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1. 发明申请

US20100227975A1 AQUEOUS DISPERSIONS OF POLYMER PARTICLES 审中-公开
标题翻译：聚合物颗粒的水分散
公开(公告)号：US20100227975A1
公开(公告)日：2010-09-09
申请号：US12780248
申请日：2010-05-14
申请人： Christopher Henry SUCH , Ezio RIZZARDO , Algirdas Kazimieras SERELIS , Brian Stanley HAWKETT , Robert Goulston GILBERT , Christopher James FERGUSON , Robert John HUGHES , Edna Olejnik
发明人： Christopher Henry SUCH , Ezio RIZZARDO , Algirdas Kazimieras SERELIS , Brian Stanley HAWKETT , Robert Goulston GILBERT , Christopher James FERGUSON , Robert John HUGHES , Edna Olejnik
IPC分类号： C08F2/44 , C07C327/04 , C07C329/06
CPC分类号： C07C329/00 , C07C329/16 , C08F2/38 , C08F4/00 , C08F293/005 , C08F2438/03
摘要： The invention provides a method for preparing an aqueous dispersion of polymer particles comprising the following steps: (i) preparing a dispersion having a continuous aqueous phase, a dispersed organic phase comprising one or more ethylenically unsaturated monomers, and an amphiphilic RAFT agent as a stabiliser for said organic phase, and (ii) polymerising said one or more ethylenically unsaturated monomers under the control of said amphiphilic RAFT agent to form said aqueous dispersion of polymer particles, novel amphiphilic RAFT agents for use in this method, novel RAFT agents useful in making these amphiphilic RAFT agents and methods for their manufacture.
摘要翻译：本发明提供一种制备聚合物颗粒的水分散体的方法，包括以下步骤：（i）制备具有连续水相的分散体，包含一种或多种烯属不饱和单体的分散有机相和两亲性RAFT剂作为稳定剂对于所述有机相，和（ii）在所述两亲RAFT试剂的控制下聚合所述一种或多种烯属不饱和单体以形成聚合物颗粒的所述水分散体，用于该方法的新型两亲性RAFT试剂，用于制备的新型RAFT试剂这些两亲RAFT药剂及其制造方法。

2. 发明申请

US20090318729A1 IMMOBILIZED LEWIS ACID CATALYSTS COATED WITH IONIC LIQUIDS AND USE THEREOF 有权
标题翻译：用离子液体涂覆的固化的LEWIS酸催化剂及其用途
公开(公告)号：US20090318729A1
公开(公告)日：2009-12-24
申请号：US12282444
申请日：2007-03-12
申请人： Shu Kobayashi , Yuichiro Mori , Gu Yanlong
发明人： Shu Kobayashi , Yuichiro Mori , Gu Yanlong
IPC分类号： B01J31/12 , C07C327/04 , C07C215/20 , C07C33/30
CPC分类号： C07C29/40 , B01J31/0252 , B01J31/0254 , B01J31/0284 , B01J31/0288 , B01J31/0292 , B01J31/1633 , B01J31/2256 , B01J2231/32 , B01J2231/342 , B01J2231/346 , B01J2531/35 , B01J2531/36 , B01J2531/38 , B01J2531/54 , B01J2531/96 , C07C221/00 , C07C327/22 , Y02P20/588 , C07C225/18 , C07C33/30
摘要： The invention provides a novel immobilized Lewis acid catalyst which exhibits high catalytic activity in an aqueous solution and which permits recovery and reuse or long-term continuous use. The invention relates to an immobilized Lewis acid catalyst comprising a solid substance and a Lewis acid supported on the surface of the solid substance by chemical bonding, wherein the surface of the solid substance and the peripheries of the Lewis acid are coated with an ionic liquid, more specifically, an immobilized Lewis acid catalyst comprising a solid substance such as silica gel or an organic polymer and a Lewis acid stable even in water which is supported on the surface of the solid substance by chemical bonding, wherein the surface of the solid substance and the peripheries of the Lewis acid are completely or partially coated with a hydrophobic ionic liquid; a process for the production of the catalyst; use thereof; and a process for the preparation of compounds with the catalyst.
摘要翻译：本发明提供了一种在水溶液中显示出高催化活性并且允许回收和再利用或长期连续使用的新型固定化路易斯酸催化剂。本发明涉及一种固定化的路易斯酸催化剂，其包含通过化学键合负载在固体物质的表面上的固体物质和路易斯酸，其中固体物质的表面和路易斯酸的外围被离子液体包覆，更具体地，包含固体物质例如硅胶或有机聚合物的固定化路易斯酸催化剂和即使在水中稳定的路易斯酸，其通过化学键合负载在固体物质的表面上，其中固体物质的表面和路易斯酸的外围部分被完全或部分地涂覆有疏水性离子液体; 催化剂的生产方法; 使用; 以及用催化剂制备化合物的方法。

3. 发明申请

US20090076289A1 Methods of Making Epothilones 有权
标题翻译：制造埃坡霉素的方法
公开(公告)号：US20090076289A1
公开(公告)日：2009-03-19
申请号：US12118432
申请日：2008-05-09
申请人： John R. Carney , Yong Li , Hugo Menzella , Ralph C. Reid
发明人： John R. Carney , Yong Li , Hugo Menzella , Ralph C. Reid
IPC分类号： C12P17/06 , C07D315/00 , C07C327/04
CPC分类号： C07D309/32 , C07D313/00 , C07D339/08 , Y02P20/582
摘要： The invention provides novel compounds that may be used as intermediates in the preparation of epothilones, epothilone analogs and derivative, as well as new synthetic methods for producing the intermediates and products.
摘要翻译：本发明提供可用作制备埃坡霉素，埃坡霉素类似物和衍生物的中间体的新型化合物，以及用于生产中间体和产物的新合成方法。

4. 发明授权

US4600540A Benzoylpropionic acid derivatives 失效
标题翻译：苯甲酰丙酸衍生物
公开(公告)号：US4600540A
公开(公告)日：1986-07-15
申请号：US741127
申请日：1985-06-04
申请人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Kaoru Sota
发明人： Kazuyuki Tomisawa , Kazuya Kameo , Toru Matsunaga , Shiuji Saito , Kaoru Sota
IPC分类号： A61K31/265 , A61K31/10 , A61K31/185 , A61P37/00 , C07C20060101 , C07C67/00 , C07C313/00 , C07C325/00 , C07C327/04 , C07C327/20 , C07C327/22 , C07C327/32 , C07C153/023
CPC分类号： C07C327/00
摘要： Benzoylpropionic acid derivatives represented by the general formula ##STR1## (wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or a benzyl group, R.sup.2 represents a lower alkyl group or a phenyl group, X represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a phenoxy group or a halogenophenoxy group, and Y represents a hydrogen atom or a lower alkyl group). The compounds have immunomodulative function and are effective for treatment of diseases caused by abnormal immunofunction.
摘要翻译：由通式（I）表示的苯甲酰基丙酸衍生物（其中R1表示氢原子，低级烷基或苄基，R2表示低级烷基或苯基，X表示氢原子，卤素原子，低级烷基，低级烷氧基，苯氧基或卤代苯氧基，Y表示氢原子或低级烷基）。该化合物具有免疫调节功能，对于治疗由异常免疫功能引起的疾病有效。

5. 发明申请

US20100130507A1 PROSTAGLANDIN DERIVATIVES 有权
标题翻译： PROSTAGLANDIN衍生物
公开(公告)号：US20100130507A1
公开(公告)日：2010-05-27
申请号：US12613985
申请日：2009-11-06
申请人： Ennio ONGINI , Valerio Chiroli , Francesca Benedini , Piero Del Soldato
发明人： Ennio ONGINI , Valerio Chiroli , Francesca Benedini , Piero Del Soldato
IPC分类号： A61K31/557 , C07C405/00 , C07C327/04 , C07D295/10 , C07D211/30 , A61K31/4965
CPC分类号： C07C405/0016
摘要： Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
摘要翻译：描述了具有改善的药理活性和增强的耐受性的前列腺素硝基衍生物。可用于治疗青光眼和高眼压症。

6. 发明授权

US5010097A Novel compounds 失效
公开(公告)号：US5010097A
公开(公告)日：1991-04-23
申请号：US287453
申请日：1988-12-20
申请人： Roger E. Markwell , Stephen A. Smith , Ian Hughes , Laramie M. Gaster
发明人： Roger E. Markwell , Stephen A. Smith , Ian Hughes , Laramie M. Gaster
IPC分类号： C07D209/18 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/22 , A61K31/335 , A61K31/357 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/55 , A61P1/02 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C319/02 , C07C323/41 , C07C323/60 , C07C327/04 , C07C327/16 , C07C327/32 , C07D317/22 , C07D317/30 , C07K1/113 , C07K5/06 , C07K14/81
CPC分类号： C07C323/60 , C07C327/32 , C07D317/22 , C07D317/30
摘要： Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; R.sub.3 is C.sub.3-6 alkyl;R.sub.4 is hydrogen, alkyl, --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl, or a group ##STR3## where R.sub.11 is hydrogen, alkyl, or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.12 is hydrogen or alkyl; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.

7. 发明授权

US09630937B2 Substituted N-acetyl-L-cysteine derivatives and related compounds 有权
公开(公告)号：US09630937B2
公开(公告)日：2017-04-25
申请号：US14535855
申请日：2014-11-07
申请人： Promentis Pharmaceuticals, Inc.
发明人： Michael Neary , James Nieman , Steven Tanis , Daniel Lawton , Garry Smith
IPC分类号： A61K31/265 , C07D277/14 , C07D241/08 , C07C323/58 , C07C323/59 , C07C323/57 , C07C327/04 , C07C327/34 , C07C327/32 , C07C329/06 , C07D327/04 , C07C323/60
CPC分类号： C07D277/08 , A61K31/165 , A61K31/265 , A61K31/426 , A61K31/513 , C07C323/57 , C07C323/58 , C07C323/59 , C07C323/60 , C07C327/26 , C07C327/32 , C07C327/34 , C07C329/06 , C07D241/08 , C07D277/14 , C07D327/04
摘要： Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.

8. 发明申请

US20100056635A1 NOVEL PROTEIN KINASE MODULATORS AND THERAPEUTIC USES THEREOF 有权
标题翻译：新型蛋白激酶调节剂及其治疗用途
公开(公告)号：US20100056635A1
公开(公告)日：2010-03-04
申请号：US12517278
申请日：2007-12-04
申请人： Hadas Reuveni , Alexander Levitzki , Lilach Steiner , Revital Sasson , Iris Ben-David , Avi Weissberg
发明人： Hadas Reuveni , Alexander Levitzki , Lilach Steiner , Revital Sasson , Iris Ben-David , Avi Weissberg
IPC分类号： A61K31/164 , C07C327/04 , A61P35/00
CPC分类号： C07C327/44
摘要： The present invention provides new tyrphostin derivatives acting as substrate competitive protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.
摘要翻译：本发明提供了作为底物竞争性蛋白酪氨酸激酶（PTK）抑制剂和受体酪氨酸激酶（RTK）抑制剂的新的酪氨酸磷酸酯衍生物，其制备方法，包括这些化合物的药物组合物，以及使用这些化合物和组合物，特别是化学治疗预防和治疗PTK和RTK相关疾病如代谢，纤维化和细胞增殖性疾病，特别是牛皮癣和癌症的药物。

9. 发明授权

US5310763A Hydroxamino acid based collagenase inhibitors 失效
标题翻译：羟基氨基酸胶原酶抑制剂
公开(公告)号：US5310763A
公开(公告)日：1994-05-10
申请号：US048413
申请日：1993-04-14
申请人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
发明人： Colin Campion , Alan H. Davidson , Jonathan P. Dickens , Michael J. Crimmin
IPC分类号： A61K31/16 , A61K31/13 , A61K31/165 , A61K31/21 , A61K31/215 , A61K31/38 , A61K31/381 , A61P3/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07C317/44 , C07C317/48 , C07C317/50 , C07C323/52 , C07C323/60 , C07C323/62 , C07C327/32 , C07D333/34 , A61K31/19 , C07C327/04
CPC分类号： C07C323/52 , C07C317/44 , C07C327/32 , C07D333/34
摘要： Compounds of general formula I: ##STR1## wherein: R.sup.1 represents a C.sub.1 -C.sub.6 alkyl, phenyl, thiophenyl, substituted phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, heterocyclyl, (C.sub.1 -C.sub.6)alkylcarbonyl phenacyl or substituted phenacyl group; or, when n=O, R.sup.1 represents SR.sup.x, wherein R.sup.x represents a group: ##STR2## R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group;R.sup.3 represents an amino acid residue with R or S stereochemistry or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6 alkoxy)benzyl or benzyloxy(C.sub.1 -C.sub.6 alkyl) group;R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group;R.sup.5 represents a hydrogen atom or a methyl group;n is an integer having the value 0, 1 or 2; andA represents a C.sub.1 -C.sub.6 hydrocarbon chain, optionaly substituted with one or more C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl groups;and their salts and N-oxides are collagenase inhibitors are and useful in the management of disease involving tissue degradation and/or the promotion of wound healing. Diseases involving tissue degradation include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption diseases and tumor invasion.
摘要翻译：通式I的化合物：其中：R1表示C1-C6烷基，苯基，噻吩基，取代的苯基，苯基（C1-C6）烷基，杂环基，（C1-C6）烷基羰基苯甲酰甲基或取代的苯甲酰甲基 ; 或者当n = O时，R1表示SRx，其中Rx表示一个基团：R 2表示氢原子或C 1 -C 6烷基，C 1 -C 6烯基，苯基（C 1 -C 6）烷基，环烷基（C 1 -C 6 ）烷基或环烯基（C 1 -C 6）烷基; R 3表示具有R或S立体化学的氨基酸残基或C1-C6烷基，苄基，（C1-C6烷氧基）苄基或苄氧基（C1-C6烷基）基团; R4表示氢原子或C1-C6烷基; R5表示氢原子或甲基; n是0或1或2的整数; 且A代表C1-C6烃链，任选被一个或多个C 1 -C 6烷基，苯基或取代的苯基取代; 其盐和N-氧化物是胶原酶抑制剂，并且可用于治疗涉及组织降解和/或促进伤口愈合的疾病。涉及组织降解的疾病包括关节病（特别是类风湿性关节炎），炎症，皮肤病，骨吸收疾病和肿瘤侵袭。

10. 发明授权

US4692458A Anti-hypertensive agents 失效
公开(公告)号：US4692458A
公开(公告)日：1987-09-08
申请号：US127472
申请日：1980-03-05
申请人： James W. Ryan , Alfred Chung
发明人： James W. Ryan , Alfred Chung
IPC分类号： A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61K38/55 , A61P43/00 , C07C327/04 , C07D207/06 , C07D207/08 , C07D207/16 , C07D207/20 , C07D207/22 , C07D207/46 , C07D207/50 , C07D209/20 , C07D211/60 , C07D211/62 , C07D211/76 , C07D211/78 , C07D211/86 , C07D233/64 , C07D277/06 , C07D333/24 , C07D403/12 , C07D417/12 , C07K5/068 , C07K5/078 , C07K5/097 , C07K7/14 , C07K14/81 , A61K31/41 , C07D207/00 , C07D211/72
CPC分类号： C07D403/12 , C07C327/00 , C07D207/16 , C07D207/22 , C07D207/46 , C07D207/50 , C07D211/60 , C07D211/62 , C07D211/76 , C07D211/86 , C07D277/06 , C07D417/12 , C07K5/06086 , C07K5/06173 , C07K5/0821 , A61K38/00
摘要： Novel inhibitors of angiotensin converting enzyme having the general formula R--A--S--Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.

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