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公开(公告)号:US06541638B2
公开(公告)日:2003-04-01
申请号:US09907135
申请日:2001-07-17
申请人: Johannes Aebi , Denise Blum , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Bernd Michael Loeffler , Ulrike Obst , Sabine Wallbaum
发明人: Johannes Aebi , Denise Blum , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Bernd Michael Loeffler , Ulrike Obst , Sabine Wallbaum
IPC分类号: A61K31454
CPC分类号: C07D401/12 , C07D207/12 , C07D207/16 , C07D207/48 , C07D403/12 , C07D413/12
摘要: The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.
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公开(公告)号:US20070099985A1
公开(公告)日:2007-05-03
申请号:US11634573
申请日:2006-12-06
IPC分类号: A61K31/381 , C07D333/72
CPC分类号: C07D417/12 , C07D231/12 , C07D233/56 , C07D249/08 , C07D275/04 , C07D275/06 , C07D333/54 , C07D409/12
摘要: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译: 本发明涉及异离子OSC抑制剂。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症,高脂血症,动脉硬化,血管疾病,霉菌病,胆结石,肿瘤和/或过度增殖性疾病相关的疾病,以及治疗和 /或预防糖耐量异常和糖尿病。
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公开(公告)号:US07189756B2
公开(公告)日:2007-03-13
申请号:US10881427
申请日:2004-06-30
申请人: Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
发明人: Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
IPC分类号: A61K31/40 , C07D207/04
CPC分类号: C07D401/12 , C07D207/36 , C07D207/48 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
摘要翻译: 本发明涉及可用作金属蛋白酶抑制剂的吡咯烷衍生物。 锌蛋白酶,并且其有效治疗与血管收缩相关的疾病状态。
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公开(公告)号:US06858651B2
公开(公告)日:2005-02-22
申请号:US09925188
申请日:2001-08-09
申请人: Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
发明人: Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
IPC分类号: C07D295/08 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/223 , A61K31/255 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/5375 , A61K31/54 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/10 , A61P31/10 , A61P33/00 , A61P35/00 , C07C233/23 , C07C233/74 , C07C235/54 , C07C235/84 , C07C255/57 , C07C269/04 , C07C271/24 , C07C271/52 , C07C271/56 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C291/04 , C07C303/38 , C07C307/08 , C07C307/10 , C07C311/07 , C07C311/13 , C07C311/20 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/22 , C07D205/04 , C07D207/12 , C07D209/42 , C07D211/14 , C07D211/22 , C07D211/44 , C07D211/70 , C07D213/81 , C07D215/36 , C07D233/84 , C07D261/10 , C07D295/092 , C07D295/135 , C07D295/14 , C07D307/38 , C07D309/12 , C07D317/58 , C07D333/24 , C07D333/34 , C07D333/40 , A61K31/14 , C07C43/20
CPC分类号: C07D295/088 , C07C233/23 , C07C233/74 , C07C235/54 , C07C235/84 , C07C255/57 , C07C271/52 , C07C271/56 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C291/04 , C07C307/08 , C07C307/10 , C07C311/07 , C07C311/13 , C07C311/20 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/22 , C07C2601/02 , C07C2601/14 , C07D295/135
摘要: The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译: 本发明涉及可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症,高脂血症,动脉硬化,血管疾病,真菌病,胆结石,肿瘤和/或过度增殖性疾病相关的疾病的氨基环己醇衍生物 ,以及治疗和/或预防糖耐量异常和糖尿病。
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公开(公告)号:US06790860B2
公开(公告)日:2004-09-14
申请号:US10373622
申请日:2003-02-25
申请人: Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
发明人: Johannes Aebi , Daniel Bur , Alexander Chucholowski , Henrietta Dehmlow , Eric Argirios Kitas , Ulrike Obst , Hans Peter Wessel
IPC分类号: C07D20704
CPC分类号: C07D401/12 , C07D207/36 , C07D207/48 , C07D403/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
摘要翻译: 本发明涉及可用作金属蛋白酶抑制剂的吡咯烷衍生物。 锌蛋白酶,并且其有效治疗与血管收缩相关的疾病状态。
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公开(公告)号:US06706751B2
公开(公告)日:2004-03-16
申请号:US10014959
申请日:2001-12-11
申请人: Johannes Aebi , Jean Ackermann , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller , Narendra Panday
发明人: Johannes Aebi , Jean Ackermann , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller , Narendra Panday
IPC分类号: A61P4300
CPC分类号: C07D215/20 , C07D209/08
摘要: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译: 本发明涉及新的二氢吲哚和四氢喹啉衍生物及其药学上可接受的盐和/或其药学上可接受的酯。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症,高脂血症,动脉硬化,血管疾病,霉菌病,胆结石,肿瘤和/或过度增殖性疾病相关的疾病,以及治疗和 /或预防糖耐量异常和糖尿病。
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公开(公告)号:US06683201B2
公开(公告)日:2004-01-27
申请号:US09906214
申请日:2001-07-16
申请人: Jean Ackermann , Johannes Aebi , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller
发明人: Jean Ackermann , Johannes Aebi , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller
IPC分类号: C07C22900
CPC分类号: C07D213/75 , C07C233/29 , C07C233/75 , C07C235/56 , C07C235/84 , C07C255/57 , C07C271/28 , C07C271/58 , C07C275/34 , C07C275/38 , C07C307/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C323/44 , C07C335/18 , C07C335/22 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/42 , C07C2603/18 , C07D207/14 , C07D207/20 , C07D209/42 , C07D211/22 , C07D211/42 , C07D211/46 , C07D211/70 , C07D213/81 , C07D213/82 , C07D215/36 , C07D239/42 , C07D261/10 , C07D295/088 , C07D307/14 , C07D307/52 , C07D317/58 , C07D319/18 , C07D333/24 , C07D333/34 , C07D333/38
摘要: The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译: 本发明涉及式(I)化合物,其中U,Y,V,W,L,X,A 1,A 2,A 3,A 4,A 5和A <6>如说明书和权利要求及其药学上可接受的盐和/或其药学上可接受的酯所定义。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶相关的疾病,例如高胆固醇血症,高脂血症,动脉硬化,血管疾病,真菌病,寄生虫感染,胆结石,肿瘤和/或过度增殖性疾病, 和/或治疗和/或预防糖耐量异常和糖尿病。
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公开(公告)号:US06503907B2
公开(公告)日:2003-01-07
申请号:US09998882
申请日:2001-11-20
申请人: Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Olivier Morand , Narendra Panday , Thomas Weller
发明人: Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Olivier Morand , Narendra Panday , Thomas Weller
IPC分类号: A61K31535
CPC分类号: C07D401/12 , C07D209/08 , C07D403/12 , C07D417/12
摘要: The present invention relates to indole derivatives, dihydroindole derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
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公开(公告)号:US5637771A
公开(公告)日:1997-06-10
申请号:US555054
申请日:1995-11-08
申请人: Johannes Aebi , Philipe Guerry , Synese Jolidon , Olivier Morand
发明人: Johannes Aebi , Philipe Guerry , Synese Jolidon , Olivier Morand
IPC分类号: A61K31/24 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/277 , A61P3/06 , A61P9/10 , C07C211/26 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/46 , C07C225/08 , C07C225/14 , C07C225/16 , C07C225/22 , C07C255/56 , C07C211/27
CPC分类号: C07C225/16 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/277 , C07C217/22
摘要: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.
摘要翻译: 一种降低胆固醇的方法,其包括向需要这种治疗的宿主施用有效量的式I化合物,其中R 1和R 2之一是C 1-7 - 烷基,另一个是C 1-7 - 烷基或C 2 -C -6-链烯基 - 甲基; L是通过O原子任选地键合到苯基的C1-11亚烷基或C2-11亚烯基,或L是1,4-亚苯基; n为0或L为O原子时,n为0或1; Q是C 1-7 - 烷基,C 2-10 - 链烯基或式(III)基团,其中R是H,卤素,CF 3,CN或NO 2; R3和R4是H,C1-4烷基或卤素; R5为H或当R为H时,R5为H或卤素; 或其药学上可接受的酸加成盐,以及某些式I化合物。
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公开(公告)号:US5495048A
公开(公告)日:1996-02-27
申请号:US261615
申请日:1994-06-17
申请人: Johannes Aebi , Philipe Guerry , Synese Jolidon , Olivier Morand
发明人: Johannes Aebi , Philipe Guerry , Synese Jolidon , Olivier Morand
IPC分类号: A61K31/24 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/277 , A61P3/06 , A61P9/10 , C07C211/26 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/46 , C07C225/08 , C07C225/14 , C07C225/16 , C07C225/22 , C07C255/56
CPC分类号: C07C225/16 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/277 , C07C217/22
摘要: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.
摘要翻译: 一种降低胆固醇的方法,其包括向需要这种治疗的宿主施用有效量的式I化合物,其中R 1和R 2之一是C 1-7 - 烷基,另一个是C 1-7 - 烷基或C 2 -C -6-链烯基 - 甲基; L是通过O原子任选地键合到苯基的C1-11亚烷基或C2-11亚烯基,或L是1,4-亚苯基; n为0或L为O原子时,n为0或1; Q是C 1-7 - 烷基,C 2-10 - 链烯基或式(III)基团,其中R是H,卤素,CF 3,CN或NO 2; R3和R4是H,C1-4烷基或卤素; R5为H或当R为H时,R5为H或卤素; 或其药学上可接受的酸加成盐,以及某些式I化合物。
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