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1. 发明授权

US06797713B2 Compounds and methods for treatment of asthma, allergy and inflammatory disorders 失效
标题翻译：用于治疗哮喘，过敏和炎性疾病的化合物和方法
公开(公告)号：US06797713B2
公开(公告)日：2004-09-28
申请号：US10242346
申请日：2002-09-12
申请人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmond Differding , James Ellis , Marie-Agnes Lassoie , Michelle Young , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
发明人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmond Differding , James Ellis , Marie-Agnes Lassoie , Michelle Young , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
IPC分类号： A61K31495
CPC分类号： C07D295/096 , C07D295/084 , C07D295/088 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/15 , C07D307/14 , C07D307/52 , C07D401/04
摘要： The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
摘要翻译：本发明提供了1,4取代的哌嗪，1,4-取代的哌啶和1-取代的4-亚烷基哌啶化合物。本发明的化合物是具有白细胞三烯抑制性质以及抗组胺能性质的双作用分子。本发明的化合物可用于治疗可能存在组胺和/或白三烯组分的病症。这些病症优选包括哮喘，季节性和常年性过敏性鼻炎，鼻窦炎，结膜炎，食物过敏症，偶发性中毒，牛皮癣，荨麻疹，瘙痒，湿疹，类风湿性关节炎，炎性肠病，慢性阻塞性肺病，血栓性疾病和中耳炎。还提供了通过向有需要的受试者施用有效的哮喘和减轻炎症的量的化合物来治疗哮喘和鼻炎的方法。

2. 发明授权

US06451801B1 Compounds and methods for treatment of asthma, allergy and inflammatory disorders 失效
标题翻译：用于治疗哮喘，过敏和炎性疾病的化合物和方法
公开(公告)号：US06451801B1
公开(公告)日：2002-09-17
申请号：US09534947
申请日：2000-03-24
申请人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmond Differding , James Ellis , Marie-Agnes Lassoie , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
发明人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmond Differding , James Ellis , Marie-Agnes Lassoie , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
IPC分类号： A61K31495
CPC分类号： C07D295/096 , C07D295/084 , C07D295/088 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/15 , C07D307/14 , C07D307/52 , C07D401/04
摘要： The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferable asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
摘要翻译：本发明提供了1,4取代的哌嗪，1,4-取代的哌啶和1-取代的4-亚烷基哌啶化合物。本发明的化合物是具有白细胞三烯抑制性质以及抗组胺能性质的双作用分子。本发明的化合物可用于治疗可能存在组胺和/或白三烯组分的病症。这些病症包括优选的哮喘，季节性和常年性变态反应性鼻炎，窦炎，结膜炎，食物过敏，偶发性中毒，牛皮癣，荨麻疹，瘙痒，湿疹，类风湿性关节炎，炎性肠病，慢性阻塞性肺病，血栓性疾病和中耳炎。还提供了通过向有需要的受试者施用有效的哮喘和减轻炎症的量的化合物来治疗哮喘和鼻炎的方法。

3. 发明授权

US06894059B1 Compounds and methods for treatment of asthma, allergy and inflammatory disorders 失效
标题翻译：用于治疗哮喘，过敏和炎性疾病的化合物和方法
公开(公告)号：US06894059B1
公开(公告)日：2005-05-17
申请号：US09937667
申请日：2000-03-23
申请人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmund Differding , James Ellis , Marie-Agnes Lassoie , Michelle Young , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
发明人： Ralph Scannell , Pierre Chatelain , Anna Toy-Palmer , Edmund Differding , James Ellis , Marie-Agnes Lassoie , Michelle Young , Xiong Cai , Sajjat Hussoin , Gurmit Grewal , Timothy Lewis
IPC分类号： C07D295/084 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/15 , C07D307/52 , A61K31/44 , A61K31/445
CPC分类号： C07D295/096 , C07D295/084 , C07D295/088 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/15 , C07D307/52
摘要： The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obsructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.
摘要翻译：本发明提供了1,4取代的哌嗪，1,4-取代的哌啶和1-取代的4-亚烷基哌啶化合物。本发明的化合物是具有白细胞三烯抑制性质以及抗组胺能性质的双作用分子。本发明的化合物可用于治疗可能存在组胺和/或白三烯组分的病症。这些病症优选包括哮喘，季节性和常年性过敏性鼻炎，窦炎，结膜炎，食物过敏，鲭鱼中毒，牛皮癣，荨麻疹，瘙痒，湿疹，类风湿性关节炎，炎性肠病，慢性损伤性肺病，血栓性疾病和中耳炎。还提供了通过向有需要的受试者施用有效的哮喘和减轻炎症的量的化合物来治疗哮喘和鼻炎的方法。

4. 发明授权

US5565484A Benzenesulphonylindole derivatives for the preparation of medicines 失效
标题翻译：苯磺酰吲哚衍生物用于制备药物
公开(公告)号：US5565484A
公开(公告)日：1996-10-15
申请号：US282288
申请日：1994-07-29
申请人： Jean-Marc Herbert , Pierre Chatelain
发明人： Jean-Marc Herbert , Pierre Chatelain
IPC分类号： C07D401/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61P9/00 , A61P9/08 , A61P9/10 , C07D209/30 , A61K31/435 , C07D213/70
CPC分类号： C07D209/30
摘要： The invention relates to use of at least one indole derivative of general formula: ##STR1## or of one of the pharmaceutically acceptable salts thereof, in which: Am is selected from radical (a) and (b) defined as follows: ##STR2## R is a C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl radical R.sub.1 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.2 and R.sub.3, which may be identical or different, represent hydrogen, the methyl or ethyl radical or a halogenR.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen, a C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy radical or a halogenR.sub.7 represents hydrogen or a halogenR.sub.8 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.9 represents hydrogen or, when R.sub.8 and R.sub.9 are taken together, form the methylene radicalm represents 1 or 2n represents 2, 3 or 4for preventing or treating diseases involving a proliferation of smooth muscle cells.
摘要翻译：本发明涉及至少一种通式如下的吲哚衍生物或其药学上可接受的盐之一：其中：Am选自如下定义的基团（a）和（b）：（a）（a）（b）R是C 1 -C 6烷基或C 3 -C 6环烷基，R 1表示氢或C 1 -C 4烷基，R 2和R 3可以相同或不同，表示氢，甲基或乙基基或卤素可以相同或不同的R 4，R 5和R 6表示氢，C 1 -C 4烷基或C 1 -C 4烷氧基或卤素R 7表示氢或卤素R 8表示氢或C 1 -C 4烷基 R9表示氢，或当R8和R9一起形成亚甲基时m表示1或2 n表示2,3或4，用于预防或治疗涉及平滑肌细胞增殖的疾病。

5. 发明授权

US5182291A Pyrozala-pyridyl aminoabkoxyphenol compounds 失效
标题翻译：吡罗扎 - 吡啶基氨基氨基苯酚化合物
公开(公告)号：US5182291A
公开(公告)日：1993-01-26
申请号：US716252
申请日：1991-06-17
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： C07D209/30 , C07D213/70 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
CPC分类号： C07D213/70 , C07C309/00 , C07C317/00 , C07D209/30 , C07D213/71 , C07D215/36 , C07D235/22 , C07D261/10 , C07D277/36 , C07D307/64 , C07D471/04 , C07D495/04
摘要： Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radical orR.sub.3 and R.sub.4 when taken together, denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by --O--, ##STR2## R.sub.6 denoting hydrogen or a lower alkyl or pheny radical, Cy represents a cyclic group with the proviso that when Cy represents a benzo[b]furyl or benzo[b]thienyl group and B represents a --SO.sub.2 -- group, R.sub.3 represents a radical --Alk--R.sub.5, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.
摘要翻译：用于治疗下列心血管系统的某些病理学综合征的氨基烷氧基苯基衍生物：其中：B表示-S-，-SO-或-SO 2 - 基团，R 1和R 2各自相同或不同，表示氢，甲基或乙基或卤素，A表示具有2至5个碳原子的直链或支链亚烷基或2-羟基亚丙基，其中羟基任选被低级烷基取代，R 3 表示烷基或式Al-R 5的基团，其中Alk表示单键或具有1至5个碳原子的直链或支链亚烷基，R5表示吡啶基，苯基，2,3-亚甲二氧基苯基或3,4-亚甲二氧基苯基或被一个或多个选自卤素原子，低级烷基或低级烷氧基的取代基取代的苯基，R4表示氢或烷基或R3和R4，当一起表示具有3至6个碳原子并且任选被苯基取代或任选地被-O - ， - 表示氢或低级烷基或苯基的-C 1-6的亚烷基或亚烯基，Cy表示环状基团，条件是当Cy表示苯并[b]呋喃基或苯并[b]噻吩基，B表示-SO 2 - 基时，R 3表示基团-Alk-R 5，以及其N-氧化物衍生物及其药学上可接受的盐。

6. 发明授权

US4957925A Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same 失效
标题翻译：氨基烷氧基苯基衍生物，制备方法和含有它们的组合物
公开(公告)号：US4957925A
公开(公告)日：1990-09-18
申请号：US82554
申请日：1987-08-07
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： An aminoalkoxyphenyl compound of formula ##STR1## as well as a pharmaceutically acceptable salt of this compound.
摘要翻译：式IMAMA的氨基烷氧基苯基化合物以及该化合物的药学上可接受的盐。

7. 发明申请

US20130336910A1 OLFACTORY RECEPTORS INVOLVED IN THE PERCEPTION OF SWEAT CARBOXYLIC ACIDS AND THE USE THEREOF 有权
标题翻译：涉及甜菜羧酸的影响的老年受体及其用途
公开(公告)号：US20130336910A1
公开(公告)日：2013-12-19
申请号：US13916282
申请日：2013-06-12
申请人： Pierre Chatelain , Alex Veithen
发明人： Pierre Chatelain , Alex Veithen
IPC分类号： G01N33/566
CPC分类号： G01N33/566 , G01N2500/04
摘要： The invention relates to the identification of carboxylic acids, present in human sweat, as natural ligands of a specific subgroup of seven olfactory receptor (OR) belonging to class 1 within the OR classification. The invention encompasses the use of the interaction of OR polypeptides and carboxylic acids as the basis of screening assays for agents that specifically modulate the activity of the seven ORs of the invention.
摘要翻译：本发明涉及作为OR分类中属于1类的七个嗅觉受体（OR）的特定亚组的天然配体，存在于人类汗液中的羧酸的鉴定。本发明包括使用OR多肽和羧酸的相互作用作为特异性调节本发明的七个OR的活性的试剂的筛选测定的基础。

8. 发明授权

US5444056A Aminoalkoxyphenyl derivatives, process for their preparation and compositions containing them 失效
标题翻译：氨基烷氧基苯基衍生物，其制备方法和含有它们的组合物
公开(公告)号：US5444056A
公开(公告)日：1995-08-22
申请号：US476342
申请日：1990-02-07
申请人： Jean Gubin , Pierre Chatelain , Henri Inion , Gilbert Rosseels
发明人： Jean Gubin , Pierre Chatelain , Henri Inion , Gilbert Rosseels
IPC分类号： A61K31/13 , A61K31/255 , A61K31/34 , A61K31/343 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P9/00 , A61P25/02 , A61P27/02 , A61P27/06 , C07C317/22 , C07D207/325 , C07D209/30 , C07D213/70 , C07D295/08 , C07D295/092 , C07D307/82 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D221/02 , A61K31/33
CPC分类号： C07D295/088 , C07C317/22 , C07D209/30 , C07D307/82 , C07D471/04 , C07C2101/14
摘要： An aminoalkoxyphenyl derivative of general formula:Cy--B--Ph--O--A--Am (1)as well as a pharmaceutically acceptable salt thereof in whichB represents a --S--, --SO-- or --SO.sub.2 -- group,Ph represents an optionally substituted phenyl radical,A denotes a straight or branched alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxy propylene radical in which the hydroxy is optionally substituted by a C.sub.1 -C.sub.4 alkyl radical.Am represents a group: ##STR1## and Cy is a cyclic group, provided that when Cy represents either a benzo[b]furyl group substituted at position 4 by a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or a benzo[b]thienyl group substituted at position 4 by a halogen atom or by a C.sub.1 -C.sub.4 alkyl group and when B represents a --SO.sub.2 -- group, R.sub.3 represents a --Alk--Ar radical.
摘要翻译：通式为Cy-B-Ph-OA-Am（1）的氨基烷氧基苯基衍生物及其药学上可接受的盐，其中B表示-S-，-SO-或-SO2-基，Ph表示任选取代的苯基，A表示具有2至5个碳原子的直链或支链亚烷基或2-羟基丙烯基，其中羟基任选被C 1 -C 4烷基取代。 Am表示一组：（F）或（G）或（H），Cy是环状基团，条件是当Cy表示在4位被取代的苯并[b]呋喃基时，卤素原子或C1-C4烷基，或在4位被卤素原子或C1-C4烷基取代的苯并[b]噻吩基，当B表示-SO 2 - 基时，R 3表示-Alk -Ar根本

9. 发明授权

US5223510A Alkylaminoalkyl derivatives of benzofuran, benzothiophene, indole and indolizine, process for their preparation and compositions containing them 失效
标题翻译：苯并呋喃，苯并苯，吲哚和吲哚的烷基胺衍生物及其制备及其组合物的制备方法
公开(公告)号：US5223510A
公开(公告)日：1993-06-29
申请号：US736580
申请日：1991-07-26
申请人： Jean Gubin , Pierre Chatelain , Jean Lucchetti , Gilbert Rosseels , Henri Inion
发明人： Jean Gubin , Pierre Chatelain , Jean Lucchetti , Gilbert Rosseels , Henri Inion
IPC分类号： A61K31/34 , A61K9/48 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/435 , A61K31/437 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D209/00 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/44 , C07D221/00 , C07D307/80 , C07D307/81 , C07D333/56 , C07D333/58 , C07D409/06 , C07D417/12 , C07D471/04
CPC分类号： C07D409/06 , C07D209/12 , C07D307/80 , C07D307/81 , C07D333/56 , C07D471/04
摘要： The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: ##STR1## in which: Het represents one of the groups: ##STR2## in which T,T' and T"represent particularly a group: ##STR3## R and R.sub.a, identical or different, represent X represent --O-- or --S--Y represents a radical ##STR4## These compounds are useful as medecines particularly for the treatment of pathological syndroms of the cardio-vascular system.
摘要翻译：本发明的主题是以下通式的苯并呋喃，苯并噻吩，吲哚或中氮茚化合物：其中：Het代表下列组之一：其中T，T'和T' “代表特别是一组：R和R a相同或不同，表示X表示-O-或-S-Y表示基团这些化合物可用作特别用于治疗心脏病理综合征的药物血管系统。

10. 发明授权

US5039700A Benzofuranyl aminoalkoxyphenyl compounds 失效
标题翻译：苯并呋喃基氨基烷氧基苯基化合物
公开(公告)号：US5039700A
公开(公告)日：1991-08-13
申请号：US495134
申请日：1990-03-19
申请人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
发明人： Jean Gubin , Pierre Chatelain , Marcel Descamps , Dino Nisato , Henri Inion , Jean Lucchetti , Jean-Marie Mahaux , Jean-Noel Vallat
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , A61P35/00 , C07D207/36 , C07D213/26 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/913
摘要： Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5 in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radicalCy represents a benzo[b]furyl, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.

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