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1. 发明授权

US5698567A Heterocyclic spiro compounds 失效
标题翻译：杂环螺环化合物
公开(公告)号：US5698567A
公开(公告)日：1997-12-16
申请号：US649020
申请日：1996-05-16
申请人： Claude Guillonneau , Yves Charton , Gilbert Regnier , Emmanuel Canet , Michel Lonchampt
发明人： Claude Guillonneau , Yves Charton , Gilbert Regnier , Emmanuel Canet , Michel Lonchampt
IPC分类号： C07D491/113 , A61K31/445 , A61K31/47 , A61P17/00 , A61P43/00 , C07D471/10 , C07D498/10 , A61K31/44 , C07D491/10
CPC分类号： C07D498/10
摘要： The invention provides new compounds pertaining to the class of: aryl methoxy phenyl alkyl heterocyclic spiro compounds, enantiomers, diastereoisomers and physiologically-tolerable salts thereof. For example: 8-{2-�3-quinol-2-yl methoxy)phenyl!ethyl}-3,8-diaza-1-oxa-2-oxo spiro�4,5!decane is described. Medicinal products containing the same are useful in the treatment of any pathology involving modifications of leukotriene metabolism.
摘要翻译：本发明提供了与以下类别有关的新化合物：芳基甲氧基苯基烷基杂环螺环化合物，对映异构体，非对映异构体及其生理上可容忍的盐。例如：描述8- {2- [3-喹啉-2-基甲氧基）苯基]乙基} -3,8-二氮杂-1-氧杂-2-氧代螺[4,5]癸烷。含有该药物的药物可用于治疗涉及白三烯代谢修饰的任何病理学。

2. 发明授权

US5708016A Pseudopeptides derived from neurokinins 失效
标题翻译：衍生自神经激肽的伪肽
公开(公告)号：US5708016A
公开(公告)日：1998-01-13
申请号：US801037
申请日：1997-02-14
申请人： Jean-Luc Fauchere , Nathalie Kucharczyk-Gentric , Emmanuel Canet , Michel Lonchampt
发明人： Jean-Luc Fauchere , Nathalie Kucharczyk-Gentric , Emmanuel Canet , Michel Lonchampt
IPC分类号： C07D403/14 , A61K31/41 , A61K38/00 , A61P1/08 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D409/14 , C07K5/02 , C07K5/023 , A01N43/713
CPC分类号： C07K5/0202 , A61K38/00
摘要： A compound of formula (I): ##STR1## in which: R.sub.1 represents an indolyl, naphthyl, tetrahydronaphthyl, thienyl, phenyl, optionally substituted, or (C.sub.3 -C.sub.7)cycloalkyl group, n represents an integer such that 1.ltoreq.n.ltoreq.8, m represents an integer such that 1.ltoreq.m.ltoreq.4, R.sub.2 represents an unsubstituted or substituted benzyl group, an unsubstituted or substituted phenyl group or a linear or branched (C.sub.1 -C.sub.6)alkyl group, its enantiomers, diastereoisomers and epimers as well as its addition salts with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as substance P antagonists.
摘要翻译：式（I）化合物：其中：R 1表示吲哚基，萘基，四氢萘基，噻吩基，苯基，任选取代的或（C 3 -C 7）环烷基，n表示1 < / =n≤8，m表示1≤n≤4的整数，R2表示未取代或取代的苄基，未取代或取代的苯基或直链或支链（C1-C6）烷基基团，其对映体，非对映异构体和差向异构体以及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作P物质拮抗剂。

3. 发明授权

US5565429A Peptides derived from trifluoromethylketones 失效
标题翻译：衍生自三氟甲基酮的肽
公开(公告)号：US5565429A
公开(公告)日：1996-10-15
申请号：US439233
申请日：1995-05-11
申请人： Michel Vincent , Guillaume de Nanteuil , Georges Remond , Bernard Portevin , Yolande Herve , Emmanuel Canet , Michel Lonchampt
发明人： Michel Vincent , Guillaume de Nanteuil , Georges Remond , Bernard Portevin , Yolande Herve , Emmanuel Canet , Michel Lonchampt
IPC分类号： A61K38/00 , A61P29/00 , C07K1/10 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/087 , C07K5/09 , C07K14/81 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/06191 , A61K38/00
摘要： Compounds of formula (I): ##STR1## wherein: R.sub.1 represents an unsubstituted or substituted alkyl,R.sub.2 represents an unsubstituted or substituted alkyl,A represents, with the nitrogen and carbon atoms to which it is attached, a nitrogenous mono- or polycyclic structure, andB represent any one of the radicals a through j as defined in the description, and medicaments containing the same, are useful as human leucocyte elastase inhibitors.
摘要翻译：式（I）的化合物：其中：R 1表示未取代或取代的烷基，R 2表示未取代或取代的烷基，A表示与其连接的氮和碳原子，或多环结构，B表示说明书中定义的基团a至j中的任一个，含有该基团的药物可用作人白细胞弹性蛋白酶抑制剂。

4. 发明授权

US5877190A Substituted biphenyl compounds 失效
标题翻译：取代的联苯化合物
公开(公告)号：US5877190A
公开(公告)日：1999-03-02
申请号：US943562
申请日：1997-10-03
申请人： Alain Dhainaut , Guillaume Poissonnet , Emmanuel Canft , Michel Lonchampt
发明人： Alain Dhainaut , Guillaume Poissonnet , Emmanuel Canft , Michel Lonchampt
IPC分类号： C07D233/64 , A61K31/05 , A61K31/11 , A61K31/135 , A61K31/15 , A61K31/165 , A61K31/275 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P11/00 , A61P11/08 , A61P25/00 , A61P27/16 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07C43/20 , C07C45/71 , C07C47/546 , C07C47/57 , C07C47/575 , C07C49/798 , C07C49/84 , C07C49/86 , C07C65/21 , C07C67/14 , C07C69/157 , C07C69/24 , C07C69/28 , C07C69/75 , C07C201/12 , C07C205/20 , C07C205/44 , C07C205/60 , C07C217/82 , C07C235/44 , C07C235/60 , C07C251/48 , C07C251/54 , C07C251/86 , C07C255/53 , C07C255/54 , C07C255/58 , C07C257/18 , C07C259/10 , C07C323/31 , C07D209/08 , C07D213/06 , C07D213/50 , C07D215/12 , C07D231/12 , C07D307/79 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D401/02
CPC分类号： C07D307/79 , C07C205/20 , C07C205/44 , C07C205/60 , C07C235/60 , C07C251/48 , C07C251/86 , C07C255/53 , C07C259/10 , C07C45/71 , C07C47/57 , C07C47/575 , C07D209/08 , C07D213/50 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/06
摘要： A compound of formula (I): ##STR1## wherein: R.sub.1 represents unsubstituted or substituted cycloalkyl, phenyl, naphthyl, heterocyclic, alkyl or alkenyl,A represents a bond, oxygen, sulphur, a group ##STR2## a group ##STR3## or a group ##STR4## wherein Rc represents hydrogen, alkyl or cycloalkyl, R.sub.2 represents halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, cycloalkyl, formyl, carboxy, alkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, cycloalkyloxycarbonyl, optionally substituted carbamoyl, optionally substituted amino, formylamino, cyano, optionally substituted amidino, hydroxyaminomethyl, amide oxime, hydrazono, or a group selected from: ##STR5## wherein R.sub.21, R.sub.22 and R.sub.23 are as defined in the description, R.sub.3 represents hydrogen or alkyl, cycloalkyl or acyl,or ##STR6## together form the ring ##STR7## X is oxygen, sulphur, or NR", B is phenyl, Ra and Rb, which may be identical or different, each represents hydrogen, halogen, or alkyl, hydroxy, alkoxy, carboxy, polyhalogenoalkyl, cyano, nitro, alkoxycarbonyl, cycloalkyloxycarbonyl, amino, carbamoyl, sulfo, alkylsulfonyl, cycloalkylsulfonyl or aminosulfonyl, their isomers, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as PDE IV inhibitors.
摘要翻译：式（I）化合物：其中：R 1表示未取代或取代的环烷基，苯基，萘基，杂环基，烷基或烯基，A表示键，氧，硫，取代或未取代的烷基，取代或未取代的链烯基，取代或未取代的炔基，环烷基，甲酰基，羧基，烷基羰基，环烷基羰基，烷氧基羰基，环烷氧基羰基，任选取代的氨基甲酰基，任选取代的氨基，甲酰氨基，氰基，任选取代的脒基，羟基氨基甲基，酰胺肟，亚氨基或选自以下的基团：其中R 21，R 22和R 23如说明书中所定义，R 3表示氢或烷基，环烷基或酰基，或一起形成环，X是氧，硫或NR“，B是苯基，R a和R b可以相同或不同，各自表示氢，卤素或烷基，羟基，烷氧基，羧基，多卤代烷基，氰基，硝基，烷氧基羰基，环烷氧基羰基，氨基，氨基甲酰基，磺基，烷基磺酰基，环烷基磺酰基或氨基磺酰基，它们的异构体及其与药学上可接受的酸或碱的加成盐，含有该药物的药物可用作PDE IV抑制剂。

5. 发明授权

US5919801A N-substituted piperidines as PDE4 inhibitors 失效
标题翻译： N-取代的哌啶类作为PDE4抑制剂
公开(公告)号：US5919801A
公开(公告)日：1999-07-06
申请号：US934409
申请日：1997-09-19
申请人： Alain Dhainaut , Andre Tizot , Emmanuel Canet , Michel Lonchampt
发明人： Alain Dhainaut , Andre Tizot , Emmanuel Canet , Michel Lonchampt
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61P11/00 , A61P11/08 , A61P29/00 , A61P43/00 , C07D211/22 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D401/06 , C07D211/22 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： New N-substituted cyclic amines of formula: ##STR1## wherein: X, R.sub.1, R.sub.2 and R are as defined in the description, their optical and geometric isomers and physiologically tolerable salts thereof. The compounds of the invention are powerful PDE4 inhibitors and can be used therapeutically.
摘要翻译：新的N-取代的环状胺，其结构如下：其中：X，R 1，R 2和R 2如说明书中所定义，它们的光学和几何异构体及其生理上可耐受的盐。本发明的化合物是强效的PDE4抑制剂，可用于治疗。

6. 发明授权

US5889003A Flavone compounds 失效
标题翻译：黄酮化合物
公开(公告)号：US5889003A
公开(公告)日：1999-03-30
申请号：US968837
申请日：1997-09-26
申请人： Alain Dhainaut , Guy Lewin , Emmanuel Canet , Michel Lonchampt , Yves Rolland
发明人： Alain Dhainaut , Guy Lewin , Emmanuel Canet , Michel Lonchampt , Yves Rolland
IPC分类号： A61K31/35 , A61K31/352 , A61P11/00 , A61P29/00 , A61P43/00 , C07D311/30 , C07D405/12
CPC分类号： C07D405/12 , C07D311/30
摘要： A compound of general formula (I): ##STR1## in which: R.sub.1 represents alkyl,X represents oxygen, --CHR'-- or --CR'.dbd.,R' is chosen from hydrogen and alkyl,R.sub.2 represents optionally substituted alkyl as is defined in the description, cycloalkyl or polycycloalkyl as are defined in the description,R.sub.3 represents hydrogen or hydroxyl,Alk represents alkylene, andY is as defined in the description,and medicinal products containing the same are useful as PDE IV inhibitors.
摘要翻译：通式（I）的化合物：其中：R 1表示烷基，X表示氧，-CHR'-或-CR'=，R'选自氢和烷基，R 2表示任选取代的烷基如描述中定义的环烷基或多环烷基，如说明书中所定义，R 3表示氢或羟基，Alk表示亚烷基，Y如说明书中所定义，并且含有该化合物的药物可用作PDE IV抑制剂。

7. 发明授权

US4968705A Benzopyrrolidinone compounds as bronchospastic agents 失效
标题翻译：苯并吡咯烷酮化合物作为支气管痉挛剂
公开(公告)号：US4968705A
公开(公告)日：1990-11-06
申请号：US391936
申请日：1989-08-10
申请人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michel Lonchampt
发明人： Gilbert Regnier , Alain Dhainaut , Jacques Duhault , Michel Lonchampt
IPC分类号： C07D491/056 , A61K31/4427 , A61K31/445 , A61P11/00 , A61P29/00 , A61P37/08 , C07D401/06
CPC分类号： C07D401/06
摘要： New benzopyrrolidinone compounds, which can be used as medicaments and correspond to the formula ##STR1## in which: either: R.sub.1 and R.sub.2 together represent, with the bond of the etherocycle to which they are attached, an optionally substituted benzene nucleus and, simultaneously, R.sub.3 and R.sub.4 are hydrogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.5 -C.sub.6)cycloalkyl;or:R.sub.1 is hydrogen, R.sub.4 is a single bond and R.sub.2 and R.sub.3 together represent, with the bond of the heterocycle to which they are bonded, an optionally substituted benzene nucleus; andA is a straight or branched hydrocarbon chain having from 2 to 6 carbon atoms that is optionally substituted by hydroxy;X is a single bond, oxygen or sulphur; andY is hydrogen, halogen or (C.sub.1 -C.sub.5)alkyl or alkoxy.These new compounds and the physiologically tolerable salts thereof can be used therapeutically, especially in the treatment of bronchospastic disorders and inflammations in the ENT area.
摘要翻译：新的苯并吡咯烷酮化合物，其可以用作药物并且对应于式“IMAGE”，其中：R 1和R 2一起表示与它们所连接的醚基的键，任选取代的苯核， R3和R4是氢，（C1-C4）烷基或（C5-C6）环烷基; 或：R 1是氢，R 4是单键，并且R 2和R 3一起表示与它们所键合的杂环的键，任选取代的苯核; 并且A是具有2-6个碳原子的直链或支链烃链，任选被羟基取代; X是单键，氧或硫; 和Y是氢，卤素或（C 1 -C 5）烷基或烷氧基。这些新化合物及其生理上可耐受的盐可用于治疗，特别是在ENT区域的支气管痉挛性障碍和炎症的治疗中。

8. 发明授权

US4824836A Spiro (4,5) decone compounds 失效
标题翻译：螺（4,5）癸酮化合物
公开(公告)号：US4824836A
公开(公告)日：1989-04-25
申请号：US196303
申请日：1988-05-20
申请人： Gilbert Regnier , Claude Guillonneau , Jacques Duhault , Michel Lonchampt
发明人： Gilbert Regnier , Claude Guillonneau , Jacques Duhault , Michel Lonchampt
IPC分类号： A61K31/435 , A61K31/625 , A61P9/12 , A61P11/00 , A61P29/00 , A61P37/08 , C07D498/10 , A61K31/445
CPC分类号： C07D498/10
摘要： Spiro (4,5) decane compounds of the formula: ##STR1## in which: X is methyl andY is hydrogen or R'--CO-- in which R' is C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, ##STR2## X and Y together represent ##STR3## in each of which A is hydrogen, methyl, carboxy, methoxycarbonyl or ethoxycarbonyl;R is C.sub.1 -C.sub.7 -alkyl optionally containing a double bond;Z is a C.sub.2 -C.sub.7 -polymethylene chain optionally carrying an OH group;R.sub.1 is hydrogen or methyl; andR.sub.2 is hydrogen, R'--CO-- or benzyloxycarbonyl;and physiologically tolerable acid addition salts thereof.These compounds may be used therapeutically especially in the treatment of asthma, allergic phenomena and bronchopathies.
摘要翻译：螺（4,5）癸烷化合物，其分子式为：其中：X为甲基，Y为氢或R'-CO-，其中R'为C 1 -C 4烷基或C 1 -C 4 - 烷氧基， X和Y一起代表其中A是氢，甲基，羧基，甲氧基羰基或乙氧基羰基的“IMAGE”; R是任选含有双键的C 1 -C 7 - 烷基; Z是可选地携带OH基团的C2-C7-聚亚甲基链; R1是氢或甲基; R2为氢，R'-CO-或苄氧基羰基; 和其生理上可耐受的酸加成盐。这些化合物可以特别用于治疗哮喘，过敏现象和支气管炎。

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