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1. 发明申请

WO1996016031A1 AMINOGUANIDINE CARBOXYLATES FOR THE TREATMENT OF NON-INSULIN-DEPENDENT DIABETES MELLITUS 审中-公开
标题翻译：用于治疗非胰岛素依赖性糖尿病的氨基葡糖胺羧酸酯
公开(公告)号：WO1996016031A1
公开(公告)日：1996-05-30
申请号：PCT/US1995014126
申请日：1995-11-13
申请人： THE UPJOHN COMPANY , LARSEN, Scott, D. , VAILLANCOURT, Valerie, A. , MAY, Paul, D. , TANIS, Steven, P. , TUCKER, John, A. , MEGLASSON, Martin, D. , SCHOSTAREZ, Heinrich, J.
发明人： THE UPJOHN COMPANY
IPC分类号： C07C281/16
CPC分类号： A61K31/195 , A61K31/198 , C07C281/16 , C07C281/18
摘要： The present invention provides novel compounds of the formulae (I): AG-(CH2)n-CO2R and (II) or pharmacologically acceptable salts thereof, wherein AG is: a) N-aminoguanidine, b) N,N'-diaminoguanidine, or c) N,N',N"-triaminoguanidine; and n, R and R have the meanings given in the description as well as a new use for the compounds of formula (III) wherein R has the meanings given in the description for the treatment of non-insulin dependent diabetes mellitus (NIDDM).
摘要翻译：本发明提供新的式（I）化合物：AG-（CH 2）n -CO 2 R 1和（II）或其药理学上可接受的盐，其中AG为：a）N-氨基胍，b）N，N' - 二氨基胍，或c）N，N'，N“ - 三氨基胍;且n，R 1和R 2具有本说明书中给出的含义以及式（III）化合物的新用途，其中 R 3具有在治疗非胰岛素依赖性糖尿病（NIDDM）的描述中给出的含义。

2. 发明申请

WO0234729A8 PROCESS FOR THE PREPARATION OF 1,5-DISUBSTITUTED-3-AMINO-1,2,4-TRIAZOLES AND SUBSTITUTED AMINOGUANIDINES AS INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：作为中间体化合物制备1,5-取代的3-氨基-1,2,4-三唑和取代的氨基葡萄糖的方法
公开(公告)号：WO0234729A8
公开(公告)日：2004-04-08
申请号：PCT/HU0100103
申请日：2001-10-25
申请人： SANOFI SYNTHELABO , BOKOTEY SANDOR , CSIKOS EVA , GOENCZI CSABA , HAJDU FELIX , HERMECZ ISTVAN , HEJA GERGELY , PODANYI BENJAMIN , SANTANE CSUTOR ANDREA , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
发明人： BOKOTEY SANDOR , CSIKOS EVA , GOENCZI CSABA , HAJDU FELIX , HERMECZ ISTVAN , HEJA GERGELY , PODANYI BENJAMIN , SANTANE CSUTOR ANDREA , SZOMOR TIBORNE , SZVOBODA GYOERGYNE
IPC分类号： C07C281/16 , C07D249/14 , C07D295/13 , C07D295/12
CPC分类号： C07D295/13 , C07C281/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D249/14
摘要： New process for the preparation of 1,5-disubstituted-3-amino-1,2,4-triazoles of the general formula (I), wherein the meaning of R is C1-5alkyl group; C3-13cycloalkyl-C0-4alkyl group, optionally substituted by one or more C1-3alkyl group; phenyl-C0-2alkyl-, (CH2)n-morpholino-, piperidino-, pyrrolidino- or piperazino-group, optionally substituted by one or more halogen atom, C1-3alkyl group, C1-3alkoxy group, n is 1-5, R , R , R , and R stand independently for hydrogen, halogen, C1-6alkyl group, C1-3alkoxy group or trifuluoromethyl group, with the proviso that of the substituents R , R , R , and R at least one stands for hydrogen.
摘要翻译：用于制备通式（I）的1,5-二取代-3-氨基-1,2,4-三唑的新方法，其中R的含义是C 1-5烷基; 任选被一个或多个C 1-3烷基取代的C 3-13环烷基-C 0-4烷基; 苯基-C 0-2烷基 - ，（CH 2）n - 吗啉代 - ，哌啶子基 - ，吡咯烷基 - 或哌嗪基，任选被一个或多个卤素原子取代，C 1-3烷基，C 1-3烷氧基，n为1-5， R 1，R 2，R 3和R 4分别独立地表示氢，卤素，C 1-6烷基，C 1-3烷氧基或三氟甲基，条件是取代基R 1 R 2，R 3和R 4中的至少一个代表氢。

3. 发明申请

WO00072800A3 IL-8 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： IL-8受体拮抗剂
公开(公告)号：WO00072800A3
公开(公告)日：2001-03-08
申请号：PCT/US2000/014655
申请日：2000-05-26
IPC分类号： C07C279/18 , C07C281/16 , C07D211/22 , C07D211/26 , C07D295/215 , C07C277/00 , A61K31/155
CPC分类号： C07D295/215 , C07C279/18 , C07C281/16 , C07D211/22 , C07D211/26
摘要： This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译：本发明涉及苯脲类治疗由趋化因子介导的疾病状态，白细胞介素-8（IL-8）的新用途。

4. 发明申请

WO9823565A3 Aminoguandines and alkoxyguandines as protease inhibitors 审中-公开
标题翻译：氨基嘌呤和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：WO9823565A3
公开(公告)日：1998-07-30
申请号：PCT/US9721649
申请日：1997-11-26
申请人： DIMENSIONAL PHARM INC
发明人： TOMCZUK BRUCE E , SOLL RICHARD M , LU TIANBAO , FEDDE CYNTHIA L , ILLIG CARL R , MARKOTAN THOMAS P , STAGNARO THOMAS P
IPC分类号： C07D295/22 , A01N1/02 , A61K20060101 , A61K31/155 , A61K31/165 , A61K31/18 , A61K31/225 , A61K31/255 , A61K31/305 , A61K31/335 , A61K31/341 , A61K31/36 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/535 , A61K33/42 , A61L33/00 , A61P7/00 , A61P7/02 , A61P9/10 , A61P29/00 , C07C20060101 , C07C69/76 , C07C279/00 , C07C279/10 , C07C281/16 , C07C291/04 , C07C303/30 , C07C303/40 , C07C305/00 , C07C309/00 , C07C309/63 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C317/26 , C07C323/17 , C07D20060101 , C07D207/14 , C07D207/16 , C07D207/48 , C07D209/04 , C07D211/22 , C07D211/58 , C07D211/64 , C07D211/96 , C07D213/24 , C07D213/42 , C07D213/74 , C07D215/12 , C07D215/36 , C07D217/12 , C07D217/22 , C07D229/00 , C07D231/04 , C07D237/02 , C07D239/42 , C07D239/72 , C07D243/04 , C07D245/02 , C07D261/02 , C07D263/54 , C07D265/02 , C07D267/04 , C07D269/00 , C07D285/14 , C07D295/12 , C07D307/02 , C07D307/52 , C07D307/66 , C07D311/66 , C07D311/74 , C07D317/08 , C07D317/14 , C07D317/34 , C07D317/40 , C07D317/64 , C07D333/06 , C07D333/34 , C07D333/54 , C07D333/62 , C07D403/04 , C07D413/04 , C07F9/22
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of formula (I) wherein X is O or NR?9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc¿, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula (I). The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

5. 发明申请

WO2009111037A2 COMPOSITIONS AND METHODS FOR TREATING NOS-ASSOCIATED DISEASES 审中-公开
标题翻译：用于治疗与NOS相关的疾病的组合物和方法
公开(公告)号：WO2009111037A2
公开(公告)日：2009-09-11
申请号：PCT/US2009/001401
申请日：2009-03-03
申请人： INDIGENE PHARMACEUTICALS INC. , KANDULA, Mahesh , VAMAN RAO, Mary, E.
发明人： KANDULA, Mahesh , VAMAN RAO, Mary, E.
IPC分类号： C07C281/16 , C07D339/04
CPC分类号： C07C281/18 , C07D339/04
摘要： The disclosures herein provide lipoic acid salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, or injection. Such compositions may be used to treat NOS-associated diseases such as inflammatory diseases, metabolic diseases and neurodegenerative diseases.
摘要翻译：本文的公开内容提供了硫辛酸盐，以及多晶型物，溶剂化物和其水合物。这些盐可以配制成药物组合物。药物组合物可以配制用于口服给药，透皮给药或注射。这些组合物可用于治疗NOS相关疾病，例如炎性疾病，代谢疾病和神经变性疾病。

6. 发明申请

WO02034729A1 PROCESS FOR THE PREPARATION OF 1,5-DISUBSTITUTED-3-AMINO-1,2,4-TRIAZOLES AND SUBSTITUTED AMINOGUANIDINES AS INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：作为中间体化合物制备1,5-取代的3-氨基-1,2,4-三唑和取代的氨基葡萄糖的方法
公开(公告)号：WO02034729A1
公开(公告)日：2002-05-02
申请号：PCT/HU2001/000103
申请日：2001-10-25
IPC分类号： C07C281/16 , C07D249/14 , C07D295/13 , C07D295/12
CPC分类号： C07D295/13 , C07C281/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D249/14
摘要： New process for the preparation of 1,5-disubstituted-3-amino-1,2,4-triazoles of the general formula (I), wherein the meaning of R is C1-5alkyl group; C3-13cycloalkyl-C0-4alkyl group, optionally substituted by one or more C1-3alkyl group; phenyl-C0-2alkyl-, (CH2)n-morpholino-, piperidino-, pyrrolidino- or piperazino-group, optionally substituted by one or more halogen atom, C1-3alkyl group, C1-3alkoxy group, n is 1-5, R , R , R , and R stand independently for hydrogen, halogen, C1-6alkyl group, C1-3alkoxy group or trifuluoromethyl group, with the proviso that of the substituents R , R , R , and R at least one stands for hydrogen.
摘要翻译：用于制备通式（I）的1,5-二取代-3-氨基-1,2,4-三唑的新方法，其中R的含义是C 1-5烷基; 任选被一个或多个C 1-3烷基取代的C 3-13环烷基-C 0-4烷基; 苯基-C 0-2烷基 - ，（CH 2）n - 吗啉代 - ，哌啶子基 - ，吡咯烷基 - 或哌嗪子基，任选被一个或多个卤素原子取代，C 1-3烷基，C 1-3烷氧基，n为1-5， R 1，R 2，R 3和R 4分别独立地表示氢，卤素，C 1-6烷基，C 1-3烷氧基或三氟甲基，条件是取代基R 1 R 2，R 3和R 4中的至少一个代表氢。

7. 发明申请

WO01005752A1 AMINOGUANIDINE BICARBONATE WITH PARTICULAR PROPERTIES AND METHOD FOR MAKING SAME 审中-公开
标题翻译：具有特殊性质的氨基胍二碳酸酯及其制备方法
公开(公告)号：WO01005752A1
公开(公告)日：2001-01-25
申请号：PCT/FR2000/001579
申请日：2000-06-08
IPC分类号： C07C277/08 , C07C277/02 , C07C279/02 , C07C281/16
CPC分类号： C07C277/02 , C07C279/02
摘要： The invention concerns a method for making aminoguanidine bicarbonate from an aqueous solution of cyanamide and an aqueous solution of hydrazine hydrate in the presence of CO2. The invention is characterised in that it consists in proceeding with an amount of cyanide slightly higher than the stoichiometric quantity. The invention also concerns quasi-spherical agglomerates of aminoguanidine bicarbonate crystals.
摘要翻译：本发明涉及一种在二氧化碳存在下由氰胺水溶液和水合肼水溶液制备氨基胍碳酸氢盐的方法。本发明的特征在于，其进行量稍微高于化学计量的氰化物。本发明还涉及氨基胍碳酸氢盐晶体的准球形附聚物。

8. 发明申请

WO99030926A2 PYROTECHNIC GAS GENERANT COMPOSITION INCLUDING HIGH OXYGEN BALANCE FUEL 审中-公开
标题翻译： PYROTECHNIC天然气生成组合物，包括高氧平衡燃料
公开(公告)号：WO99030926A2
公开(公告)日：1999-06-24
申请号：PCT/US1998/025716
申请日：1998-12-10
IPC分类号： A62D1/00 , C06B25/34 , C06B43/00 , C06B45/10 , C06B49/00 , C06D5/04 , C06D5/06 , C07C281/16 , B60R
CPC分类号： C06D5/06 , C06B25/34 , C07C281/16
摘要： A pyrotechnic gas generant composition including a high oxygen balance compound or fuel which is the resulting reaction product of aminoguanidine nitrate and nitric acid. Specifically, the resulting reaction product is a yellow precipitate that can be used alone, with or without oxidizers or other additives, for very rapid self-deflagration or in combination with oxidizers and additives. In each instance, the gas generant composition provides both high gas output and low production of solid combustion products. Further, the precipitant is relatively non-hygroscopic and has a high burn rate. Specifically, the gas generating composition is useful as a gas generator for an air bag of an occupant restraint system for an automobile, gun propellants, inflation and expulsion devices, flotation devices, pyrotechnics, fire suppression devices and smokeless, reduced smoke and smokey rocket propellants.
摘要翻译：一种包含高氧平衡化合物或燃料的烟火气体发生剂组合物，其是硝酸氨基胍和硝酸的反应产物。具体地说，所得到的反应产物是一种黄色沉淀物，可以单独使用，具有或不具有氧化剂或其它添加剂，用于非常快速的自燃或与氧化剂和添加剂的组合。在每种情况下，气体发生剂组合物提供高的气体输出和低固体燃烧产物的生产。此外，沉淀剂相对不吸湿并且具有高燃烧率。具体地说，气体发生组合物可用作用于汽车乘客约束系统，枪推进剂，充气和排出装置，浮选装置，烟火，灭火装置和无烟，减少烟雾和烟雾火箭推进剂的气囊的气体发生器。

9. 发明申请

WO2012032257A1 NOUVEAUX DÉRIVÉS GUANIDINES EN SÉRIE CINNAMIQUE 审中-公开
标题翻译：新闻系列中的新型胍基衍生物
公开(公告)号：WO2012032257A1
公开(公告)日：2012-03-15
申请号：PCT/FR2011/052035
申请日：2011-09-06
申请人： PRODUITS CHIMIQUES AUXILIAIRES ET DE SYNTHESE , LANCELOT, Jean Charles , SUZANNE, Peggy , VOISIN-CHIRET, Anne-Sophie , PECQUET, Régis , JOSEPH, Jean-Christophe , RAULT, Sylvain
发明人： LANCELOT, Jean Charles , SUZANNE, Peggy , VOISIN-CHIRET, Anne-Sophie , PECQUET, Régis , JOSEPH, Jean-Christophe , RAULT, Sylvain
IPC分类号： C07C243/32 , C07C243/34 , C07C281/16 , C07D249/18 , A61K8/43 , A61Q19/08
CPC分类号： C07C281/16 , A61K8/43 , A61Q19/08 , C07C243/32 , C07C243/34 , C07C277/08 , C07C279/00 , C07D249/18 , C07D317/46
摘要： L'invention concerne de nouveaux dérivés guanidines en série cinnamique de formule générale (I) : L'invention concerne également le procédé de préparation desdits dérivés guanidine ainsi que des intermédiaires de synthèse. L'invention concerne enfin l'utilisation des dérivés guanidine pour la préparation de compositions aux propriétés anti-glycation, notamment en cosmétologie.
摘要翻译：本发明涉及通式（I）肉桂系列中的新型胍衍生物。本发明还涉及制备所述胍衍生物的方法以及合成中间体。最后，本发明涉及胍衍生物用于制备具有抗糖化性质的组合物的用途，特别是在美容方面。

10. 发明申请

WO2011138410A1 AMINOGUANIDINEPHENYLPHOSPHINATE FLAME RETARDANT COMPOSITIONS 审中-公开
标题翻译：氨基苯甲酸磷酸酯阻燃剂组合物
公开(公告)号：WO2011138410A1
公开(公告)日：2011-11-10
申请号：PCT/EP2011/057236
申请日：2011-05-05
申请人： BASF SE , XALTER, Rainer , WEIß, Thomas
发明人： XALTER, Rainer , WEIß, Thomas
IPC分类号： C07C281/16 , C08K5/00 , C08K5/31 , C08K5/5313
CPC分类号： C09K21/12 , C07C279/02 , C07C281/16 , C07F9/304 , C08K5/0066 , C08K5/5205 , C08K5/5313 , C08L63/00
摘要： The present invention relates to flame retardant polymer compositions which comprise aminoguanidine phenylphosphinates and mixtures with additional flame retardants. The compositions are especially useful for the manufacture of flame retardant compounds based on polyfunctional epoxides or polycondensates like polyesters, polyamides and polycarbonates.
摘要翻译：本发明涉及包含氨基胍苯基次膦酸盐和与另外的阻燃剂的混合物的阻燃聚合物组合物。该组合物特别可用于制造基于多官能环氧化物或缩聚物如聚酯，聚酰胺和聚碳酸酯的阻燃化合物。

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