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1. 发明授权

US6410532B2 Substituted 1,2,3,4-tetrahydronaphthalene derivatives 失效
标题翻译：取代的1,2,3,4-四氢萘衍生物
公开(公告)号：US6410532B2
公开(公告)日：2002-06-25
申请号：US90200001
申请日：2001-07-10
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： C07D295/12 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61P3/04 , A61P9/00 , A61P9/10 , A61P13/12 , A61P15/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P35/00 , A61P43/00 , C07C237/24 , C07D211/22 , C07D211/26 , C07D211/34 , C07D295/135 , C07D295/155 , C07D295/192 , C07D295/20 , C07D295/205
CPC分类号： C07D295/192 , C07C237/24 , C07C2602/10 , C07D295/135 , C07D295/155 , C07D295/205
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula IwhereinX is N or CH;Y is NR2CH2, CH2-NR2, NR2-CO, CO-NR2 or NR2SO2 wherein R2 is H or C1-6 alkyl;R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl;R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substitutedn is 0-4;R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above,as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及具有式I的新的哌啶基或哌嗪基取代的-1,2,3,4-四氢萘衍生物，其中X是N或CH; Y是NR2CH2，CH2-NR2，NR2-CO，CO-NR2或NR2SO2，其中 R2是H或C1-6烷基; R1是H，C1-C6烷基或C3-C6环烷基; R3是C1-C6烷基，C3-C6环烷基或（CH2）n-芳基，其中芳基是苯基或杂芳环含有一个或两个选自N，O和S且可被单取代或二取代的杂原子为0-4; R9为C1-C6烷基，C3-C6环烷基，OCF3，OCHF2，OCH2F，卤素，CN，CF3 ，OH，C1-C6烷氧基，C1-C6烷氧基-C1-C6烷基，NR6R7，SO3CH3，SO3CF3，SO2NR6R7，含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环，其中取代基）是（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，为游离碱形式的（R） - 对映体，（S） - 对映异构体或外消旋物或其药学上可接受的盐，其制备方法，含有所述治疗活性的药物组合物化合物和所述活性化合物在治疗中的用途。

2. 发明专利

DE69825912T2 未知
公开(公告)号：DE69825912T2
公开(公告)日：2005-09-01
申请号：DE69825912
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , FLORVALL LENNART , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： C07D295/14 , A61K31/445 , A61K31/451 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61P1/04 , A61P3/04 , A61P9/10 , A61P9/12 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/32 , A61P25/34 , A61P29/00 , A61P35/00 , C07D211/26 , C07D211/34 , C07D295/135 , C07D295/155
摘要： The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR 2 wherein R 2 is H or C 1 -C 6 alkyl; R 3 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl or (CH 2 ) n -aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R 4 and/or R 5 , wherein R 4 and R 5 are as defined in the specification; and R 9 is H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, OCF 3 , OCHF 2 , OCH 2 F, halogen, CN, CF 3 , OH, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy-C 1 -C 6 alkyl, NR 6 R 7 , SO 3 CH 3 , SO 3 CF 3 , SO 2 NR 6 R 7 , an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C 1 -C 6 alkyl; or COR 8 ; wherein R 6 , R 7 and R 8 are as defined in the specification. The invention further relates to a process for the preparation of the intermediates.

3. 发明专利

DE69822490T2 未知
公开(公告)号：DE69822490T2
公开(公告)日：2005-03-03
申请号：DE69822490
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/352 , A61K31/353 , A61K31/495 , A61K31/535 , A61P25/18 , A61P25/22 , A61P25/24 , A61K31/35
摘要： PCT No. PCT/SE98/01600 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13876 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having the formula I wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having the formula II wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alky, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is R4 and R5 independently are H or C1-C4 alkyl as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

4. 发明专利

PT1014986E 未知
公开(公告)号：PT1014986E
公开(公告)日：2004-10-29
申请号：PT98944376
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： THORBERG SETH-OLOV , BERG STEFAN , ROSS SVANTE
IPC分类号： A61K45/00 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00
摘要： PCT No. PCT/SE98/01602 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13878 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a monoamine oxidase inhibitor and a second component (b) which is selective h5-HT1B antagonist or partial agonist having the formula I wherein X is CH2, O; Y is CONH, NHCO; R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl; R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen; R3 is R4 and R5 independently are H or C1-C4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

5. 发明专利

SI1021183T1 A COMBINATION OF A SELECTIVE 5-HT1A ANTAGONIST AND A SELECTIVE h5-HT1B ANTAGONIST OR PARTIAL AGONIST 未知
公开(公告)号：SI1021183T1
公开(公告)日：2004-08-31
申请号：SI9830629
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/35 , A61K31/495 , A61K31/535 , A61P25/24

6. 发明专利

PT1021183E 未知
公开(公告)号：PT1021183E
公开(公告)日：2004-07-30
申请号：PT98944374
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： THORBERG SETH-OLOV , BERG STEFAN , ROSS SVANTE
IPC分类号： A61K31/352 , A61K31/353 , A61K31/495 , A61K31/535 , A61P25/18 , A61P25/22 , A61P25/24 , A61K31/35
摘要： PCT No. PCT/SE98/01600 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13876 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having the formula I wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having the formula II wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alky, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is R4 and R5 independently are H or C1-C4 alkyl as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

7. 发明专利

AT261728T 未知
公开(公告)号：AT261728T
公开(公告)日：2004-04-15
申请号：AT98944374
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/352 , A61K31/353 , A61K31/495 , A61K31/535 , A61P25/18 , A61P25/22 , A61P25/24 , A61K31/35
摘要： PCT No. PCT/SE98/01600 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13876 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having the formula I wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having the formula II wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alky, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is R4 and R5 independently are H or C1-C4 alkyl as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

8. 发明专利

AT255098T 未知
公开(公告)号：AT255098T
公开(公告)日：2003-12-15
申请号：AT98944377
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , NYLOEF MARTIN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/496 , A61K31/5377 , A61K31/551 , A61P1/14 , A61P3/04 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/32 , A61P25/34 , A61P29/00 , C07D311/58 , C07D405/12 , A61K31/495 , A61K31/535
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR 2 CH 2 , CH 2 NR 2 , NR 2 CO, CONR 2 , NR 2 SO 2 or NR 2 CONR 2 wherein R 2 is H or C 1 -C 6 alkyl; R 1 is H, C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl; R 3 is C 1 -C 6 alkyl, C 3 -C 6 cycoalkyl or (CH 2 ) n -aryl, wherein aryl is a heteromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R 4 and/or R 5 ; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.

9. 发明专利

PT1014985E 未知
公开(公告)号：PT1014985E
公开(公告)日：2003-10-31
申请号：PT98944375
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/495 , A61K31/535 , A61K31/55 , A61K31/496 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24
摘要： PCT No. PCT/SE98/01601 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13877 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT1B antagonist or partial agonist having the formula I wherein X is CH2, O; Y is CONH, NHCO; R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl; R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen; R3 is R4 and R5 independently are H or C1-C4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

10. 发明专利

EE04141B1 未知
公开(公告)号：EE04141B1
公开(公告)日：2003-10-15
申请号：EEP200000141
申请日：1998-09-09
申请人： ASTRAZENECA AB
发明人： BERG STEFAN , ROSS SVANTE , THORBERG SETH-OLOV
IPC分类号： A61K31/496 , A61K31/495 , A61K31/535 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24
摘要： PCT No. PCT/SE98/01601 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13877 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is selective h5-HT1B antagonist or partial agonist having the formula I wherein X is CH2, O; Y is CONH, NHCO; R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl; R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen; R3 is R4 and R5 independently are H or C1-C4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.

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