专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5484804A Perhydroisoindole derivatives as antagonists of substance P 失效
标题翻译：全氟异吲哚衍生物作为P物质的拮抗剂
公开(公告)号：US5484804A
公开(公告)日：1996-01-16
申请号：US313121
申请日：1994-10-11
申请人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
发明人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
IPC分类号： C07D405/06 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61P9/02 , A61P9/12 , A61P11/00 , A61P11/06 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/44 , C07D403/06 , C07D409/06 , C07D401/06
CPC分类号： C07D403/06 , C07D209/44 , C07D409/06
摘要： This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; R.sub.3 is optionally 2-substituted phenyl; R.sub.4 is OH or fluorine when R.sub.5 is H, or R.sub.4 and R.sub.5 are OH or R.sub.4 and R.sub.5 together form a bond; isomeric forms and mixtures thereof; optionally salts thereof where applicable; and preparation thereof. The novel derivatives are particularly useful as P substance antagonists.
摘要翻译： PCT No。PTC / FR93 / 00352 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。公开号WO93 / 21155 本发明涉及通式（I）的新型全氢异吲哚衍生物，其中基团R是任选被卤素原子或甲基取代的2-或3-取代的苯基; R1是任选取代的苯基，环己二烯基，萘基，茚基或任选取代的杂环基; R2是H，卤素，OH，烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基，烷硫基，酰氧基，羧基，任选取代的烷氧基羰基，苄氧羰基，氨基或酰氨基; R3是任选的2-取代的苯基; 当R 5为H或R 4和R 5为OH或R 4和R 5一起形成键时，R 4为OH或氟; 异构形式及其混合物; 任选的盐; 及其制备。新型衍生物作为P物质拮抗剂是特别有用的。

2. 发明授权

US5463077A Perhydroisoindole derivatives and preparation 失效
标题翻译：全氢异吲哚衍生物及其制备方法
公开(公告)号：US5463077A
公开(公告)日：1995-10-31
申请号：US313120
申请日：1994-10-11
申请人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
发明人： Daniel Achard , Serge Grisoni , Jean-Luc Malleron , Jean-Francois Peyronel , Michel Tabart
IPC分类号： C07D209/44 , C07D403/06 , C07D409/06 , C07D209/04
CPC分类号： C07D403/06 , C07D209/44 , C07D409/06 , Y02P20/55
摘要： This ivention relates to novel perhydroisoindole derivatives having formula (I), ##STR1## wherein the symbols R, which are the same or different, are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical, R' is a phenyl radical optionally 2-substituted by a C.sub.1-2 alkylk or alkyloxy radical, R" is a fluorine atom or a hydroxy radical, and R'" is a hydrogen atom, or else R' and R'" are hydroxy radicals, or R" and R'" together form a bond, and R.sup.o is a hydrogen atom or a protective radical; salts thereof whereever applicable; and preparation thereof. These products are synthetic intermediates for the preparation of derivatives having P substance antagonist activity.
摘要翻译： PCT No.PCT / FR93 / 00351 Sec。 371日期：1994年10月11日 102（e）日期1994年10月11日PCT提交1993年4月8日PCT公布。出版物WO93 / 21154 日本公开日1993年10月28日。本说明书涉及具有式（I），其中符号R相同或不同的式（I）的新型全氢异吲哚衍生物是任选被2-或3-取代的苯基卤素原子或甲基，R'是任选被C 1-2烷基或烷氧基取代的苯基，R“是氟原子或羟基，R”'是氢原子，或其中R'和R“'是羟基，或者R”和R“'一起形成键，而Ro是氢原子或保护基; 其盐适用; 及其制备。这些产品是用于制备具有P物质拮抗剂活性的衍生物的合成中间体。

3. 发明授权

US5624950A Perhydroisoindole derivatives as substance P antagonists 失效
标题翻译：全氢异吲哚衍生物作为P物质拮抗剂
公开(公告)号：US5624950A
公开(公告)日：1997-04-29
申请号：US586708
申请日：1996-01-29
申请人： Daniel Achard , Serge Grisoni , Evelyne James-Surcouf , Jean-Luc Malleron , Anne Morgat , Jean-Fran.cedilla.ois Peyronel , Jean-Fran.cedilla.ois Sabuco , Michel Tabart
发明人： Daniel Achard , Serge Grisoni , Evelyne James-Surcouf , Jean-Luc Malleron , Anne Morgat , Jean-Fran.cedilla.ois Peyronel , Jean-Fran.cedilla.ois Sabuco , Michel Tabart
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/44
CPC分类号： C07D209/44
摘要： Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught. ##STR1##
摘要翻译： PCT No.PCT / FR94 / 00952 Sec。 371日期1996年1月29日 102（e）日期1996年1月29日PCT提交1994年7月28日PCT公布。出版物WO95 / 04040 日期：1995年2月9日，式I的泛氢异吲哚衍生物，其中取代基如说明书中所定义，特别适合作为P物质拮抗剂。还教导了几种制备化合物的方法。（一）

4. 发明授权

US5036075A Derivatives of (AZA) naphthalensultam, their preparation and compositions containing them 失效
标题翻译：（AZA）萘磺酸的衍生物，它们的制备和含有它们的组合物
公开(公告)号：US5036075A
公开(公告)日：1991-07-30
申请号：US609506
申请日：1990-11-06
申请人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P11/00 , A61P25/00 , A61P43/00 , C07D275/06 , C07D417/00 , C07D417/06 , C07D417/14 , C07D513/06
CPC分类号： C07D275/06 , C07D417/06 , C07D417/14 , C07D513/06
摘要： This invention relates to a compound of the formula: ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position.a 1-piperazinyl radical substituted in the 4-position.a piperidino radical substituted in the 4-positioneither:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

5. 发明授权

US5631279A Perhydroisoindole derivatives, preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：全氢异吲哚衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5631279A
公开(公告)日：1997-05-20
申请号：US448402
申请日：1995-06-07
申请人： Andre Crespo , Veronique Fardin , Jean-Marc Guillaume , Jean-Luc Malleron , Jean-Francois Peyronel
发明人： Andre Crespo , Veronique Fardin , Jean-Marc Guillaume , Jean-Luc Malleron , Jean-Francois Peyronel
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61P1/00 , A61P9/08 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D209/44 , C07D403/06
CPC分类号： C07D403/06 , C07D209/44
摘要： This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists. ##STR1##
摘要翻译： PCT No.PCT / FR94 / 00371 Sec。 371日期：1995年6月7日 102（e）日期1995年6月7日PCT 1994年4月1日PCT PCT。第WO94 / 22822号公报日本特开1994年10月13日本发明涉及08 / 448,402式（I）的全氢异吲哚衍生物，其中基团R是任选被卤素原子或甲基取代的2-或3-取代的苯基; R1是任选取代的苯基，环己二烯基，萘基，茚基或任选取代的杂环基; R 2是H，卤素，OH，烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基，烷硫基，酰氧基，酰氧基，羧基，任选取代的烷氧基羰基，苄氧羰基，氨基或酰氨基; 并且R 3是任选的2-取代的苯基; 任选的盐; 及其制备。所述衍生物特别可用作神经激肽A拮抗剂。（一）

6. 发明授权

US5130313A Serotonin antagonists, their preparation and medications containing them 失效
标题翻译：丝氨酸蛋白酶拮抗剂，其制备和药物含有它们
公开(公告)号：US5130313A
公开(公告)日：1992-07-14
申请号：US627101
申请日：1990-12-13
申请人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Jean-Francois Peyronel , Alain Truchon
IPC分类号： C07D209/92 , A61K31/425 , A61K31/428 , A61K31/445 , A61K31/495 , A61K31/54 , A61P43/00 , C07C311/08 , C07C311/21 , C07D211/70 , C07D227/087 , C07D275/06 , C07D279/02 , C07D285/16 , C07D295/13 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/06 , C07D513/06
CPC分类号： C07D275/06 , C07D227/087 , C07D279/02 , C07D285/16 , C07D295/13 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/10 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/06 , C07D513/06
摘要： This invention relates to compounds of formula: ##STR1## in which R.sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical,a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR.sub.2 denotes a radical SO.sub.2 R.sub.4 in which R.sub.4 denotes an alkyl or phenyl radical,R.sub.3 denotes a phenyl or naphthyl radical,or else R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached form a ring,n is equal to 2, 3 or 4, processes for their preparation and medications containing them.The invention relates to treating a disease ameliorated by serotonin.
摘要翻译：本发明涉及下式的化合物：其中R 1表示在4位上被任意取代的苯基任意取代的3-吲哚基取代的1,2,3,6-四氢-1-吡啶基或3-（5-羟基吲哚基）基，在4-位上被任意取代的苯基取代的1-哌嗪基，1,2-苯并异噻唑-3-基，1,2-苯并异恶唑-3-基或2-吡啶基二（4-氟苯基）亚甲基，4-氟苯甲酰基，任选取代的2-氧代-1-苯并咪唑啉基，任选取代的3-吲哚基或3-（5-氯苯基）羟基吲哚基）基团，由两个苯基或羟基和任选取代的苯基R2表示基团SO 2 R 4，其中R 4表示烷基或苯基，R 3表示苯基或萘基，或者R 2和R 3与氮它们所连接的原子形成环，n等于2,3或4 ir准备和含有它们的药物。本发明涉及治疗5-羟色胺改善的疾病。

7. 发明授权

US5021420A Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效
公开(公告)号：US5021420A
公开(公告)日：1991-06-04
申请号：US375934
申请日：1989-07-06
申请人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P11/00 , A61P25/00 , A61P43/00 , C07D275/06 , C07D417/00 , C07D417/06 , C07D417/14 , C07D513/06
CPC分类号： C07D275/06 , C07D417/06 , C07D417/14 , C07D513/06
摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

8. 发明授权

US06903217B2 Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them 失效
标题翻译：杂环基烷基哌啶衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US06903217B2
公开(公告)日：2005-06-07
申请号：US10607220
申请日：2003-06-27
申请人： Eric Bacqué , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
发明人： Eric Bacqué , Jean-Christophe Carry , Youssef El-Ahmad , Michel Evers , Philippe Hubert , Jean-Luc Malleron , Serge Mignani , Guy Pantel , Michel Tabart , Fabrice Viviani
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/02 , C07D215/18 , C07D237/26
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Heterocyclylalkylpiperidine derivatives of general formula (I) in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.
摘要翻译：通式（I）的杂环基烷基哌啶衍生物在它们的对映体或非对映异构体形式或这些形式的混合物中，和/或在适当的情况下以其顺式或反式或其混合物以及其任何盐。

9. 发明授权

US06841562B2 Quinolylpropylpiperidine derivatives, intermediates and compositions containing them, and preparation therefor 失效
标题翻译：醌基丙基哌啶衍生物，含有它们的中间体和组合物及其制备方法
公开(公告)号：US06841562B2
公开(公告)日：2005-01-11
申请号：US10659095
申请日：2003-09-10
申请人： Eric Bacqué , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
发明人： Eric Bacqué , Antony Bigot , Youssef El Ahmad , Jean-Luc Malleron , Serge Mignani , Baptiste Ronan , Michel Tabart , Fabrice Viviani
IPC分类号： A61P31/04 , C07D211/60 , C07D401/06 , C07D409/14 , A61K31/44 , C07D215/12 , C07D215/18
CPC分类号： C07D401/06 , C07D211/60 , C07D409/14 , Y02P20/55
摘要： Quinolylpropylpiperidine derivatives of general formula (I) in which R1a is hydrogen, halogen, hydroxyl, amino, alkylamino, dialkylamino, hydroxyamino, alkoxyamino or alkylalkoxyamino and R1b is hydrogen, or R1a and R1b form an oxo, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl either substituted with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkoxycarbonyl, cyano or amino or R3 is propargyl substituted with phenyl or heteroaryl as defined above, R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them. These novel derivatives are potent antibacterial agents.
摘要翻译：通式（I）的喹啉基丙基哌啶衍生物，其中R 1a是氢，卤素，羟基，氨基，烷基氨基，二烷基氨基，羟基氨基，烷氧基氨基或烷基烷氧基氨基，R 1b是氢，或者R 1a和R 1b形成氧代，R 2是羧基，羧甲基或羟甲基，羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基，或与任选被卤素或三氟甲基取代的环烷硫基（3至7个成员）或与杂芳硫基（羟基，烷基，烷氧基，三氟甲基，三氟甲氧基，羧基，烷氧基羰基，氰基或氨基或R3是被苯基或杂芳基取代的炔丙基，被苯基或杂芳基取代 R4是烷基，烯基-CH 2 - 或炔基-CH 2 - ，环烷基或环烷基烷基，其各种异构体形式，分别或混合物，和它们的盐，它们的制备方法和中间体以及含有它们的组合物。这些新型衍生物是有效的抗菌剂。

10. 发明授权

US06602884B2 Quinolylpropylpiperidine derivatives, their preparation, and compositions containing them 失效
公开(公告)号：US06602884B2
公开(公告)日：2003-08-05
申请号：US10096482
申请日：2002-03-13
申请人： Eric Bacqué , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
发明人： Eric Bacqué , Serge Mignani , Jean-Luc Malleron , Michel Tabart , Michel Evers , Fabrice Viviani , Youssef El Ahmad , Stéphane Mutti , Christophe Daubié
IPC分类号： A01N4342
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/14
摘要： Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式