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公开(公告)号：EP1053235A1
公开(公告)日：2000-11-22
申请号：EP99905632.8
申请日：1999-02-02
IPC分类号： C07D413/06 , A61K31/42 , C07D471/04
CPC分类号： C07D413/06 , C07D471/04
摘要： This invention provides compounds of Formula (1), wherein R1 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, benzyloxy, trifluoromethyl, chloro, bromo, or fluoro; a dashed line indicates an optional bond; X is NR4, or no atom; R2 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, cycloalkylalkyl wherein the cycloalkyl moiety is 3-8 cabon atoms and the alkyl moiety is 1-6 carbon atoms, aryl of 5-12 carbon atoms, or arylalkyl of 6-12 carbon atoms; R3 is aryl of 5-12 carbon atoms, arylalkyl of 6-12 carbon atoms, or heteroaryl of 5-12 ring atoms; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of psychosis (e.g. schizophrenia), anxiety, depression and related CNS disorders and other conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and memory deficits associated with Alzheimer's disease and other dementias.
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公开(公告)号：EP0713490A1
公开(公告)日：1996-05-29
申请号：EP94925809.0
申请日：1994-08-10
CPC分类号： C07D498/18
摘要： This invention provides C-22 substituted rapamycin derivatives of formulas (Ia) or (Ib) or a pharmaceutically acceptable salt thereof or a proline analogue thereof or a pharmaceutically acceptable salt of a proline analogue thereof which are useful for inducing immunosuppression and treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphomas and hyperproliferative vascular disorders.
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公开(公告)号：EP0730598A1
公开(公告)日：1996-09-11
申请号：EP95903559.0
申请日：1994-11-18
CPC分类号： C07D498/18
摘要： A compound of structure (I) wherein R and R1 are each, independently, (A), (B), or hydrogen; R?2 and R3¿ are each, independently, alkyl, arylalkyl, or R?2 and R3¿ may be taken together to form a cycloalkyl ring; R4 is a heterocyclic radical which may be optionally substituted; R5 is alkyl or arylalkyl; R?6 and R7¿ are taken together to form a saturated heterocyclic ring which may be optionally substituted; k=0-1; m=0-1; n=1-6; with the proviso that R and R1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppresive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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5.发明授权HETEROCYCLIC ESTERS OF RAPAMYCIN AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 失效雷帕霉素和杂环酯含有YOU的药物组合物
公开(公告)号：EP0730597B1
公开(公告)日：2001-03-07
申请号：EP95901258.4
申请日：1994-11-16
IPC分类号： C07D498/18 , A61K31/435
CPC分类号： C07D498/18
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公开(公告)号：EP0713490B1
公开(公告)日：1998-02-25
申请号：EP94925809.9
申请日：1994-08-10
IPC分类号： C07D498/18 , A61K31/445 , A61K31/40 , C07F7/18
CPC分类号： C07D498/18
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公开(公告)号：EP0794955A1
公开(公告)日：1997-09-17
申请号：EP95941467.0
申请日：1995-11-22
CPC分类号： C07D498/18
摘要： A compound of structure (I), wherein R and R1 are each, independently, (a), (b), or hydrogen; R?2 and R3¿ are each, independently, alkyl, arylalkyl, or R?2 and R3¿ may be taken together to form a cycloalkyl ring; R4 is a heterocyclic N-oxide radical, which may be optionally substituted; R5 is alkyl or arylalkyl; R?6 and R7¿ are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k = 0-1, m = 0.1; n = 1-6; with the previso that R and R1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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8.发明公开HETEROCYCLIC ESTERS OF RAPAMYCIN AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 失效雷帕霉素和杂环酯含有YOU的药物组合物
公开(公告)号：EP0730597A1
公开(公告)日：1996-09-11
申请号：EP95901258.0
申请日：1994-11-16
CPC分类号： C07D498/18
摘要： A compound of structure (I), wherein R and R1 are each, independently, (a) or hydrogen; R2 is a heterocyclic radical which may be optionally substituted; n = 0-6; with the proviso that R and R1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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公开(公告)号：EP0794955B1
公开(公告)日：2001-07-25
申请号：EP95941467.3
申请日：1995-11-22
IPC分类号： C07D498/18 , A61K31/435
CPC分类号： C07D498/18
摘要： A compound of structure (I), wherein R and R1 are each, independently, (a), (b), or hydrogen; R?2 and R3¿ are each, independently, alkyl, arylalkyl, or R?2 and R3¿ may be taken together to form a cycloalkyl ring; R4 is a heterocyclic N-oxide radical, which may be optionally substituted; R5 is alkyl or arylalkyl; R?6 and R7¿ are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k = 0-1, m = 0.1; n = 1-6; with the previso that R and R1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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公开(公告)号：EP0730598B1
公开(公告)日：1999-06-09
申请号：EP95903559.3
申请日：1994-11-18
IPC分类号： C07D498/18 , A61K31/435 , A61K31/71
CPC分类号： C07D498/18
摘要： A compound of structure (I) wherein R and R1 are each, independently, (A), (B), or hydrogen; R?2 and R3¿ are each, independently, alkyl, arylalkyl, or R?2 and R3¿ may be taken together to form a cycloalkyl ring; R4 is a heterocyclic radical which may be optionally substituted; R5 is alkyl or arylalkyl; R?6 and R7¿ are taken together to form a saturated heterocyclic ring which may be optionally substituted; k=0-1; m=0-1; n=1-6; with the proviso that R and R1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppresive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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