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1. 发明申请

WO2006078995A1 CARDIOVASCULAR COMPOUNDS COMPRISING HETEROCYCLIC NITRIC OXIDE DONOR GROUP COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：包含杂环氧化物二氧化碳基团组合物的心血管化合物及其使用方法
公开(公告)号：WO2006078995A1
公开(公告)日：2006-07-27
申请号：PCT/US2006/002199
申请日：2006-01-23
申请人： NITROMED, INC. , GARVEY, David, S.
发明人： GARVEY, David, S.
IPC分类号： C07D271/08
CPC分类号： C07D285/10 , C07C217/30 , C07C233/30 , C07C233/65 , C07C255/54 , C07C275/34 , C07D207/16 , C07D209/08 , C07D209/16 , C07D209/52 , C07D209/88 , C07D217/26 , C07D223/16 , C07D233/38 , C07D271/08 , C07D273/00 , C07D281/06 , C07D311/18 , C07D413/12 , C07D413/14 , C07D487/04 , C07D495/10
摘要： The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing 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; (k) treating nephropathy; (1) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably β-adrenergic antagonists, angiotensin- converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds. The heterocyclic nitric oxide donor groups are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.
摘要翻译：本发明描述了包含至少一种包含至少一种杂环一氧化氮供体基团的心血管化合物和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂的组合物和试剂盒。本发明还提供了（a）治疗心血管疾病的方法; （b）治疗血管性疾病; （c）治疗糖尿病; （d）治疗由氧化应激引起的疾病; （e）治疗内皮功能障碍; （f）治疗由内皮功能障碍引起的疾病; （g）治疗肝硬化; （h）治疗先兆子痫; （j）治疗骨质疏松症; （k）治疗肾病; （1）治疗外周血管疾病; （m）治疗门静脉高压和（n）治疗眼科疾病。心血管化合物优选是β-肾上腺素能拮抗剂，血管紧张素转换酶（ACE）抑制剂，抗高脂血症化合物和抗血栓形成和血管扩张剂化合物。杂环一氧化氮供体基团优选为呋喃糖，苏氨酸，氧杂三唑-5-酮和/或氧杂三唑-5-亚胺。

2. 发明申请

WO2003018019A2 NEW USE OF CYCLIC COMPOUND 审中-公开
标题翻译：循环化合物的新用途
公开(公告)号：WO2003018019A2
公开(公告)日：2003-03-06
申请号：PCT/JP2002/008443
申请日：2002-08-21
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , OKU, Takuma , HIRAYAMA, Yoshitaka , YAMAGAMI, Kaoru , OHKUBO, Yoshitaka , MATSUOKA, Hideaki
发明人： OKU, Takuma , HIRAYAMA, Yoshitaka , YAMAGAMI, Kaoru , OHKUBO, Yoshitaka , MATSUOKA, Hideaki
IPC分类号： A61K31/495
CPC分类号： C07D417/14 , A61K31/495 , C07D281/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： An agent comprising a compound of Formula (I-a) and the like, or a salt thereof, use of a compound of Formula (I-a) and the like, or a salt thereof for the manufacture of a medicament, or a method comprising administering a compound of Formula (I-a) and the like, or a salt thereof, for the treatment of Inflammatory respiratory disease in which: A a is a sulfonyl or a carbonyl; R 1a is an optionally substituted aryl, etc; R 2a is a hydrogen, etc; R 3a is an optionally substituted lower alkyl, etc; R 4a is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R 5a is a hydrogen, etc; and R 6a is a hydroxy or a protected hydroxy.
摘要翻译：包含式（Ia）等化合物或其盐的试剂，式（Ia）化合物或其盐或其盐在制备药物中的用途，或包括给予化合物的式（Ia）等或其盐用于治疗炎症性呼吸道疾病，其中：A a是磺酰基或羰基; R 1a是任选取代的芳基等; R 2a是氢等; R 3a是任选取代的低级烷基等; R 4a是氢，任选取代的低级烷基，任选取代的芳基或任选取代的杂环基; R 5a是氢等; R 6a是羟基或保护的羟基。

3. 发明申请

WO0044709A3 ACETYLENIC alpha -AMINO ACID-BASED SULFONAMIDE HYDROXAMIC ACID TACE INHIBITORS 审中-公开
标题翻译：乙炔基α-氨基酸磺酰胺羟基酸酸缓蚀剂
公开(公告)号：WO0044709A3
公开(公告)日：2000-12-21
申请号：PCT/US0001981
申请日：2000-01-27
申请人： AMERICAN CYANAMID CO
发明人： LEVIN JEREMY IAN , CHEN JAMES MING , COLE DEREK CECIL
IPC分类号： A61K31/18 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/4164 , A61K31/4184 , A61K31/42 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/4468 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/54 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/554 , A61P1/00 , A61P3/10 , A61P7/00 , A61P9/04 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/18 , A61P37/06 , A61P43/00 , C07C303/40 , C07C309/42 , C07C309/87 , C07C311/29 , C07C311/39 , C07C311/44 , C07C311/47 , C07C311/64 , C07C319/20 , C07C323/60 , C07D207/12 , C07D207/16 , C07D207/26 , C07D207/27 , C07D209/20 , C07D211/66 , C07D213/32 , C07D213/42 , C07D213/70 , C07D213/71 , C07D213/76 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/60 , C07D235/06 , C07D235/08 , C07D241/04 , C07D243/08 , C07D261/10 , C07D261/18 , C07D265/30 , C07D277/06 , C07D277/24 , C07D279/12 , C07D279/14 , C07D279/16 , C07D281/06 , C07D295/08 , C07D295/092 , C07D295/125 , C07D295/13 , C07D333/40 , C07D401/06 , C07D409/06 , C07D513/10 , C07D521/00
CPC分类号： C07D207/27 , C07C311/29 , C07C311/39 , C07C311/47 , C07C311/64 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/16 , C07D209/20 , C07D211/66 , C07D213/32 , C07D213/42 , C07D213/70 , C07D213/71 , C07D213/81 , C07D213/82 , C07D215/48 , C07D217/26 , C07D231/12 , C07D233/56 , C07D235/06 , C07D241/04 , C07D243/08 , C07D249/08 , C07D261/18 , C07D265/30 , C07D277/06 , C07D277/24 , C07D279/12 , C07D279/14 , C07D279/16 , C07D281/06 , C07D295/088 , C07D295/125 , C07D295/13 , C07D401/06 , C07D409/06 , C07D513/10
摘要： Compound of the formula (B) are useful in treating disease conditions mediated by TNF- alpha , such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：式（B）化合物可用于治疗由TNF-α介导的疾病，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化症，克罗恩氏病和退行性软骨损失。

4. 发明申请

WO00050396A1 AROMATIC SULFONE HYDROXAMIC ACID METALLOPROTEASE INHIBITOR 审中-公开
标题翻译：芳香磺化羟基酸金属蛋白酶抑制剂
公开(公告)号：WO00050396A1
公开(公告)日：2000-08-31
申请号：PCT/US2000/002518
申请日：2000-02-22
IPC分类号： A61K31/382 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , C07D211/08 , C07D215/38 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/10 , C07D409/14 , C07D451/02 , C07D491/20 , C07D211/66 , C07C317/44 , C07D211/94 , A61K31/35 , A61K31/16 , C07D239/04 , C07D309/08 , C07D335/02 , C07D409/12 , C07D417/12
CPC分类号： C07D451/02 , A61K31/445 , C07D207/16 , C07D211/66 , C07D211/78 , C07D221/22 , C07D221/24 , C07D225/02 , C07D239/04 , C07D239/10 , C07D239/14 , C07D239/22 , C07D263/06 , C07D265/30 , C07D277/06 , C07D279/06 , C07D281/06 , C07D285/16 , C07D307/24 , C07D309/08 , C07D319/06 , C07D327/02 , C07D333/38 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , Y02A50/411
摘要： A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
摘要翻译：公开了一种治疗方法，其包括施用有效量的一种或多种基质金属蛋白酶（MMP）酶如MMP-2，MMP-9和MMP-13的优异抑制活性的芳香族砜异羟肟酸，同时基本上至少具有MMP-1对具有与病理基质金属蛋白酶活性相关的病症的宿主的抑制作用较小。还公开了具有这些选择活性的金属蛋白酶抑制剂化合物，制备这种化合物的方法和使用抑制剂的药物组合物。

5. 发明申请

WO1994008977A1 SUBSTITUTED CAPROLACTAMS AND DERIVATIVES THEREOF USEFUL FOR TREATMENT OF AIDS 审中-公开
标题翻译：替代性CAPROLACTATA及其有效治疗艾滋病的衍生物
公开(公告)号：WO1994008977A1
公开(公告)日：1994-04-28
申请号：PCT/US1993009807
申请日：1993-10-20
申请人： THE DU PONT MERCK PHARMACEUTICAL COMPANY
发明人： THE DU PONT MERCK PHARMACEUTICAL COMPANY , HODGE, Carl, Nicholas , FERNANDEZ, Christina, Howard
IPC分类号： C07D243/08
CPC分类号： C07D281/06 , C07D243/08 , C07D245/02 , C07D255/02 , C07D257/02 , C07D267/10
摘要： This invention relates to novel substituted caprolactams of formula (I), including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pharmaceutical compositions containing such substituted caprolactams and to methods of using such caprolactams for the treatment of HIV disease.
摘要翻译：本发明涉及抑制HIV蛋白酶并可用于治疗HIV疾病的式（I）的新型取代己内酰胺，包括4-氮杂己内酰胺及其衍生物。本发明还包括含有这种取代的己内酰胺的药物组合物以及使用这些己内酰胺来治疗HIV疾病的方法。

6. 发明申请

WO2012063085A3 DRUG DERIVATIVES 审中-公开
标题翻译：药物衍生物
公开(公告)号：WO2012063085A3
公开(公告)日：2012-08-02
申请号：PCT/GB2011052211
申请日：2011-11-11
申请人： REDX PHARMA LTD , CRAIGHEAD MARK , PALIN RONALD , MURRAY NEIL , LINDSAY DEREK
发明人： CRAIGHEAD MARK , PALIN RONALD , MURRAY NEIL , LINDSAY DEREK
IPC分类号： C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12
CPC分类号： C07D487/04 , C07C43/205 , C07C57/00 , C07C63/64 , C07C63/66 , C07C69/12 , C07C215/46 , C07C217/58 , C07C229/18 , C07C233/22 , C07C233/36 , C07C235/16 , C07C235/28 , C07C237/20 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/58 , C07C255/25 , C07C257/14 , C07C2601/16 , C07C2602/10 , C07C2603/74 , C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D407/06 , C07D411/10 , C07D413/04 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , C07D498/06 , C07D499/88 , C07D501/00 , C07D513/06 , C07D519/00 , C07H19/052 , C07H19/06 , C07H19/173 , C07J5/00 , C07J71/0031
摘要： The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
摘要翻译：本发明涉及已知的活性药物化合物的衍生物。由于活性化合物的氧化还原衍生物，这些衍生物与母体活性化合物不同。这意味着活性化合物中的一个或多个官能团已经在一个或多个反应中被转化为另一个基团，这可被认为代表氧化态的变化。我们通常将这些化合物称为氧化还原衍生物。本发明的衍生物可以仅通过单步转化与原始的母体活性药物化合物相关，或者可以通过包括氧化态的一个或多个变化的几个合成步骤相关。在某些情况下，两次或多次转化后获得的官能团可能与母体活性化合物处于相同的氧化态（我们在我们的氧化还原衍生物定义中包括这些化合物）。在其他情况下，本发明衍生物的氧化态可认为与母体化合物的氧化态不同。在许多情况下，本发明的化合物本身具有固有的治疗活性。在某些情况下，相对于母体化合物的相同靶标或靶标的此活性与母体化合物对靶点或靶标的活性相同或更好。

7. 发明申请

WO2007104933A8 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2007104933A8
公开(公告)日：2008-09-18
申请号：PCT/GB2007000813
申请日：2007-03-09
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , HUDSON KEVIN , LAING NAOMI , LEWIS PAULA
发明人： HUDSON KEVIN , LAING NAOMI , LEWIS PAULA
IPC分类号： A61K31/55 , A61K31/553 , A61K31/554 , A61P25/28 , A61P31/00 , A61P35/00 , A61P43/00 , C07D223/16 , C07D267/10 , C07D267/14 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/12 , C07D417/14
CPC分类号： C07D223/16 , C07D267/10 , C07D267/14 , C07D281/06 , C07D281/10 , C07D413/06 , C07D417/04 , C07D417/12
摘要： The invention provides a new method for treating disorders associated with activation of the Notch signal transduction pathway comprising administering an effective amount of a compound of Formula (I), in free form or in a pharmaceutically acceptable salt form or in the form of a pharmaceutically acceptable solvate of the compound or the salt, to a human or animal patient in need thereof.
摘要翻译：本发明提供了一种用于治疗与Notch信号转导途径的激活相关的疾病的新方法，其包括给予有效量的游离形式或药学上可接受的盐形式或药学上可接受的形式的式（I）化合物化合物或盐的溶剂化物，与需要的人或动物患者接触。

8. 发明申请

WO2006056696A2 2-ALCOXY-3,4,5-TRIHYDROXY-ALKYLAMIDES, PREPARATION THEREOF, COMPOSITIONS CONTAINING THEM AND USE THEREOF 审中-公开
标题翻译： 2-ALCOXY-3,4,5-三羟基烷基胺，其制备方法，包含它们的组合物及其用途
公开(公告)号：WO2006056696A2
公开(公告)日：2006-06-01
申请号：PCT/FR2005002932
申请日：2005-11-25
申请人： AVENTIS PHARMA SA , ZHANG JIDONG , BHATNAGAR NEERJA , RUXER JEAN-MARIE
发明人： ZHANG JIDONG , BHATNAGAR NEERJA , RUXER JEAN-MARIE
IPC分类号： C07D223/12 , A61K31/397 , A61K31/401 , A61K31/47 , A61K31/55 , A61K31/554 , A61P35/00 , C07D205/04 , C07D207/14 , C07D211/56 , C07D215/38 , C07D223/16 , C07D281/06 , C07D471/04
CPC分类号： C07D223/12 , C07D205/085 , C07D207/273 , C07D207/277 , C07D211/76 , C07D215/38 , C07D223/16 , C07D243/08 , C07D281/06 , C07D281/08 , C07D417/06 , C07D471/04
摘要： 2-alcoxy-3,4,5-trihydroxy-alkylamides, the preparation thereof, compositions containing them and use thereof. The invention relates particularly to 2-alcoxy-3,4,5-trihydroxy-alkylamides, the preparation thereof, compositions containing them, and the use thereof as a medicament, particularly as anti-canceral agents.
摘要翻译： 2-烷氧基-3,4,5-三羟基烷基酰胺，其制备方法，含有它们的组合物及其用途。本发明特别涉及2-烷氧基-3,4,5-三羟基烷基酰胺，其制备方法，含有它们的组合物及其作为药物的用途，特别是作为抗癌剂。

9. 发明申请

WO0179187A8 SUBSTITUTED 1,4-THIAZEPINE AND ANALOGS AND THEIR USE AS ACTIVATORS OF CASPASES 审中-公开
标题翻译：取代的1,4-噻唑和类似物及其作为活化剂的使用
公开(公告)号：WO0179187A8
公开(公告)日：2003-02-20
申请号：PCT/US0112581
申请日：2001-04-18
申请人： CYTOVIA INC , CAI SUI XIONG , DREWE JOHN A , SHELTON EMMA JANE , LITVAK JOANE , SPERANDIO DAVID , SPENCER JEFFREY R , AXYS PHARM INC
发明人： CAI SUI XIONG , DREWE JOHN A , SHELTON EMMA JANE , LITVAK JOANE , SPERANDIO DAVID , SPENCER JEFFREY R
IPC分类号： A61P35/00 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/04 , C07D417/14 , C07D513/04 , C07D513/14 , A61K31/55
CPC分类号： C07D417/14 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/04 , C07D513/04 , C07D513/14
摘要： The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula (I): wherein the dashed lines, A , A , A , X and R are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of capases and inducers of apoptosis. Therefore, the activators of caspases and inducers of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及由通式（I）表示的取代的1,4-硫氮杂和其类似物：其中虚线A 1，A 2，A 3，X 1和 R 1在本文中定义。本发明还涉及发现具有式I的化合物是抑制剂的活化剂和凋亡诱导剂。因此，胱天蛋白酶的活化剂和胱天蛋白酶的诱导剂和本发明的细胞凋亡诱导剂可以用于在异常细胞发生不受控制的生长和扩散的各种临床条件下诱导细胞死亡。

10. 发明申请

WO02046167A1 BENZYL (IDENE)-LACTAMS AND THEIR USE AS 5HT1-RECEPTOR LIGANDS 审中-公开
标题翻译： BENZYL（IDENE）-LACTAMS及其作为5HT1受体配体使用
公开(公告)号：WO02046167A1
公开(公告)日：2002-06-13
申请号：PCT/IB2001/002139
申请日：2001-11-12
IPC分类号： A61K31/135 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P5/00 , A61P5/10 , A61P9/12 , A61P13/02 , A61P15/08 , A61P17/14 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P35/00 , A61P43/00 , C07D233/70 , C07D233/76 , C07D233/78 , C07D233/96 , C07D241/08 , C07D265/28 , C07D265/32 , C07D267/10 , C07D273/06 , C07D277/20 , C07D277/34 , C07D279/12 , C07D281/06 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D487/04
CPC分类号： C07D277/20 , A61K31/135 , A61K31/496 , C07D233/70 , C07D233/96 , C07D241/08 , C07D265/32 , C07D267/10 , C07D273/06 , C07D277/34 , C07D279/12 , C07D281/06 , C07D417/04 , C07D417/10 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The present invention relates to compounds of the formula I wherein 1) Y is a bridge containing bridging heteroatoms and to their medicinal use; 2) As serotonin 1 (5-HT1) receptor ligands, particularly in psychotherapeutic agents.
摘要翻译：本发明涉及式I化合物，其中1）Y是含有桥连杂原子的桥和其药用用途; 2）作为5-羟色胺1（5-HT1）受体配体，特别是在精神治疗药物中。

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