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1. 发明授权

US08710091B2 Imidazolidine-2,4-dione derivatives, and use thereof as a cancer drug 有权
标题翻译：咪唑烷-2,4-二酮衍生物及其作为癌症药物的用途
公开(公告)号：US08710091B2
公开(公告)日：2014-04-29
申请号：US13264971
申请日：2010-04-16
申请人： Grégorie Prevost , Serge Auvin , Christophe Lanco , Anne-Marie Liberatore , Olivier Lavergne
发明人： Grégorie Prevost , Serge Auvin , Christophe Lanco , Anne-Marie Liberatore , Olivier Lavergne
IPC分类号： A61K31/4166 , C07D233/40
CPC分类号： C07D233/72 , C07D233/76
摘要： The present application relates to novel imidazolidine-2,4-dione derivatives of the general formula (I), where R1, R2, R3, R4, X, and Y are variables. Said materials have an antiproliferative activity. They are particularly useful for treating pathological conditions and diseases, such as cancer, that are linked to abnormal cell proliferation. The invention also relates to pharmaceutical compositions containing said materials and to the use thereof for preparing a drug.
摘要翻译：本申请涉及通式（I）的新咪唑烷-2,4-二酮衍生物，其中R 1，R 2，R 3，R 4，X和Y是变量。所述材料具有抗增殖活性。它们特别可用于治疗与异常细胞增殖相关的病理状况和疾病，例如癌症。本发明还涉及含有所述材料的药物组合物及其用于制备药物的用途。

2. 发明授权

US07960560B2 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione 失效
标题翻译： 1-（联苯-4-基甲基）咪唑烷-2,4-二酮
公开(公告)号：US07960560B2
公开(公告)日：2011-06-14
申请号：US12628523
申请日：2009-12-01
申请人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
发明人： Marcelis van der Stelt , Joseph Maria Gerardus Barbara Cals
IPC分类号： C07D487/10 , C07D233/40 , C07D401/10 , C07D417/10 , C07D413/10 , A61K31/54 , A61K31/5377 , A61K31/4523 , A61K31/4166
CPC分类号： C07D233/74 , C07D401/10
摘要： The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2′ are independently H or (C1-3)alkyl; or R2 and R2′ form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式I的1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物，其中R 1是H，（C 1-6）烷基（任选被氧代取代，OR 4，COOR 5，卤素或 CN），（C2-6）烯基，（C2-6）炔基，（C3-6）环烷基或（C3-6）环烷基（C1-3）烷基; R2和R2'独立地为H或（C1-3）烷基; 或R 2和R 2'与它们所连接的碳原子一起形成（C 3-5）环烷基; R 3表示H或1至4个F取代基; Y表示或NR8R9; X表示CHR6，CF2，O，S，SO或SO2; R4和R5是（C1-6）烷基; R6是H，OR7或CN; R7是（C1-3）烷基; R8是包含选自O，S，SO和SO 2的杂原子的（C5-7）环烷基; R 9为H或（C 1-4）烷基; o和m表示取代基Y-CH 2的邻位或间位; 或其药学上可接受的盐; 以及所述1-（联苯-4-基甲基）咪唑烷-2,4-二酮衍生物在治疗疼痛中的用途，例如手术前疼痛，慢性疼痛，神经性疼痛，癌症疼痛和疼痛，以及与多发性硬化有关的痉挛症。

3. 发明申请

US20100113547A1 NOVEL IMIDAZOLIDINE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS 有权
标题翻译：新型咪唑烷化合物作为雄激素受体调节剂
公开(公告)号：US20100113547A1
公开(公告)日：2010-05-06
申请号：US12557368
申请日：2009-09-10
申请人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
发明人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
IPC分类号： A61K31/4166 , C07D233/40 , A61P35/00 , A61P19/10 , A61P15/00
CPC分类号： C07D233/60 , C07D233/66
摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.
摘要翻译：公开了具有由下式表示的式的新化合物：其中X，R1，R2a，R2b，R2c，R3a R3b，R4a，R4b，R4c和m1如本文所述。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，恶病质，骨质疏松症，肌肉减少症，性欲下降和/或性功能障碍。

4. 发明申请

US20080171881A1 Method for Producing Organic Compound and Method for Decomposing Compound Having Dicarboximide Skeleton 失效
标题翻译：生产有机化合物的方法和分解具有二酰亚胺骨架的化合物的方法
公开(公告)号：US20080171881A1
公开(公告)日：2008-07-17
申请号：US11885125
申请日：2006-03-22
申请人： Naruhisa Hirai , Jun Kuwana
发明人： Naruhisa Hirai , Jun Kuwana
IPC分类号： C07D211/22 , C07C233/00 , C07D233/40 , C07D249/12
CPC分类号： C07D251/32 , Y02P20/55
摘要： It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity.Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.
摘要翻译：期望提供一种通过催化具有二羧酰亚胺骨架的化合物从反应产物中容易地除去催化剂衍生的杂质的方法，从而有效地产生高纯度的目标化合物。公开了一种在催化剂存在下通过底物的反应制备有机化合物的方法，所述催化剂包括具有由下式（i）表示的二羧酰亚胺骨架的化合物：其中R表示氢原子或羟基保护基。该方法包括用热水处理反应产物以分解和除去由催化剂衍生的杂质的步骤。热水的温度优选为100℃以上。

5. 发明授权

US07115620B2 1,3-disubstituted-2-thioxo-imidazolidine-4,5-diones as potassium channel openers 失效
标题翻译： 1,3-二取代-2-硫代 - 咪唑烷-4,5-二酮作为钾通道开放剂
公开(公告)号：US07115620B2
公开(公告)日：2006-10-03
申请号：US10282540
申请日：2002-10-29
申请人： John A Butera , Hassan M Elokdah , Theodore S Sulkowski , John L Primeau , Joseph R Lennox , Russell F Graceffa
发明人： John A Butera , Hassan M Elokdah , Theodore S Sulkowski , John L Primeau , Joseph R Lennox , Russell F Graceffa
IPC分类号： A61K31/415 , C07D233/42 , C07D233/40
CPC分类号： C07D233/96
摘要： Compounds of Formula I are provided: wherein: R is lower alkyl or branched lower alkyl; and Ar is phenyl, phenyl substituted with one or more of halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyano, or perfluoroalkoxy, or a heteroaromatic moiety; and pharmaceutically acceptable salts thereof.
摘要翻译：提供式I化合物：其中：R是低级烷基或支链低级烷基; 和Ar是苯基，被一个或多个卤素，低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基，氰基或全氟烷氧基取代的苯基或杂芳族部分; 及其药学上可接受的盐。

6. 发明授权

US07102013B2 Methods of making amidino compounds useful as nitric oxide synthase inhibitors 有权
标题翻译：制备脒基化合物可用作一氧化氮合酶抑制剂的方法
公开(公告)号：US07102013B2
公开(公告)日：2006-09-05
申请号：US10321969
申请日：2002-12-17
申请人： Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
发明人： Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
IPC分类号： C07D233/40 , C07C271/00 , C07C323/00
CPC分类号： C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要： Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.
摘要翻译：制备具有式32结构的α-氨基酸化合物的方法：包括在水解条件下处理具有结构式33的乙内酰脲化合物：其中取代基在本文中描述。

7. 发明申请

US20020025980A1 Single morphic forms of metalloproteinase inhibitors 审中-公开
标题翻译：单一形态的金属蛋白酶抑制剂
公开(公告)号：US20020025980A1
公开(公告)日：2002-02-28
申请号：US09924839
申请日：2001-08-08
发明人： Ruth Bernice Katz , Graham Robert Evans
IPC分类号： A61K031/4166 , A61K031/4015 , C07D233/40 , C07D207/40
CPC分类号： C07K5/06052
摘要： The present invention pertains to single morphic forms of a compound selected from 2S-null4-(2,5-dioxopyrrolidin-1-yl)-2S-mercaptobutyrylaminonull-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide and 2S-null2S-mercapto-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butyrylaminonull-4-methylpentanoic acid (2,2-dimethyl-1S-methylcarbamoylpropyl)amide, isolable as such.
摘要翻译：本发明涉及选自2S- [4-（2,5-二氧代吡咯烷-1-基）-2S-巯基丁酰氨基] -4-甲基戊酸（2,2-二甲基-1-甲基氨基甲酰基丙基）酯的化合物的单一形式，酰胺和2S- [2S-巯基-4-（3,4,4-三甲基-2,5-二氧代咪唑烷-1-基）丁酰氨基] -4-甲基戊酸（2,2-二甲基-1-甲基氨基甲酰基丙基）这样可以隔离。

8. 发明授权

US5977155A Imidazole-5-carboxamides 失效
标题翻译：咪唑-5-甲酰胺
公开(公告)号：US5977155A
公开(公告)日：1999-11-02
申请号：US88156
申请日：1998-06-01
申请人： Alain Corbier , Pierre Deprez , Michel Fortin , Jacques Guillaume , Bertrand Heckmann
发明人： Alain Corbier , Pierre Deprez , Michel Fortin , Jacques Guillaume , Bertrand Heckmann
IPC分类号： C07D233/64 , A61K31/415 , A61K31/4166 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/12 , A61P15/00 , C07D233/54 , C07D233/68 , C07D233/70 , C07D233/72 , C07D233/84 , C07D233/86 , C07D233/90 , C07D403/06 , C07D409/12 , C07D233/02 , C07D233/38 , C07D233/40
CPC分类号： C07D233/64 , C07D233/68 , C07D233/84 , C07D233/90
摘要： Products of formula (1), wherein R.sub.1 is particularly ##STR1## alkyl, alkylthio or alkoxy; R.sub.2 is particularly halogen, --S--R, --O--R or --C(OH)(R)--COOH, where R is alkyl or alkenyl; R.sub.3 is particularly carboxy, acyl, halogen, alkyl, alkenyl or alkylthio; and R.sub.4 is particularly --(CH.sub.2).sub.m1 --COOR.sub.4, --(CH.sub.2).sub.m1 --CONHR.sub.14, --(CH.sub.2).sub.m1 --CN, --SO.sub.2 --NH--SO.sub.2 --R.sub.14, 13 NH--SO.sub.2 --R.sub.14, --PO.sub.3 R.sub.14, or --NH--SO.sub.2 --CF.sub.3, where m1 is 0-4 and R.sub.14 is hydrogen, alkyl or alkenyl; are useful for preparing pharmaceutical compositions for treating disorders resulting from abnormal stimulation of angiotensin II receptors AT.sub.1 and AT.sub.2.
摘要翻译：式（1）的产物，其中R 1特别是烷基，烷硫基或烷氧基; R2特别是卤素，-S-R，-O-R或-C（OH）（R）-COOH，其中R是烷基或烯基; R3特别是羧基，酰基，卤素，烷基，烯基或烷硫基; （CH 2）m1-CONHR 14， - （CH 2）m1-CN，-SO 2 -NH-SO 2 -R 14，13 NH-SO 2 -R 14，-PO 3 R 14或-NH- -SO2-CF3，其中m1为0-4且R14为氢，烷基或烯基; 可用于制备用于治疗由血管紧张素II受体AT1和AT2的异常刺激引起的疾病的药物组合物。

9. 发明授权

US5847153A .beta.-sulfonyl hydroxamic acids 失效
标题翻译： β-磺酰基异羟肟酸
公开(公告)号：US5847153A
公开(公告)日：1998-12-08
申请号：US934408
申请日：1997-09-19
申请人： Martha A. Warpehoski , Donald E. Harper
发明人： Martha A. Warpehoski , Donald E. Harper
IPC分类号： C07C317/44 , C07C317/46 , C07D233/72 , C07D233/40
CPC分类号： C07C317/44 , C07D233/72
摘要： The present invention provides a compound of formula I ##STR1## or pharmaceutical acceptable salts thereof wherein R.sub.1 is C.sub.4-12 alkyl, C.sub.4-12 alkenyl, C.sub.4-12 alkynyl, --(CH.sub.2).sub.h -C.sub.3-8 cycloalkyl, --(CH.sub.2).sub.h -aryl, or --(CH.sub.2).sub.h -het; R.sub.2 is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, --(CH.sub.2).sub.h -C.sub.3-8 cycloalkyl, --(CH.sub.2).sub.h -C.sub.3-8 cycloalkenyl, --(CH.sub.2).sub.h -aryl, --(CH.sub.2).sub.h -het, --(CH.sub.2).sub.h -Q, --(CH.sub.2).sub.i -X-R.sub.4, or --(CH.sub.2).sub.i CHR.sub.5 R.sub.6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐，其中R 1是C 4-12烷基，C 4-12烯基，C 4-12炔基， - （CH 2）h -C 3-8环烷基， - （CH 2 ） - 芳基或 - （CH 2）h-het; R2是C1-12烷基，C2-12烯基，C2-12炔基， - （CH2）h-C3-8环烷基， - （CH2）h-C3-8环烯基， - （CH2）h-芳基 - （CH2 ） - （CH2）hQ， - （CH2）iX-R4或 - （CH2）iCHR5R6。这些化合物是参与组织降解的基质金属蛋白酶的抑制剂。

10. 发明授权

US5658930A Aromatic heterocyclic derivatives as enzyme inhibitors 失效
标题翻译：芳香杂环衍生物作为酶抑制剂
公开(公告)号：US5658930A
公开(公告)日：1997-08-19
申请号：US481660
申请日：1995-06-07
申请人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
发明人： Susan Yoshiko Tamura , Joseph Edward Semple , William Charles Ripka , Robert John Ardecky , Yu Ge , Stephen H. Carpenter , Terence K. Brunck
IPC分类号： A61K38/00 , C07D211/56 , C07D211/76 , C07D213/75 , C07D239/46 , C07D239/54 , C07D239/545 , C07D401/12 , C07K5/06 , C07K5/078 , A61K31/445 , A61K31/505 , C07D213/64 , C07D233/32 , C07D233/40
CPC分类号： C07D211/56 , C07D211/76 , C07D213/75 , C07D239/47 , C07D239/545 , C07D401/12 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要： The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要翻译：本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。

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