公开(公告)号：US06797713B2

公开(公告)日：2004-09-28

申请号：US10242346

申请日：2002-09-12

Applicant: Ralph Scannell ,  Pierre Chatelain ,  Anna Toy-Palmer ,  Edmond Differding ,  James Ellis ,  Marie-Agnes Lassoie ,  Michelle Young ,  Xiong Cai ,  Sajjat Hussoin ,  Gurmit Grewal ,  Timothy Lewis

Inventor： 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: A61K31495

CPC classification number: C07D295/096 ,  C07D295/084 ,  C07D295/088 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/15 ,  C07D307/14 ,  C07D307/52 ,  C07D401/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5658938A

公开(公告)日：1997-08-19

申请号：US569947

申请日：1995-12-08

Applicant: Jean-Pierre Geerts ,  Genevieve Motte ,  Edmond Differding ,  Jean-Pierre Henichart

Inventor： Jean-Pierre Geerts ,  Genevieve Motte ,  Edmond Differding ,  Jean-Pierre Henichart

IPC: C07D233/64 ,  A61K31/415 ,  A61K31/4164 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D233/54 ,  C07D233/56

CPC classification number: C07D233/64

Abstract: Substituted 4-(1,2,3,4-tetrahydro-1-naphthalenyl)-1H-imidazoles and 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles, their optical isomers and their racemic mixtures, their salts, methods for preparing them and therapeutic compositions containing them. These compounds have the general formula ##STR1## wherein n=1 or 2,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 =hydrogen, halogen, hydroxyl C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy,R.sub.5 = hydrogen of C.sub.1 -C.sub.4 alkyl with the proviso that R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, cannot simultaneously be hydrogen when n is equal to 2.These new compounds exhibit anti-ischemic and anti-hypertensive activities.

Abstract translation: 取代的4-（1,2,3,4-四氢-1-萘基）-1H-咪唑和4-（2,3-二氢-1H-茚-1-基）-1H-咪唑，它们的旋光异构体及其 外消旋混合物，其盐，制备它们的方法和含有它们的治疗组合物。 这些化合物具有通式如下：卤素，羟基C 1 -C 4烷基或C 1 -C 4烷氧基，R 5 = C 1 -C 4烷基的氢，条件是R 1，R 2，R 3，R 4和R 5不能同时为氢 当n等于2.这些新化合物表现出抗缺血和抗高血压活性。

公开(公告)号：US5457209A

公开(公告)日：1995-10-10

申请号：US306864

申请日：1994-09-15

Applicant: Marc Lang ,  Edmond Differding ,  Jaroslav Stanek

Inventor： Marc Lang ,  Edmond Differding ,  Jaroslav Stanek

IPC: A61K31/41 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/496 ,  A61K31/505 ,  A61P5/32 ,  A61P35/00 ,  A61P43/00 ,  C07D209/10 ,  C07D209/44 ,  C07D213/26 ,  C07D213/57 ,  C07D215/12 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D233/64 ,  C07D235/12 ,  C07D235/16 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D403/06 ,  C07D405/06 ,  C07D521/00

CPC classification number: C07D239/26 ,  C07D213/26 ,  C07D231/12 ,  C07D233/56 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04

Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.

Abstract translation: 其中Z，R，R 1，R 2和X如说明书中所定义的式I化合物（I）具有有价值的药物性质，尤其对肿瘤有效。 它们是以本身已知的方式准备的。

公开(公告)号：US5227393A

公开(公告)日：1993-07-13

申请号：US805261

申请日：1991-12-09

Applicant: Marc Lang ,  Edmond Differding ,  Jaroslav Stanek

Inventor： Marc Lang ,  Edmond Differding ,  Jaroslav Stanek

IPC: A61K31/41 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/496 ,  A61K31/505 ,  A61P5/32 ,  A61P35/00 ,  A61P43/00 ,  C07D209/10 ,  C07D209/44 ,  C07D213/26 ,  C07D213/57 ,  C07D215/12 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D233/64 ,  C07D235/12 ,  C07D235/16 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D403/06 ,  C07D405/06 ,  C07D521/00

CPC classification number: C07D239/26 ,  C07D213/26 ,  C07D231/12 ,  C07D233/56 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04

Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.

Abstract translation: 其中Z，R，R 1，R 2和X如说明书中所定义的式I化合物（I）具有有价值的药物性质，尤其对肿瘤有效。 它们是以本身已知的方式准备的。