C5-C9); Y es CH2 o O; X está ausente, O, NR4 o alquilo (C1-C4); R4 es H o alquilo (C1-C6); m es 1 ó 2; y Z está seleccionado de cicloalquilo (C3-C10), alquil (C1-C6)cicloalquilo (C3-C10), heterocicloalquilo (C2-C9), alquil (C1-C6)heterocicloalquilo (C2-C9), arilo (C6-C10), alquil (C1-C6)arilo (C6-C10), heteroarilo (C5-C9) y alquil (C1- C6)heteroarilo (C5-C9), en el que cualquiera de los anteriores está opcionalmente sustituido con uno o más sustituyentes; o Z es NR8R9 en la que R8 y R9 están seleccionados cada uno independientemente de H, alquilo (C1-C6), cicloalquilo (C3-C10) , a l q u i l ( C1-C6)cicloalquilo (C3-C10), arilo (C6-C10), alquil (C1-C6)arilo (C6-C10), heterocicloalquilo (C2-C9), alquil (C1-C6)heterocicloalquilo (C2-C9), heteroarilo (C5-C9) y alquil (C1-C6)heteroarilo (C5-C9), en el que cualquiera de los anteriores, con la excepción de H, está opcionalmente sustituido con uno o más sustituyentes y a condición de que R8 y R9 no sean ambos H; o R8 y R9 se toman conjuntamente para formar un anillo de heterocicloalquilo (C2-C9) que está opcionalmente sustituido con uno o más sustituyentes; y en los que dichos sustituyentes están seleccionados del grupo que consiste en H, halógeno, alquilo (C1-C6), alcoxi (C1-C6), alcoxi (C1-C6)alquilo (C1-C4), COOH, formilo, acilo (C1-C6), haloalquilo (C1-C6), haloalcoxi (C1- C6), OH, aminoalquilo (C1-C6), hidroxialquilo (C1-C6), NO2, CN, NH2, mono- o di-alquil (C1-C6)amino, oxo, arilo (C6-C10), alquil (C1-C6)arilo (C6-C10), ariloxi (C6-C10), alcoxi (C1-C6)arilo (C6-C10), heteroarilo (C5-C9), heteroariloxi (C5-C9), alquil (C1-C6)heteroarilo (C5-C9), alcoxi (C1-C6)heteroarilo (C5-C9), alcoxi (C1-C6)carbonilo, cicloalquilo (C3-C10), cicloalquiloxi (C3-C10), cicloalquil (C3-C10)alcoxi (C1-C6), alquil (C1-C6)cicloalquilo (C3-C10), heterocicloalquilo (C2-C9), heterocicloalquiloxi (C2-C9), alquil (C1-C6)heterocicloalquilo (C2-C9), alcoxi (C1- C6)heterocicloalquilo (C2-C9), alquil (C1-C6)alcoxi (C1-C6)carbonilo, alquil (C1-C6)sulfinilo, alquil (C1-C6)sulfonilo, mono- y di-alquil (C1-C6)aminocarbonilo, aciltio (C1-C6) y aciloxi (C1-C6).

10. 发明专利

HK1174918A1 SUBSTITUTED HEXAHYDROCHROMENO[3,4-B]PYRROLES WITH AFFINITY FOR THE SEROTONIN RECEPTOR (5-HT) FAMILY 5-(5-HT)[3,4-B] 未知
公开(公告)号：HK1174918A1
公开(公告)日：2013-06-21
申请号：HK13102197
申请日：2013-02-21
申请人： CEPHALON INC
发明人： ALLWEIN SHAWN P , MORTON GEORGE C , ROSSE GERARD C , WANG YI
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101

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