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1. 发明授权

US10308597B2 Inhibitors of creatine transport and uses thereof 有权
公开(公告)号：US10308597B2
公开(公告)日：2019-06-04
申请号：US15307178
申请日：2015-04-30
申请人： Rgenix, Inc.
发明人： Eduardo J. Martinez , Sohail F. Tavazoie
IPC分类号： C07C279/14 , C07D233/46 , A61K31/4168 , C07D239/14 , A61K31/505 , C07D233/06 , C07D253/06 , A61K31/53 , A61K31/155 , C07D213/74 , A61K31/4402 , C07C279/16 , C07C313/34 , C07F9/48 , C07F9/09 , C07F9/24 , C07F9/38 , C07F9/40 , A61K31/00 , C07D213/76 , C07C257/14 , C07C259/14 , C07C279/26 , C07C279/36 , C07C281/16 , C07C281/18 , C07D231/12 , C07C309/15 , C07D233/26 , C07D233/52 , C07D233/64 , C07D233/88 , C07D401/04 , C07D239/06 , C07D405/04 , C07D249/08 , C07D249/14 , C07D257/08 , C07D487/04 , C07D205/04 , C07D207/16 , C07D207/22 , C07D295/32 , A61K31/397 , A61K31/40 , A61K31/4427 , A61K31/7068 , A61K45/06 , C07C275/70 , C07D205/08 , C07H19/06 , A61K31/337 , A61K31/704 , A61K31/7105 , C07F9/568 , C07F9/572 , C07F9/6506
摘要： This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

2. 发明申请

US20050203170A1 1,3-Diarylprop-2-en-1-ones, compositions containing them and use thereof 审中-公开
标题翻译： 1,3-二芳基丙-2-烯-1-酮，含有它们的组合物及其用途
公开(公告)号：US20050203170A1
公开(公告)日：2005-09-15
申请号：US11108855
申请日：2005-04-19
申请人： Patrick Mailliet , Cecile Combeau , Marie-Christine Bissery , Marie-Pierre Cherrier , Thomas Caulfield , Gilles Tiraboschi
发明人： Patrick Mailliet , Cecile Combeau , Marie-Christine Bissery , Marie-Pierre Cherrier , Thomas Caulfield , Gilles Tiraboschi
IPC分类号： C07C225/22 , C07C237/04 , C07C279/36 , C07D207/16 , C07D209/08 , C07D405/06 , A61K31/401 , A61K31/135 , A61K31/198
CPC分类号： C07D405/06 , C07C225/22 , C07C237/04 , C07C279/36 , C07D207/16 , C07D209/08
摘要： 1,3-Diarylprop-2-en-1-ones and derivatives, compositions containing them, manufacturing process and use. Substituted 1,3-diarylprop-2-en-1-ones with therapeutic activity may be used in oncology.
摘要翻译： 1,3-二芳基丙-2-烯-1-酮及其衍生物，含有它们的组合物，制造方法和用途。具有治疗活性的取代的1,3-二芳基丙-2-烯-1-酮可用于肿瘤学。

3. 发明授权

US5453441A Substituted arginines and substituted homoarginines and use thereof 失效
标题翻译：取代的精氨酸和取代的高精氨酸及其用途
公开(公告)号：US5453441A
公开(公告)日：1995-09-26
申请号：US328956
申请日：1994-10-24
申请人： Owen W. Griffith
发明人： Owen W. Griffith
IPC分类号： A61K31/195 , A61K31/198 , A61P9/02 , A61P43/00 , C07C279/14 , C07C279/36 , C07C281/16
CPC分类号： A61K31/195 , C07C279/14 , C07C279/36 , C07C281/16
摘要： Guanidino substituted arginines or homoarginines based on monoalkyl carbon-substituted ornithines or lysines, having the formula ##STR1## wherein R is (CH.sub.2).sub.y CH.sub.3 or H, R' is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, and R" is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, with y ranging from 0 to 5, and x is 0 or 1 and Q is an alkyl group containing from 1 to 6 carbon atoms or NH.sub.2 or NO.sub.2, and only one of R, R' and R" providing an alkyl substituent on the ornithine or lysine moiety. Preferred compounds are .alpha.-methyl-N.sup..omega. -methyl-DL-arginine, RS-.beta.-methyl-N.sup..omega. -methyl-DL-arginine, RS-.gamma.-methyl-N.sup..omega. -methyl-DL-arginine, .alpha.-methyl-N.sup..omega. -amino-DL-arginine, RS-.beta.-methyl-N.sup..omega. -amino-DL-arginine, RS-.gamma.-methyl-N.sup..omega. -amino-DL-arginine, .alpha.-methyl-N.sup..omega. -nitro-DL-arginine, RS-.beta.-methyl-N.sup..omega. -nitro-DL-arginine, and RS-.gamma.-methyl-N.sup..omega. -nitro-DL-arginine. A composition includes said compound together with a pharmaceutically acceptable carrier. Methods of use are directed to delivering said compound to inducible nitric oxide synthase to inhibit the ability of the enzyme to catalyze the conversion of arginine to nitric oxide, to administering said compound to inhibit pathological overproduction of nitric oxide from arginine and to administering said compound to a subject having systemic hypotension due to the pathological overproduction of nitric oxide and an .alpha..sub.1 adrenergic agonist to increase blood pressure in the subject to a clinically acceptable level.
摘要翻译：胍基取代的基于单烷基碳取代的鸟氨酸或赖氨酸的精氨酸或高精氨酸，其具有式，其中R是（CH 2）y CH 3或H，R'是CH 2或C（H）（CH 2）y CH 3，R“ CH2或C（H）（CH2）yCH3，y范围为0至5，x为0或1，Q为含有1至6个碳原子的烷基或NH2或NO2，只有一个R，R '和R“在鸟氨酸或赖氨酸部分提供烷基取代基。优选的化合物是α-甲基-Nω-甲基-DL-精氨酸，RS-β-甲基-Nω-甲基-DL-精氨酸，RS-γ-甲基-Nω-甲基-DL-精氨酸，α-甲基-N'- N-ω-氨基-DL-精氨酸，RS-β-甲基-Nω-氨基-DL-精氨酸，RS-γ-甲基-Nω-氨基-DL-精氨酸，α-甲基-Nω-硝基-L- 精氨酸，RS-β-甲基-Nω-硝基-DL-精氨酸和RS-γ-甲基-Nω-硝基-DL-精氨酸。组合物包括所述化合物和药学上可接受的载体。使用的方法是将所述化合物递送到诱导型一氧化氮合酶，以抑制酶催化精氨酸转化为一氧化氮的能力，以使所述化合物抑制来自精氨酸的一氧化氮的病理过度产生，并将所述化合物施用于由于一氧化氮的病理性过量产生的系统性低血压的受试者和α1肾上腺素能激动剂，以将受试者的血压升高到临床可接受的水平。

4. 发明授权

US5380945A Guanidino compounds as regulators of nitric oxide synthase 失效
标题翻译：胍基化合物作为一氧化氮合酶的调节剂
公开(公告)号：US5380945A
公开(公告)日：1995-01-10
申请号：US159972
申请日：1993-11-30
申请人： Ferid Murad , James F. Kerwin , Lee D. Gorsky
发明人： Ferid Murad , James F. Kerwin , Lee D. Gorsky
IPC分类号： C07C279/12 , C07C279/36 , C07C281/16 , C07C249/00 , A01N37/52
CPC分类号： C07C279/12 , C07C279/36 , C07C281/16
摘要： Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.
摘要翻译：用作间接调节环鸟嘌呤一磷酸（cGMP）的一氧化氮合酶的调节剂的化学式，其药物组合物，用于治疗血管平滑肌，巨噬细胞，神经元，血小板，支气管平滑肌，视神经肌肉的病症和胃肠道平滑肌，镰状细胞性贫血和糖尿病。

5. 发明授权

US5292770A Butenoic acid derivatives 失效
标题翻译：丁烯酸衍生物
公开(公告)号：US5292770A
公开(公告)日：1994-03-08
申请号：US960883
申请日：1992-10-14
申请人： Norio Minami , Fumihiro Ozaki , Keiji Ishibashi , Yasuhiro Kabasawa , Toshiaki Ogawa , Hideyuki Adachi , Takanori Kawamura
发明人： Norio Minami , Fumihiro Ozaki , Keiji Ishibashi , Yasuhiro Kabasawa , Toshiaki Ogawa , Hideyuki Adachi , Takanori Kawamura
IPC分类号： C07C275/42 , C07C279/24 , C07C279/28 , C07C279/36 , C07C323/27 , C07C335/22 , C07D213/56 , C07D213/64 , C07D213/68 , C07D213/89 , C07D233/08 , C07D233/28 , C07D233/88 , C07D233/95 , C07D239/46 , C07D405/04 , C07D409/04 , C07D521/00 , A61K31/44 , A61K31/415 , C07D401/04
CPC分类号： C07C275/42 , C07C279/24 , C07C279/28 , C07C279/36 , C07C323/27 , C07C335/22 , C07D213/56 , C07D213/64 , C07D213/68 , C07D213/89 , C07D231/12 , C07D233/08 , C07D233/28 , C07D233/56 , C07D233/88 , C07D233/95 , C07D239/47 , C07D249/08 , C07D405/04 , C07D409/04
摘要： A butenoic acid compound is defined by the following formula: ##STR1## in which Z is O,S, vinylene or azomethyne, A is an alkylene and J is phenyl or etc. It is useful to treat the heart desease.
摘要翻译：丁烯酸化合物由下式定义：其中Z为O，S，亚乙烯基或偶氮甲炔的A（Ⅰ），A为亚烷基，J为苯基等。治疗心脏病是有用的。

6. 发明申请

US20190315680A1 INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF 审中-公开
公开(公告)号：US20190315680A1
公开(公告)日：2019-10-17
申请号：US16389008
申请日：2019-04-19
申请人： Rgenix, Inc.
发明人： Eduardo J. Martinez , Sohail F. Tavazoie
IPC分类号： C07C279/14 , C07D253/06 , C07C279/16 , C07C313/34 , C07F9/6506 , C07F9/572 , C07F9/568 , A61K31/7105 , A61K31/704 , A61K31/337 , A61K31/155 , A61K31/53 , A61K31/7068 , A61K45/06 , C07C275/70 , C07D205/08 , C07D213/74 , C07H19/06 , A61K31/397 , A61K31/40 , A61K31/4168 , A61K31/4402 , A61K31/4427 , A61K31/505 , C07D295/32 , C07D207/22 , C07D207/16 , C07D205/04 , C07D487/04 , C07D257/08 , C07D249/14 , C07D249/08 , C07D239/14 , C07D405/04 , C07D239/06 , C07D401/04 , C07D233/88 , C07D233/64 , C07D233/52 , C07D233/46 , C07D233/26 , C07C309/15 , C07D231/12 , C07C281/18 , C07C281/16 , C07C279/36 , C07C279/26 , C07C259/14 , C07C257/14 , C07D213/76 , A61K31/00 , C07F9/40 , C07F9/38 , C07F9/24 , C07F9/09 , C07F9/48
摘要： This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

7. 发明授权

US06124466A Nitroisourea derivative 有权
标题翻译：硝基异脲衍生物
公开(公告)号：US06124466A
公开(公告)日：2000-09-26
申请号：US357001
申请日：1999-07-19
申请人： Hirozumi Matsuno , Kiyoshi Arai , Takeshi Oura , Kenji Kodaka
发明人： Hirozumi Matsuno , Kiyoshi Arai , Takeshi Oura , Kenji Kodaka
IPC分类号： C07C273/00 , C07C275/70 , C07C277/08 , C07C279/36 , C07D213/61 , C07D277/28 , C07D277/32 , C07D307/14 , C07D213/53
CPC分类号： C07D277/32 , C07C273/00 , C07C275/70 , C07C277/08 , C07D213/61 , C07D307/14
摘要： A novel nitroisourea derivative and a process for producing the same, which is an important intermediate for the production of a nitroguanidine derivative having an insecticidal activity, and a process for producing a nitroguanidine derivative having an insecticidal activity using the nitroisourea derivative. The process for producing a nitroguanidine derivative represented by formula (1), effective as an insecticide is shown by reaction scheme (2): ##STR1## wherein R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms or a benzyl group; R.sub.2 represents an alkyl group having from 1 to 4 carbon atoms; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; and Q represents a 5-membered or 6-membered heterocyclic ring having at least one of the following: a nitrogen atom, an oxygen atom or a sulfur atom, one of the hydrogen atoms being substitutable with a halogen atom.
摘要翻译：一种新型的硝基异脲衍生物及其制备方法，其是生产具有杀虫活性的硝基胍衍生物的重要中间体，以及使用硝基异脲衍生物制备具有杀虫活性的硝基胍衍生物的方法。由式（1）表示的硝基胍衍生物的制备方法如反应方案（2）所示：其中R 1表示具有1至4个碳原子的烷基或苄基; R 2表示具有1至4个碳原子的烷基; R3，R4，R5和R6各自独立地表示氢原子或具有1至4个碳原子的烷基; Q表示具有以下至少一个的5元或6元杂环：氮原子，氧原子或硫原子，其中一个氢原子可与卤素原子取代。

8. 发明授权

US5990083A Multicatalytic protease inhibitors 失效
标题翻译：多分解蛋白酶抑制剂
公开(公告)号：US5990083A
公开(公告)日：1999-11-23
申请号：US816510
申请日：1997-03-13
申请人： Mohamed Iqbal , James L. Diebold , Robert Siman , Sankar Chatterjee , James C. Kauer
发明人： Mohamed Iqbal , James L. Diebold , Robert Siman , Sankar Chatterjee , James C. Kauer
IPC分类号： A61K31/18 , A61K31/216 , A61K31/22 , A61K31/275 , A61K31/277 , A61K31/353 , A61K31/4035 , A61K31/69 , A61K38/00 , A61K38/55 , A61K45/00 , A61P19/00 , A61P21/00 , A61P43/00 , C07C279/14 , C07C279/34 , C07C279/36 , C07C311/01 , C07C311/06 , C07C311/09 , C07C311/47 , C07C311/64 , C07C337/06 , C07C337/08 , C07D209/48 , C07D311/70 , C07F5/02 , C07K5/02 , C07K5/023 , C07K5/072 , C07C231/00 , C07C235/00 , C07C255/00
CPC分类号： C07D209/48 , A61K31/18 , A61K31/216 , A61K31/22 , A61K31/277 , A61K31/353 , A61K31/4035 , C07C279/36 , C07C311/09 , C07C311/47 , C07C311/64 , C07C337/08 , C07D311/70 , C07F5/025 , C07K5/0207 , C07K5/06095 , A61K38/00 , C07C2101/08
摘要： Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
摘要翻译：本文公开了由以下通式表示的多分析蛋白酶的抑制剂：本文公开了组成成分和优选的组成成分。制备和使用所公开的化合物的方法也在本文中阐述。

9. 发明授权

US5807875A Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：氨基酸衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5807875A
公开(公告)日：1998-09-15
申请号：US763504
申请日：1996-12-11
申请人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Henri Doods , Heike Andrea Wieland , Klaus-Dieter Willim , Jurgen Krause , Horst Dollinger , Franz Esser , Gerd Schnorrenberg , Michael Entzeroth , Wolfgang Wienen
发明人： Klaus Rudolf , Wolfgang Eberlein , Wolfhard Engel , Gerhard Mihm , Henri Doods , Heike Andrea Wieland , Klaus-Dieter Willim , Jurgen Krause , Horst Dollinger , Franz Esser , Gerd Schnorrenberg , Michael Entzeroth , Wolfgang Wienen
IPC分类号： A61K31/155 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/4245 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4468 , A61K31/454 , A61K31/47 , A61K38/00 , A61P9/12 , A61P43/00 , C07C237/22 , C07C237/42 , C07C255/60 , C07C257/12 , C07C257/14 , C07C257/18 , C07C259/10 , C07C259/18 , C07C261/04 , C07C275/40 , C07C279/10 , C07C279/12 , C07C279/14 , C07C279/18 , C07C279/36 , C07C307/02 , C07C307/10 , C07C311/08 , C07C311/15 , C07C311/19 , C07C311/39 , C07C311/42 , C07D209/14 , C07D209/16 , C07D209/42 , C07D209/44 , C07D211/28 , C07D213/38 , C07D213/55 , C07D215/12 , C07D215/38 , C07D223/20 , C07D233/24 , C07D233/48 , C07D233/54 , C07D233/64 , C07D233/66 , C07D233/72 , C07D233/88 , C07D235/06 , C07D235/08 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D271/06 , C07D271/07 , C07D295/15 , C07D333/20 , C07D333/36 , C07D401/12 , C07D471/04 , C07K5/072 , C07C273/00 , C07C275/00
CPC分类号： C07D233/64 , C07C237/22 , C07C237/42 , C07C255/60 , C07C257/12 , C07C257/14 , C07C257/18 , C07C259/10 , C07C259/18 , C07C261/04 , C07C275/40 , C07C279/14 , C07C279/18 , C07C279/36 , C07C307/02 , C07C307/10 , C07C311/08 , C07C311/19 , C07C311/39 , C07C311/42 , C07D209/16 , C07D209/42 , C07D209/44 , C07D213/38 , C07D215/38 , C07D223/20 , C07D233/24 , C07D233/48 , C07D233/72 , C07D233/88 , C07D235/06 , C07D249/12 , C07D249/14 , C07D271/07 , C07D295/15 , C07D333/20 , C07D471/04 , C07K5/06095 , A61K38/00 , C07C2101/08 , C07C2101/14 , C07C2103/18 , C07C2103/74
摘要： Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-�(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
摘要翻译：氨基酸衍生物，适用于治疗肥胖症。以下化合物是以下类别的示例：（R，S）-N 2 - （二苯基乙酰基）-N - [（4-羟基苯基）甲基] -N 5 - （1H-咪唑-2-基） - 甲硅烷基酰胺。

10. 发明授权

US5783734A Process for preparing N-methyl-N'-nitroguanidine 失效
标题翻译：制备N-甲基-N'-硝基胍的方法
公开(公告)号：US5783734A
公开(公告)日：1998-07-21
申请号：US820274
申请日：1997-03-18
申请人： Bernd Gallenkamp , Lothar Rohe
发明人： Bernd Gallenkamp , Lothar Rohe
IPC分类号： C07C277/08 , C07C279/36
CPC分类号： C07C279/36
摘要： The present invention relates to a novel process for preparing N-methyl-N'-nitroguanidine by reacting nitroguanidine with aqueous methylamine solution at 0.degree. to 40.degree. C.
摘要翻译：本发明涉及通过硝基胍与甲胺水溶液在0-40℃下反应制备N-甲基-N'-硝基胍的新方法。

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