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1. 发明授权

US5086053A Derivatives of 1,3,4-thiadiazole, a method of obtaining them and pharmaceutical compositions containing them 失效
标题翻译： 1,3,4-噻二唑的衍生物，获得它们的方法和含有它们的药物组合物
公开(公告)号：US5086053A
公开(公告)日：1992-02-04
申请号：US394321
申请日：1989-08-16
申请人： Roger Brodin , Dominique Olliero , Paul Worms
发明人： Roger Brodin , Dominique Olliero , Paul Worms
IPC分类号： C07D285/12 , A61K31/41 , A61K31/433 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P25/00 , C07D285/135 , C07D417/04 , C07D417/12
CPC分类号： C07D285/135 , C07D417/04 , C07D417/12
摘要： The present invention relates to thiadiazole derivatives having the formula: ##STR1## in which: R.sub.1 represents a phenyl group, non-substituted or substitued 1 to 3 times by a halogen atom, preferably chlorine or fluorine, or by a C.sub.1 -C.sub.4 alkyl group, preferably the methyl group, or by a C.sub.1 -C.sub.4 alkoxy group, preferably the methoxy group, or by a hydroxy group or by a trifluoromethyl group or a phenyl group substituted simultaneously by 1 to 3 halogen atoms and by 1 or 2 methyl groupings;R.sub.2 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group,R.sub.3 represents an alkylamino group or a heterocyclic group,Application: Drugs for treatment of notably senile dementia.
摘要翻译：本发明涉及具有下式的噻二唑衍生物：其中：R 1表示苯基，被卤素原子，优选氯或氟或未被取代或取代1至3倍的苯基，或由C1- C4烷基，优选甲基，或通过C1-C4烷氧基，优选甲氧基，或羟基或被同时被1至3个卤素原子取代的三氟甲基或苯基取代，以及1或2个甲基组; R2表示氢或C1-C4烷基，R3表示烷基氨基或杂环基。应用：用于治疗特别是老年性痴呆的药物。

2. 发明授权

US5656631A Pyridazine derivatives 失效
标题翻译：哒嗪衍生物
公开(公告)号：US5656631A
公开(公告)日：1997-08-12
申请号：US473580
申请日：1995-06-07
申请人： Robert Boigegrain , Roger Brodin , Jean Paul Kan , Dominique Olliero , Camille Georges Wermuth , Jean-Jacques Bourguignon , Paul Worms
发明人： Robert Boigegrain , Roger Brodin , Jean Paul Kan , Dominique Olliero , Camille Georges Wermuth , Jean-Jacques Bourguignon , Paul Worms
IPC分类号： C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D451/04 , C07D487/04 , A61K31/50
CPC分类号： C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D451/04 , C07D487/04
摘要： The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
摘要翻译：本发明涉及可用作胆碱能受体的配体，特别是M1型受体的下式的哒嗪衍生物：（I）图像（IA）（ⅠB）。

3. 发明授权

US5081119A Use of 5-alkylpyridazine derivatives as drugs active on the cholinergic system 失效
标题翻译：作为药物活性成分的5-烷基吡啶衍生物的使用
公开(公告)号：US5081119A
公开(公告)日：1992-01-14
申请号：US475490
申请日：1990-02-07
申请人： Robert Boigegrain , Camille G. Wermuth , Paul Worms
发明人： Robert Boigegrain , Camille G. Wermuth , Paul Worms
IPC分类号： A61K31/50 , A61K31/535 , A61P25/28 , C07D237/20
CPC分类号： A61K31/50 , A61K31/535 , C07D237/20
摘要： The invention relates to the use of 5-alkylpyridazine derivatives of the formula ##STR1## in which R.sub.1 is a C.sub.1 -C.sub.4 alkyl group or a phenyl group and R.sub.2 and R.sub.3 independently are a C.sub.1 -C.sub.4 alkyl group, or R.sub.2 and R.sub.3, taken with the nitrogen atom to which they are bonded, form a morpholino group, or one of their pharmaceutically acceptable salts, for the preparation of pharmaceutical compositions for combating pathological conditions associated with a cortical cholinergic deficiency, especially for the treatment of degenerative syndromes associated with senescence.
摘要翻译：本发明涉及式（Ⅱ）的5-烷基哒嗪衍生物，其中R 1是C 1 -C 4烷基或苯基，R 2和R 3独立地是C 1 -C 4烷基，或R 2和 R3与其键合的氮原子一起形成吗啉基或其药学上可接受的盐之一，用于制备用于对抗与皮层胆碱能缺乏相关的病理状况的药物组合物，特别是用于治疗退行性综合征与衰老有关。

4. 发明授权

US4977152A Novel tricyclic derivatives which are agonists of cholinergic receptors, and drugs in which they are present 失效
标题翻译：作为胆碱能受体的激动剂的新型三环衍生物及其存在的药物
公开(公告)号：US4977152A
公开(公告)日：1990-12-11
申请号：US471680
申请日：1990-01-25
申请人： Kathleen Biziere , Camille G. Wermuth , Paul Worms , Jean-Jacques Bourguignon
发明人： Kathleen Biziere , Camille G. Wermuth , Paul Worms , Jean-Jacques Bourguignon
IPC分类号： A61K31/50 , A61K31/502 , A61K31/535 , A61P25/28 , C07D237/26 , C07D237/36 , C07D403/12 , C07D413/12
CPC分类号： C07D403/12 , C07D237/26 , C07D237/36 , C07D413/12
摘要： The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them.These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;R.sub.1 and R.sub.2, considered independently, represent hydrogen or a substituent occupying one of the free positions of the benzene ring and selected from the group comprising halogens, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a thiol group, a nitro group and an optionally substituted amino group;Y represents oxygen, sulfur or a group --NH--; andR.sub.3 is an amino groupApplication: agonists of the cholinergic receptors.
摘要翻译：本发明涉及作为胆碱能受体的激动剂的新型三环衍生物和含有它们的药物。这些衍生物具有下式：其中：X表示基团（CH 2）n，n表示等于2,3或4的整数，或者可选地是亚乙烯基或甲基亚乙烯基; 独立地考虑的R 1和R 2表示氢或占据苯环的一个游离位置的取代基，并且选自卤素，低级烷基，低级烷氧基，羟基，硫醇基，硝基基团和任选取代的氨基; Y表示氧，硫或基团-NH-; 并且R3是氨基应用：胆碱能受体的激动剂。

5. 发明授权

US1774428A Dyeing process 失效
标题翻译：染色工艺
公开(公告)号：US1774428A
公开(公告)日：1930-08-26
申请号：US67596023
申请日：1923-11-20
申请人： AUGUSTE ESCAICH , PAUL WORMS JEAN
发明人： AUGUSTE ESCAICH , PAUL WORMS JEAN
IPC分类号： D06P1/32 , D06P3/04 , D06P3/14 , D06P3/60
CPC分类号： D06P1/32 , D06P3/04 , D06P3/14 , D06P3/60

6. 发明授权

US5232921A Thiazole derivatives active on the cholinergic system, process for obtention and pharmaceutical compositions 失效
标题翻译：在胆碱能系统上活性的噻唑衍生物，获得的过程和药物组合物
公开(公告)号：US5232921A
公开(公告)日：1993-08-03
申请号：US632609
申请日：1990-12-27
申请人： Kathleen Biziere , Dominique Olliero , Paul Worms
发明人： Kathleen Biziere , Dominique Olliero , Paul Worms
IPC分类号： C07D277/42 , C07D277/60 , C07D277/84
CPC分类号： C07D277/60 , C07D277/42 , C07D277/84
摘要： The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group of an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pyridino group.
摘要翻译：本发明涉及对应于以下通式的噻唑衍生物：其中：R 1和R 2各自独立地表示氢; C1-C4烷基; 苯基或被卤素原子，C1-C4烷基，C1-C4烷氧基，硝基或羟基单取代或多取代的苯基; 或者R1和R2中的一个表示氢，另一个表示萘基; 苄基; α，α-二甲基 - 苄基; 环己基; 联苯基金刚烷基的噻吩基; 或者R1和R2一起表示一个基团; 其中苯基与噻唑的4-位键合（CH2）m至5-位，m表示等于2或3的整数，R 5表示氢或硝基，R 3 是H或烷基，R4特别是被氨基，吡咯烷子基或吡啶基取代的烷基。

7. 发明授权

US4983603A Tricyclic cholinergic receptor agonists 失效
标题翻译：三环胆碱能受体激动剂
公开(公告)号：US4983603A
公开(公告)日：1991-01-08
申请号：US288861
申请日：1988-12-23
申请人： Camille G. Wermuth , Paul Worms , Jean-Jacques Bourguignon , Roger Brodin
发明人： Camille G. Wermuth , Paul Worms , Jean-Jacques Bourguignon , Roger Brodin
IPC分类号： A61K31/50 , A61P25/02 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04
CPC分类号： C07D491/04 , C07D495/04
摘要： The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors.These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.
摘要翻译：本发明涉及作为胆碱能受体激动剂的新型三环衍生物。这些衍生物具有其中X = O，S，-OCH 2 - 或-SCH 2 - 的式（I） R1 = H或卤素; 和其中Alk是亚烷基的R 2 =＆lt; IMAGE＆gt; R 3，相同或不同的R 4是氢或低级烷基，或者R 3和R 4与它们相连的氮原子形成任选地含有第二杂原子的5-或6-元环氨基; 或R 2为基团，其中R 5 = C 1 -C 4 - 烷基。应用：胆碱能受体的激动剂。

8. 发明授权

US1716218A Dyeing process 失效
公开(公告)号：US1716218A
公开(公告)日：1929-06-04
申请号：US67596123
申请日：1923-11-20
申请人： AUGUSTE ESCAICH , PAUL WORMS JEAN
发明人： AUGUSTE ESCAICH , PAUL WORMS JEAN
IPC分类号： D06P1/00
CPC分类号： D06P1/0076

9. 发明授权

US5461053A Pyridazine derivatives 失效
标题翻译：哒嗪衍生物
公开(公告)号：US5461053A
公开(公告)日：1995-10-24
申请号：US964901
申请日：1992-10-22
申请人： Robert Boigegrain , Roger Brodin , Jean P. Kan , Dominique Olliero , Camille G. Wermuth , Jean-Jacques Bourguignon , Paul Worms
发明人： Robert Boigegrain , Roger Brodin , Jean P. Kan , Dominique Olliero , Camille G. Wermuth , Jean-Jacques Bourguignon , Paul Worms
IPC分类号： C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D451/04 , C07D487/04 , A61K31/50 , C07D413/12
CPC分类号： C07D451/04 , C07D237/04 , C07D237/12 , C07D237/14 , C07D237/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D451/02 , C07D487/04
摘要： The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
摘要翻译：本发明涉及可用作胆碱能受体的配体，特别是M1型受体的下式的哒嗪衍生物：（I）图像（IA）（ⅠB）。

10. 发明授权

US5378706A Fused-thiazole derivatives active on the cholinergic system, and pharmaceutical compositions containing same 失效
标题翻译：在胆碱能系统上活性的熔融 - 噻唑衍生物和含有它们的药物组合物
公开(公告)号：US5378706A
公开(公告)日：1995-01-03
申请号：US68224
申请日：1993-05-28
申请人： Kathleen Biziere , Dominique Olliero , Paul Worms
发明人： Kathleen Biziere , Dominique Olliero , Paul Worms
IPC分类号： C07D277/42 , C07D277/60 , C07D277/84 , A61K31/425 , C07D401/12 , C07D417/12
CPC分类号： C07D277/60 , C07D277/42 , C07D277/84
摘要： The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: - R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group or an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pydridino group.
摘要翻译：本发明涉及对应于以下通式的噻唑衍生物：其中：R 1和R 2各自独立地表示氢; C1-C4烷基; 苯基或被卤素原子，C1-C4烷基，C1-C4烷氧基，硝基或羟基单取代或多取代的苯基; 或者R1和R2中的一个表示氢，另一个表示萘基; 苄基; α，α-二甲基 - 苄基; 环己基; 联苯基噻吩基或金刚烷基; 或者R1和R2一起表示一个基团; 其中苯基与噻唑的4-位键合（CH2）m至5-位，m表示等于2或3的整数，R 5表示氢或硝基，R 3 是H或烷基，R4特别是被氨基，吡咯烷子基或吡啶基取代的烷基。

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