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1. 发明申请

US20180169277A1 CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT 审中-公开
公开(公告)号：US20180169277A1
公开(公告)日：2018-06-21
申请号：US15899644
申请日：2018-02-20
申请人： The General Hospital Corporation
发明人： David R. Elmaleh
IPC分类号： A61K51/04 , C07D311/24
CPC分类号： A61K51/0421 , C07D311/24
摘要： Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: wherein: X is OH, C1-C6 alkoxyl; Y and Z are independently selected form a C1-C6 alkyl, C1-C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.

2. 发明申请

US20160263257A1 CROMOLYN DERIVATIVES AND RELATED METHODS OF IMAGING AND TREATMENT 审中-公开
标题翻译：克拉莫衍生物和相关成像和处理方法
公开(公告)号：US20160263257A1
公开(公告)日：2016-09-15
申请号：US15031098
申请日：2014-10-22
申请人： David R. ELMALEH , Timothy SHOUP
发明人： David R. Elmaleh , Timothy M. Shoup
IPC分类号： A61K51/04 , A61K31/352 , A61K31/192 , A61K9/48 , A61K9/00
CPC分类号： A61K51/0421 , A61K9/0019 , A61K9/0053 , A61K9/0073 , A61K9/0075 , A61K9/4808 , A61K31/192 , A61K31/352 , A61K31/353 , C07D311/24
摘要： Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula; wherein X is OH, C1-C6 alkoxyl; Y and Z are independently selected from a C1-C6 alkyl, C1-C6 alkoxyl, halogen, mi-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.
摘要翻译：其中X是OH，C 1 -C 6烷氧基; Y和Z独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，取代或C 1 -C 6取代的胺，18 F，19 F或H; n为1,2或3; 并且其中对于结构（I），如果n均为1且Y和Z均为H且X为OH。

3. 发明申请

US20160228404A1 THERAPEUTIC AGENT FOR DISEASE BASED ON INHIBITORY EFFECT OF MACROPHAGE MIGRATION INHIBITORY FACTOR 审中-公开
标题翻译：基于大量移动抑制因子的抑制作用的疾病治疗药物
公开(公告)号：US20160228404A1
公开(公告)日：2016-08-11
申请号：US15132892
申请日：2016-04-19
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： Keiichi TANAKA , Kimiko MORIMOTO
IPC分类号： A61K31/352
CPC分类号： A61K31/352 , C07D311/22 , C07D311/24 , C07D311/30
摘要： A method for treating the relapsing-remitting or secondary progressive multiple sclerosis at the time of relapse, by administering a benzopyran derivative of the following formula or a salt thereof, where R1 represents an optionally substituted C1-6 alkyl group, one of R2 and R3 represents a hydrogen atom, and the other of R2 and R3 represents a hydrogen atom, an optionally substituted amino group, an optionally substituted acylamino group, an optionally substituted carbamoyl group or an optionally substituted aryl group.
摘要翻译：一种在复发时治疗复发缓解或继发性进行性多发性硬化症的方法，其通过给予下式的苯并吡喃衍生物或其盐，其中R 1表示任选取代的C 1-6烷基，R 2和R 3之一表示氢原子，R2和R3中的另一个表示氢原子，任选取代的氨基，任选取代的酰基氨基，任选取代的氨基甲酰基或任选取代的芳基。

4. 发明申请

US20150306122A1 APP SPECIFIC BACE INHIBITORS (ASBIs) AND USES THEREOF 审中-公开
标题翻译： APP特异性抑制剂（ASBIs）及其用途
公开(公告)号：US20150306122A1
公开(公告)日：2015-10-29
申请号：US14384641
申请日：2013-03-15
申请人： BUCK INSTITUTE FOR RESEARCH ON AGING
发明人： Varghese John , Dale E. Bredesen
IPC分类号： A61K31/7048 , A61K31/352
CPC分类号： A61K31/7048 , A61K31/352 , A61K31/366 , C07D311/24
摘要： In certain embodiments APP-specific BACE inhibitors (ASBIs) are provided as well as uses thereof. In certain embodiments methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction, or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease are provided where the method involves administering to a subject in need thereof an APP specific BACE inhibitor (ASBI) in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease. In certain embodiments the ASBI is a flavonoid (e.g. galangin) or flavonoid progrug (e.g., galangin prodrug).
摘要翻译：在某些实施方案中，提供APP特异性BACE抑制剂（ASBI）及其用途。在某些实施方案中，预防或延迟阿尔茨海默病前状态和/或认知功能障碍发作和/或改善阿尔茨海默病前状态和/或认知功能障碍的一种或多种症状的预防或延迟的方法，或预防或延迟前阿尔茨海默病提供阿尔茨海默氏病的前阿尔茨海默症状或认知功能障碍到阿尔茨海默氏病，其中所述方法涉及向有需要的受试者施用足以预防或延迟阿尔茨海默氏综合征认知功能障碍发作的APP特异性BACE抑制剂（ASBI），以及 /或改善前阿尔茨海默病认知功能障碍的一种或多种症状，和/或预防或延迟阿尔茨海默氏病的认知功能障碍进展为阿尔茨海默氏病。在某些实施方案中，ASBI是类黄酮（例如高良姜）或类黄酮前体（例如高良姜前药）。

5. 发明授权

US08563776B2 L-Threonine derivatives of high therapeutic index 有权
公开(公告)号：US08563776B2
公开(公告)日：2013-10-22
申请号：US12556968
申请日：2009-09-10
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07C229/00
CPC分类号： A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要： The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

6. 发明申请

US20120289471A1 NOVEL COMPOUNDS WITH HIGH THERAPEUTIC INDEX 审中-公开
标题翻译：具有高效治疗指数的新型化合物
公开(公告)号：US20120289471A1
公开(公告)日：2012-11-15
申请号：US13449791
申请日：2012-04-18
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： C07K7/64 , A61K31/702 , A61K38/13 , C07D499/68 , A61K31/43 , C07H17/08 , A61K31/7048 , C07C229/36 , A61K31/223 , C07D207/16 , A61K31/401 , C07C69/612 , A61K31/24 , C07C69/757 , A61K31/215 , A61K31/616 , C07D491/16 , A61K31/436 , C07D495/04 , A61K31/4365 , C07J71/00 , A61K31/58 , A61P29/00 , A61P37/06 , C07H15/203
CPC分类号： A61K38/12 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616 , Y02A50/411
摘要： The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的氨基酸组成的新型治疗化合物。这些高治疗指数衍生物与其制备的药物具有相同的效用，并且它们具有增强的药理学和药物性质。事实上，本发明的新型药物衍生物增强至少一种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

7. 发明申请

US20100069489A1 L-THREONINE DERIVATIVES OF HIGH THERAPEUTIC INDEX 审中-公开
标题翻译：高效治疗指数的L-THRONINE衍生物
公开(公告)号：US20100069489A1
公开(公告)日：2010-03-18
申请号：US12557080
申请日：2009-09-10
申请人： V. Ravi Chandran
发明人： V. Ravi Chandran
IPC分类号： A61K31/216 , A61P29/00
CPC分类号： A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要： The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的L-苏氨酸组成的衍生物。该衍生物与其制备的药物具有相同的效用，但具有增强的治疗性质。事实上，本发明的衍生物增强至少一种或多种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

8. 发明申请

US20080032982A1 Butanoic Acid Derivatives, Processes For The Preparation Thereof, Pharmaceutical Compositions Comprising Them, And Therapeutic Applications Thereof 失效
标题翻译：丁酸衍生物，其制备方法，药物组合物及其治疗应用
公开(公告)号：US20080032982A1
公开(公告)日：2008-02-07
申请号：US11579362
申请日：2005-04-06
申请人： Jean Zeiller , Herve Dumas , Valerie Guyard-Dangremont , Isabelle Berard , Francis Contard , Daniel Guerrier , Gerard Ferrand , Yves Bonhomme
发明人： Jean Zeiller , Herve Dumas , Valerie Guyard-Dangremont , Isabelle Berard , Francis Contard , Daniel Guerrier , Gerard Ferrand , Yves Bonhomme
IPC分类号： A61K31/192 , A61K31/352 , A61K31/381 , A61K31/42 , A61K31/426 , A61K31/44 , A61K31/5375 , A61P3/00 , A61P9/10 , C07C59/215 , C07D213/55 , C07D261/08 , C07D277/24 , C07D295/14 , C07D311/30 , C07D333/24
CPC分类号： C07D277/24 , C07D213/30 , C07D213/50 , C07D213/64 , C07D213/65 , C07D213/89 , C07D215/14 , C07D215/20 , C07D217/02 , C07D231/12 , C07D231/28 , C07D239/52 , C07D241/44 , C07D249/08 , C07D261/08 , C07D263/57 , C07D265/38 , C07D277/66 , C07D285/06 , C07D295/096 , C07D307/42 , C07D307/46 , C07D307/60 , C07D307/79 , C07D307/80 , C07D307/82 , C07D307/86 , C07D307/91 , C07D311/14 , C07D311/16 , C07D311/18 , C07D311/22 , C07D311/24 , C07D311/30 , C07D311/54 , C07D311/56 , C07D311/74 , C07D311/76 , C07D317/64 , C07D327/04 , C07D333/22 , C07D333/28 , C07D333/56 , C07D409/04 , C07D471/04
摘要： Compounds of the formula (I): in which R, R1 and R2 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and . processes for the preparation of these compounds. Compounds of formula (I) are activators of PPARα and PPARα isoforms.
摘要翻译：式（I）的化合物：其中R 1，R 1和R 2 2如说明书中所定义，其用于治疗血脂异常，动脉粥样硬化和糖尿病的用途，包含它们的药物组合物，和。制备这些化合物的方法。式（I）化合物是PPARα和PPARα同工型的活化剂。

9. 发明申请

US20060241017A1 Novel compounds with high therapeutic index 有权
标题翻译：具有高治疗指数的新型化合物
公开(公告)号：US20060241017A1
公开(公告)日：2006-10-26
申请号：US11343557
申请日：2006-01-30
申请人： V. Chandran
发明人： V. Chandran
IPC分类号： A61K38/16
CPC分类号： A61K38/12 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616 , Y02A50/411
摘要： The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
摘要翻译：本发明涉及由与其上具有羟基，氨基，羧基或酰化衍生物的药物或药物结合的氨基酸组成的新型治疗化合物。这些高治疗指数衍生物与其制备的药物具有相同的效用，并且它们具有增强的药理学和药物性质。事实上，本发明的新型药物衍生物增强至少一种如本文所定义的治疗质量。本发明还涉及含有其的药物组合物。

10. 发明授权

US07015339B2 Process for isolating phenolic compounds 失效
公开(公告)号：US07015339B2
公开(公告)日：2006-03-21
申请号：US10201191
申请日：2002-07-23
申请人： Anil Bhagwan Khare , Brent Howard Hilbert
发明人： Anil Bhagwan Khare , Brent Howard Hilbert
IPC分类号： C07D319/14
CPC分类号： A61K36/00 , C07D311/24 , C07D311/30 , A61K2300/00
摘要： The invention provides compositions and methods for isolating phenolic compounds, particularly isoflavones, from aqueous extracts of plant materials that contain such compounds. The process comprising: (a) providing an aqueous plant extract at a first pH less than 10, the aqueous plant extract comprising a plurality of phenolic compounds; (b) extracting the aqueous plant extract with a first organic solvent to yield a first organic extract; (c) extracting the first organic extract with an aqueous phase of pH greater than 10 to yield a phenol rich aqueous phase; (d) adjusting the pH of the phenol rich aqueous phase to a pH of less than 9; and (e) isolating the phenolic compounds from the phenol rich aqueous phase.

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