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21. 发明申请

US20070066647A1 Conformationally constrained 3-(4-hydroxy-phenyl)-substituted-propanoic acids useful for treating metabolic disorders 有权
标题翻译：构型受限的3-（4-羟基 - 苯基） - 取代 - 丙酸，可用于治疗代谢紊乱
公开(公告)号：US20070066647A1
公开(公告)日：2007-03-22
申请号：US11517992
申请日：2006-09-08
申请人： Michelle Akerman , Sean Brown , Jonathan Houze , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio Medina , Wei Qiu , Michael Schmitt , Rajiv Sharma , Yingcai Wang , Liusheng Zhu
发明人： Michelle Akerman , Sean Brown , Jonathan Houze , Jinqian Liu , Jiwen Liu , Zhihua Ma , Julio Medina , Wei Qiu , Michael Schmitt , Rajiv Sharma , Yingcai Wang , Liusheng Zhu
IPC分类号： A61K31/47 , A61K31/426 , A61K31/353 , A61K31/343 , A61K31/192 , A61K31/155
CPC分类号： C07D333/24 , C07C59/72 , C07D231/12 , C07D233/26 , C07D233/64 , C07D239/26 , C07D249/04 , C07D249/08 , C07D257/04 , C07D261/04 , C07D261/08 , C07D263/32 , C07D317/54 , C07D333/16
摘要： The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
摘要翻译：本发明提供了可用于例如治疗受试者的代谢紊乱的化合物。这些化合物具有通式I：其中变量Q，L 1，L 2，M，X，L 3，和A。本发明还提供了组合物，其包括化合物在制备药物和用于治疗代谢性疾病例如II型糖尿病中的使用方法。

22. 发明申请

US20060135559A1 Novel imidazoline compounds 失效
标题翻译：新型咪唑啉化合物
公开(公告)号：US20060135559A1
公开(公告)日：2006-06-22
申请号：US11348459
申请日：2006-02-07
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/4709 , A61K31/4439 , A61K31/4178 , C07D409/02 , C07D403/02
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

23. 发明授权

US07064142B2 Imidazonline compounds 失效
标题翻译：咪唑啉化合物
公开(公告)号：US07064142B2
公开(公告)日：2006-06-20
申请号：US10204267
申请日：2001-02-22
申请人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
发明人： Nagaaki Sato , Osamu Okamoto , Makoto Jitsuoka , Keita Nagai , Akio Kanatani , Akane Ishihara , Yasuyuki Ishii , Takehiro Fukami
IPC分类号： A61K31/415 , C07D233/26
CPC分类号： C07D401/04 , C07D233/26 , C07D401/14 , C07D403/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds represented by the general formula (I): wherein Ar1 and Ar2 are each aryl or heteroaryl; R1 is lower cycloalkyl, —Ar3, or a group of the general formula (a), (b) or (c): and R2 and R3 are each hydrogen, lower cycloalkyl, lower alkenyl, or optionally substituted lower alkyl (with the proviso that when R2 and R3 are simultaneously hydrogen, Ar1, Ar2 and R1 do not simultaneously represent unsubstituted phenyl). The compounds are useful as treating agents for various NPY-related diseases, for example, circulatory diseases including hypertension, kidney diseases, cardiac diseases, vasospasm and arteriosclerosis; central nervous system diseases including hyperphagia, depression, anxiety, convulsion, epilepsy, dementia, pain, alcohol dependence, and withdrawal symptoms due to abstinence from drugs; metabolic diseases including obesity, diabetes, hormonal disorders, hypercholesterolemia, and hyperlipidemia; sexual dysfunction and reproductive function disorders; digestive diseases including enterokinetic disorders; respiratory diseases; inflammation; or glaucoma.
摘要翻译：由通式（I）表示的化合物：其中Ar 1和Ar 2各自为芳基或杂芳基; R 1是低级环烷基，-Ar 3或通式（a），（b）或（c）的基团：R 2， R 3和R 3各自为氢，低级环烷基，低级烯基或任选取代的低级烷基（条件是当R 2和R 3' / SUP>同时为氢，Ar 1，Ar 2和R 1不同时表示未取代的苯基）。这些化合物可用作各种NPY相关疾病的治疗剂，例如包括高血压，肾脏疾病，心脏病，血管痉挛和动脉硬化的循环系统疾病; 中枢神经系统疾病，包括食欲过多，抑郁，焦虑，惊厥，癫痫，痴呆，疼痛，酒精依赖以及戒毒症状; 代谢疾病包括肥胖，糖尿病，激素失调，高胆固醇血症和高脂血症; 性功能障碍和生殖功能障碍; 消化疾病包括肠动力障碍; 呼吸疾病; 炎; 或青光眼。

24. 发明申请

US20060111347A1 Substituted sulfones and methods of use 审中-公开
标题翻译：取代的砜和使用方法
公开(公告)号：US20060111347A1
公开(公告)日：2006-05-25
申请号：US11243645
申请日：2005-10-05
申请人： Benny Askew , Toshihiro Aya , Kaustav Biswas , Jian Chen , Jason Human , Wenyuan Qian
发明人： Benny Askew , Toshihiro Aya , Kaustav Biswas , Jian Chen , Jason Human , Wenyuan Qian
IPC分类号： A61K31/5415 , A61K31/47 , A61K31/382 , A61K31/353
CPC分类号： C07D295/135 , C07C317/46 , C07C2602/10 , C07D233/26 , C07D311/68 , C07D401/04
摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

25. 发明申请

US20060063759A1 Tricyclic steroid hormone nuclear receptor modulators 有权
标题翻译：三环类固醇激素核受体调节剂
公开(公告)号：US20060063759A1
公开(公告)日：2006-03-23
申请号：US10517010
申请日：2003-06-13
申请人： Michael Coghlan , Jonathan Green , Timothy Grese , Prabhakar Kondaji , Doanald Matthews , Mitchell Steinberg , Kevin Fales , Michael Bell
发明人： Michael Coghlan , Jonathan Green , Timothy Grese , Prabhakar Kondaji , Doanald Matthews , Mitchell Steinberg , Kevin Fales , Michael Bell
IPC分类号： A61K31/551 , A61K31/473
CPC分类号： C07D213/16 , C07C22/04 , C07C22/08 , C07C25/24 , C07C33/38 , C07C39/17 , C07C39/23 , C07C39/42 , C07C43/215 , C07C43/225 , C07C43/23 , C07C47/548 , C07C47/57 , C07C49/835 , C07C69/00 , C07C69/618 , C07C69/65 , C07C205/06 , C07C205/34 , C07C205/35 , C07C211/28 , C07C211/32 , C07C211/45 , C07C215/76 , C07C217/84 , C07C233/07 , C07C233/65 , C07C233/84 , C07C235/16 , C07C251/40 , C07C251/48 , C07C255/50 , C07C261/04 , C07C271/14 , C07C275/28 , C07C307/10 , C07C311/03 , C07C311/08 , C07C311/09 , C07C311/16 , C07C311/20 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/32 , C07C321/28 , C07C323/49 , C07C2601/02 , C07C2603/32 , C07C2603/40 , C07C2603/78 , C07C2603/86 , C07D209/08 , C07D209/34 , C07D211/96 , C07D213/06 , C07D213/73 , C07D213/76 , C07D213/81 , C07D221/16 , C07D223/20 , C07D231/12 , C07D231/18 , C07D233/26 , C07D233/68 , C07D233/84 , C07D235/26 , C07D241/12 , C07D241/20 , C07D261/08 , C07D261/10 , C07D263/52 , C07D263/56 , C07D263/58 , C07D277/60 , C07D295/088 , C07D295/26 , C07D313/12 , C07D333/78 , C07D333/80 , C07D337/12 , C07D401/06 , C07D405/06 , C07D409/04 , C07D471/04 , C07D471/06 , C07D487/04 , C07D491/044
摘要： The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).
摘要翻译：本发明涉及治疗对类固醇激素核受体调节敏感的病理学障碍的方法，包括向有需要的患者施用有效量的式（I）化合物或其药学上可接受的盐。此外，本发明提供新的式（I）的药物化合物，包括其药学上可接受的盐，以及包含作为活性成分的式（I）的化合物的药物组合物。

26. 发明申请

US20050288287A1 Chiral cis-imidazolines 失效
标题翻译：手性顺式 - 咪唑啉
公开(公告)号：US20050288287A1
公开(公告)日：2005-12-29
申请号：US11129621
申请日：2005-05-13
申请人： Nader Fotouhi , Gregory Haley , Klaus Simonsen , Binh Vu , Stephen Webber
发明人： Nader Fotouhi , Gregory Haley , Klaus Simonsen , Binh Vu , Stephen Webber
IPC分类号： A61K31/4164 , A61K31/496 , A61K31/5377 , A61P35/00 , C07D233/22 , C07D233/26 , C07D403/06 , C07D413/14 , C07D43/02
CPC分类号： C07D403/06 , C07D233/22 , C07D233/26
摘要： and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3, Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proliferative activity.
摘要翻译：及其药学上可接受的盐和酯，其中X 1，X 2，X 3，Y 1，本文描述的Y 2和R 2抑制MDM2蛋白与p53样肽的相互作用，因此具有抗增殖活性。

27. 发明申请

US20020161237A1 Dehydroamino acids 失效
公开(公告)号：US20020161237A1
公开(公告)日：2002-10-31
申请号：US09754888
申请日：2001-01-05
发明人： Nader Fotouhi , Paul Gillespie , Robert William Guthrie , Sherrie Lynn Pietranico-Cole , Weiya Yun
IPC分类号： C07C235/84 , C07C255/50 , C07D257/04
CPC分类号： C07D249/08 , C07B2200/07 , C07C233/85 , C07C233/87 , C07C311/46 , C07D209/08 , C07D211/34 , C07D213/55 , C07D215/14 , C07D233/26 , C07D235/16 , C07D237/28 , C07D239/52 , C07D249/18 , C07D261/08 , C07D271/12 , C07D277/30 , C07D277/38 , C07D277/62 , C07D277/64 , C07D285/14 , C07D307/16 , C07D317/60 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/04 , C07D417/04 , C07F9/4006 , C07F9/5728 , C07F9/6524 , C07F9/65583
摘要： Compounds of formula 1 and 1-1, 1 wherein R1 is hydrogen, hydroxy, amino or halogen, R2 is hydrogen, hydroxy, or halogen and R3 is hydrogen (Formula 1) or R1 is hydrogen and R2 and R3 taken together with the ethenylene group connecting them form phenyl, pyrrole, pyrroline, oxopyrroline, pyrazole, triazole, or imidazole (Formula 1-1), A is 2 R4 R5 are hydrogen, methyl, ethyl or halogen except that R4 r5 cannot both be hydrogen; and 1) B is hydrogen, or lower alkyl; or 2) B is 3 where R6 R7 R8 and R9 are independently hydrogen, hydroxy, aminosulfonyl, halogen, lower alkoxy, cyano, amino, lower alkyl, lower alkyl amino, or nitro; or 3) B is 4 where R10 is hydrogen, hydroxy, halogen, or lower alkyl and C is a five- or six- membered ring with 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur, which ring may be unsubstituted or mono- or di- substituted with lower alkyl, cycloalkyl, amino, or substituted amino; 4) B is 5 where X and Y are independently methylene or nitrogen; or 5) B is 6 where at leat one of T, U, V, or W is nitrogen, and any of T, U, V or W which is carbon may be substituted with lower alkyl, lower alkyl amino, lower alkoxy, hydroxy, aminosulfonyl, halogen, cyano, amino, or nitro; or 6) B is 7 where Y is carbon or nitrogen; or 7) B is a five-membered aromatic ring with 1 to 3 heteratoms selected from nitrogen, oxygen, and sulfur which ring may be unsubstituted or mono- or di-substituted with lower alkyl, cycloalky, trifluoroloweralkyl, amino, halogen, substituted amino, or which ring may be fused with a 5 or 6 membered aromatic ring containing 0 to 3 heteroatoms which heteroatoms are selected from nitrogen, oxygen, and sulfur; and pharmaceutically acceptable salts thereof, and related prodrugs, pharmaceutical compositions and methods of treatment, which compounds are useful for treating psoriasis.

28. 发明申请

US20020107290A1 Benzamidine derivative 失效
标题翻译：苄脒衍生物
公开(公告)号：US20020107290A1
公开(公告)日：2002-08-08
申请号：US10073985
申请日：2002-02-14
申请人： AJINOMOTO CO., INC.
发明人： Tadakiyo Nakagawa , Kazuyuki Sagi , Kaoru Yoshida , Yumiko Fukuda , Masataka Shoji , Shunji Takehana , Takashi Kayahara , Akira Takahara
IPC分类号： A61K031/165 , A61K031/155 , C07D291/02
CPC分类号： C07D401/04 , C07C257/18 , C07D207/48 , C07D211/46 , C07D233/26 , C07D401/06 , C07D417/04 , C07F9/4015 , C07F9/4056 , C07F9/59 , C07F9/65583
摘要： Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli. 1
摘要翻译：提供下式的苄脒衍生物，其类似物和其药学上可接受的盐。这些化合物具有抑制活化凝血因子X的作用，可用作预防或治疗由血栓或栓塞引起的各种疾病的药剂。

29. 发明授权

US06409812B1 AZO compounds and process for producing the same 失效
标题翻译： AZO化合物及其制备方法
公开(公告)号：US06409812B1
公开(公告)日：2002-06-25
申请号：US09581704
申请日：2000-06-16
申请人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori
发明人： Ryuzo Ueno , Masaya Kitayama , Kenji Minami , Hiroyuki Wakamori
IPC分类号： C09D1100
CPC分类号： G03G9/091 , C07D215/44 , C07D233/26 , C09B29/20 , C09B62/0083 , C09B62/085 , C09B62/51 , G03G5/0677
摘要： A diamide type azo compound represented by the general formula (I): which is derived from 2-hydroxy-3,6-dicarboxylic acid and at least one of the amide moieties in the compound is an aliphatic amide moiety, various use of the same and process for preparing the same are provided.
摘要翻译：由通式（I）表示的二酰胺型偶氮化合物：其衍生自2-羟基-3,6-二羧酸和化合物中至少一个酰胺部分是脂族酰胺部分，其各种用途并提供其制备方法。

30. 发明授权

US6114390A 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：US6114390A
公开(公告)日：2000-09-05
申请号：US950113
申请日：1997-10-14
申请人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim , Michael Entzeroth , Wolfgang Wienen
发明人： Wolfhard Engel , Wolfgang Eberlein , Klaus Rudolf , Henri Doods , Heike-Andrea Wieland , Klaus-Dieter Willim , Michael Entzeroth , Wolfgang Wienen
IPC分类号： A61K38/00 , C07C257/18 , C07C275/24 , C07C275/56 , C07C279/14 , C07C279/24 , C07C279/36 , C07C307/06 , C07C311/35 , C07D209/08 , C07D209/18 , C07D209/24 , C07D209/42 , C07D209/44 , C07D223/20 , C07D233/26 , C07D233/36 , C07D233/72 , C07D233/88 , C07D235/06 , C07D235/08 , C07D239/46 , C07D249/14 , C07D271/06 , C07D307/85 , C07K5/078 , A61K31/17 , C07C275/14
CPC分类号： C07D235/06 , C07C257/18 , C07C275/24 , C07C275/56 , C07C279/14 , C07C279/24 , C07C279/36 , C07C307/06 , C07C311/35 , C07D209/08 , C07D209/18 , C07D209/24 , C07D209/42 , C07D209/44 , C07D223/20 , C07D233/26 , C07D233/36 , C07D233/72 , C07D233/88 , C07D235/08 , C07D239/47 , C07D249/14 , C07D271/06 , C07D307/85 , C07K5/06139 , A61K38/00
摘要： NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate;(B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate;(C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate;(D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phenyl]methyl]-argininamide-trifluoroacetate;(E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride;(F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate;(G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-argininamide-bis-(trifluoroacetate); and,(H) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl)phenyl]methyl]-argininamide-trifluoroacetate.
摘要翻译：式（A）（R）-N - [[4-（氨基羰基氨基甲基）苯基]甲基] -N2-双（4-羟基苯基）乙酰基] - 炔丙酰胺 - 三氟乙酸盐; （B）（R）-N - [[4-（氨基羰基氨基甲基）苯基]甲基] -N 2 - [双（4-氯苯基）乙酰基] - 炔丙酰胺 - 三氟乙酸盐; （C）（R）-N - [[4-氨基羰基氨基甲基）苯基]甲基] -N2-（二苯基乙酰基） - 炔丙酰胺 - 三氟乙酸盐; （D）（R）-N2-（二苯基乙酰基）-N - [[4-（乙氧基羰基甲基氨基 - 羰基氨基甲基）苯基]甲基] - 炔丙酰胺 - 三氟乙酸盐; （E）（R，S）-N5-（氨基亚氨基甲基）-N2-（二苯基乙酰基）-N - [（4-羟基苯基）甲基] -N5-甲基 - 鸟氨酰胺 - 盐酸盐; （F）（R）-N - [[4-（氨基羰基甲基）苯基]甲基] -N2-（二苯基 - 乙酰基） - 鸟氨酰胺 - 二乙酸酯; （G）（R）-N2-（二苯基乙酰基）-N - [[4-（乙基氨基羰基氨基 - 甲基） - 苯基]甲基] - 炔丙酰胺 - 双 - （三氟乙酸盐）和（H）（R）-N2-（二苯基乙酰基）-N - [[4-（乙氧基羰基氨基 - 羰基氨基甲基）苯基]甲基] - 炔丙酰胺 - 三氟乙酸盐。

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