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1. 发明公开

EP0591426A4 SIGMA RECEPTOR LIGANDS AND THE USE THEREOF 失效
标题翻译： SIGMA受体配体及其用途
公开(公告)号：EP0591426A4
公开(公告)日：1996-08-21
申请号：EP92914789
申请日：1992-06-26
申请人： UNIV VIRGINIA COMMONWEALTH
发明人： GLENNON RICHARD A
IPC分类号： A61K31/135 , A61K31/17 , A61K31/215 , A61K31/275 , A61K31/395 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P1/00 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/30 , A61P43/00 , C07C211/08 , C07C211/17 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/52 , C07C217/16 , C07C217/48 , C07C217/60 , C07C219/10 , C07C219/12 , C07C225/16 , C07C229/46 , C07C237/06 , C07C243/18 , C07C255/30 , C07C255/58 , C07C311/30 , C07C317/26 , C07C323/23 , C07D207/12 , C07D209/48 , C07D211/14 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/70 , C07D223/16 , C07D239/42 , C07D241/06 , C07D265/30 , C07D295/02 , C07D295/03 , C07D295/033 , C07D295/06 , C07D295/073 , C07D295/096 , C07D295/108 , C07D295/192 , C07D317/58 , C07D451/02 , C07D471/08 , A61K31/50
CPC分类号： C07D209/48 , A61K31/135 , A61K31/215 , A61K31/40 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/55 , C07C211/08 , C07C211/17 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/52 , C07C217/16 , C07C217/60 , C07C219/10 , C07C219/12 , C07C225/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2603/18 , C07D207/12 , C07D211/14 , C07D211/46 , C07D211/52 , C07D211/70 , C07D223/16 , C07D239/42 , C07D265/30 , C07D295/03 , C07D295/033 , C07D295/073 , C07D295/096 , C07D295/108 , C07D295/192 , C07D317/58 , C07D471/08
摘要： The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT1A receptors.
摘要翻译：本发明涉及通过向需要这种治疗的患者施用包含有效量的某些σ受体配体的药物组合物来治疗中枢神经系统疾病，胃肠道疾病，药物滥用，心绞痛，偏头痛，高血压和抑郁症的方法。本发明还涉及具有与σ受体高度结合的新型σ受体配体及其药物组合物。出乎意料的是，某些本发明的σ受体配体在DA，PCP和5-HT 1A受体上对σ受体具有选择性。

2. 发明公开

EP2970116A1 ARYL SULFAMIDE AND SULFAMATE DERIVATIVES AS RORc MODULATORS 审中-公开
标题翻译：芳基磺酰胺和硫酸酯衍生物作为反式调节剂
公开(公告)号：EP2970116A1
公开(公告)日：2016-01-20
申请号：EP14709306.6
申请日：2014-03-12
申请人： F.Hoffmann-La Roche AG
发明人： BODIL VAN NIEL, Monique , FAUBER, Benjamin , RENE, Olivier , WARD, Stuart
IPC分类号： C07C303/40 , C07C307/04 , C07C307/06 , C07C307/08 , C07C311/03 , C07C311/08 , C07C311/22 , C07C311/30 , C07D241/04 , C07D417/10 , C07D417/12 , C07D285/04 , C07D285/06 , C07D285/16 , C07D285/36
CPC分类号： C07D417/12 , C07D211/96 , C07D285/16 , C07D285/36 , C07D295/185 , C07D401/12
摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
摘要翻译：其中m，n，p，q，r，A，X 1，X 2，X 3，X 4，X 5，X 6，Y，Z，G，R 1a，R 2a，R 1b，R 2b，R 3，R 4，R 5和R 6如本文所定义。还公开了制备所述化合物和使用所述化合物治疗炎性疾病如关节炎的方法。

3. 发明公开

EP0273369A2 New alkanesulfonanilide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译： Alkansulfonanilid衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0273369A2
公开(公告)日：1988-07-06
申请号：EP87119063.3
申请日：1987-12-22
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Matsuo, Masaaki , Tsuji, Kiyoshi , Konishi, Nobukiyo
IPC分类号： C07C311/08 , C07C311/30 , C07D307/58 , C07D307/32 , C07D213/04 , C07D277/40 , C07D257/04 , C07D277/46 , C07D271/06
CPC分类号： C07D213/20 , C07D257/04 , C07D271/07 , C07D277/40 , C07D277/46 , C07D295/192
摘要： Alkanesulfonanilide derivatives of the formula:
wherein
R¹, R² and R⁸ are each hydrogen or certain substituents
R³ is lower alkyl, or mono or di-lower alkylamino,
R⁴ is acyl, cyano, carboxy, hydroxy(lower)alkyl, mercapto, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, 5-membered unsaturated heterocyclic group which may have amino, lower alkanoylamino, lower alkylthio or lower alkylsulfonyl, phenylthio which may have nitro or amino, lower alkanoyl(lower)alkenyl or a group of the formula :
wherein
R⁶ is hydrogen, amino or lower alkyl and
R⁷ is hydroxy, lower alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy, ureido or thioureido, and
R⁵ is hydrogen, halogen, lower alkyl or lower alkanoyl, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them as an active ingredient.
摘要翻译：式的烷烃磺酰苯胺衍生物： worin - [R <1>，R <2>和R <8>各自为氢或某些取代基R <3>是低级烷基，或单或二低级烷基氨基，R <4> 是酰基，氰基，羧基，羟基（低级）烷基，巯基，低级烷硫基，低级烷基亚磺酰，低级烷基磺酰基，5元不饱和杂环基可具有氨基，低级链烷酰氨基，低级烷硫基或低级烷基磺酰基，苯硫基可具有硝基或氨基，低级烷酰基（低级）链烯基或下式基团的： worin - [R <6>是氢，氨基或低级烷基，R <7>是羟基，低级烷氧基，羧基（低级）烷氧基，低级烷氧基羰基（低级）烷氧基，脲基或硫脲基，且R为氢<5>为卤素，低级烷基或低级烷酰基，和其可药用盐，用于制备药物和它们的组合物的方法，包括它们作为在活性成分。

4. 发明授权

EP0878463B1 Excitatory amino acid receptor modulators 失效
标题翻译： Modoatoren von durchAminosäurenanregbare Rezeptoren
公开(公告)号：EP0878463B1
公开(公告)日：2000-12-20
申请号：EP98303730.0
申请日：1998-05-13
申请人： ELI LILLY AND COMPANY
发明人： Massey, Steven Marc , Monn, James Allen , Valli, Matthew John
IPC分类号： C07C229/50 , C07C251/34 , C07C247/14 , C07C233/81 , C07C311/30 , C07C255/31 , C07C255/47 , C07C237/48 , C07F9/38 , A61K31/195 , A61K31/275
CPC分类号： C07D235/02 , C07C229/50 , C07C233/52 , C07C233/81 , C07C247/14 , C07C251/44 , C07C275/26 , C07C311/07 , C07C2601/02 , C07C2602/18 , C07F9/383

5. 发明授权

EP0273369B1 New alkanesulfonanilide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：新的碱金属络合物衍生物，其制备方法和包含其的药物组合物
公开(公告)号：EP0273369B1
公开(公告)日：1992-03-04
申请号：EP87119063.3
申请日：1987-12-22
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Matsuo, Masaaki , Tsuji, Kiyoshi , Konishi, Nobukiyo
IPC分类号： C07C311/08 , C07C311/30 , C07D307/58 , C07D307/32 , C07D213/04 , C07D277/40 , C07D257/04 , C07D277/46 , C07D271/06
CPC分类号： C07D213/20 , C07D257/04 , C07D271/07 , C07D277/40 , C07D277/46 , C07D295/192

6. 发明公开

EP3442533A1 TG2 INHIBITOR COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：EP3442533A1
公开(公告)日：2019-02-20
申请号：EP17782038.8
申请日：2017-04-13
申请人： University Of Ottawa , University Of Maryland, Baltimore , University of Rochester
发明人： KEILLOR, Jeffrey W. , AKBAR, Abdullah , ECKERT, Richard L. , FISHER, Matthew , JOHNSON, Gail V.W.
IPC分类号： A61K31/495 , A61K31/496 , C07C271/22 , C07C311/30 , C07C241/02

7. 发明公开

EP2407167A2 Therapeutic agent for neurodegenerative disease 审中-公开
标题翻译：治疗神经退行性疾病的药物
公开(公告)号：EP2407167A2
公开(公告)日：2012-01-18
申请号：EP11006919.2
申请日：2006-11-17
申请人： National University Corporation Hokkaido University
发明人： The designation of the inventor has not yet been filed
IPC分类号： A61K31/52 , A61K31/36 , A61K31/7072 , A61K38/00 , A61P25/00 , A61P25/16 , A61P25/28 , C07D317/62 , C07D473/34 , C07D519/00 , C07H19/067 , C07H19/167 , C07C1/00 , C07H7/06 , C07C311/30
CPC分类号： C07D317/62 , C07D473/34 , C07D519/00 , C07H7/06 , C07H19/067 , C07H19/167
摘要： [PROBLEMS] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Perkinson's disease.
[MEANS FOR SOLVING PROBLEMS] It is known that DJ―1 protein is involved in Perkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ―1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of -60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.
摘要翻译： [问题]提供神经元细胞死亡抑制剂和神经退行性疾病特别是帕金森病的治疗剂。解决问题的手段众所周知，DJ-1蛋白参与帕金森氏病，并且能够抑制由氧化应激引起的神经元细胞死亡。基于这些知识，使用分析软件FastDock（Fujitsu Ltd.）筛选能够结合DJ-1蛋白质活性位点的低分子量分子（即位置-106处的半胱氨酸残基周围的区域）。当使用各自具有约60kcal / mol或更低的结合能的候选低分子量化合物进行各种测试时，这些化合物对神经退行性疾病显示治疗效果。

8. 发明公开

EP1086063A4 NOVEL POTASSIUM CHANNEL DRUGS AND THEIR USES 审中-公开
标题翻译：镓通道活性物质及其使用
公开(公告)号：EP1086063A4
公开(公告)日：2001-03-28
申请号：EP99927330
申请日：1999-06-07
申请人： ADVANCED MEDICINE INC
发明人： JACOBSEN JOHN R , EASTMAN DONNA , GRIFFIN JOHN H
IPC分类号： G01N33/50 , A61K9/06 , A61K31/18 , A61K31/343 , A61K31/395 , A61K31/407 , A61K31/4178 , A61K31/4427 , A61K31/443 , A61K31/4545 , A61K45/00 , A61K47/48 , A61P9/00 , A61P43/00 , C07C311/08 , C07C311/10 , C07C311/12 , C07C311/22 , C07C311/30 , C07D257/02 , C07D307/80 , C07D401/06 , C07D405/12 , C07D487/04 , C07D487/08 , C07K5/09 , C07K5/11 , C07K7/06 , C07K7/08 , G01N33/15 , G01N33/566 , G01N33/68 , C07B61/00 , A61K38/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00 , G01N33/53 , G01N33/543
CPC分类号： G01N33/6872 , A61K47/55 , A61K47/65

9. 发明公开

EP0217286A1 Phenylalanine derivative and proteinase inhibitor 失效
标题翻译：苯丙氨酸和蛋白酶抑制剂。
公开(公告)号：EP0217286A1
公开(公告)日：1987-04-08
申请号：EP86113166.2
申请日：1986-09-24
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi SHOWA DENKO K.K. , Kimura, Yoshio SHOWA DENKO K.K. , Yamada, Morihiko SHOWA DENKO K.K. , Ohno, Norio SHOWA DENKO K.K. , Katsuura, Yasuhiro SHOWA DENKO K.K. , Seki, Yumi SHOWA DENKO K.K.
IPC分类号： C07C233/57 , C07C233/63 , C07C257/00 , C07C311/30 , C07C311/35 , C07C323/31 , C07D207/16 , C07D211/16 , C07D211/32 , C07D211/58 , C07D211/62
CPC分类号： C07D213/30 , A61K38/00 , C07D211/16 , C07D211/32 , C07D211/62 , C07D213/40 , C07D213/643 , C07D213/75 , C07D239/42 , C07D295/185 , C07D307/14 , C07D401/12 , C07K5/06078
摘要： A phenylalanine derivative having the formula (I):
where R' and R 2 are independently hydrogen provided that both R' and R 2 are nof hydrogen at the same time;

C 1 -C 5 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, C 1 -C 4 alkyl- mercapto, C,-C4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C 1 -C 4 alkoxy, or halogen;
C 6 -C 3 cycloalkyl which may be substituted with hydroxy, C 1 -C 4 alkoxy, hydroxylcarbonyl, C 1 -C 4 alkoxycarbonyl, or C 1 -C 4 alkyl;
phenyl which may be substituted with halogen, nitro, trifluoromethyl, C,-C 4 alkoxy, C 1 -C 4 alkylmer- capto, C 1 -C 4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C 1 -C 6 alkyl which may further be substituted with C 1 -C 4 alkylcarbonyl, hydroxycarbonyl, or C 1 -C 4 alkoxycarbonyl;
pyridyl which may be substituted with halogen or C 1 -C 4 alkoxy;
pyrimidyl;
N-benzylazacyclohexyl; and
R' and R 2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; or piperidyl which may be substituted with phenylcarbonyl, benzyl, or C 1 -C 4 alkyl;
pyrrolidyl which may be substituted with hydroxycarbonyl or C 1 -C 4 alkoxycarbonyl; and
piperidine substituted with C 1 -C 4 alkyl, phenyl C 1 -C 4 alkyl, phenylcarbonyl, or C,-C 4 alkoxycarbonyl;
X is hydrogen; nitro; amino; or -OZ wherein Z is hydrogen: C 1 -C 4 alkyl; C 2 -C 4 alkenyl; benzyl which may be substituted with halogen, C 1 -C 4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, or cyano; phenylcarbonylmethyl, pyridylmethyl; phenyl which may be substituted with nitro or halogen; pyridyl or pyrimidyl which may be substituted with nitro; phenylsulfonyl which may be substituted with C 1 -C 4 alkyl; or benzyloxycarbonyl which may be substituted with halogen;
n is 4 to 10; and
the mark indicates that the configuration of the carbon may be either one of D-configuration, L-configuration and DL-configuration or a pharmaceutical acceptable salt thereof.

This phenylalanine derivative is effective as a proteinase inhibitor.
摘要翻译：具有式（I）的苯丙氨酸衍生物：其中R1和R2独立地为氢，条件是R1和R2不同时为氢; 可以被羟基，羟基羰基，C 1 -C 4烷氧基羰基，C 1 -C 4烷基巯基，C 1 -C 4烷氧基，氨基甲酰基，氨磺酰基，吡啶基或可以进一步被硝基，C 1 -C 4烷氧基取代的苯基取代的C 1 -C 8烷基卤素; 可被羟基，C 1 -C 4烷氧基，羟基羰基，C 1 -C 4烷氧羰基或C 1 -C 4烷基取代的C 6 -C 8环烷基; 可以被卤素，硝基，三氟甲基，C 1 -C 4烷氧基C 1 -C 4烷基巯基，C 1 -C 4烷基羰基，苯基羰基，羟基羰基，C 1 -C 4烷氧基羰基，氨基甲酰基，氨磺酰基，脒基，吡啶基羰基或C 1 -C 6烷基取代的苯基，被C1-C4烷基羰基，羟基羰基或C1-C4烷氧基羰基取代; 可被卤素或C 1 -C 4烷氧基取代的吡啶基; 嘧啶; 的N- benzylazacyclohexyl; 并且R1和R2可以与其上连接的氮原子形成为环状结构作为吗啉代; 硫吗啉; 可被苯基羰基，苄基或C 1 -C 4烷基取代的哌嗪基; 可被羟基羰基或C 1 -C 4烷氧基羰基取代的吡咯烷基; 被C 1 -C 4烷基，苯基C 1 -C 4烷基，苯羰基或C 1 -C 4烷氧基羰基取代的哌啶子基; X是氢; 硝基; 氨基; 或-OZ，其中Z是氢; C 1 -C 4烷基; C 2 -C 4烯基; 可被卤素取代的苄基，C 1 -C 4烷基，硝基，三氟甲基，羟基羰基，C 1 -C 4烷氧基羰基或氰基; 苯基羰基; 吡啶; 可以被硝基或卤素取代的苯基; 可以被硝基取代的吡啶基或嘧啶基; 可被C 1 -C 4烷基取代的苯基磺酰基; 或可被卤素取代的苄氧基羰基; n为4〜10; 标记*表示碳的构型可以是D构型，L-构型和DL构型中的任一种或其药学上可接受的盐。该苯丙氨酸衍生物作为蛋白酶抑制剂是有效的。

10. 发明公开

EP0878463A1 Excitatory amino acid receptor modulators 失效
标题翻译：受体的调节剂可通过氨基酸被激发
公开(公告)号：EP0878463A1
公开(公告)日：1998-11-18
申请号：EP98303730.0
申请日：1998-05-13
申请人： ELI LILLY AND COMPANY
发明人： Massey, Steven Marc , Monn, James Allen , Valli, Matthew John
IPC分类号： C07C229/50 , C07C251/34 , C07C247/14 , C07C233/81 , C07C311/30 , C07C255/31 , C07C255/47 , C07C237/48 , C07F9/38 , A61K31/195 , A61K31/275
CPC分类号： C07D235/02 , C07C229/50 , C07C233/52 , C07C233/81 , C07C247/14 , C07C251/44 , C07C275/26 , C07C311/07 , C07C2601/02 , C07C2602/18 , C07F9/383
摘要： Compounds of the formula
in which R 1 and R 2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

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