| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 101 | PROCESS FOR PREPARING A POTENT THIAZOLE COMPOUND, PHARMACEUTICAL FORMULATION AND USES THEREOF | EP19793762.6 | 2019-04-26 | EP3799593A1 | 2021-04-07 | GANJU, Parul; PRASAD, Sudhanand; VERMA, Mahesh, Kumar; KOMIRISHETTY, Kashinath; RICHHARIA, Annie |
| The present invention relates to a process for preparing N-[2-[2-(4-chlorophenyl)-4- thiazolyl] ethyl]-butanamide. The present invention further relates to a pharmaceutical formulation and the use of said pharmaceutical formulation consisting of N-[2-[2-(4-chlorophenyl)-4-thiazolyl] ethyl]-butanamide or pharmaceutically acceptable salts thereof as active compound for the treatment and prevention of autoimmune diseases and diseases involving skin immunology, skin autoimmune diseases and pigmentation disorders. | ||||||
| 102 | DETERGENT COMPOSITIONS | EP14793278.4 | 2014-11-03 | EP3063146B1 | 2017-08-16 | GILES, Matthew Robert |
| A compound of formula (I): wherein R1 is a C5 to C39 alkyl or alkenyl group and R2 is selected from (a), (b) and (c): wherein one of W, X, Y and Z is a covalent bond and the remaining groups are independently selected from H, M, SO3M and P(O)R3R4 provided at least one of W, X, Y and Z is SO3M or P(O)R3R4; each M is independently a hydrogen ion, an ammonium ion or a metal ion; A is an anion; each of R3 and R4 is independently selected from OH, OM and OR5 wherein R5 may be a C1 to C39 hydrocarbyl group or the residue of a further compound of the present invention including an R2 group of formula (a). | ||||||
| 103 | ALPHA-KETOAMIDE MULTICATALYTIC PROTEASE INHIBITORS | EP98953274.2 | 1998-10-07 | EP1027056B1 | 2009-02-25 | CHATTERJEE, Sankar; MALLAMO, John, P. |
| This invention relates to α-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states. | ||||||
| 104 | NOVEL 4-ARYLPIPERAZINES AND 4-ARYLPIPERIDINES | EP92906123 | 1991-12-20 | EP0562049A4 | 1994-09-28 | REITZ ALAN B |
| Compounds of the general formula (I) are disclosed as novel antipsychotic agents. | ||||||
| 105 | Verfahren zur Herstellung von Pyrimidinderivaten | EP89108309.9 | 1989-05-09 | EP0342482B1 | 1994-08-03 | Hengartner, Urs, Dr.; Moine, Gérard, Dr. |
| 106 | Adduct of mutually stabilizing menadione and thiamine | EP83105975.3 | 1983-06-18 | EP0098995B1 | 1987-03-18 | Ghelli, Giovanni; Conti, Luciano; Barbon, Alessandro; Oliari, Luigi |
| 107 | PROCESS FOR PREPARING A POTENT THIAZOLE COMPOUND, PHARMACEUTICAL FORMULATION AND USES THEREOF | PCT/IB2019/053459 | 2019-04-26 | WO2019207548A4 | 2019-10-31 | GANJU, Parul; PRASAD, Sudhanand; VERMA, Mahesh, Kumar; KOMIRISHETTY, Kashinath; RICHHARIA, Annie |
The present invention relates to a process for preparing N-[2-[2-(4-chlorophenyl)-4- thiazolyl] ethyl]-butanamide. The present invention further relates to a pharmaceutical formulation and the use of said pharmaceutical formulation consisting of N-[2-[2-(4-chlorophenyl)-4-thiazolyl] ethyl]-butanamide or pharmaceutically acceptable salts thereof as active compound for the treatment and prevention of autoimmune diseases and diseases involving skin immunology, skin autoimmune diseases and pigmentation disorders. |
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| 108 | PROCESS FOR PREPARING A POTENT THIAZOLE COMPOUND, PHARMACEUTICAL FORMULATION AND USES THEREOF | PCT/IB2019/053459 | 2019-04-26 | WO2019207548A1 | 2019-10-31 | GANJU, Parul; PRASAD, Sudhanand; VERMA, Mahesh, Kumar; KOMIRISHETTY, Kashinath; RICHHARIA, Annie |
The present invention relates to a process for preparing N-[2-[2-(4-chlorophenyl)-4- thiazolyl] ethyl]-butanamide. The present invention further relates to a pharmaceutical formulation and the use of said pharmaceutical formulation consisting of N-[2-[2-(4-chlorophenyl)-4-thiazolyl] ethyl]-butanamide or pharmaceutically acceptable salts thereof as active compound for the treatment and prevention of autoimmune diseases and diseases involving skin immunology, skin autoimmune diseases and pigmentation disorders. |
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| 109 | 1,2,3-3H吡啶杂环化合物、其农用组合物、用途及制备方法 | PCT/CN2010/072232 | 2010-04-27 | WO2010124619A1 | 2010-11-04 | 李忠; 钱旭红; 张文文; 徐晓勇; 邵旭升; 陶黎明; 宋恭华 |
| 110 | RIBOSWITCHES | PCT/IB2009006607 | 2009-06-01 | WO2009144588A2 | 2009-12-03 | BAN NENAD; THORE STEPHANE |
| The TPP riboswitch is a target for antibiotics, herbicides, algicides, fungicides and other utilities. The atomic structure of the binding pocket of the TPP riboswitch has been resolved. Compounds identified and optimized using this information can be used to stimulate, activate, inhibit and/or inactivate the TPP riboswitch. | ||||||
| 111 | NITROSATED AND NITROSYLATED CARDIOVASCULAR COMPOUNDS, COMPOSITIONS AND METHODS OF USE | PCT/US2004026909 | 2004-08-20 | WO2005018561A2 | 2005-03-03 | GARVEY DAVID S; LETTS GORDON L; WORCEL MANUEL; GASTON RICKY D |
| The invention describes novel nitrosated and/or nitrosylated cardiovascular compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated cardiovascular compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at,least one cardiovascular compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; and (k) treating nephropathy. The nitrosated and/or nitrosylated cardiovascular compounds are preferably nitrosated and/or nitrosylated P-adrenergic antagonists, nitrosated and/or nitrosylated angiotensinconverting enzyme (ACE) inhibitors, nitrosated and/or nitrosylated anti-hyperlipidemic compounds, and nitrosated and/or nitrosylated antithrombotic and vasodilator compounds. | ||||||
| 112 | PROTEASE INHIBITORS | PCT/US0326358 | 2003-08-22 | WO2004017911A3 | 2004-07-01 | BONDINELL WILLIAM E; HALL RALPH F; JIN QI; KERNS JEFFREY K; NIE HONG; WIDDOWSON KATHERINE L |
| This invention relates 4-amino-azepan-3-ones of formula (1) which are useful as protease inhibitors, particularly of cathepsin S, and as such are useful for preventing a number of diseases amongst which are atherosclerotic lesions and pulmonary diseases such as asthma and allergic reactions. | ||||||
| 113 | POLYMORPHS OF DASATINIB | PCT/IN2008000822 | 2008-12-08 | WO2010067374A3 | 2011-05-26 | PARTHASARADHI REDDY BANDI; RATHNAKAR REDDY KURA; RAJI REDDY RAPOLU; MURALIDHARA REDDY DASARI; SRINIVASA ROA THUNGATHURTHY |
| The present invention provides a novel crystalline form I of dasatinib, process for its preparation and to pharmaceutical composition containing it. The present invention also provides dasatinib dimethylformamide solvate, dasatinib dimethyl sulfoxide solvate, dasatinib toluene solvate and dasatinib isopropyl acetate solvate, processes for its preparation. The present invention further provides a process for preparation of crystalline dasatinib monohydrate. | ||||||
| 114 | UREA SUBSTITUTED SULPHONAMIDE DERIVATIVES | PCT/FI2010/050495 | 2010-06-14 | WO2010146236A1 | 2010-12-23 | KORHONEN, Jani; MARJAMÄKI, Anne; NISSINEN, Liisa; PIHLAVISTO, Marjo |
The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially α2β1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I'). |
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| 115 | ヘテロ環スルホンアミド化合物を含有する医薬 | PCT/JP2010/057362 | 2010-04-26 | WO2010126002A1 | 2010-11-04 | 西冨 晃平; 鹿野 一也; 加藤 一生; 酒匂 佑介 |
アミロイドβタンパク質の産生、分泌または沈着により誘発される疾患の治療剤として、例えば以下の化合物（Ｉａ）を提供する。（式中、Ｘは－Ｏ－または－Ｓ－であり、環Ａはベンゼン環等であり、Ｒ１ａ、Ｒ２ａおよびＲ３ａは各々独立して水素、ハロゲン、置換もしくは非置換のアルコキシカルボニルまたは置換もしくは非置換の炭素環等であり、Ｒ４はハロゲン、ヒドロキシまたは置換もしくは非置換のアルキル等であり、Ｒ５ａは置換もしくは非置換の５員もしくは６員の不飽和へテロ環式基またはＣ（＝Ｏ）Ｒ６等であり、ｐは０～２の整数であり、Ｒ６はヒドロキシまたは置換もしくは非置換のアルコキシ等であり、Ｌａは－ＳＯ２ＮＨ－または－Ｃ（＝Ｏ）ＮＨ－等であり、Ａｋ１およびＡｋ２は各々独立して単結合等である。） で示される化合物、もしくはその製薬上許容される塩またはそれらの溶媒和物。 |
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| 116 | POLYMORPHS OF DASATINIB | PCT/IN2008/000822 | 2008-12-08 | WO2010067374A2 | 2010-06-17 | PARTHASARADHI REDDY, Bandi; RATHNAKAR REDDY, Kura; RAJI REDDY, Rapolu; MURALIDHARA REDDY, Dasari; SRINIVASA ROA, Thungathurthy |
The present invention provides a novel crystalline form I of dasatinib, process for its preparation and to pharmaceutical composition containing it. The present invention also provides dasatinib dimethylformamide solvate, dasatinib dimethyl sulfoxide solvate, dasatinib toluene solvate and dasatinib isopropyl acetate solvate, processes for its preparation. The present invention further provides a process for preparation of crystalline dasatinib monohydrate. |
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| 117 | OXIMYL HCV SERINE PROTEASE INHIBITORS | PCT/US2008/085524 | 2008-12-04 | WO2009076166A2 | 2009-06-18 | GAI, Yonghua; OR, Yat, Sun; WANG, Zhe |
The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: Formula (I) which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. |
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| 118 | PROTEASE INHIBITORS | PCT/US2001/019062 | 2001-06-14 | WO01095911A1 | 2001-12-20 | |
| The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention. | ||||||
| 119 | 치환된 4-아미노-피리미딘의 신규한 합성 방법 | KR1020117003956 | 2009-07-22 | KR101675604B1 | 2016-11-11 | 카르게라인하르트; 레티노이스울라; 쉬에페르게르하르트 |
| 본발명은 a) 하기화학식 Ia의화합물을용매중의화학식 NHX(여기서, X는음이온, 바람직하게는클로라이드, 브로마이드, 설페이트및 아세테이트로구성된군에서선택되는음이온이다)의암모늄염과반응시켜하기화학식 II의화합물을수득하는단계;b) 염기의존재하에서하기화학식 II의화합물을화학식 R-CN의니트릴과반응시켜하기화학식 IV의화합물을수득하는단계를포함하는, 하기화학식 IV의화합물의제조방법에관한것이다:화학식 IV화학식 Ia화학식 II상기식에서,R은아미노보호기이고,R는수소또는 C알킬이고,M는양이온, 바람직하게는 Li, Na, K, 1/2Mg및 1/2Zn로구성된군에서선택되는양이온이다. 본발명은또한화학식 II의화합물및 비타민 B의제조를위한이의용도에관한것이다. | ||||||
| 120 | ＢＡＣＥ 억제제로서의 이미노티아디아진 디옥시드 화합물, 조성물, 및 그의 용도 | KR1020127011742 | 2010-10-06 | KR101435301B1 | 2014-08-27 | 스콧,잭,디.; 스탬포드,앤드류,더블유.; 길버트,에릭,제이.; 커밍,제러드,엔.; 아이설로,울리치; 미시아스제크,제프리,에이.; 리,구오큉 |
| 본 발명의 다수의 실시양태에서, 본 발명은 화학식 I의 화합물을 포함하는 특정한 이미노티아디아진 디옥시드 화합물을 제공하고, 그의 입체이성질체, 및 상기 화합물 및 입체이성질체의 제약상 허용되는 염을 포함한다.
<화학식 I> 상기 식에서, 각각의 R 1 , R 2 , R 3 , R 4 , R 5 , R 9 , 고리 A, 고리 B, m, n, p, -L 1 -, L 2 - 및 L 3 -은 독립적으로 선택되며, 본원에 정의된 바와 같다. 본 발명의 신규 이미노티아디아진 디옥시드 화합물은 놀랍게도 그를 BACE 억제제로서 및/또는 β-아밀로이드 (Aβ) 생산과 관련된 다양한 병리상태의 치료 또는 예방을 위해 유리하게 하는 것으로 예상되는 특성을 나타내는 것으로 밝혀졌다. 하나 이상의 이러한 화합물을 포함하는 (단독으로 및 하나 이상의 다른 활성제와 조합하여) 제약 조성물, 및 그의 제조 방법 및 알츠하이머병을 비롯한 아밀로이드 베타 (Aβ) 단백질과 관련된 병리상태의 치료의 용도가 또한 개시되어 있다. |
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