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1. 发明授权

US08063068B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US08063068B2
公开(公告)日：2011-11-22
申请号：US12348605
申请日：2009-01-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D401/02 , A61K31/351
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

2. 发明申请

US20100010042A1 ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 有权
公开(公告)号：US20100010042A1
公开(公告)日：2010-01-14
申请号：US12348605
申请日：2009-01-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Craig Harrison Miller , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： A61K31/454 , A61K31/4545 , C07D401/02 , A61P25/00 , A61P1/00
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

3. 发明授权

US08633222B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US08633222B2
公开(公告)日：2014-01-21
申请号：US13033719
申请日：2011-02-24
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve , Craig Harrison Miller
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve , Craig Harrison Miller
IPC分类号： A61K31/351 , C07D401/02
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

4. 发明申请

US20110152293A1 ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 有权
标题翻译：阿维林霉素化合物及其制备和使用方法
公开(公告)号：US20110152293A1
公开(公告)日：2011-06-23
申请号：US13033719
申请日：2011-02-24
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve , Craig Harrison Miller
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve , Craig Harrison Miller
IPC分类号： A61K31/506 , A61P1/00 , A61P25/28 , A61P25/16 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/02 , A61K31/4439
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

5. 发明授权

US07714001B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US07714001B2
公开(公告)日：2010-05-11
申请号：US12187584
申请日：2008-08-07
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D401/02 , A61K31/351
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

6. 发明授权

US07098331B2 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US07098331B2
公开(公告)日：2006-08-29
申请号：US10379868
申请日：2003-03-05
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： C07D405/12 , C07D239/26
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

7. 发明申请

US20080293778A1 Arylvinylazacycloalkane Compounds and Methods of Preparation and Use Thereof 有权
标题翻译：芳基乙烯基氮杂环烷烃化合物及其制备和使用方法
公开(公告)号：US20080293778A1
公开(公告)日：2008-11-27
申请号：US12187584
申请日：2008-08-07
申请人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Daniel Schmitt , Gary Maurice Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： A61K31/4439 , C07D401/14 , A61P25/00
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
摘要翻译：公开了式（I）的新型乙烯基氮杂环烷化合物。这些化合物是各种nAChR的配体。化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

8. 发明申请

US20060094732A1 Arylvinylazacycloalkane compounds and methods of preparation and use thereof 审中-公开
公开(公告)号：US20060094732A1
公开(公告)日：2006-05-04
申请号：US11206243
申请日：2005-08-17
申请人： Jeffrey Schmitt , Gary Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
发明人： Jeffrey Schmitt , Gary Dull , Arielle Genevois-Borella , Marc Capet , Michel Cheve
IPC分类号： A61K31/513 , A61K31/506
CPC分类号： A61K31/506 , C07D405/14
摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

9. 发明授权

US6013662A Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
标题翻译：法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途
公开(公告)号：US6013662A
公开(公告)日：2000-01-11
申请号：US999408
申请日：1997-12-29
申请人： Jean-Dominique Bourzat , Alain Commer.cedilla.on , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
发明人： Jean-Dominique Bourzat , Alain Commer.cedilla.on , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
IPC分类号： C07D209/56 , C07D209/72 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , A01N43/38 , C07D235/08 , C07D401/08
CPC分类号： C07D401/12 , C07D209/56 , C07D209/72 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14
摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or elsea ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要翻译：式（I）的新产品，其制备方法，含有它们的药物组合物及其在制备药物中的用途。在式（I）中，以下取代基是优选的：Ar表示取代或稠合的苯基或多环或杂环芳族基，R表示通式 - （CH 2）m -X1（CH 2）n Z 其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或者基团，R 1和R 2 =氢或卤素或任选被取代的烷基，烷基硫代，烷氧基羰基，或者R1和R2相对于彼此的邻位，形成任选取代的含有1或2个杂原子的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基， R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S 外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。

10. 发明授权

US06218406B1 Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
标题翻译：法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途
公开(公告)号：US06218406B1
公开(公告)日：2001-04-17
申请号：US09346303
申请日：1999-07-02
申请人： Jean-Dominique Bourzat , Alain Commerçon , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
发明人： Jean-Dominique Bourzat , Alain Commerçon , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
IPC分类号： A61K314439
CPC分类号： C07D401/12 , C07D209/56 , C07D209/72 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14
摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula —(CH2)m—X1—(CH2)n—Z in which X1=single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH2 radicals to be substituted; Z represents carboxyl, COOR6 (R6=alkyl), CON(R7)(R8) (R7=hydrogen or alkyl and R8=hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR9)2 (R9=hydrogen or alkyl), an —NH—CO—T (T=hydrogen or optionally substituted alkyl) radical, or else—a radical, R1 and R2=hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R3 and R4=hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R5=hydrogen, alkyl, alkylthio, X=O or S or —NH—, —CO—, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要翻译：式（I）的新型产物，其制备方法，含有它们的药物组合物及其在制备药物中的用途。在式（I）中，以下取代基是优选的：Ar表示取代或缩合的苯基或多环或杂环芳族基团，R表示通式为（CH 2）m -X1（CH 2）n Z的基团，其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或不相关的，R 1和R 2 =氢或卤素或烷基，烷氧基，其被任选取代，烷硫基，烷氧基羰基或其它R1和R2在相邻的邻位形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S，外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。

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