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公开(公告)号:US06642389B2
公开(公告)日:2003-11-04
申请号:US10142567
申请日:2002-05-09
申请人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人: Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号: C07D26332
CPC分类号: C07D413/12 , C07D263/32 , C07D413/14
摘要: The present invention relates to novel oxazole compounds which act as PPAR&agr; and PPAR&ggr; agonists and are accordingly useful for the treatment of diseases modulated by PPAR&agr; and PPAR&ggr; such as diabetes.
摘要翻译: 本发明涉及作为PPARα和PPARγ激动剂的新型恶唑化合物,因此可用于治疗由PPARα和PPARγ等调节的疾病如糖尿病。
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公开(公告)号:US06610877B1
公开(公告)日:2003-08-26
申请号:US08904522
申请日:1997-08-01
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: C07C6976
CPC分类号: C07C59/72 , C07C57/50 , C07C63/66 , C07C65/28 , C07C69/618 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2602/10 , C07C2602/12
摘要: Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
摘要翻译: 化学式R 1的化合物是式的残基,R2-R10具有本说明书中给出的含义,可用作药物,特别是用于修复光损伤皮肤,其它皮肤病学条件和肿瘤适应症。
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公开(公告)号:US5726191A
公开(公告)日:1998-03-10
申请号:US735941
申请日:1996-10-23
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: C07D213/79 , A61K31/44 , A61K31/455 , A61K31/57 , A61P17/00 , A61P17/02 , A61P35/00 , A61P43/00 , C07D213/80 , C07D213/803 , C07D215/48 , C07D213/63 , C07D213/70
CPC分类号: C07D213/80 , A61K31/44 , A61K31/455
摘要: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl; R.sup.2 is C.sub.1-6 -alkyl or adamantyl; R.sup.3 is C.sub.1-6 -alkyl or hydroxy; or R.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --; R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy; R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl; R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl; Y is oxygen or sulphur; and n is 3, 4 or 5, and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.
摘要翻译: 式Ⅰ化合物,其中R 1是氢或C 1-6 - 烷基; R2是C1-6烷基或金刚烷基; R3是C1-6烷基或羟基; 或R 2和R 3一起为 - (CR 6 R 7)n - ; R 4是C 2-8 - 烷基,C 2-8 - 烯基,C 2-8 - 炔基,-OCH 2 R 5或C 2-8 - 烷酰基; 当R3为羟基时为氢; R5是C1-6-烷基,C2-6-烯基或C2-6-炔基; R6和R7是氢或C1-6烷基; Y是氧或硫; 并且n为3,4或5,并且式I的羧酸的药学上可用的盐作为视黄酸γ-受体的选择性配体,并且可用于治疗上皮损伤。
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公开(公告)号:US5378705A
公开(公告)日:1995-01-03
申请号:US102609
申请日:1993-08-05
申请人: Michael Klaus , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Mohr , Ekkehard Weiss
IPC分类号: C07C211/10 , C07C317/18 , C07C323/12 , C07C323/25 , C07D295/092 , C07D295/13 , A61K31/38 , C07D279/12
CPC分类号: C07D295/088 , C07C211/10 , C07C317/18 , C07C323/12 , C07C323/25 , C07D295/13 , C07C2102/08 , C07C2102/10
摘要: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
摘要翻译: 式Ⅰ的化合物,其中R 1和R 2各自独立地为低级烷基; 或一起是直链中具有3-5个C原子的亚烷基; 残基R3和R4之一是氢,另一个是氢或低级烷基; R6和R7是氢或低级烷基; R5和R8是氢,低级烷基,低级烷氧基或卤素; X表示-O - , - S - , - SO - , - SO 2 - 或-NR 9; R9是氢,低级烷基或酰基; Y是-S(O)m R 10或-NHet,且其中X是-NR 9 - , - S - , - SO-或-SO 2 - ,以及-N(R 11)2或-OR 12; R10为低级烷基; R 11和R 12是氢,低级烷基或酰基; -NHet是通过N-原子连接的5-8元饱和或不饱和的单环杂环; n为2,3或4,m为0,1或2。 式I的化合物可用作治疗诸如赘生物,皮肤病或皮肤老化的病症的药剂。
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公开(公告)号:US5216148A
公开(公告)日:1993-06-01
申请号:US842662
申请日:1992-02-27
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: A61K31/55 , A61P17/00 , A61P35/00 , A61P43/00 , C07D209/34 , C07D215/38 , C07D215/48 , C07D223/16 , C07D243/12
CPC分类号: C07D223/16 , C07D215/38 , C07D215/48 , C07D243/12
摘要: Described herein are compounds of the formula ##STR1## wherein R.sup.1 signifies hydrogen, lower-alkyl or a cation;R.sup.2 signifies hydrogen, lower-alkyl, lower-alkoxy or halogen;M signifies --CONH-- or --NHCO--;X and Y are each independently selected from the group consisting of >CR.sup.3 R.sup.4 and --CONR.sup.5 --;Z signifies >CR.sup.6 R.sup.7 ;R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are each independently selected from the group consisting of hydrogen and lower-alkyl;R.sup.5 signifies alkyl; andn signifies 0, 1 or 2;provided that at least one of X or Y is --CONR.sup.5 -- which is bonded to the phenyl ring via the N atom.These compounds are useful in the treatment and prophylaxis of neoplasms, dermatoses and aging of the skin.
摘要翻译: 本文描述的是其中R 1表示氢,低级烷基或阳离子的式Ⅰ化合物; R2表示氢,低级烷基,低级烷氧基或卤素; M表示-CONH-或-NHCO-; X和Y各自独立地选自> CR 3 R 4和-CONR 5 - ; Z表示> CR6R7; R3,R4,R6和R7各自独立地选自氢和低级烷基; R5表示烷基; n表示0,1或2; 条件是X或Y中的至少一个是-CONR 5 - 其经由N原子键合到苯环。 这些化合物可用于治疗和预防皮肤赘生物,皮肤病和老化。
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公开(公告)号:US5030765A
公开(公告)日:1991-07-09
申请号:US605204
申请日:1990-10-16
申请人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
发明人: Michael Klaus , Peter Loeliger , Peter Mohr , Ekkehard Weiss
IPC分类号: A61K31/015 , A61K31/035 , C07C13/465 , C07C13/48 , C07C25/24 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/223 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/755 , C07C205/06
CPC分类号: C07C205/06 , A61K31/015 , A61K31/035 , C07C13/465 , C07C13/48 , C07C25/24 , C07C35/32 , C07C35/36 , C07C39/23 , C07C43/215 , C07C43/23 , C07C45/72 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/755
摘要: The present invention is concerned with novel tetrahydronaphthalene and indane derivatives of the formula ##STR1## useful as for combatting dermatoses as well as neoplasmas.
摘要翻译: 本发明涉及用于对抗皮肤病和赘生物的新颖的四氢萘和茚满衍生物。
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公开(公告)号:US4992574A
公开(公告)日:1991-02-12
申请号:US263651
申请日:1988-10-27
申请人: Michael Klaus , Peter Mohr
发明人: Michael Klaus , Peter Mohr
IPC分类号: C07C69/76 , A61K31/015 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/235 , A61P3/06 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/08 , C07C13/39 , C07C15/24 , C07C33/16 , C07C45/46 , C07C45/51 , C07C45/61 , C07C45/68 , C07C47/457 , C07C49/67 , C07C49/697 , C07C49/792 , C07C51/00 , C07C51/353 , C07C63/66 , C07C63/74 , C07C65/19 , C07C65/38 , C07C67/00 , C07C69/94 , C07C231/00 , C07C233/61 , C07C233/65 , C07C235/42 , C07C235/44
CPC分类号: C07C65/19 , C07C33/16 , C07C45/46 , C07C45/513 , C07C45/61 , C07C45/68 , C07C47/457 , C07C49/67 , C07C49/697 , C07C49/792 , C07C63/66 , C07C63/74 , C07C2102/32
摘要: A compound of the formula ##STR1## wherein R.sup.1 is hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino;R.sup.2 is hydrogen, alkyl, akoxy or halogen;R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11 and R.sup.12 independently are hydrogen or lower-alkyl;R.sup.3 and R.sup.5 taken together are methylene or hydroxymethylene;R.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently are hydrogen or lower-alkyl;R.sup.11 and R.sup.12 taken together are oxo or spiro-cyclo-lower alkyl; or R.sup.11 is hydrogen and R.sup.12 is hydroxy or acetoxy; and one of the residues R.sup.13 and R.sup.14 is hydrogen and the other is lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I, which can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis, are described. The compounds of the invention can be prepared by the synthesis of the C(R.sup.13).dbd.C(R.sup.14) double bond according to Wittig from a corresponding bicyclic component and a corresponding monocyclic component and optional subsequent transformation of functional groups.
摘要翻译: 式I的化合物,其中R 1是羟基,低级烷氧基,氨基,一或二低级烷基氨基; R2是氢,烷基,烷氧基或卤素; R3,R4,R5,R6,R11和R12独立地为氢或低级烷基; R3和R5一起是亚甲基或羟基亚甲基; R 7,R 8,R 9和R 10独立地为氢或低级烷基; R 11和R 12一起是氧代或螺环 - 低级烷基; 或R 11为氢,R 12为羟基或乙酰氧基; 残基R13和R14之一是氢,另一个是低级烷基或三氟甲基,以及式I的羧酸的生理上相容的盐,其可以用作药物,特别是用于治疗肿瘤,痤疮和牛皮癣 ,被描述。 本发明的化合物可以通过根据Wittig从相应的双环组分和相应的单环组分合成C(R 13)= C(R 14)双键并任选随后的官能团转化来制备。
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公开(公告)号:US09353081B2
公开(公告)日:2016-05-31
申请号:US13615901
申请日:2012-09-14
申请人: Johannes Aebi , Kurt Amrein , Serena Maria Fantasia , Benoit Hornsperger , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Michelangelo Scalone , Xuefei Tan , Mingwei Zhou
发明人: Johannes Aebi , Kurt Amrein , Serena Maria Fantasia , Benoit Hornsperger , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Michelangelo Scalone , Xuefei Tan , Mingwei Zhou
IPC分类号: C07D471/02 , C07D401/04 , C07D471/04
CPC分类号: C07D401/04 , C07D471/04
摘要: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 A3 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
摘要翻译: 本发明提供具有通式(I)的新化合物,其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,R12,A1,A2 A3和n如本文所述, 使用化合物的化合物和方法。 本发明的化合物可用作醛固酮合酶的抑制剂。 该化合物可用于例如治疗或预防慢性肾脏疾病,充血性心力衰竭,高血压,原发性醛固酮增多症和库兴综合征。
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公开(公告)号:US20130079365A1
公开(公告)日:2013-03-28
申请号:US13615901
申请日:2012-09-14
申请人: Johannes Aebi , Kurt Amrein , Serena Maria Fantasia , Benoit Hornsperger , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Michelangelo Scalone , Xuefei Tan , Mingwei Zhou
发明人: Johannes Aebi , Kurt Amrein , Serena Maria Fantasia , Benoit Hornsperger , Bernd Kuhn , Yongfu Liu , Hans P. Maerki , Alexander V. Mayweg , Peter Mohr , Michelangelo Scalone , Xuefei Tan , Mingwei Zhou
IPC分类号: A61K31/4709 , A61K31/4725 , A61P9/12 , A61P13/12 , A61P9/04 , C07D401/10 , C07D471/04
CPC分类号: C07D401/04 , C07D471/04
摘要: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 A3 and n are as described herein, compositions including the compounds and methods of using the compounds.The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
摘要翻译: 本发明提供具有通式(I)的新化合物,其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,R12,A1,A2 A3和n如本文所述, 使用化合物的化合物和方法。 本发明的化合物可用作醛固酮合酶的抑制剂。 该化合物可用于例如治疗或预防慢性肾脏疾病,充血性心力衰竭,高血压,原发性醛固酮增多症和库兴综合征。
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公开(公告)号:US20130065876A1
公开(公告)日:2013-03-14
申请号:US13609429
申请日:2012-09-11
申请人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
发明人: Uwe Grether , Paul Hebeisen , Peter Mohr , Fabienne Ricklin , Stephan Roever
IPC分类号: A61K31/4545 , A61K31/4439 , A61K31/5377 , A61K31/496 , C07D405/04 , A61K31/501 , C07D405/14 , C07D401/06 , A61K31/44 , C07D417/12 , C07D413/12 , A61K31/4433 , C07D401/12 , C07D213/78 , C07D401/14
CPC分类号: C07D213/87 , C07D401/06 , C07D405/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
摘要翻译: 本发明涉及式I化合物,其中R 1至R 5在说明书和权利要求书中定义,以及其药学上可接受的盐。 本发明还涉及所述化合物的制造,含有它们的药物组合物以及用于治疗和/或预防可用HDL-胆固醇升高剂如血脂异常,动脉粥样硬化和心血管疾病治疗的疾病的方法。
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