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1. 发明申请

WO2008148710A3 ARYLOXAZOLE, ARYLOXADIAZOLE AND BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF SOMATOSTATINS RECEPTOR ACTIVITY 审中-公开
标题翻译：作为SOMATOSTATINS受体活性的调节剂的阿唑氧唑，阿魏酸和苯并咪唑衍生物
公开(公告)号：WO2008148710A3
公开(公告)日：2009-04-09
申请号：PCT/EP2008056674
申请日：2008-05-30
申请人： HOFFMANN LA ROCHE , CHRIST ANDREAS D , MARTIN RAINER E , MOHR PETER
发明人： CHRIST ANDREAS D , MARTIN RAINER E , MOHR PETER
IPC分类号： C07D401/12 , A61K31/4468 , A61P3/10 , C07D413/12
CPC分类号： C07D413/12 , C07D401/12
摘要： This invention relates to compounds of the formula (I) wherein X is O or NR8, Y is CR7 or N, and R1 to R8 are as defined in the specification, and pharmaceutically acceptable salts 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 associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的化合物，其中X为O或NR8，Y为CR7或N，R1至R8如说明书中所定义，及其药学上可接受的盐。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/或预防与调节SST受体亚型5相关的疾病的用途。

2. 发明申请

WO2008145524A2 4,4-DISUBSTITUTED PIPERIDINE DERIVATIVES 审中-公开
标题翻译： 4,4-取代的哌啶衍生物
公开(公告)号：WO2008145524A2
公开(公告)日：2008-12-04
申请号：PCT/EP2008055935
申请日：2008-05-15
申请人： HOFFMANN LA ROCHE , CHRIST ANDREAS D , MARTIN RAINER E , MOHR PETER
发明人： CHRIST ANDREAS D , MARTIN RAINER E , MOHR PETER
IPC分类号： C07D471/10 , A61K31/435 , A61K31/4468 , A61K31/455 , A61P3/00 , C07D211/66 , C07D401/12
CPC分类号： C07D471/10 , C07D211/66 , C07D401/12
摘要： This invention relates to 4,4-disubstituted piperidine derivatives of the formula (I) wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts 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 associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）的4,4-二取代哌啶衍生物，其中A和R 1至R 5如说明书中所定义，及其药学上可接受的盐。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/或预防与调节SST受体亚型5相关的疾病的用途。

3. 发明申请

WO2007025897A3 BENZOOXAZOLE, OXAZOLOPYRIDINE, BENZOTHIAZOLE AND THIAZOLOPYRIDINE DERIVATIVES 审中-公开
标题翻译：苯并恶唑，恶唑并吡啶，苯并噻唑和噻唑并吡啶衍生物
公开(公告)号：WO2007025897A3
公开(公告)日：2007-05-10
申请号：PCT/EP2006065522
申请日：2006-08-21
申请人： HOFFMANN LA ROCHE , BINGGELI ALFRED , CHRIST ANDREAS D , GREEN LUKE , GUBA WOLFGANG , MAERKI HANS P , MARTIN RAINER E , MOHR PETER
发明人： BINGGELI ALFRED , CHRIST ANDREAS D , GREEN LUKE , GUBA WOLFGANG , MAERKI HANS P , MARTIN RAINER E , MOHR PETER
IPC分类号： C07D413/12 , A61K31/423 , A61K31/428 , A61K31/437 , A61P3/04 , A61P3/10 , A61P17/06 , A61P19/02 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： This invention is concerned with compounds of the formula (I) wherein X, A, B, R 1 , R 2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to then- use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及式（I）化合物，其中X，A，B，R 1，R 2和G如说明书和权利要求书中所定义，且其药学上可接受的盐。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，然后用于治疗和/或预防与调节SST受体亚型5相关的疾病。

4. 发明申请

WO2009068468A3 PYRIDINE COMPOUNDS 审中-公开
标题翻译：吡啶化合物
公开(公告)号：WO2009068468A3
公开(公告)日：2010-04-22
申请号：PCT/EP2008065911
申请日：2008-11-20
申请人： HOFFMANN LA ROCHE , HAAP WOLFGANG , HEBEISEN PAUL , KITAS ERIC A , KUHN BERND , MOHR PETER , WESSEL HANS PETER
发明人： HAAP WOLFGANG , HEBEISEN PAUL , KITAS ERIC A , KUHN BERND , MOHR PETER , WESSEL HANS PETER
IPC分类号： C07D213/75 , A61K31/64 , A61P3/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14
CPC分类号： C07D213/75 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
摘要翻译：式（I）化合物及其药学上可接受的盐和酯，其中残基具有权利要求1中给出的含义，其可以以药物组合物的形式使用。

5. 发明专利

JP2010132671A NEW 2-ARYLTHIAZOLE COMPOUND AS PPARα AND PPARγ AGONISTS 审中-公开
标题翻译：新的2-ARYLTHIAZOLE化合物作为PPARα和PPARGAMMA AGONISTS
公开(公告)号：JP2010132671A
公开(公告)日：2010-06-17
申请号：JP2010006072
申请日：2010-01-14
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： BINGGELI ALFRED , GRETHER UWE , HILPERT HANS , HIRTH GEORGES , MAERKI HANS-PETER , MEYER MARKUS , MOHR PETER
IPC分类号： C07D277/20 , A61K31/422 , A61K31/426 , A61K31/427 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P13/08 , A61P15/00 , A61P15/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07B51/00 , C07D277/22 , C07D277/24 , C07D277/34 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12
CPC分类号： C07D417/06 , C07D277/24 , C07D417/12
摘要： PROBLEM TO BE SOLVED: To provide new 2-arylthiazole compounds as PPARα and PPARγ agonists which are useful for the treatment of diseases such as diabetes. SOLUTION: The compounds expressed by formula (I), and pharmaceutically acceptable salts and esters thereof are disclosed. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供新的2-芳基噻唑化合物作为PPARα和PPARγ激动剂，其可用于治疗疾病如糖尿病。解决方案：公开了由式（I）表示的化合物及其药学上可接受的盐和酯。版权所有（C）2010，JPO＆INPIT

6. 发明专利

JP2009138011A CARBOXYLIC ACID-SUBSTITUTED OXAZOLE DERIVATIVE FOR USE AS PPAR-α AND -γ ACTIVATOR IN TREATMENT OF DIABETES 审中-公开
标题翻译：用于PPAR-α和γ-氨基转移酶治疗糖尿病的羧酸取代的奥沙唑衍生物
公开(公告)号：JP2009138011A
公开(公告)日：2009-06-25
申请号：JP2009028181
申请日：2009-02-10
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
发明人： BINGGELI ALFRED , BOEHRINGER MARKUS , GRETHER UWE , HILPERT HANS , MAERKI HANS-PETER , MEYER MARKUS , MOHR PETER , RICKLIN FABIENNE
IPC分类号： C07D263/22 , C07D263/32 , A61K31/421 , A61K31/422 , A61P3/00 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P43/00 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14
CPC分类号： C07D413/12 , C07D263/32 , C07D413/14
摘要： PROBLEM TO BE SOLVED: To provide carboxylic acid-substituted oxazole derivatives for use as PPAR-α (peroxisome proliferator-activated receptor-α) and PPAR-γ activators in the treatment of diabetes. SOLUTION: The invention relates to compounds represented by formula (I), pharmaceutically acceptable salts and esters thereof. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供用作PPAR-α（过氧化物酶体增殖物激活受体-α）和PPAR-γ激活剂用于治疗糖尿病的羧酸取代的恶唑衍生物。解决方案：本发明涉及由式（I）表示的化合物，其药学上可接受的盐和酯。版权所有（C）2009，JPO＆INPIT

7. 发明专利

JP2011093913A Phenyl derivatives as ppar agonists 审中-公开
标题翻译：苯丙酸衍生物作为PPAR激动剂
公开(公告)号：JP2011093913A
公开(公告)日：2011-05-12
申请号：JP2010281960
申请日：2010-12-17
申请人： F Hoffmann La Roche Ag , エフ.ホフマン−ラロシュアーゲーF. Hoffmann−La Roche Aktiengesellschaft
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： C07D213/38 , A61K31/4418 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/506 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/02 , A61P9/10 , A61P9/12 , A61P15/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/30 , C07D213/32 , C07D213/56 , C07D213/82 , C07D237/08 , C07D239/26 , C07D239/28 , C07D241/12 , C07D401/04
CPC分类号： C07D213/30 , C07D213/32 , C07D213/38 , C07D213/56 , C07D213/82 , C07D237/08 , C07D239/26 , C07D239/28 , C07D241/12
摘要： PROBLEM TO BE SOLVED: To provide phenyl derivatives as PPARδ and/or PPARα agonists. SOLUTION: This invention relates to compounds of formula (I-A), 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. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供苯基衍生物作为PPARδ和/或PPARα激动剂。解决方案：本发明涉及式（I-A）化合物及其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。版权所有（C）2011，JPO＆INPIT

8. 发明专利

JPH1036343A NEW RETINOID 失效
公开(公告)号：JPH1036343A
公开(公告)日：1998-02-10
申请号：JP8897697
申请日：1997-04-08
申请人： HOFFMANN LA ROCHE
发明人： KLAUS MICHAEL , MOHR PETER
IPC分类号： A61K31/07 , A61K20060101 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/23 , A61K31/35 , A61P3/02 , A61P17/00 , A61P29/00 , A61P35/00 , C07C20060101 , C07C57/30 , C07C57/34 , C07C59/147 , C07C59/40 , C07C59/46 , C07C59/62 , C07C59/76 , C07C59/82 , C07C69/013 , C07C69/587 , C07C69/602 , C07C69/73 , C07C69/732 , C07C403/20 , C07D309/00
摘要： PROBLEM TO BE SOLVED: To obtain a new compound which is useful for treatment of epithelial lesions, for example, acne, psoriasis, and of dermatopathy accompanied by inflammation and for treatment and prevention of tumors and precancerous change in oral cavity, tongue, pharynx, esophagus, bladder, neck and colonic mucous membrane. SOLUTION: This new compound is represented by formula I [X is oxo in 4-, 5-position, OR (R is H, an alkyl, an acyl); dotted line can be arbitrarily present and a double bond is present between 3- and 4-positions only in the case that X is present on 5-position], typically (2Z,4E,6E,8E)-(R)-9-(4-hydroxy-2,6,6- trimethyl-cyclohex-1-enyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid. The compound of formula I is prepared by reaction of a compound of formula II [A is a (substituted) phenyl; Y is an anion] with 5-hydroxy-4-methyl-5H-furan-2-one in the presence of a base followed by isomerization of the C=C double bond formed in the preceding reaction from the cis to the trans form.

9. 发明申请

WO0114360A3 BENZOPYRANS AND BENZOTHIOPYRANS AS RAR SELECTIVE RETINOID AGONISTS 审中-公开
标题翻译：苯并噻吩和苯并噻吩作为选择性反义寡核苷酸
公开(公告)号：WO0114360A3
公开(公告)日：2001-05-17
申请号：PCT/EP0008065
申请日：2000-08-18
申请人： HOFFMANN LA ROCHE
发明人： BELLONI PAULA NANETTE , MOHR PETER
IPC分类号： C07D335/06 , A61K31/335 , A61K31/352 , A61K31/38 , A61K31/382 , A61P11/00 , A61P43/00 , C07D311/20 , C07D311/58 , C07D313/08 , C07D337/08
CPC分类号： C07D313/08 , C07D311/20 , C07D337/08
摘要： This invention relates to new RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.
摘要翻译：本发明涉及式（I）的新的RAR选择性类视黄醇激动剂，其中符号如本说明书中对其药学上可接受的盐，单个异构体或外消旋或非外消旋混合物所定义; 含有它们的药物组合物及其用作治疗剂的方法。

10. 发明申请

WO9847866A2 ARYLSECOCHOLADIENE DERIVATIVES 审中-公开
标题翻译： ARYLSECOCHOLADIENE衍生物
公开(公告)号：WO9847866A2
公开(公告)日：1998-10-29
申请号：PCT/EP9802116
申请日：1998-04-11
申请人： HOFFMANN LA ROCHE
发明人： BARBIER PIERRE , BAUER FRANZ , MOHR PETER , MULLER MARC , PIRSON WOLFGANG
IPC分类号： A61K31/59 , A61P3/02 , A61P17/00 , A61P19/10 , A61P37/06 , C07C35/23 , C07C35/32 , C07C49/403 , C07C49/497 , C07C69/88 , C07C401/00 , C07F7/18
CPC分类号： C07C69/88 , C07C35/32 , C07C401/00 , C07F7/1856
摘要： 24-Nor-secochola-5,7-diene derivatives of formula (I) wherein A is a single or double bond, B is a group CH2CH2, CH=CH or CC, T is a group CH2 or CH2CH2, R and R are H or OH, C(R,R) is CH2 or C=CH2, R is CH3 and R is H, or R is H and R is CH3, L is phenyl and R is OH or C(C1-4-alkyl)2OH, or L-R is 2-furyl which is 5-substituted by C(C1-4-alkyl)2OH, with the proviso that when L is phenyl, A is a single bond, B is CC, T is CH2, each R and R are OH, C(R,R) is C=CH2, R is CH3, R is H, and R is C(CH3)2OH, then R must be in position ortho or para, are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.
摘要翻译：其中A是单键或双键的式（I）的24-去甲 - 仲 - 5,7-二烯衍生物，B是基团CH 2 CH 2，CH = CH或CC，T是基团CH 2或CH 2 CH 2，R 1，且R 3为H或OH，C（R，R）为CH 2或C = CH 2，R 2为CH 3且R 4为H或R 2为H且R 4为 CH 3，L是苯基，R 5是OH或C（C 1-4 - 烷基）2 OH，或者LR 5是被C（C 1-4 - 烷基）2 OH取代的2-呋喃基，其中条件是当L为苯基时，A为单键，B为CC，T为CH 2，每个R 1和R 3为OH，C（R，R）为C = CH 2，R 2为 CH 3，R 4为H，R 5为C（CH 3）2 OH，则R 5必须在邻位或对位，可用于治疗或预防维生素D依赖性疾病，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症，移植排斥反应和移植物抗宿主病。

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