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41. 发明授权

US07557143B2 Thyroid receptor ligands 失效
标题翻译：甲状腺受体配体
公开(公告)号：US07557143B2
公开(公告)日：2009-07-07
申请号：US10826100
申请日：2004-04-15
申请人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
发明人： Denis E. Ryono , Jon J. Hangeland , Todd J. Friends , Tamara Dejneka , Pratik Devasthale , Yolanda V. Caringal , Minsheng Zhang , Arthur M. P. Doweyko , Johan Malm , Andrei Sanin
IPC分类号： A61K31/165 , A61K31/19 , C07C239/00 , C07C325/00 , C07C229/00 , C07C59/00
CPC分类号： C07C311/46 , A61K31/4439 , A61K31/662 , A61K45/06 , C07C43/29 , C07C43/295 , C07C59/68 , C07C59/72 , C07C65/24 , C07C65/26 , C07C69/16 , C07C69/736 , C07C69/94 , C07C205/38 , C07C217/58 , C07C233/29 , C07C235/34 , C07C235/42 , C07C235/46 , C07C235/52 , C07C235/60 , C07C235/62 , C07C235/64 , C07C311/37 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D239/26 , C07D257/04 , C07D263/14 , C07D263/32 , C07D277/24 , C07D285/06 , C07D307/42 , C07D307/52 , C07D307/87 , C07D317/58 , C07D317/60 , C07D333/32 , C07F9/306 , C07F9/3241 , C07F9/4056 , A61K2300/00
摘要： Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
摘要翻译：提供具有通式I的甲状腺受体配体，其中：R 1是R 2和R 3相同或不同，是氢，卤素，1至4个碳的烷基或3至5个碳原子的环烷基，条件是R2中的至少一个并且R 3不是氢; R 4是R 5和R 6相同或不同，并且选自氢，芳基，杂芳基，烷基，环烷基，芳烷基或杂芳烷基。 R7是芳基，杂芳基，烷基，芳烷基或杂芳烷基; R8是芳基，杂芳基或环烷基; R9为R7或氢; R 10是氢，卤素，氰基或烷基; R 11和R 12各自独立地选自氢，卤素，烷氧基，羟基（-OH）氰基和烷基; R13是羧酸（COOH）或其酯，膦酸和次膦酸或其酯，磺酸，四唑，异羟肟酸，噻唑烷二酮，酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同，并且选自氢和烷基，或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - （CH 2）m - ，m = 2,3,4或 5]，从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同，选自氢，卤素和烷基; n为0或1至4的整数; X是氧（-O-），硫（-S-），磺酰基（-SO 2 - ），亚磺酰基（-SO-），硒（-Se-），羰基（-CO-），氨基（-NH-）或亚甲基（-CH2-）; 其中取代基如本文所述。此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法，其中如上所述的化合物以治疗有效量施用。

42. 发明授权

US07544833B2 Methods for producing N-(8-[2-hydroxybenzoyl]-amino) caprylic acid 有权
标题翻译：制备N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的方法
公开(公告)号：US07544833B2
公开(公告)日：2009-06-09
申请号：US11847415
申请日：2007-08-30
申请人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
发明人： William Elliott Bay , Joseph Norman Bernadino , George Frederick Klein , Yi Ren , Pingsheng Zhang
IPC分类号： C07C229/02 , C07C231/10
CPC分类号： C07C231/10 , C07C231/24 , C07C235/60
摘要： Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino)caprylic acid.
摘要翻译：公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的改进方法。已经发现某些化合物在包含在酯水解反应中时可用于防止形成有色杂质。还发现在厌氧条件下进行酯水解使色彩杂质的形成最小化。还公开了用于合成N-（8- [2-羟基苯甲酰基] - 氨基）辛酸的钠盐的改进方法。

43. 发明申请

US20090143330A1 Crystalline Polymorphic Forms Of Monosodium N-[-8-(2-Hydroxybenzoyl)Amino]Caprylate 有权
标题翻译： N - [ - 8-（2-羟基苯甲酰基）氨基]辛酸钠的结晶多晶型
公开(公告)号：US20090143330A1
公开(公告)日：2009-06-04
申请号：US11568753
申请日：2005-05-06
申请人： Halina Levchik , Shingai Majuru , Brahma Singh , Jamila Harris
发明人： Halina Levchik , Shingai Majuru , Brahma Singh , Jamila Harris
IPC分类号： A61K31/727 , C07C229/42
CPC分类号： A61K31/197 , A61J3/02 , A61K9/2095 , A61K31/198 , A61K45/06 , A61K2300/00 , C07C235/60
摘要： The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino] caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.
摘要翻译：本发明涉及SNAC的包括两种水合物，甲醇溶剂化物和乙醇溶剂合物的N- [8-（2-羟基苯甲酰基）氨基]辛酸单钠（“SNAC”）的结晶多晶形式。更具体地说，本发明提供了六种多晶型的SNAC（以下称为形式I-VI）。本发明还提供了无定形形式的SNAC。

44. 发明授权

US07534813B2 Levodopa prodrugs, and compositions and uses thereof 有权
标题翻译：左旋多巴前药及其组合物和用途
公开(公告)号：US07534813B2
公开(公告)日：2009-05-19
申请号：US12008473
申请日：2008-01-10
申请人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
发明人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou , Mark Nguyen , Xuedong Dai , Jianhua Li , Kenneth C. Cundy , Nelson L. Jumbe
IPC分类号： A01N47/10 , A61K31/27
CPC分类号： C07C235/60 , C07C229/34 , C07C229/36 , C07C235/48 , C07C2601/14 , C07D213/79 , C07D213/80 , C07D213/803
摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
摘要翻译：公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

45. 发明申请

US20090062340A1 NOVEL BIAROMATIC COMPOUNDS WHICH ACTIVATE PPARY TYPE RECEPTORS AND COSMETIC/PHARMACEUTICAL COMPOSITIONS COMPRISED THEREOF 失效
标题翻译：启动PPary型受体的新型二异氰酸酯化合物及其包含的化妆品/药物组合物
公开(公告)号：US20090062340A1
公开(公告)日：2009-03-05
申请号：US12266096
申请日：2008-11-06
申请人： LAURENCE CLARY , CLAIRE BOUIX-PETER , MICHEL RIVIER , PASCAL COLLETTE , ANDRE JOMARD
发明人： LAURENCE CLARY , CLAIRE BOUIX-PETER , MICHEL RIVIER , PASCAL COLLETTE , ANDRE JOMARD
IPC分类号： A61K31/445 , C07D271/10 , A61K31/4245 , C07D211/00 , C07C229/34 , A61K31/216
CPC分类号： C07D207/27 , A61K8/44 , A61K8/49 , A61Q5/00 , A61Q19/00 , A61Q19/08 , C07C229/36 , C07C233/47 , C07C233/54 , C07C233/55 , C07C233/65 , C07C233/81 , C07C233/87 , C07C235/52 , C07C235/60 , C07C235/74 , C07C235/84 , C07C237/20 , C07C237/40 , C07C243/28 , C07C271/22 , C07C275/42 , C07C323/60 , C07C335/22 , C07C2601/02 , C07C2601/14 , C07D207/335 , C07D211/16 , C07D211/34 , C07D211/62 , C07D213/38 , C07D213/40 , C07D263/32 , C07D265/30 , C07D271/06 , C07D271/10 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/81 , C07D333/20
摘要： Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
摘要翻译：具有下述结构式（I）的新颖的双芳族化合物被配制成适用于人或兽医药物（皮肤病学以及与心血管疾病，免疫疾病和/或脂质代谢相关的疾病领域）的药物组合物，或替代地，进入化妆品组合物。

46. 发明申请

US20090023928A1 PHTHALAMIDE-LANTHANIDE COMPLEXES FOR USE AS LUMINESCENT MARKERS 审中-公开
标题翻译：用作紫外线标记物的羟乙基磺酰胺化合物复合物
公开(公告)号：US20090023928A1
公开(公告)日：2009-01-22
申请号：US12202367
申请日：2008-09-01
申请人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
IPC分类号： C07D277/04
CPC分类号： C12Q1/37 , A61K41/0057 , A61K49/0002 , A61K49/0019 , A61K49/103 , A61K49/106 , A61K49/122 , A61K49/124 , A61K51/0478 , A61K51/0482 , A61K51/06 , C07C235/60 , C07D487/08 , C07D487/18 , C07D487/22 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80 , Y10S436/804
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
摘要翻译：本发明提供了包含镧系元素的金属离子的发光镧系元素金属螯合物和包含至少一个邻苯二甲酰亚胺基部分的络合剂。还提供了掺入本发明的邻苯二甲酰氨基配体的探针和利用本发明配体的方法和包含本发明配体的探针。

47. 发明授权

US07420085B2 Polymorphs of sodium 4-[(4-chloro-2-hydroxybenzoyl) amino] butanoate 有权
标题翻译： 4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的多晶型物
公开(公告)号：US07420085B2
公开(公告)日：2008-09-02
申请号：US11734591
申请日：2007-04-12
申请人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
发明人： Satej Bhandarkar , Shingai Majuru , Halina Levchik
IPC分类号： C07C229/00
CPC分类号： C07C235/60 , A61K31/00 , A61K38/28 , A61K45/06 , A61K47/16 , A61K2300/00
摘要： The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as insulin, to a target.
摘要翻译：本发明涉及4 - [（4-氯-2-羟基苯甲酰基）氨基]丁酸钠的无定形和多晶型形式及其用于促进活性剂如胰岛素向靶标递送的用途。

48. 发明申请

US20080132570A1 Levodopa prodrugs, and compositions and uses thereof 有权
标题翻译：左旋多巴前药及其组合物和用途
公开(公告)号：US20080132570A1
公开(公告)日：2008-06-05
申请号：US12008473
申请日：2008-01-10
申请人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou
发明人： Jia-Ning Xiang , Mark A. Gallop , Cindy X. Zhou
IPC分类号： A61K31/216 , A61P25/00
CPC分类号： C07C235/60 , C07C229/34 , C07C229/36 , C07C235/48 , C07C2601/14 , C07D213/79 , C07D213/80 , C07D213/803
摘要： Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
摘要翻译：公开了左旋多巴的前药，制备左旋多巴的前药的方法，使用左旋多巴的前药的方法和左旋多巴的前药组合物。

49. 发明授权

US07361783B2 (2S)-2-ethylphenylpropionic acid derivative 失效
标题翻译：（2S）-2-乙基苯基丙酸衍生物
公开(公告)号：US07361783B2
公开(公告)日：2008-04-22
申请号：US10515176
申请日：2003-05-26
申请人： Jun Asano , Shigeki Isogai , Wataru Hori
发明人： Jun Asano , Shigeki Isogai , Wataru Hori
IPC分类号： C07C409/44 , A01N37/12 , A01N25/00
CPC分类号： C07D209/48 , C07C235/60 , C07D263/26
摘要： The invention provides novel (2S)-2-ethylphenylpropanoic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) α to activate and exhibit lipid-lowering effect, inhibitory effect on the arteriosclerosis, antiobesity effect, blood glucose-lowering effect, etc., their addition salts, and their medicinal compositions.(2S)-2-Ethylphenylpropanoic acid derivatives represented by a general formula (1) [wherein R1 denotes a halogen atom or trifluoromethyl group, R2 denotes a hydrogen atom, halogen atom or trifluoromethyl group, and, when R2 denotes a hydrogen atom, R3 denotes a halogen atom or trifluoromethyl group and, when R2 denotes a halogen atom or trifluoromethyl group, R3 denotes a hydrogen atom, halogen atom or trifluoromethyl group], and their addition salts.
摘要翻译：本发明提供了与受体作为人类过氧化物酶体增殖物激活受体（PPAR）α的配体结合的新型（2S）-2-乙基苯基丙酸衍生物，以激活并表现出降脂作用，对动脉硬化的抑制作用，抗肥胖作用，血液葡萄糖降低作用等，其加成盐及其药物组合物。（2S）-2-乙基苯基丙酸衍生物[其中R1表示卤素原子或三氟甲基，R2表示氢原子，卤素原子或三氟甲基，当R2表示氢原子时，R3 表示卤素原子或三氟甲基，当R 2表示卤素原子或三氟甲基时，R 3表示氢原子，卤素原子或三氟甲基]及其加成盐。

50. 发明授权

US07351741B2 Compounds and compositions for delivering active agents 有权
标题翻译：用于递送活性剂的化合物和组合物
公开(公告)号：US07351741B2
公开(公告)日：2008-04-01
申请号：US10312703
申请日：2001-06-29
申请人： John J. Weidner , Bruce F. Variano , Shingai Majuru , Satej Bhandarkar , William E. Bay , Lynn Sheilds
发明人： John J. Weidner , Bruce F. Variano , Shingai Majuru , Satej Bhandarkar , William E. Bay , Lynn Sheilds
IPC分类号： A61K31/19 , A61K38/00 , A61K31/715 , C07C229/00
CPC分类号： A61K38/21 , A61K9/0095 , A61K38/27 , A61K38/28 , A61K45/06 , C07C235/60 , Y02P20/55 , A61K2300/00
摘要： Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provide as well.
摘要翻译：提供用于递送活性剂的化合物和组合物。也提供给药和制备方法。

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