| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 非全身性TGR5激动剂 | CN201280069126.3 | 2012-12-21 | CN104220429A | 2014-12-17 | 詹森·G·刘易斯; 尼古拉斯·雷奇; 陈涛; 杰弗里·W·雅各布斯; 多米尼克·沙尔莫; 马克·纳夫雷亚; 帕特丽夏·芬; 克里斯多佛·卡雷拉斯; 安德鲁·斯宾塞 |
| 结构(I)的化合物，或者其立体异构体、互变异构体、药学可接受的盐或前药，其中R1、R2、R3、R4、R8、R9、R10、R11、R12、A1、A2、X、Y和Z如本文所定义。还提供了该化合物作为TGR5激动剂的用途以及用于治疗包括II型糖尿病在内的各种适应征的用途。 | ||||||
| 2 | 激酶抑制剂的合成和用途 | CN201180042174.9 | 2011-06-28 | CN103168037A | 2013-06-19 | Y.雷; C.H.贝伦斯; H-Y.李; C.L.孙 |
| 本发明提供一类黏着斑激酶(FAK)抑制剂的改良合成方法，其中减少了昂贵的钯基催化剂的使用，并提高了反应产率和产品的纯度。对芳基卤化物和苯胺的偶联的两个关键反应进行了优化，出人意料的发现在所述反应之一中可以完全不使用所述钯基催化剂。本发明也提供了使用所述FAK抑制性化合物治疗炎症、免疫疾病和关节炎的方法。 | ||||||
| 3 | Acetylenic alpha-amino acid-based sulfonamide hydroxamic acid tace inhibitors | US10376871 | 2003-02-27 | US20030212049A1 | 2003-11-13 | Jeremy I. Levin; James Ming Chen; Derek C. Cole; Mila T. Du; Leif M. Laakso |
| Compounds of the formula: 1 are useful in treating disease conditions mediated by TNF-null, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss. | ||||||
| 4 | Acetylenic alpha -amino acid-based sulfonamide hydroxamic acid tace inhibitors | US09748912 | 2000-12-27 | US20030008849A1 | 2003-01-09 | Jeremy I. Levin; James M. Chen; Derek C. Cole; Mila T. Du; Leif M. Laakso |
| Compounds of the formula: 1 are useful in treating disease conditions mediated by TNF-null, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss. | ||||||
| 5 | Imidazo-heterocyclic compounds and pharmaceutical composition comprising the same | US583609 | 1984-02-27 | US4621084A | 1986-11-04 | Takao Takaya; Hisashi Takasugi |
| New imidazo-heterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or halogen,R.sup.2 is hydrogen, lower alkyl, halogen, aminomethyl optionally substituted with lower alkyl, or piperazin-1-yl-methyl optionally substituted with lower alkyl,R.sup.3 is a partially suturated heterocyclic group selected from benzothiazolinyl, benzoxazolinyl, benzimidazolinyl, 3,4-dihydro-2H-1,4-benzothiazinyl, 3,4-dihydro-2H-1,4-benzoxazinyl and 1,2,3,4-tetrahydroquinoxalinyl, which is substituted with oxo, thioxo, imino or lower alkylimino, and which may be substituted with lower alkyl optionally substituted with lower alkanoyloxy, lower alkoxycarbonyl, pyridyl or lower alkylamino; or an unsaturated heterocyclic group selected from benzoxazolyl and benzimidazolyl, which may be substituted with lower alkyl or pyridyl(lower)alkylthio, andY is .dbd.N-- or a group of the formula: ##STR2## in which R.sup.4 is hydrogen, hydroxy, lower alkyl, lower alkoxy or ar(lower)alkoxy,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and pharmaceutically acceptable salts thereof are useful as cardiotonic agents and untiulcer agents. | ||||||
| 6 | Method of preparing haloiminium salts | US30393663 | 1963-08-22 | US3282924A | 1966-11-01 | ALT GERHARD H; JOHN SPEZIALE ANGELO |
| 7 | 2-aroylmethyl-3-oxo-3,4-dihydro - 1,4,2-benzothiazines and their preparation | US59248356 | 1956-06-20 | US2894946A | 1959-07-14 | KIRCHNER FREDERICK K |
| 8 | A method of treating a tricyclic compound and herpes virus | JP2001551861 | 2000-11-30 | JP2003519693A | 2003-06-24 | ジョスユラ，ヴァラ・プラサド・ヴェンカタ・ナゲンドラ; スタインボーグ，ブルース・アラン; ブース，リチャード・ジョン; メイアー，アネッテ・リン |
| (57)【要約】 本発明は、ヘルペス科のウイルスに対する有用な抗ウイルス活性を有する、式（Ｉ）の化合物とその薬学的に許容される塩を提供する。 前記の式で、Ｘは、Ｏ、（ＣＨ 2 ） m 、Ｓ、ＳＯ、ＳＯ 2 、ＮＨ、ＮＲ 8又は化学結合であり；Ｙは、Ｏ、（ＣＨ 2 ） m 、Ｓ、ＳＯ、ＳＯ 2 、ＮＨ、ＮＲ 8であり；Ｚは、Ｎ、ＮＨ、Ｏ、ＮＨＲ 8 、ＮＲ 8 、Ｓ、ＳＯ、ＳＯ 2である。 残りの置換基は本明細書に記載される。 【化１】 | ||||||
| 9 | JPH0557989B2 - | JP3507284 | 1984-02-24 | JPH0557989B2 | 1993-08-25 | TAKATANI TAKAO; TAKASUGI HISASHI |
| 10 | 3-aryl - pyrrolidine-2,4-dione derivatives | JP22544290 | 1990-08-29 | JP3154715B2 | 2001-04-09 | アルブレヒト・マルホルト; アンドレアス・クレプス; クラウス・リユルセン; クリストフ・エルデレン; ハンス‐ヨアヒム・ザンテル; ビルヘルム・シユテンデル; ベネデイクト・ベツカー; ヘルマン・ハーゲマン; ライナー・フイツシヤー; ロベルト・アール・シユミツト |
| 11 | 3-aryl-pyrrolidine-2,4-dione derivative | JP22544290 | 1990-08-29 | JPH0393785A | 1991-04-18 | RAINAA FUITSUSHIYAA; HERUMAN HAAGEMAN; ANDOREASU KUREPUSU; ARUBUREHITO MARUHORUTO; HANSUUYOAHIMU ZANTERU; ROBERUTO AARU SHIYUMITSUTO; KURAUSU RIYURUSEN; BENEDEIKUTO BETSUKAA; BIRUHERUMU SHIYUTENDERU; KURISUTOFU ERUDEREN |
| NEW MATERIAL: A compound of formula I {-A-B- is -S-CH 2-, -SO-CH 2-, -SO 2-CH 2, -CH 2-S, -CH 2-SO-, -S-, -SO-, etc.; X is an alkyl, halogen or alkoxy; Y is H, an alkyl, a halogen, an alkoxy, etc.; Z is an alkyl, halogen or alkoxy; n is 0-3; R is H, E (E is a metal cation equiv. or ammonium ion), -CO-R 1 [R 1 is a (substituted) alkyl, (substituted) phenyl, etc.], etc.}. EXAMPLE: A compound of formula II. USE: Insecticides, acaricides and herbicides. PROCESS: An N-acylamino acid ester of formula III (R 3 is an alkyl) is subjected to intramolecular condensation in the presence of a diluent and a base to give a compound of formula I when R is H. COPYRIGHT: (C)1991,JPO | ||||||
| 12 | Filamin a binding anti-inflammatory and analgesic | EP15156157.8 | 2009-10-30 | EP2918587A2 | 2015-09-16 | Burns Barbier, Lindsay; Wang, Hoau-Yan; Lin, Nan-Horng; Blasko, Andrei |
A compound or its pharmaceutically acceptable salt, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula II, wherein the R group substituents, D, F, X, W and A are defined within.
|
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| 13 | SYNTHESIS AND USE OF KINASE INHIBITORS | EP11810100 | 2011-06-28 | EP2588476A4 | 2014-07-23 | LEI YIXIONG; BEHRENS CARL HENRY; LI HUI-YIN; SUN CONNIE L |
| 14 | TRICYCLIC COMPOUNDS WITH ANTIVIRAL ACTIVITY | EP00980882.5 | 2000-11-30 | EP1248777A2 | 2002-10-16 | BOOTH, Richard, John; JOSYULA, Vara, Prasad, Venkata, Nagendra; MEYER, Annette, Lynn; STEINBAUGH, Bruce, Allan |
| The present invention provides a compound of the formula (I) and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. In said formula, X = O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Y = O, (CH2)m, S, SO, SO2, NH, NR8; Z = NH, O, NR8, S, SO, SO2. The remaining substituents are described in the specification. | ||||||
| 15 | 3-Aryl-pyrrolidin-2,4-dion-derivate | EP90115872.5 | 1990-08-18 | EP0415211B1 | 1994-12-21 | Fischer, Reiner, Dr.; Hagemann, Hermann, Dr.; Krebs, Andreas, Dr.; Marhold, Albrecht, Dr.; Santel, Hans-Joachim, Dr.; Schmidt, Robert-R., Dr.; Lürssen, Klaus, Dr.; Becker, Benedikt, Dr.; Stendel, Wilhelm, Dr.; Erdelen, Christoph, Dr. |
| 16 | Imidazo-heterocyclic compounds, processes for preparation thereof and pharmaceutical composition comprising the same | EP84301058.8 | 1984-02-17 | EP0120589B1 | 1988-06-08 | Takaya, Takao; Takasugi, Hisashi |
| 17 | キナーゼインヒビターの合成および使用 | JP2013518575 | 2011-06-28 | JP5923499B2 | 2016-05-24 | レイ, イーション; ベーレンス, カール ヘンリー; リー, フイ−イン; サン, コニー エル. |
| 18 | The synthesis and use of kinase inhibitors | JP2013518575 | 2011-06-28 | JP2013529687A | 2013-07-22 | イーション レイ，; カール ヘンリー ベーレンス，; フイ−イン リー，; コニー エル． サン， |
| 接着斑キナーゼ（ＦＡＫ）のクラスのインヒビターの改善された合成が提供され、ここで高価なパラジウムベースの触媒の使用は低減され、反応収率および生成物純度は改善される。 ハロゲン化アリールとアニリンとのカップリングの２つの重要な反応は、パラジウムベースの触媒が反応のうちの１つにおいて完全に不要とされ得るという驚くべき発見により最適化される。 本発明はまた、炎症性障害および免疫障害、ならびに関節炎の処置におけるＦＡＫ阻害化合物の使用を提供する。 | ||||||
| 19 | Heterocycle-containing compound and its application | JP2006141219 | 2006-05-22 | JP2007308441A | 2007-11-29 | SHIRAKI HIROAKI; AZUMA SEISHI; TOMIGAHARA YOSHITAKA; TAKAHASHI JUNYA |
| <P>PROBLEM TO BE SOLVED: To develop and provide a composition that improves tissue fibrosis (namely, an extracellular matrix accumulation inhibitor, a fibrosis-treating agent or a heart failure-treating agent) or the like by decreasing an expression level of an extracellular matrix gene in a tissue thereby lowering the accumulation amount of an extracellular matrix. <P>SOLUTION: The extracellular matrix gene transcription-inhibiting composition comprises a heterocycle-containing compound represented by formula (I) and an inactive carrier. <P>COPYRIGHT: (C)2008,JPO&INPIT | ||||||
| 20 | Imidazo-heterocyclic compound | JP3507284 | 1984-02-24 | JPS59186983A | 1984-10-23 | TAKATANI TAKAO; TAKASUGI HISASHI |
| NEW MATERIAL:The imidazo-heterocyclic compound of formula I [R 1 is H, lower alkyl or halogen; R 2 is R 1, or aminomethyl or piperazin-1-ylmethyl each of which may be substituted with lower alkyl; R 3 is benzothiazolinyl, benzoxazolinyl, etc.; Y is N cr CR 4 (R 4 is H, OH, lower alkyl, etc.)] and its salt. EXAMPLE: 5-[3-( 4-Methylpiperazin-1-ylmethyl )imidazo[1,2-a]pyridin-2-yl]-3-methyl- 2-benzothiazolinone. USE: Cardiotonic agent and antiulcer agent. PREPARATION: The compound of formula I a can be prepared by reacting the compound of formula II or its salt with the compound of formula III in a solvent such as water, methanol, THF, etc. in the presence of an alkali metal hydride, alkali metal carbonate, etc. COPYRIGHT: (C)1984,JPO&Japio | ||||||
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