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1. 发明授权

US08748412B2 Phenylalanine derivatives and their use as non-peptide GLP-1 receptor modulators 有权
标题翻译：苯丙氨酸衍生物及其作为非肽GLP-1受体调节剂的用途
公开(公告)号：US08748412B2
公开(公告)日：2014-06-10
申请号：US13019851
申请日：2011-02-02
申请人： Jiayu Liao , Yufeng Hong , Yong Wang , Thomas W. Von Geldern , Kanyin E. Zhang
发明人： Jiayu Liao , Yufeng Hong , Yong Wang , Thomas W. Von Geldern , Kanyin E. Zhang
IPC分类号： A61K31/635 , A61K31/341 , A61K31/27 , A61K31/4245 , A61K31/4439 , A61K31/506 , A61K31/454 , A61K31/5377 , A61K31/551 , C07C271/28 , C07D271/06 , C07D413/12 , C07D413/14 , C07D307/68
CPC分类号： C07D413/12 , C07C233/47 , C07C233/51 , C07C233/87 , C07C275/28 , C07C323/59 , C07C323/60 , C07C2601/10 , C07D207/09 , C07D209/32 , C07D217/08 , C07D231/04 , C07D233/16 , C07D241/04 , C07D249/06 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/22 , C07D307/42 , C07D333/10 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/14
摘要： Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.
摘要翻译：本文提供了非肽GLP-1受体调节剂化合物，例如式I，包含这些化合物的药物组合物及其制备方法。还提供了它们用于治疗代谢紊乱的方法。

2. 发明申请

US20070066594A1 Crystalline forms fenoldopam mesylate 审中-公开
标题翻译：结晶形式甲磺酸非诺多泮
公开(公告)号：US20070066594A1
公开(公告)日：2007-03-22
申请号：US11505229
申请日：2006-08-15
申请人： Peter MacDonald , Ettore Bigatti , Pierluigi Rossetto , Judith Aronhime , Sigalit Levi
发明人： Peter MacDonald , Ettore Bigatti , Pierluigi Rossetto , Judith Aronhime , Sigalit Levi
IPC分类号： A61K31/55 , C07D223/16
CPC分类号： C07D223/16 , C07D233/16
摘要： The invention provides new crystalline forms of fenoldopam mesylate, i.e. fenoldopam mesylate Type I, fenoldopam mesylate Type III, fenoldopam mesylate Type V, and fenoldopam mesylate Type VI, methods of preparing the crystalline forms, and pharmaceutical compositions comprising the fenoldopam mesylate crystalline forms of the invention.
摘要翻译：本发明提供了甲磺酸非诺多泮的新结晶形式，即I型甲氟苯泮，III型非诺多泮甲磺酸盐，V型甲氟苯泮，V型甲磺酸en诺帕姆，VI型甲氟苯泮，制备结晶形式的方法，以及包含甲磺酸非诺多泮甲磺酸盐结晶形式的药物组合物发明。

3. 发明授权

US06911546B2 Catalytic depolymerization of polymers containing electrophilic linkages using nucleophilic reagents 有权
标题翻译：使用亲核试剂催化解聚包含亲电键的聚合物
公开(公告)号：US06911546B2
公开(公告)日：2005-06-28
申请号：US10330853
申请日：2002-12-26
申请人： James Lupton Hedrick , Pinar Kilickiran , Gregory Walker Nyce , Robert M. Waymouth
发明人： James Lupton Hedrick , Pinar Kilickiran , Gregory Walker Nyce , Robert M. Waymouth
IPC分类号： C07C59/285 , C07C67/03 , C07C68/06 , C07D233/02 , C07D233/04 , C07D233/06 , C07D233/16 , C07D233/54 , C07D307/33 , C07F1/00 , C07D233/38 , C07F2/46
CPC分类号： C07D233/16 , C07C59/285 , C07C67/03 , C07C68/06 , C07D233/02 , C07D233/04 , C07D233/06 , C07D233/54 , C07D307/33 , C07F1/00 , C07C69/82 , C07C69/96
摘要： A method is provided for carrying out depolymerization of a polymer containing electrophilic linkages in the presence of a catalyst and a nucleophilic reagent, wherein production of undesirable byproducts resulting from polymer degradation is minimized. The reaction can be carried out at a temperature of 80° C. or less, and generally involves the use of an organic, nonmetallic catalyst, thereby ensuring that the depolymerization product(s) are substantially free of metal contaminants. In an exemplary depolymerization method, the catalyst is a carbene compound such as an N-heterocyclic carbene, or is a precursor to a carbene compound. The method provides an important alternative to current recycling techniques such as those used in the degradation of polyesters, polyamides, and the like.
摘要翻译：提供了一种在催化剂和亲核试剂的存在下进行含有亲电键的聚合物解聚的方法，其中由聚合物降解产生的不需要的副产物的产生最小化。反应可以在80℃或更低的温度下进行，通常涉及使用有机非金属催化剂，从而确保解聚产物基本上不含金属污染物。在示例性的解聚方法中，催化剂是卡宾化合物如N-杂环卡宾，或是卡宾化合物的前体。该方法提供了当前回收技术的重要替代方法，例如用于降解聚酯，聚酰胺等的那些。

4. 发明授权

US06635630B2 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06635630B2
公开(公告)日：2003-10-21
申请号：US10163663
申请日：2002-06-06
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K31330
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15; is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are ═O; R6 is R7 or —OH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO-，-SO 2 - ，-NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15选自X 2是-O - ， - S-或-NR 5 - ; Y是= O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - （CH 2）n6 - ， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O） R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5，G是H，-CF 3，-CHF 2，-CH 2 F，-OH，-O-（C 1 -C 6 烷基），-SO 2 R 13，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15， NR 13 R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 芳基，R 19 - 杂芳基，并且当n 1 = 0时，G不为H; R 1，R 2，R 3和R 7为H，烷基，环烷基，-CHF 2 ，-CH2F或-CF3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6为R 7或-OH;其余变量如本说明书中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法，所述化合物和包含所述化合物的药物组合物。还公开了药物组合物，其包含有效量的权利要求1的化合物，至少一种药学上可接受的载体，并与有效量的选择性5-羟色胺再摄取抑制剂组合。

5. 发明授权

US06436928B1 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06436928B1
公开(公告)日：2002-08-20
申请号：US09737036
申请日：2000-12-14
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K314166
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： A compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —SO0-2—, —NR12—, —NCOR12— or —NR12SO2R15; is X2 is —O—, —S— or optionally substituted nitrogen; Y is ═O, ═S or ═NR11; Y1 is H, alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6-heterocycloalkyl, -alkyl-NH—C(O)O-alkyl or —NHC(O)R15; R1, R2, R3 and R7 are H, alkyl, OH-alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2 form an alkylene ring; or R1 and R2 together are ═O; R6 is H, alkyl, —OR13 or —SR12; and the remaining variables are as defined in the specification, is disclosed, as well as a pharmaceutical compositions comprising said compound, methods of using said compound as a neurokinin antagonist, and the combination of said compounds with a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O-，-SOO 2 - ， - NR 12 - ， - NRCOR 12 - 或-NR 12 SO 2 R 15; isX2是-O - ， - S-或任选取代的氮; Y是= O，= S或= NR 11; Y 1是H，烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - ，R 19 - （CH2）n6-， - （CH2）n6-杂环烷基， - 烷基-NH-C（O）O-烷基或-NHC（O）R15; R1，R2，R3和R7是H，烷基，环烷基，-CHF 2，-CH 2 F或-CF 3; 或R 1和R 2形成亚烷基环; 或R 1和R 2一起为= O; R 6为H，烷基，-OR 13或-SR 12;其余变量如本说明书中所定义，以及包含所述化合物的药物组合物，使用所述化合物的方法作为神经激肽拮抗剂，以及所述化合物与选择性5-羟色胺再摄取抑制剂的组合。

6. 发明授权

US6133283A Mono- or polyenic carboxylic acid derivatives 失效
标题翻译：单或多元羧酸衍生物
公开(公告)号：US6133283A
公开(公告)日：2000-10-17
申请号：US236644
申请日：1999-01-26
申请人： Shigeki Hibi , Kouichi Kikuchi , Hiroyuki Yoshimura , Mitsuo Nagai , Katsuya Tagami , Shinya Abe , Ieharu Hishinuma , Junichi Nagakawa , Norimasa Miyamoto , Takayuki Hida , Aichi Ogasawara , Seiko Higashi , Kenji Tai , Takashi Yamanaka , Makoto Asada
发明人： Shigeki Hibi , Kouichi Kikuchi , Hiroyuki Yoshimura , Mitsuo Nagai , Katsuya Tagami , Shinya Abe , Ieharu Hishinuma , Junichi Nagakawa , Norimasa Miyamoto , Takayuki Hida , Aichi Ogasawara , Seiko Higashi , Kenji Tai , Takashi Yamanaka , Makoto Asada
IPC分类号： A61P19/02 , C07C57/03 , C07C229/44 , C07D209/08 , C07D213/69 , C07D215/12 , C07D215/14 , C07D215/18 , C07D223/16 , C07D225/06 , C07D231/12 , C07D241/38 , C07D241/42 , C07D241/46 , C07D261/18 , C07D263/32 , C07D265/36 , C07D333/76 , C07D405/14 , C07D455/04 , C07D487/04 , C07D495/04 , G06F17/30 , C07D455/06 , A61K31/44
CPC分类号： C07D213/69 , C07C229/44 , C07C57/03 , C07D209/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D223/16 , C07D225/06 , C07D231/12 , C07D233/16 , C07D241/38 , C07D241/42 , C07D241/46 , C07D261/18 , C07D263/32 , C07D265/36 , C07D333/76 , C07D405/14 , C07D455/04 , C07D487/04 , C07D495/04 , G06F17/30607 , Y02P20/55
摘要： To provide novel compounds relating to retinoid which can substitute for retinoic acid used for preventing and treating several diseases and having antagonism against retinoid. Heterocyclic compounds represented by the general formula (1-I) or physiologically acceptable salts thereof:Z--(CR.sup.3 .dbd.CR.sup.2).sub.n --COOR.sup.1-- (1-I)Compounds represented by the general formula (2-I) or physiologically acceptable salts thereof: ##STR1## The compounds according to the present invention exhibit extremely high ability to bind RARs and are effective for treating various kind of diseases such as abnormality in cornification and rheumatoid arthritis.
摘要翻译：提供与维甲酸相关的新化合物，其可以代替用于预防和治疗几种疾病并对类视黄醇具有拮抗作用的视黄酸。由通式（1-I）表示的杂环化合物或其生理学上可接受的盐：Z-（CR 3 = CR 2）n -COOR1-（1-I）由通式（2-I）表示的化合物或其生理学上可接受的盐：根据本发明的化合物显示出极高的结合RAR的能力，并且对于治疗各种类型的疾病如角质化和类风湿性关节炎的异常是有效的。

7. 发明授权

US6030964A Mono- or polyenic carboxylic acid derivatives 失效
标题翻译：单或多元羧酸衍生物
公开(公告)号：US6030964A
公开(公告)日：2000-02-29
申请号：US106112
申请日：1998-06-29
申请人： Shigeki Hibi , Kouichi Kikuchi , Hiroyuki Yoshimura , Mitsuo Nagai , Katsuya Tagami , Shinya Abe , Ieharu Hishinuma , Junichi Nagakawa , Norimasa Miyamoto , Takayuki Hida , Aichi Ogasawara , Seiko Higashi , Kenji Tai , Takashi Yamanaka , Makoto Asada
发明人： Shigeki Hibi , Kouichi Kikuchi , Hiroyuki Yoshimura , Mitsuo Nagai , Katsuya Tagami , Shinya Abe , Ieharu Hishinuma , Junichi Nagakawa , Norimasa Miyamoto , Takayuki Hida , Aichi Ogasawara , Seiko Higashi , Kenji Tai , Takashi Yamanaka , Makoto Asada
IPC分类号： A61P19/02 , C07C57/03 , C07C229/44 , C07D209/08 , C07D213/69 , C07D215/12 , C07D215/14 , C07D215/18 , C07D223/16 , C07D225/06 , C07D231/12 , C07D241/38 , C07D241/42 , C07D241/46 , C07D261/18 , C07D263/32 , C07D265/36 , C07D333/76 , C07D405/14 , C07D455/04 , C07D487/04 , C07D495/04 , G06F17/30 , A61K31/55
CPC分类号： C07D213/69 , C07C229/44 , C07C57/03 , C07D209/08 , C07D215/12 , C07D215/14 , C07D215/18 , C07D223/16 , C07D225/06 , C07D231/12 , C07D233/16 , C07D241/38 , C07D241/42 , C07D241/46 , C07D261/18 , C07D263/32 , C07D265/36 , C07D333/76 , C07D405/14 , C07D455/04 , C07D487/04 , C07D495/04 , G06F17/30607 , Y02P20/55
摘要： Compounds of the formula and compounds of the formula ##STR1## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.
摘要翻译：下式的化合物和下式化合物或其盐具有结合视黄酸受体的有效能力，因此可用于治疗牛皮癣和类风湿性关节炎。

8. 发明授权

US4865614A Quaternary 2-alkylimidazolinium salts as fabric softeners 失效
标题翻译：第四纪2-烷基咪唑啉鎓盐作为织物柔软剂
公开(公告)号：US4865614A
公开(公告)日：1989-09-12
申请号：US57555
申请日：1987-06-03
申请人： Uwe Ploog , Guenter Uphues
发明人： Uwe Ploog , Guenter Uphues
IPC分类号： C07D233/06 , C07D233/14 , C07D233/16 , D06M13/02 , D06M13/322 , D06M13/352 , D06M13/46 , D06M13/47 , D06M13/473
CPC分类号： C07D233/14 , C07D233/16 , D06M13/352
摘要： The reaction of 2-alkylimidazolines with ethylene oxide or propylene oxide gives quaternary 2-alkyl-2-imidazolinium salts corresponding to the following general formula ##STR1## wherein R.sup.1 represents a straight-chain or branched-chain substituted or unsubstituted alkyl or alkenyl radical containing from 7 to 21 carbon atoms,R.sup.2 represents one of the following radicals ##STR2## R.sup.3 represents hydrogen or methyl, R.sup.4 represents hydrogen or methyl,X.sup..crclbar. represents the anion of a non-oxidizing and non-corrosive inorganic acid or of an organic mono- or polycarboxylic acid,n statistically represents a whole or fraction number of from 1 to 20, andm represents an integer of from 1 to 3, which may be used for softening laundered fabrics.
摘要翻译： 2-烷基咪唑与环氧乙烷或环氧丙烷的反应产生对应于下列通式（I）的季铵-2-烷基-2-咪唑啉鎓盐，其中R 1表示直链或支链取代或未取代的烷基或含有7〜21个碳原子的链烯基，R2代表下列基团之一：R 3表示氢或甲基，R 4表示氢或甲基，X（ - ）表示非氧化性和非腐蚀性无机酸的阴离子或有机单羧酸或多元羧酸，n统计学上表示1至20的整数或级分数，m表示1至3的整数，其可用于软化洗涤织物。

9. 发明授权

US4399044A Textile softening composition 失效
标题翻译：纺织软化组成
公开(公告)号：US4399044A
公开(公告)日：1983-08-16
申请号：US344685
申请日：1982-02-01
申请人： James M. Richmond
发明人： James M. Richmond
IPC分类号： C07D233/16 , C07F5/04 , D06M13/46 , D06M13/47 , D06M13/40
CPC分类号： C07D233/16 , C07F5/04 , D06M13/461 , D06M13/47
摘要： A composition for imparting softness to textile materials, comprising an ethoxylated amido amine quaternary salt or an ethoxylated imidazolinium quaternary salt.
摘要翻译：用于赋予纺织材料柔软性的组合物，其包含乙氧基化酰胺胺季盐或乙氧基化咪唑啉季盐。

10. 发明授权

US3766203A Process for preparing imidazoline compounds 失效
标题翻译：制备咪唑啉化合物的方法
公开(公告)号：US3766203A
公开(公告)日：1973-10-16
申请号：US3766203D
申请日：1971-12-27
申请人： AJINOMOTO KK
发明人： SUMIDA S , HACHIYA T
IPC分类号： C07D233/06 , C07D233/16 , C07D49/34
CPC分类号： C07D233/06 , C07D233/16
摘要： IMIDAZOLINE COMPOUNDS ARE PREPARED IN HIGH YIELD AND IN HIGH PURITY BY REACTING A 1,2-DIAMINE COMPOUND OR AN N-SUBSTITUTED 1,2-DIAMINE COMPOUND WITH A NITRILE COMPOUND IN THE PRESENCE OF A CATALYSTIC AMOUNT OF CYSTEINE OR CYSTINE.

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