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81. 发明授权

US07098228B2 Indolyl derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US07098228B2
公开(公告)日：2006-08-29
申请号：US10719556
申请日：2003-11-21
申请人： Alfred Binggeli , Uwe Grether , Hans Hilpert , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr
发明人： Alfred Binggeli , Uwe Grether , Hans Hilpert , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr
IPC分类号： A61K31/425 , A61K31/42 , A61K31/40 , C07D277/30 , C07D263/30
CPC分类号： C07D413/06 , C07D417/06
摘要： The present invention provides compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4, A and n have the significance given in the specification. The compounds or their salts may be administered to a patient for treating non-insulin dependent diabetes mellitus.
摘要翻译：本发明提供式I化合物及其药学上可接受的盐和酯，其中R 1至R 4，A和n具有说明书中给出的含义。化合物或其盐可以施用于患者以治疗非胰岛素依赖性糖尿病。

82. 发明申请

US20050267180A1 Novel oxazole derivatives 失效
标题翻译：新型恶唑衍生物
公开(公告)号：US20050267180A1
公开(公告)日：2005-12-01
申请号：US11183360
申请日：2005-07-18
申请人： Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
发明人： Alfred Binggeli , Markus Boehringer , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Fabienne Ricklin
IPC分类号： A61K31/421 , A61P3/10 , C07D263/32
CPC分类号： C07D263/32
摘要： The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPARα and/or PPARγ agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6和n如本文所述。本发明的化合物可用作治疗和/或预防由PPARα和/或PPARγ激动剂调节的疾病的药物。这些疾病的例子包括糖尿病，特别是非胰岛素依赖性糖尿病，升高的血压，升高的脂质和胆固醇水平，动脉粥样硬化疾病，代谢综合征，内皮功能障碍，促凝血状态，血脂异常，多囊卵巢综合征，炎性疾病（例如冠疾病，炎性肠病，结肠炎，胰腺炎，胆汁郁积/肝脏纤维化，以及具有诸如阿尔茨海默病和受损/可改善的认知功能等炎症成分的疾病）和增殖性疾病。

83. 发明申请

US20050203160A1 Indolyl derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US20050203160A1
公开(公告)日：2005-09-15
申请号：US11074474
申请日：2005-03-08
申请人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
发明人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
IPC分类号： C07D403/12 , C07D43/02 , A61K31/416
CPC分类号： C07D403/12
摘要： This invention relates to compounds of the formula I: wherein one of R6, R7 and R8 is and R1 to R15 and n are as defined in the description, and all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR δ and/or PPARα agonists.
摘要翻译：本发明涉及式I化合物：其中R 6，R 7和R 8中的一个是R 1和R 2， R 15和R 15如在说明书中所定义，以及所有对映异构体及其药学上可接受的盐和/或酯。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防由PPARδ和/或PPARα激动剂调节的疾病的用途。

84. 发明申请

US20050096336A1 Benzannelated derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：苄基化衍生物，其制造和用作药剂
公开(公告)号：US20050096336A1
公开(公告)日：2005-05-05
申请号：US10977651
申请日：2004-10-29
申请人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
发明人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
IPC分类号： C07D213/30 , C07D213/38 , C07D239/26 , A61K31/44 , A61K31/192 , A61K31/277 , A61K31/343 , A61K31/381
CPC分类号： C07D213/30 , C07D213/38 , C07D239/26
摘要： There are presented compounds of the formula wherein R6 and R7 is R4 and R5 or R5 and R6 together with the carbon atoms to which they are attached, form a ring as defined in the description and X1, X2, Y1 to Y4, R1 to R13 and n are as specified in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
摘要翻译：提出下式的化合物其中R 6和R 7是R 4和R 5或R 5， SUP> 5和R 6以及它们所连接的碳原子一起形成如说明书中所定义的环，X ^{2 ，Y 1至Y 4，R 1至R 13和n分别为在本说明书中指定，以及所有对映异构体及其药学上可接受的盐和/或酯。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防由PPARδ和/或PPARα激动剂调节的疾病的用途。}

85. 发明授权

US06821980B1 Substituted 5-benzyl-2,4-diaminopyrimidines 失效
标题翻译：取代的5-苄基-2,4-二氨基嘧啶
公开(公告)号：US06821980B1
公开(公告)日：2004-11-23
申请号：US10129461
申请日：2002-07-18
申请人： Philippe Guerry , Peter Mohr , Marc Muller , Werner Mueller , Philippe Pflieger
发明人： Philippe Guerry , Peter Mohr , Marc Muller , Werner Mueller , Philippe Pflieger
IPC分类号： A61K31505
CPC分类号： C07D239/49 , A61K31/505
摘要： The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1 is C2-C3 alkyl an R2 is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3 is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2 and R3 can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations. The products have antibiotic properties and are useful for combating or preventing infectious diseases.
摘要翻译：本发明涉及通式（A）的取代的5-苄基-2,4-二氨基嘧啶，其中R 1是C 2 -C 3烷基，R 2是其一个C原子键合的杂环基，苯基或萘基， R 3为C 2 -C 6烷基，烯基，环烷基，环烷基烷基，杂环基烷基，烷基磺酰基，环烷基磺酰基，环烷基烷基氨磺酰基，杂芳基磺酰基，杂环基烷基磺酰基或二烷基氨磺酰基。其中烷基，环烷基和亚烯基可以单独或组合物中携带多达6个碳原子，并且可以单独携带多达6个环成员，或者在组合物中并且基团R 2和R 3可以被取代; 和化合物的酸加成盐。本发明还涉及制备上述5-苄基-2,4-二氨基嘧啶的方法。生产的产品，相应的药物和使用5-苄基-2,4-二氨基嘧啶作为药物制剂。该产品具有抗生素特性，可用于对抗或预防传染病。

86. 发明授权

US06809110B2 Thiazole derivatives 失效
标题翻译：噻唑衍生物
公开(公告)号：US06809110B2
公开(公告)日：2004-10-26
申请号：US10650434
申请日：2003-08-28
申请人： Alfred Binggeli , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr
发明人： Alfred Binggeli , Uwe Grether , Hans Hilpert , Georges Hirth , Hans-Peter Maerki , Markus Meyer , Peter Mohr
IPC分类号： C07D27724
CPC分类号： C07D417/06 , C07D277/24 , C07D417/12
摘要： The present invention provides compounds of formula (I) wherein R1 to R10, X, Y and n are indicated in the specification, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of non-insulin dependent diabetes mellitus.
摘要翻译：本发明提供其中R 1至R 10，X，Y和n在说明书中表示的式（I）化合物及其药学上可接受的盐和酯。该化合物可用于治疗非胰岛素依赖性糖尿病。

87. 发明授权

US5994569A Dihomo-seco-cholestanes 失效
公开(公告)号：US5994569A
公开(公告)日：1999-11-30
申请号：US115188
申请日：1998-07-14
申请人： Pierre Barbier , Peter Mohr , Marc Muller , Christopher Self
发明人： Pierre Barbier , Peter Mohr , Marc Muller , Christopher Self
IPC分类号： A61K31/59 , A61P3/02 , A61P3/10 , A61P19/10 , A61P29/00 , A61P35/00 , A61P37/00 , C07C401/00
CPC分类号： C07C401/00
摘要： Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula ##STR1## wherein A is a single or double bond,B.sup.1 and B.sup.2 are each independently CH.dbd.CH or C.tbd.C,T is CH.sub.2 or CH.sub.2 CH.sub.2,X is --CH.sub.2 -- or >C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently lower alkyl or CF.sub.3, orC(R.sup.2,R.sup.3) is C.sub.3-6 -cycloalkyl,are useful in the treatment or prevention of vitamin D dependent disorders and of IL-12-dependent autoimmune diseases, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, multiple sclerosis, transplant rejection, graft vs. host disease, rheumatoid arthritis, insulin-dependent diabetes mellitus, inflammatory bowel disease, septic shock and allergic encephalomyelitis.
摘要翻译：多不饱和的24a，24b-二氢-9,10-断氧胆甾烷衍生物，其中A为单键或双键，B1和B2各自独立地为CH = CH或C，3BOND C，T为CH2或CH2CH2，X为-CH2-或 > C = CH 2，R 1为H，F或OH，R 2和R 3各自独立地为低级烷基或CF 3，或C（R 2，R 3）为C 3-6环烷基，可用于治疗或预防维生素D依赖性疾病和IL-12依赖性自身免疫性疾病，特别是牛皮癣，基底细胞癌，角质化和角化病，白血病，骨质疏松症，伴随肾衰竭的甲状旁腺功能亢进，多发性硬化，移植排斥，移植物抗宿主病，类风湿性关节炎，胰岛素依赖性糖尿病，炎性肠病，败血性休克和过敏性脑脊髓炎。

88. 发明授权

US5919986A D-homo vitamin D.sub.3 derivatives 失效
标题翻译： D-homo维生素D3衍生物
公开(公告)号：US5919986A
公开(公告)日：1999-07-06
申请号：US170453
申请日：1998-10-13
申请人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
发明人： Pierre Barbier , Franz Bauer , Peter Mohr , Marc Muller , Wolfgang Pirson
IPC分类号： C07C35/36 , C07C45/29 , C07C49/743 , C07F7/18 , C07C49/115 , C07C35/08
CPC分类号： C07F7/1856 , C07C35/36 , C07C45/292 , C07C49/743
摘要： Compounds of formula I: ##STR1## wherein the dotted carbon-carbon bond in the D-ring is C--C or C.dbd.C; C(R,R) is CH.sub.2 or C.dbd.CH.sub.2,R.sup.1 is H, F or OH,R.sup.2 and R.sup.3 are each independently C.sub.1-4 -alkyl or CF.sub.3, or together with the carbon to which they are bound form C.sub.3-6 -cycloalkyl.are useful in the treatment of vitamin D dependent disorders, such as psoriasis, leukemia; acne and seborrhoic dermatitis; osteoporosis hyperparathyroidism accompanying renal failure; and multiple sclerosis.
摘要翻译：式I化合物：其中D环中的点状碳 - 碳键为C-C或C = C; C（R，R）是CH 2或C = CH 2，R 1是H，F或OH，R 2和R 3各自独立地是C 1-4 - 烷基或CF 3，或与它们结合的碳一起形成C 3-6 - 环烷基。可用于治疗维生素D依赖性疾病，如牛皮癣，白血病; 痤疮和脂溢性皮炎; 伴有肾衰竭的骨质疏松性甲状旁腺功能亢进; 和多发性硬化症。

89. 发明授权

US5801253A Retinoic acid X-receptor ligands 失效
标题翻译：视黄酸X受体配体
公开(公告)号：US5801253A
公开(公告)日：1998-09-01
申请号：US776087
申请日：1997-01-21
申请人： Michael Klaus , Allen John Lovey , Peter Mohr , Michael Rosenberger
发明人： Michael Klaus , Allen John Lovey , Peter Mohr , Michael Rosenberger
IPC分类号： A01N20060101 , A61K31/07 , A61K31/19 , A61K31/215 , A61K31/38 , A61K31/381 , A61P3/02 , A61P17/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07C45/29 , C07C45/63 , C07C47/235 , C07C47/238 , C07C47/24 , C07C47/277 , C07C51/09 , C07C57/02 , C07C57/50 , C07C57/62 , C07C63/00 , C07C67/343 , C07C69/618 , C07C69/65 , C07C69/734 , C07D333/24 , C07F9/40 , C07F9/48 , C07F9/54 , C07D333/08 , C07C69/76 , C07C233/00
CPC分类号： C07F9/4056 , C07C45/29 , C07C45/298 , C07C45/63 , C07C47/24 , C07C47/277 , C07C57/50 , C07D333/24 , C07C2101/16
摘要： Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.
摘要翻译： PCT No.PCT / EP95 / 03021 Sec。 371日期1997年1月21日 102（e）日期1997年1月21日PCT提交1995年7月29日PCT公布。公开号WO96 / 05165 日期1996年2月22日其中R1-R7，R10，X和点键具有说明书中给出的含义的式（I）化合物选择性地结合于类视黄醇RXR受体，并且可用作皮肤病学和肿瘤学适应症的抗增生剂。

90. 发明授权

US5391766A Alkyl or alkoxy substituted S-heterocyclic retinoids 失效
标题翻译：烷基或烷氧基取代的S-杂环类视黄醇
公开(公告)号：US5391766A
公开(公告)日：1995-02-21
申请号：US57949
申请日：1993-05-05
申请人： Michael Klaus , Peter Mohr
发明人： Michael Klaus , Peter Mohr
IPC分类号： A61K31/38 , A61K31/381 , A61K31/382 , A61P17/00 , A61P37/06 , C07D333/54 , C07D335/06 , C07D337/08
CPC分类号： C07D333/54 , C07D335/06 , C07D337/08
摘要： Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.
摘要翻译：其中X是-S-，-SO-或-SO 2 - 的式I的化合物; R1是C7-10-烷基或C7-10-烷氧基; R 2是下式的残基：（a）或（b）R 3是羧基或低级烷氧基羰基; n为1,2或3的整数; 式I的羧酸盐可用于治疗具有强免疫组分的自身免疫性疾病和疾病，例如牛皮癣。

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