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1.发明公开DIHOMO-SECO-CHOLESTANES WITH TWO UNSATURATED BONES IN THE SIDE CHAIN 失效二高SECO胆甾带有两个侧链不饱和化合物CONNECTIONS
公开(公告)号：EP0998455A1
公开(公告)日：2000-05-10
申请号：EP98940201.1
申请日：1998-07-10
发明人： BARBIER, Pierre , MOHR, Peter , MULLER, Marc , SELF, Christopher
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula (I) wherein A is a single or double bond, B?1 and B2¿ are each independently CH=CH or C≡C, T is CH¿2? or CH2CH2, X is -CH2- or > C=CH2, R?1¿ is H, F or OH, R?2 and R3¿ are each independently lower alkyl or CF¿3?, or C(R?2,R3¿) is C¿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.
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2.发明公开SOLID FORMS OF (S)-2-METHOXY-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-BENZO[B]THIOPHEN-7-YL}-PROPIONIC ACID AND OF SALTS THEREOF 有权FESTE FORMEN VON（S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 氧杂-4-基） - 乙氧基] - 苯并[b]噻吩-7-基}} - 丙酸 SAUER UND SALZE DAVON
公开(公告)号：EP2895469A1
公开(公告)日：2015-07-22
申请号：EP13759215.0
申请日：2013-09-09
发明人： DREIER, Lukas , EGLI, André , FAEHNRICH, Karsten , GRASSMANN, Olaf , MOHR, Peter , SCHWITTER, Urs , STAHR, Helmut , WYTTENBACH, Nicole
IPC分类号： C07D263/22 , A61K31/421
CPC分类号： A61K31/422 , C07D263/22
摘要： The present invention relates to solid forms of (S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl- oxazol-4-yl)-ethoxy]-benzo[b]thiophen-7-yl}-propionic acid, and of salts of (S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-benzo[b]thiophen-7-yl}- propionic acid.
摘要翻译： 本发明涉及（S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 恶唑-4-基） - 乙氧基] - 苯并[b]噻吩-7 （S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 恶唑-4-基） - 乙氧基] - 苯并[b]吡啶的盐 噻吩-7-基} - 丙酸。
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公开(公告)号：EP2814814A1
公开(公告)日：2014-12-24
申请号：EP13703073.0
申请日：2013-02-08
发明人： AEBI, Johannes , AMREIN, Kurt , HORNSPERGER, Benoit , MAERKI, Hans, P. , MAYWEG, Alexander , MOHR, Peter , TAN, Xuefei
IPC分类号： C07D233/64 , C07D401/06 , C07D409/06 , A61K31/4164 , A61K31/4178 , A61K31/4709 , A61P5/00 , A61P9/00 , A61P13/00
CPC分类号： C07D233/64 , C07D401/06 , C07D409/06
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
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公开(公告)号：EP1742923A1
公开(公告)日：2007-01-17
申请号：EP05735100.9
申请日：2005-04-20
发明人： ACKERMANN, Jean , AEBI, Johannes , BINGGELI, Alfred , GRETHER, Uwe , HIRTH, Georges , KUHN, Bernd , MAERKI, Hans-Peter , MEYER, Markus , MOHR, Peter , WRIGHT, Matthew, Blake
IPC分类号： C07D231/12 , A61K31/41 , A61P3/00
CPC分类号： C07D231/12
摘要： This invention is concerned with compounds of the formula (I) wherein one of R5, R6 and R7 is (a) and X1, X2, R1 to R15 and n are as defined in the description, 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.
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5.发明授权
公开(公告)号：EP0998455B1
公开(公告)日：2003-10-01
申请号：EP98940201.1
申请日：1998-07-10
发明人： BARBIER, Pierre , MOHR, Peter , MULLER, Marc , SELF, Christopher
IPC分类号： C07C401/00 , A61K31/59
CPC分类号： C07C401/00
摘要： Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula (I) wherein A is a single or double bond, B?1 and B2¿ are each independently CH=CH or C≡C, T is CH¿2? or CH2CH2, X is -CH2- or > C=CH2, R?1¿ is H, F or OH, R?2 and R3¿ are each independently lower alkyl or CF¿3?, or C(R?2,R3¿) is C¿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.
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6.发明授权SMALL MOLECULE CONJUGATES FOR INTRACELLULAR DELIVERY OF NUCLEIC ACIDS 有权KLEINMOLEKÜLIGEKONJUGATE ZURINTRAZELLULÄRENFREISETZUNG VONNUKLEINSÄUREN
公开(公告)号：EP2658981B1
公开(公告)日：2016-09-28
申请号：EP11739076.5
申请日：2011-08-04
发明人： HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
IPC分类号： A61K38/00 , A61K31/7088 , A61K48/00 , A61K47/48 , C07C271/20 , C07C69/96 , C07K7/02 , C12N15/87
CPC分类号： A61K38/00 , A61K31/7088 , A61K47/60 , A61K47/65 , A61K48/00 , C07C69/96 , C07C271/20 , C07H15/04 , C07H15/20 , C07H15/26 , C07K7/02 , C07K2317/77 , C12N15/1138 , C12N15/87 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2320/30
摘要： The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.
摘要翻译： 本发明提供了用于递送核酸的新化合物的用途，以及这些化合物与核酸的缀合物的用途。 在其中公开了当共价连接到所述化合物并与递送聚合物共同施用以实现体内mRNA敲低时特别有用的化学稳定的siRNA的新颖设计标准。
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7.发明授权SMALL MOLECULE CONJUGATES FOR INTRACELLULAR DELIVERY OF BIOLOGICALLY ACTIVE COMPOUNDS 有权小分子偶联物生物活性化合物的细胞内输送
公开(公告)号：EP2658982B1
公开(公告)日：2016-04-20
申请号：EP11802425.6
申请日：2011-12-22
发明人： HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
IPC分类号： C12N15/87 , C12N15/11 , A61K48/00 , A61K31/713 , A61K47/18
CPC分类号： A61K38/00 , A61K31/7088 , A61K47/60 , A61K47/65 , A61K48/00 , C07C69/96 , C07C271/20 , C07H15/04 , C07H15/20 , C07H15/26 , C07K7/02 , C07K2317/77 , C12N15/1138 , C12N15/87 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2320/30
摘要： The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.
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公开(公告)号：EP1725546B1
公开(公告)日：2008-10-08
申请号：EP05715587.1
申请日：2005-02-28
发明人： ACKERMANN, Jean , AEBI, Johannes , BINGGELI, Alfred , GRETHER, Uwe , HIRTH, Georges , KUHN, Bernd , MAERKI, Hans-Peter , MEYER, Markus , MOHR, Peter , WRIGHT, Matthew, Blake
IPC分类号： C07D403/12 , A61K31/4155 , A61P9/00
CPC分类号： C07D403/12
摘要： This invention is concerned with compounds of the formula (I), wherein one of R6, R7 and R8 is (II), 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 PPARδ 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（II），并且R 1至R 15和n如说明书中所定义，且所有对映异构体和药学上可接受的盐和/或酯 它们。 本发明进一步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。
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9.发明公开NOVEL 2-ARYLTHIAZOLE COMPOUNDS AS PPARALPHA AND PPARGAMMA AGONISTS 有权新的2 ARYLTHIAZOLVERBINDUNGEN AS PPAR-α和-gamma激动剂
公开(公告)号：EP1537091A1
公开(公告)日：2005-06-08
申请号：EP03757762.4
申请日：2003-08-21
发明人： BINGGELI, Alfred , GRETHER, Uwe , HILPERT, Hans , HIRTH, Georges , MAERKI, Hans-Peter , MEYER, Markus , MOHR, Peter
IPC分类号： C07D277/22 , C07D417/12
CPC分类号： C07D417/06 , C07D277/24 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein Rl to R10, X, Y and n are as defined in the description and claims, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of diseases such as diabetes.
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公开(公告)号：EP2785695A1
公开(公告)日：2014-10-08
申请号：EP12797817.9
申请日：2012-11-27
发明人： AEBI, Johannes , AMREIN, Kurt , CHEN, Wenming , HORNSPERGER, Benoit , KUHN, Bernd , LIU, Yongfu , MAERKI, Hans P. , MAYWEG, Alexander V. , MOHR, Peter , TAN, Xuefei , WANG, Zhanguo , ZHOU, Mingwei
IPC分类号： C07D217/22 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/113 , C07D491/107 , A61K31/4375 , A61K31/4725 , A61P9/12
CPC分类号： C07D401/04 , C07D217/22 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/107 , C07D491/113
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for 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，A1，A2，A3，A4，A5和n如本文所述，包括该化合物的组合物和使用 化合物。 该化合物可用作例如用于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的醛固酮合酶（CYP11B2或CYP11B1）抑制剂。
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