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1. 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。

2. 发明申请

WO2013120921A1 NOVEL PYRROLIDINE DERIVATIVES 审中-公开
标题翻译：新型吡咯烷衍生物
公开(公告)号：WO2013120921A1
公开(公告)日：2013-08-22
申请号：PCT/EP2013052914
申请日：2013-02-14
申请人： HOFFMANN LA ROCHE , BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
发明人： BANNER DAVID , HAAP WOLFGANG , LUEBBERS THOMAS , PETERS JENS-UWE
IPC分类号： C07D401/14 , A61K31/401 , A61P3/00 , C07D403/06 , C07D405/14 , C07D409/14 , C07D417/08 , C07D417/14
CPC分类号： C07D417/14 , C07D207/10 , C07D401/14 , C07D403/06 , C07D403/08 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/08
摘要： The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
摘要翻译：本发明涉及式（I）化合物，其中A1至A3和R1至R3如在说明书和权利要求书中所定义。式（I）化合物可以用作药物。

3. 发明申请

WO2008138754A3 NEW SOLID FORMS OF FXA INHIBITORS 审中-公开
标题翻译： FXA抑制剂的新固体形式
公开(公告)号：WO2008138754A3
公开(公告)日：2009-01-22
申请号：PCT/EP2008055291
申请日：2008-04-30
申请人： HOFFMANN LA ROCHE , ADAM JEAN-MICHEL , BUBENDORF ANDRE , DEYNET-VUCENOVIC ANNETTE , DOTT PASCAL , GLOMME ALEXANDER , GRASSMANN OLAF , HAAP WOLFGANG , KUENTZ MARTIN , MEIER ROLAND
发明人： ADAM JEAN-MICHEL , BUBENDORF ANDRE , DEYNET-VUCENOVIC ANNETTE , DOTT PASCAL , GLOMME ALEXANDER , GRASSMANN OLAF , HAAP WOLFGANG , KUENTZ MARTIN , MEIER ROLAND
IPC分类号： C07D401/14 , A61K31/4412 , A61P7/02
CPC分类号： C07D401/14
摘要： The invention is concerned with crystalline forms or amorphous forms of a pyrrolidine- 3,4-dicarboxamide derivative, which is useful as an active ingredient of medicaments for the diseases which can be treated by the coagulation factor Xa inhibitors.
摘要翻译：本发明涉及吡咯烷-3,4-二甲酰胺衍生物的结晶形式或无定形形式，其可用作可由凝血因子Xa抑制剂治疗的疾病的药物的活性成分。

4. 发明申请

WO2006066778A3 NOVEL HETEROARYLACETAMIDES 审中-公开
标题翻译：新型异辛二胺
公开(公告)号：WO2006066778A3
公开(公告)日：2006-08-10
申请号：PCT/EP2005013460
申请日：2005-12-14
申请人： HOFFMANN LA ROCHE , BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , PANDAY NARENDRA , RICKLIN FABIENNE
发明人： BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , PANDAY NARENDRA , RICKLIN FABIENNE
IPC分类号： C07D277/46 , C07D401/10 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/10 , C07D417/14
CPC分类号： C07D401/10 , C07D277/46 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/10 , C07D417/14
摘要： The invention is concerned with novel heteroarylacetamides of formula (I) R d -C(O)-N(R e )-R c -CH 2 -C(O)-N(R a )(R b ), wherein R a to R e are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型杂芳基乙酰胺R 2 -C（O）-N（R e） - R c - CH 2 -C（O）-N（R a）a（R b）b）其中R a a至 R e如在说明书和权利要求书中所定义的，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

5. 发明申请

WO2006048152A2 NOVEL DICARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：新型二恶唑衍生物
公开(公告)号：WO2006048152A2
公开(公告)日：2006-05-11
申请号：PCT/EP2005011430
申请日：2005-10-25
申请人： HOFFMANN LA ROCHE , BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , HIMBER JACQUES , HUMM ROLAND , IDING HANS , KNOPP DIETMAR , PANDAY NARENDRA , RICKLIN FABIENNE , STAHL CHRISTOPH MARTIN
发明人： BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , HIMBER JACQUES , HUMM ROLAND , IDING HANS , KNOPP DIETMAR , PANDAY NARENDRA , RICKLIN FABIENNE , STAHL CHRISTOPH MARTIN
CPC分类号： C07D213/64 , C07D213/75 , C07D233/64 , C07D279/02 , C07D295/135 , C07D295/185 , C07D401/12
摘要： The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, R C , D and E are as defined in the description and in the claims, as well 5as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型二甲酰胺衍生物，其中A，B，R，D和E如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

6. 发明申请

WO2007054453A3 CARBOCYCLIC FUSED CYCLIC AMINES AS INHIBITORS OF THE COAGULATION FACTOR XA 审中-公开
标题翻译：作为凝血因子XA的抑制剂的CARBOCYCLIC FUSED CYCLIC AMINES
公开(公告)号：WO2007054453A3
公开(公告)日：2007-07-19
申请号：PCT/EP2006068012
申请日：2006-11-01
申请人： HOFFMANN LA ROCHE , BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , PANDAY NARENDRA , RICKLIN FABIENNE , STAHL MARTIN , SCHMITZ PETRA
发明人： BOEHRINGER MARKUS , GROEBKE ZBINDEN KATRIN , HAAP WOLFGANG , PANDAY NARENDRA , RICKLIN FABIENNE , STAHL MARTIN , SCHMITZ PETRA
IPC分类号： C07D401/12 , A61K31/40 , A61K31/47 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X 1 to X 3 , Y 1 to Y 3 , Z, R 1 , R 2 , m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型碳环稠合环胺，其中A，X 1至X 3，Y 1至Y 1， Z，R 1，R 2，m和n如说明书和权利要求书中所定义，以及生理上可接受的盐它们。这些化合物抑制凝血因子Xa，并且可以用作药物。

7. 发明申请

WO2006114401A2 NOVEL CYCLIC AMINES 审中-公开
标题翻译：新的循环系列
公开(公告)号：WO2006114401A2
公开(公告)日：2006-11-02
申请号：PCT/EP2006061776
申请日：2006-04-24
申请人： HOFFMANN LA ROCHE , GROEBKE-ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , PANDAY NARENDRA , RICKLIN FABIENNE , WIRZ BEAT
发明人： GROEBKE-ZBINDEN KATRIN , HAAP WOLFGANG , HILPERT HANS , PANDAY NARENDRA , RICKLIN FABIENNE , WIRZ BEAT
CPC分类号： C07D207/12 , C07D207/14 , C07D207/16 , C07D401/14 , C07D409/14 , C07D413/14 , C07D513/04
摘要： The invention is concerned with novel cyclic amines of formula (I) wherein X 1 to X 3 , Y 1 to Y 3 , R 1' , R 1'' and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及新的式（I）的环胺，其中X 1至X 3，Y 1至Y 3， R 1，R 1，R 1和R 2如在说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

8. 发明申请

WO0162082A3 USE OF PHENYLETHYLAMINE DERIVATIVES FOR THE ANITMICROBIAL TREATMENT OF SURFACES 审中-公开
标题翻译：苯乙烯衍生物用于治疗表面抗微生物剂的用途
公开(公告)号：WO0162082A3
公开(公告)日：2002-05-02
申请号：PCT/EP0101561
申请日：2001-02-13
申请人： CIBA SC HOLDING AG , HAAP WOLFGANG , HOELZL WERNER , OCHS DIETMAR , PUCHTLER KARIN , SCHNYDER MARCEL
发明人： HAAP WOLFGANG , HOELZL WERNER , OCHS DIETMAR , PUCHTLER KARIN , SCHNYDER MARCEL
IPC分类号： A61K8/30 , A01N33/10 , A01N35/04 , A01N37/34 , A01N37/36 , A01N37/38 , A01N39/00 , A01N39/02 , A01N39/04 , A61K8/00 , A61K8/41 , A61K8/44 , A61K31/138 , A61K31/225 , A61K31/24 , A61K31/277 , A61P1/02 , A61P17/00 , A61Q1/00 , A61Q1/04 , A61Q1/06 , A61Q1/10 , A61Q1/12 , A61Q3/02 , A61Q3/04 , A61Q5/02 , A61Q5/04 , A61Q5/08 , A61Q5/10 , A61Q9/04 , A61Q11/00 , A61Q15/00 , A61Q17/02 , C07C213/06 , C07C217/60 , C07C253/30 , C07C255/54 , C09D11/00 , C09D201/00 , C11D3/48 , D06M13/328 , D21H21/36
CPC分类号： A01N39/00 , A01N33/10 , A01N37/38 , A01N39/02 , A01N39/04 , C07C217/60 , C07C255/54 , C07C2601/08
摘要： The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl; C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, indolyl, pyridyl, pyridazinyl, pyrimidinyl, pyridazinyl, quinolinyl or isoquinolinyl; R4, R5, R6 and R7 are each independently of the others hydrogen; C1-C20alkyl; C3-C7 cycloalky; C2-C20 alkenyl; C4-C7 cycloalkenyl; C2-C20 alkynyl; or C4-C7 cycloalkynyl; and m and n are each independently of the other 0 or 1, for antimicrobial treatment of surfaces. The compounds exhibit a pronounced activity against pathogenic gram-positive and gram-negative bacteria, and also against yeasts and moulds. They are accordingly suitable for the antimicrobial treatment, especially preservation and disinfection, of surfaces.
摘要翻译：描述了式（1）化合物的用途，其中化合物R1，R2和R3各自独立地为氢; C1-C20烷基; C3-C7环烷基; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl; C4-C7cycloalkynyl; 或未取代的或C 1 -C 5烷基 - ，C 3 -C 7烷基烷基 - ，C 1 -C 5烷氧基 - ，C 3 -C 7环烷氧基 - ，卤代 - ，氧代 - ，羧基 - ，羧基-C 1 -C 7烷基酯 - ，羧基-C 3 -C 7环烷基酯 - 氰基 - 三氟甲基 - ，五氟乙基 - ，氨基 - ，N，N-单或二-C 1 -C 20烷基氨基或硝基取代的苯基-C 1 -C 5烷基，萘基-C 1 -C 5烷基，苯基羰基-C 1 -C 5烷基，萘基羰基-C 1 -C 5烷基，吡咯基烷基，呋喃基烷基，噻吩基烷基，吡唑基烷基，咪唑基烷基，恶唑基烷基，噻唑烷基，异恶唑基烷基，异噻唑基烷基，1,2,3-三唑基烷基，1,2,4-三唑基烷基，1,2,3-恶二唑基烷基，1,3,4-恶二唑基烷基 1,2,3-噻二唑基烷基，1,3,4-噻二唑基烷基，吲哚基烷基，吡啶基烷基，哒嗪基烷基，嘧啶基烷基，哒嗪基烷基，喹啉基烷基，异喹啉基烷基，吡咯基，呋喃基，噻吩基，吡唑基，咪唑基，恶唑基，噻唑基，异恶唑基，异噻唑基，，2,3-三唑基，1,2,4-三唑基，1,2,3-恶二唑基，1,3,4-恶二唑基，1,2,3-噻二唑基，1,3,4-噻二唑基，吲哚基，吡啶基，哒嗪基，嘧啶基，哒嗪基，喹啉基或异喹啉基; R4，R5，R6和R7各自独立地为氢; C1-C20烷基; C3-C7环状; C2-C20烯基; C4-C7环烯基; C2-C20炔基; 或C 4 -C 7环炔基; m和n各自独立地为0或1，用于表面的抗微生物处理。该化合物对病原性革兰氏阳性菌和革兰氏阴性细菌以及酵母和霉菌均表现出明显的活性。因此它们适用于表面的抗菌处理，特别是保存和消毒。

9. 发明申请

WO2004013120A8 NOVEL BENZODIOXOLES 审中-公开
标题翻译：新的胆甾醇
公开(公告)号：WO2004013120A8
公开(公告)日：2005-04-14
申请号：PCT/EP0307890
申请日：2003-07-18
申请人： HOFFMANN LA ROCHE
发明人： ALANINE ALEXANDER , BLEICHER KONRAD , GUBA WOLFGANG , HAAP WOLFGANG , KUBE DAGMAR , LUEBBERS THOMAS , PLANCHER JEAN-MARC , ROGERS-EVANS MARK , SCHNEIDER GISBERT , ZUEGGE JOCHEN , ROCHE OLIVIER
IPC分类号： A61K31/36 , C07D317/46 , C07D317/54 , C07D317/62 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
CPC分类号： C07D317/46 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compound of formula (I) wherein R , R , R , R , R , R , R , and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases, which are associated with the modulation of CB1 receptors.
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 6，R 7和X分别为如在说明书和权利要求书中所定义的，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体相关的疾病。

10. 发明申请

WO02058016A3 SILANYL PHENOLS AND NAPHTHOLS 审中-公开
标题翻译： SILANYL苯酚和萘酚
公开(公告)号：WO02058016A3
公开(公告)日：2002-12-19
申请号：PCT/EP0200192
申请日：2002-01-10
申请人： CIBA SC HOLDING AG , HOELZL WERNER , HAAP WOLFGANG , KOPPOLD JUERGEN
发明人： HOELZL WERNER , HAAP WOLFGANG , KOPPOLD JUERGEN
IPC分类号： A61L12/14 , C07C39/19 , C07C39/225 , C07F7/08 , C07F7/18 , D21H25/18
CPC分类号： C07F7/0852 , C07F7/0818
摘要： There are described silanyl phenols and naphthols of formula (1a) or (1b), wherein R1 is hydrogen; halogen; hydroxy; C1-C20alkyl; C3-C12cycloalkyl; C1-C20alkoxy; trifluoromethyl; pentafluoroethyl; mono- or di-C1-C5alkylamino; hydroxy-C1-C5alkyl; or phenyl, phenyl-C1-C20alkyl, phenoxy, phenyl-C1-C20alkoxy, naphthyl or naphthyl-C1-C20alkyl each unsubstituted or substituted by C1-C5alkyl, C3-C12cycloalkyl, C1-C5alkoxy, C3-C12cycloalkoxy, halogen, oxo, carboxy, carboxy-C1-C7alkyl ester, carboxy-C3-C12cycloalkyl ester, cyano, trifluoromethyl, pentafluoroethyl, amino, N,N-mono- or di-C1-C20alkylamino or by nitro; R2, R3 and R4 are each independently of the others hydrogen; C1-C20alkyl; or C3-C12-cycloalkyl; R5, R6 and R7 are each independently of the others C1-C20alkyl, C5-C10aryl, C1-C20alkoxy, phenyl-C1-C20alkyl, phenyl-C1-C20alkoxy, C2-C5alkenyl, -O-Si-(C1-C5alkyl)3; or O-Si-(C1-C5alkyl)2-O-Si(C1-C5alkyl)3 and n is 0 or 1. The compounds exhibit a pronounced activity against Gram positive and Gram negative bacteria, and also against yeasts and moulds.
摘要翻译：描述了式（1a）或（1b）的硅烷基酚和萘酚，其中R 1是氢; 卤素; 羟基; C1-C20烷基; C3-C12环烷基; C1-C20alkoxy; 三氟甲基; 五氟; 单 - 或二-C 1 -C 5烷基氨基; 羟基C1-C5烷基; 或苯基，苯基-C 1 -C 20烷基，苯氧基，苯基-C 1 -C 20烷氧基，萘基或萘基-C 1 -C 20烷基，各自为未取代的或被C 1 -C 5烷基，C 3 -C 12环烷基，C 1 -C 5烷氧基，C 3 -C 12环烷氧基，卤素，氧代，，羧基-C 1 -C 7烷基酯，羧基-C 3 -C 12环烷基酯，氰基，三氟甲基，五氟乙基，氨基，N，N-单或二-C 1 -C 20烷基氨基或被硝基取代; R2，R3和R4各自独立为氢; C1-C20烷基; 或C 3 -C 12 - 环烷基; R5，R6和R7各自独立地为C1-C20烷基，C5-C10芳基，C1-C20烷氧基，苯基-C1-C20烷基，苯基-C1-C20烷氧基，C2-C5链烯基，-O-Si-（C1-C5烷基）3 ; 或O-Si-（C 1 -C 5烷基）2 -O-Si（C 1 -C 5烷基）3并且n是0或1.所述化合物对革兰氏阳性菌和革兰氏阴性菌表现出显着的活性，并且还针对酵母菌和霉菌。

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