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1. 发明申请

US20200239452A1 IDO/TDO Inhibitor 审中-公开
公开(公告)号：US20200239452A1
公开(公告)日：2020-07-30
申请号：US16755953
申请日：2018-10-17
申请人： GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION , CanBas Co., Ltd.
发明人： Akira Asai , Naohisa Ogo , Daisuke Muraoka , Osamu Takikawa , Takumi Kawabe , Takuji Sato
IPC分类号： C07D403/12 , C07C335/32 , C07D209/42 , C07D409/14 , C07D213/81 , C07C391/00 , C07D241/42 , C07D333/54 , C07D333/18 , C07D213/32 , A61P35/04
摘要： A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R1 and R2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R4 represents, for example, —C(═NH)—HN2, and R6 represents, for example, a substituted or unsubstituted aryl group].

2. 发明授权

US09718770B2 Substituted thioureas as heat shock protein 70 inhibitors 有权
公开(公告)号：US09718770B2
公开(公告)日：2017-08-01
申请号：US15105426
申请日：2014-12-18
申请人： Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
发明人： Wu Zhong , Song Li , Yanqun Zeng , Junhai Xiao , Xinbo Zhou , Zhibing Zheng , Xingzhou Li , Xiaokui Wang
IPC分类号： A61K31/155 , A61K31/17 , C07C335/04 , C07C391/00 , C07D213/75 , C07C335/08 , C07C335/14 , C07C335/16 , C07C335/18 , C07D295/16 , C07C335/20 , C07D211/06
CPC分类号： C07C391/00 , C07C335/08 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07D211/06 , C07D213/75 , C07D295/16
摘要： The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic.

3. 发明授权

US09505714B2 Conversion of alkanes to organoseleniums and organotelluriums 有权
标题翻译：烷烃转化为有机硒和有机碲
公开(公告)号：US09505714B2
公开(公告)日：2016-11-29
申请号：US14910275
申请日：2014-08-06
申请人： The Scripps Research Institute
发明人： Roy A. Periana , Michael M. Konnick , Brian G. Hashiguchi
IPC分类号： C07C45/00 , C07C395/00 , C07C1/00 , C07C209/00 , C07C319/00 , C07F7/00 , C07C391/00 , C07C1/32 , C07C319/02 , C07C319/14 , C07C17/093 , C07B39/00 , C07B41/06 , C07B43/04 , C07B45/00 , C07B47/00 , C07C209/22 , C07C231/10 , C07F7/22 , C07F9/50
CPC分类号： C07C395/00 , C07B39/00 , C07B41/06 , C07B43/04 , C07B45/00 , C07B47/00 , C07C1/321 , C07C17/093 , C07C45/00 , C07C209/22 , C07C231/10 , C07C319/02 , C07C319/14 , C07C391/00 , C07F7/2208 , C07F9/5004 , C07C321/04 , C07C321/14 , C07C11/02
摘要： The invention provides processes and materials for the efficient and costeffective functionalization of alkanes and heteroalkanes, comprising contacting the alkane or heteroalkane and a soft oxidizing electrophile comprising Se(VI) or Te(VI), in an acidic medium, optionally further comprising an aprotic medium, which can be carried out at a temperature of less than 300 C. Isolation of the alkylselenium or alkyltellurium intermediate allows the subsequent conversion to products not necessarily compatible with the initial reaction conditions, such as amines, stannanes, organosulfur compounds, acyls, halocarbons, and olefins.
摘要翻译：本发明提供用于烷烃和杂烷烃的有效和成本有效的功能化的方法和材料，包括在酸性介质中使烷烃或杂烷烃与包含Se（VI）或Te（VI）的软氧化亲电试剂接触，任选地还包含非质子介质可以在小于300℃的温度下进行。烷基硒或烷基碲中间体的分离允许随后转化成与初始反应条件不一致的产物，例如胺，锡烷，有机硫化合物，酰基，卤代烃，和烯烃。

4. 发明申请

US20160176812A1 CONVERSION OF ALKANES TO ORGANOSELENIUMS AND ORGANOTELLURIUMS 有权
标题翻译：碱向有机物和有机物的转化
公开(公告)号：US20160176812A1
公开(公告)日：2016-06-23
申请号：US14910275
申请日：2014-08-06
申请人： Roy A. PERIANA , Michael M. KONNICK , Brian G. HASHIGUCHI , THE SCRIPPS RESEARCH INSTITUTE
发明人： Roy A. PERIANA , Michael M. KONNICK , Brian G. HASHIGUCHI
IPC分类号： C07C395/00 , C07C209/22 , C07F7/22 , C07C319/02 , C07C231/10 , C07F9/50 , C07C45/00 , C07C17/093 , C07B47/00 , C07B45/00 , C07B43/04 , C07B41/06 , C07B39/00 , C07C1/32 , C07C391/00
CPC分类号： C07C395/00 , C07B39/00 , C07B41/06 , C07B43/04 , C07B45/00 , C07B47/00 , C07C1/321 , C07C17/093 , C07C45/00 , C07C209/22 , C07C231/10 , C07C319/02 , C07C319/14 , C07C391/00 , C07F7/2208 , C07F9/5004 , C07C321/04 , C07C321/14 , C07C11/02
摘要： The invention provides processes and materials for the efficient and costeffective functionalization of alkanes and heteroalkanes, comprising contacting the alkane or heteroalkane and a soft oxidizing electrophile comprising Se(VI) or Te(VI), in an acidic medium, optionally further comprising an aprotic medium, which can be carried out at a temperature of less than 300 C. Isolation of the alkylselenium or alkyltellurium intermediate allows the subsequent conversion to products not necessarily compatible with the initial reaction conditions, such as amines, stannanes, organosulfur compounds, acyls, halocarbons, and olefins.
摘要翻译：本发明提供用于烷烃和杂烷烃的有效和成本有效的功能化的方法和材料，包括在酸性介质中使烷烃或杂烷烃与包含Se（VI）或Te（VI）的软氧化亲电试剂接触，任选地还包含非质子介质可以在小于300℃的温度下进行。烷基硒或烷基碲中间体的分离允许随后转化成与初始反应条件不一致的产物，例如胺，锡烷，有机硫化合物，酰基，卤代烃，和烯烃。

5. 发明授权

US08309541B1 Anti-cancer compositions and methods 有权
标题翻译：抗癌成分和方法
公开(公告)号：US08309541B1
公开(公告)日：2012-11-13
申请号：US13107494
申请日：2011-05-13
申请人： Gavin P. Robertson , SubbRao V. Madhunapantula , Shantu Amin , Dhimant Desai
发明人： Gavin P. Robertson , SubbRao V. Madhunapantula , Shantu Amin , Dhimant Desai
IPC分类号： A01N43/00 , A01N31/00 , A61K31/33 , A61K31/095 , C07C391/00 , C07C395/00
CPC分类号： C07C391/00 , A61K8/23 , A61K31/095 , A61K31/155 , A61K31/33
摘要： Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: R2-R-R1, where R is phenyl, where R1 is (CH2)nSe—C(═NH)—NH2, where R2 is (CH2)nSe—C(═NH)—NH2 or R2 is H, and where each n is independently 2, 3, 4, 5, 6, 7, or 8. Methods of treating a subject are provided according to embodiments of the present invention which include administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject having a condition characterized by Akt dysregulation. Administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject detectably increases apoptosis and/or decreases proliferation of cancer cells, particularly cancer cells characterized by Akt dysregulation. Compositions of the present invention inhibit Akt enzymes, iNOS, and increase MAP kinase activity such that cancer cells contacted with the compositions are inhibited.
摘要翻译：描述了抗癌组合物和方法，包括一种或多种具有结构式I的化合物：R2-R-R1，其中R是苯基，其中R1是（CH2）nSe-C（= NHN）-NH2，其中R2是（ CH2）nSe-C（= NH）-NH2或R2是H，并且其中每个n独立地是2,3,4,5,6,7或8.根据本发明的实施方案提供了治疗受试者的方法其包括将治疗有效量的包含一种或多种具有结构式I的化合物的组合物施用于具有由Akt调节异常表征的病症的受试者。向受试者施用治疗有效量的包含一种或多种具有结构式I的化合物的组合物可检测地增加癌细胞，特别是Akt失调特征的癌细胞的凋亡和/或降低增殖。本发明的组合物抑制Akt酶，iNOS，并且增加MAP激酶活性，使得与组合物接触的癌细胞被抑制。

6. 发明授权

US07855232B2 Organoselenium compound for cancer chemoprevention 有权
标题翻译：有机硒化合物用于癌症化学预防
公开(公告)号：US07855232B2
公开(公告)日：2010-12-21
申请号：US11980875
申请日：2007-10-31
申请人： Luke K. T. Lam , Nayaz Ahmed
发明人： Luke K. T. Lam , Nayaz Ahmed
IPC分类号： A61K31/195 , A61K31/33 , A61K31/095 , A61K31/381 , A61K31/34 , C07C391/00
CPC分类号： C07D333/14 , A23L33/10 , A61K38/00 , C07C323/58 , C07C323/59 , C07C391/00 , C07D333/20 , C07D333/22 , C07D345/00 , C07K5/0215 , C07K5/0606
摘要： A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.
摘要翻译：含有亚硒基异氰酸酯或亚烷基异氰酸酯部分的化合物有效地防止癌症或癌前病症的发生或发展。化合物可以以药物组合物，化妆品，食品添加剂，补充剂等的形式提供和施用。还提供了本发明的化学预防化合物的合成和使用方法。

7. 发明授权

US07772428B2 Creatine hydroxycitric acids salts and methods for their production and use in individuals 有权
标题翻译：肌酸羟基柠檬酸盐及其生产和使用方法
公开(公告)号：US07772428B2
公开(公告)日：2010-08-10
申请号：US12108822
申请日：2008-04-24
申请人： Marvin Heuer , Michele Molino
发明人： Marvin Heuer , Michele Molino
IPC分类号： C07C229/00 , C07C391/00
CPC分类号： C07C59/285 , A23L33/175 , A23V2002/00 , C07C279/14 , A23V2250/306 , A23V2200/30 , A23V2200/332 , A23V2200/33
摘要： Methods of production for Tricreatine Hydroxycitrate are disclosed. Tricreatine hydroxycitrate can be used as supplemental dietary ingredient for the purposes of reducing adiposity, suppression of appetite, improvement of muscle and exercise performance and recovery. The salts are useful in the dietetic, food supplement and food industries.
摘要翻译：公开了三羟甲基柠檬酸的生产方法。羟基柠檬酸肌酸可用作补充膳食成分，用于减少肥胖，抑制食欲，改善肌肉和锻炼性能和恢复。这些盐可用于饮食，食品添加剂和食品工业。

8. 发明授权

US07270728B2 Photochemical transformation of metallic and non-metallic ions in an aqueous environment 有权
公开(公告)号：US07270728B2
公开(公告)日：2007-09-18
申请号：US11521410
申请日：2006-09-15
申请人： Xuming Guo , Ralph E. Sturgeon , Zoltan Mester
发明人： Xuming Guo , Ralph E. Sturgeon , Zoltan Mester
IPC分类号： B01J19/08 , C07F15/00 , C07F395/00 , C07C391/00
CPC分类号： C22B61/00 , C02F1/32 , C02F1/66 , C02F2101/20 , C02F2101/322 , C02F2305/10 , C22B3/205 , C22B23/0461 , Y02P10/234 , Y02W10/37
摘要： The invention comprises a method of photochemical transformation of metallic and non-metallic ions in an aqueous environment. The method comprises exposing the ions to UV irradiation in the presence of an organic acid. The aqueous ions are reduced by the method and may form hydrides, alkyl or carbonyl compounds.

9. 发明授权

US06911550B2 Derivatives of seleno-amino acids with improved bioavailability and method for their preparation 有权
标题翻译：具有改善的生物利用度的硒氨基酸的衍生物及其制备方法
公开(公告)号：US06911550B2
公开(公告)日：2005-06-28
申请号：US10372491
申请日：2003-02-21
申请人： Mahmoud M. Abdel-Monem , Michael D. Anderson
发明人： Mahmoud M. Abdel-Monem , Michael D. Anderson
IPC分类号： A23K1/16 , A23K1/175 , A23K1/18 , C07C391/00 , C07F3/06 , A23K1/00
CPC分类号： C07C391/00 , A23K20/142 , A23K20/30 , A23K50/10 , A23K50/75
摘要： Metal L-seleno-alpha-amino acids salts and their use as a bioavailable feed and water ration supplement for domesticated animals such as cattle, pigs and poultry.
摘要翻译：金属L-硒代-α-氨基酸盐及其作为生物可利用的饲料和用于驯养动物例如牛，猪和家禽的补充饲料的用途。

10. 发明申请

US20030166979A1 Chemical methods 审中-公开
标题翻译：化学方法
公开(公告)号：US20030166979A1
公开(公告)日：2003-09-04
申请号：US10263360
申请日：2002-10-01
发明人： Dainis Dakternieks , Carl H. Schiesser , Tamara Perchyonok
IPC分类号： C07C029/136 , C07C215/08 , C07C319/02 , C07C391/00 , C07C395/00
CPC分类号： C07C233/47 , C07B53/00 , C07B2200/07 , C07C45/65 , C07C67/31 , C07C67/317 , C07C69/732 , C07C69/734 , C07C69/612
摘要： Disclosed is a method for enantioselectively-reducing a prochiral carbon-centered radical having one or more electron donator groups attached directly to the central prochiral carbon atom of the radical, and/or attached to a carbon atom within 1 to 4 atoms of the central prochiral carbon atom, comprising treating said radical with a chiral non-racemic organotin hydride in the presence of a Lewis acid.
摘要翻译：公开了一种用于对映选择性还原具有一个或多个电子给体基团的前手性碳中心自由基的方法，所述电子给体基团直接连接到基团的中心前手性碳原子上，和/或连接到中心原纤维的1至4个原子内的碳原子包括在路易斯酸存在下用手性非外消旋有机锡氢化物处理所述基团。

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