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 JPH0565515B2 - JP10698082 1982-06-23 JPH0565515B2 1993-09-17 MAIKERU TOOMASU KURAAKU; IAN JEIMUZU GIRUMOA
2 Rifamycin analog and methods of use thereof JP2006543971 2004-12-09 JP2007513961A 2007-05-31 ウィリアム ビー. ガイス; ジェームス エム. シエドレキ; ダグラス ジー. スタッフォード; ドゥーザー ジョーン エイチ. バン; アーサー エフ. マイケリス; イグフェイ ヤン; シャン ワイ. ユ
本発明は、種々の細菌感染症を治療または予防するための治療薬として使用することができるリファマイシンアナログを特徴とする。 一形態において、アナログは、リファマイシン同様に、25位がアセチル化されている。 別の形態において、アナログは25位が脱アセチル化されている。 さらに他の形態において、ベンゾキサジノリファマイシン、ベンズチアジノリファマイシンおよびベンズジアジノリファマイシンアナログは、3'-ヒドロキシアナログを含むベンゼン環、および/または4'、5' 位、または4'、6' 位においてベンゼン環を有する様々な融合環系の種々の位置が誘導体化されている。
3 Herbicidal composition containing heterocyclic pentalene JP10698082 1982-06-23 JPS58987A 1983-01-06 CLARK MICHAEL THOMAS; GILMORE IAN JAMES
4 Herbicidal heterocyclic pentalenes US418370 1982-09-15 US4441911A 1984-04-10 Michael T. Clark; Ian J. Gilmore
Herbicidal heterocyclic pentalenes of the formula: ##STR1## wherein the symbols have assigned meanings.
5 Macrocyclic indole derivatives useful as hepatitis C virus inhibitors US13000583 2009-07-08 US08921355B2 2014-12-30 Sandrine Marie Helene Vendeville; Pierre Jean-Marie Bernard Raboisson; Tse-I Lin; Abdellah Tahri; Katie Ingrid Eduard Amssoms
Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
6 Rifamycin analogs and uses thereof US11008597 2004-12-09 US20050137189A1 2005-06-23 John van Duzer; Arthur Michaelis; William Geiss; Douglas Stafford; Xiang Yu; James Siedlecki; Yingfei Yang
The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
7 Preparation of 1H-imidazo [4,5-C] quinolin-4-amines via 1H-imidazo [4,5-C] quinolin-4-phthalimide intermediates US10626036 2003-07-23 US06852861B2 2005-02-08 Valeriano Merli; Silvia Mantovani; Stefano Bianchi
The invention provides 1H-imidazo(4,5-C)quinolin-4-phthalimide intermediates useful in the synthesis of 1H-imidazo(4,5-C)quinoline-4-amines, particularly Imiquimod. The invention further provides a method for making the intermediates and a method for making 1H-imidazo(4,5-C)quinoline-4-amines via the intermediates.
8 Imidazoindolizine derivatives process for preparation thereof and use thereof to treat hypertension US939652 1992-09-03 US5268377A 1993-12-07 Yasushi Honma; Yasuo Sekine; Sumihiro Nomura; Kazuaki Naito; Hiroshi Narita
An inidazoindolizine derivative of the formula [I]: ##STR1## wherein R.sup.1 is lower alkyl, R.sup.2 is hydrogen, cyano, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, phenyl-lower alkoxycarbonyl, lower alkylsulfonyl, substituted or unsubstituted phenyl, arylcarbonyl, or 5- or 6-membered nitrogen-containing heteromonocyclic group-substituted carbonyl, Ring A is substituted or unsubstituted phenyl, and m is 0 or 1, or a pharmaceutically acceptable salt thereof, and process for preparation thereof, said imidazoindolizine derivatives and pharmaceutically acceptable salts thereof show excellent angiotensin II inhibitory activities and are useful in the prophylaxis or treatment of hypertension.
9 Aryl sultam derivatives as RORc modulators US13939962 2013-07-11 US09115101B2 2015-08-25 Monique Bodil van Niel; Benjamin Fauber; Simon Gaines; Alberto Gobbi; Olivier Rene; David Vesey; Stuart Ward
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
10 Tricyclic Benzopyrane Compound as Anti-Arrhythmic Agents US10590975 2005-03-23 US20080004262A1 2008-01-03 Kazuhiko Ohrai; Yukohiro Shigeta; Osamu Uesugi; Takumi Okada; Tomoyuki Matsuda
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
11 Heterocyclic pentalenes as herbicides US418369 1982-09-15 US4440564A 1984-04-03 Michael T. Clark; Ian J. Gilmore
Use as herbicides of, and herbicidal compositions containing as active ingredients, compounds of the formula: ##STR1## wherein the symbols have assigned meanings.
12 RIFAMYCIN ANALOGS AND USES THEREOF EP04813534 2004-12-09 EP1697382A4 2008-11-05 VAN DUZER JOHN H; MICHAELIS ARTHUR F; GEISS WILLIAM B; STAFFORD DOUGLAS G; YU XIANG Y; SIEDLECKI JAMES M; YANG YINGFEI
13 RIFAMYCIN ANALOGS AND USES THEREOF PCT/US2004041222 2004-12-09 WO2005058231A3 2005-12-22 VAN DUZER JOHN H; MICHAELIS ARTHUR F; GEISS WILLIAM B; STAFFORD DOUGLAS G; YU XIANG Y; SIEDLECKI JAMES M; YANG YINGFEI
The present invention features rifamycin analogs that can be used as therapeutics for treatics or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3'- hydrxyl analogs, and/or various fused ring systems with the benzene ring at the 4', 5' or 5', 6' positions.
14 마크로시클릭 인테그라제 억제제 KR1020127009345 2010-10-13 KR1020120087916A 2012-08-07 투링,조한네스,윌헬무스,제이.; 본판티,쟌-프랑수아; 포틴,제롬,미첼,클라우드
화학식 I의 화합물 및 그의 제약상 허용되는 염, 그의 제약 제제 및 HIV 억제제로서의 용도.
<화학식 I>

상기 식에서,
- W는 NH-, -N(CH 3 )- 또는 피페라진이고,
- X는 결합, -C(=O)- 또는 S(=O) 2 -이고,
- Y는 C 3 - 7 알킬렌이고,
- Z는 NH-C(=O)- 또는 -O-이다.
15 IMIDAZOIDOLIZINE DERIVATIVES AND PROCESS FOR PREPARATION THEREOF. MYPI9201597 1992-09-07 MY129927A 2007-05-31 HONMA YASUSHI; SEKINE YASUO; NOMURA SUMIHIRO; NAITO KAZUAKI; NARITA HIROSHI
AN IMIDAZOINDOLIZINE DERIVATIVE OF THE FORMULA [I]: WHEREIN RL IS LOWER ALKYL, R2 IS HYDROGEN, CYANO, LOWER ALKYL, LOWER ALKANOYL, LOWER ALKOXYCARBONYL, PHENYL-LOWER ALKOXYCARBONYL, LOWER ALKYLSULFONYL, SUBSTITUTED OR UNSUBSTITUTED PHENYL, ARYLCARBONYL, OR 5- OR 6-MEMBERED NITROGEN-CONTAINING HETEROMONOCYCLIC GROUP-SUBSTITUTED CARBONYL, RING A IS SUBSTITUTED OR UNSUBSTITUTED PHENYL, AND M IS 0 OR 1, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PROCESS FOR PREPARATION THEREOF, SAID IMIDAZOINDOLIZINE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF SHOW EXCELLENT ANGIOTENSIN II INHIBITORY ACTIVITIES AND ARE USEFUL IN THE PROPHYLAXIS OR TREATMENT OF HYPERTENSION.
16 DIBENZO-AZEPINE DERIVATIVES AS .ALPHA.V INTEGRIN RECEPTOR ANTAGONISTS CA2362334 2000-02-14 CA2362334A1 2000-08-24 PATANE MICHAEL A; NEWTON RANDALL C
The present invention relates to dibenzo-azepine derivatives and their use a s alphaV integrin receptor antagonists. More particularly, the compounds of th e present invention are antagonists of the integrin receptors alphaVbeta3, alphaVbeta5, and/or alphaVbeta6 and are useful for inhibiting bone resorptio n, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
17 PREPARATION OF N-OXO-TETRAHYDRO-ß-CARBOLINES IE199690 1990-06-05 IE901996L 1990-12-08
18 Herbicide preparations oxa- or dioxa-heterodiaza-2,5-pentalener for use in the preparation, procedure for the control of undesirable plant growth DK282982 1982-06-23 DK159130B 1990-09-10 CLARK MICHAEL THOMAS; GILMORE IAN JAMES
19 HERBICIDAL COMPOSITIONS CONTAINING HETEROCYCLIC PENTALENES DE3277815 1982-06-14 DE3277815D1 1988-01-21 CLARK MICHAEL THOMAS; GILMORE IAN JAMES
20 ANTIMICROBIC PREPARATIVES CONTAINING HETEROCYCLIC DERIVATIVES OF PENTALENE AND PROCESS FOR PRODUCTION THEREOF HU294786 1986-07-17 HUT42919A 1987-09-28 TURNER SUSAN J; CLARK MICHAEL T
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