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61. 发明授权

US07534797B2 6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors 有权
标题翻译： 6,6-双环取代杂双环蛋白激酶抑制剂
公开(公告)号：US07534797B2
公开(公告)日：2009-05-19
申请号：US11095162
申请日：2005-03-31
申请人： Lee D. Arnold , Mark Joseph Mulvihill
发明人： Lee D. Arnold , Mark Joseph Mulvihill
IPC分类号： A61K31/4965 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07F5/025 , C07D471/04 , C07D487/04
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
摘要翻译：其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，R 1和Q 1在本文中定义的式及其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防过度增生性疾病如癌症，炎症，牛皮癣，过敏/哮喘，免疫系统的疾病和状况，中枢神经系统的疾病和状况。

62. 发明授权

US07534475B2 Liquid crystal compound comprising two condensed and substituted rings 有权
标题翻译：包含两个稠合和取代的环的液晶化合物
公开(公告)号：US07534475B2
公开(公告)日：2009-05-19
申请号：US10592110
申请日：2005-03-08
申请人： Hideyuki Nishikawa , Ryo Hamasaki , Atsuhiro Ohkawa
发明人： Hideyuki Nishikawa , Ryo Hamasaki , Atsuhiro Ohkawa
IPC分类号： C09K19/32 , C09K19/34 , C09K19/38 , C09K19/20 , G02F1/13363 , C07D277/62 , C07D307/78 , C07D333/52 , C07D493/00 , C07D495/00 , C07C69/74 , C07C69/76
CPC分类号： C09K19/18 , C09K19/3477 , C09K19/3491 , C09K2019/0448 , C09K2019/3408 , Y10T428/1041
摘要： A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged λ/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.
摘要翻译：新的液晶化合物包含两个稠合和取代的环。该环优选为五元杂环。杂环优选与苯环或芳族六元杂环稠合。苯环或芳香族六元杂环优选被包含环状结构和链结构的基团取代。液晶化合物有利地用于制备薄相延迟剂，例如宽范围的λ/ 4板，其产生反向波长分布。通过使用新的液晶化合物，可以通过简单的工艺容易地制造相延迟器。

63. 发明授权

US07511041B2 Fused azole-pyrimidine derivatives 有权
标题翻译：熔融唑 - 嘧啶衍生物
公开(公告)号：US07511041B2
公开(公告)日：2009-03-31
申请号：US10527376
申请日：2003-09-18
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D237/26 , C07D237/36 , C07D241/36 , C07D239/00 , C07D471/00 , C07D471/04 , C07D401/04 , C07D401/22 , C07D487/00 , C07D487/04 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

64. 发明授权

US07501418B2 Fused heterocyclic isoxazoline derivatives and their use as anti-depressants 有权
标题翻译：稠合杂环异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07501418B2
公开(公告)日：2009-03-10
申请号：US10524123
申请日：2003-08-13
申请人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
发明人： José Ignacio Andrés-Gil , Manuel Jesús Alcázar-Vaca , José Manuel Bartolomé -Nebreda , Francisco Javier Fernández-Gadea , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Megens
IPC分类号： A01N43/54 , A01N43/40 , A61K31/445 , A61K31/497 , C07D211/32 , C07D211/68 , C07D211/80 , C07D213/02 , C07D261/20 , C07D239/00 , C07D237/26 , C07D237/36 , C07D413/00 , C07D417/00 , C07D419/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D498/14
摘要： The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1. The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity as well as α2-adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
摘要翻译：本发明涉及式（I）的稠合杂环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构体形式及其N-氧化物形式，更特别是四氢吡喃异恶唑，六氢异恶唑并吡啶，四氢噻喃异恶唑和六氢苯并异恶唑衍生物通过双环部分的6元环以及其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑症，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重紊乱，其中变量如权利要求1中所定义。化合物惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性以及α2-肾上腺素受体拮抗剂活性，根据发明也适用于f 或治疗和/或预防疾病，其中单独的一种活性或所述活性的组合可能具有治疗用途。

65. 发明授权

US07459554B2 Imidazopyrazine tyrosine kinase inhibitors 有权
标题翻译：咪唑吡嗪酪氨酸激酶抑制剂
公开(公告)号：US07459554B2
公开(公告)日：2008-12-02
申请号：US10965182
申请日：2004-10-14
申请人： Han-Qing Dong , Kenneth Foreman , Mark Joseph Mulvihill , Anthony Innocenzo Nigro , Arno G. Steinig , Douglas Werner , Robin Wilkes
发明人： Han-Qing Dong , Kenneth Foreman , Mark Joseph Mulvihill , Anthony Innocenzo Nigro , Arno G. Steinig , Douglas Werner , Robin Wilkes
IPC分类号： C07D413/00 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D415/00
CPC分类号： C07D487/04
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
摘要翻译：其中Q1和R1在本文中定义的式和其药学上可接受的盐的化合物抑制IGF-1R酶，并且可用于治疗和/或预防通过抑制酪氨酸激酶对治疗反应的各种疾病和病症。

66. 发明授权

US07439264B2 Therapeutic compounds 有权
标题翻译：治疗化合物
公开(公告)号：US07439264B2
公开(公告)日：2008-10-21
申请号：US10364028
申请日：2003-02-10
申请人： Peter C. Meltzer , Bertha K. Madras , Paul Blundell , Shanghao Liu
发明人： Peter C. Meltzer , Bertha K. Madras , Paul Blundell , Shanghao Liu
IPC分类号： A61K31/38 , A61K31/336 , C07D313/02 , C07D495/00
CPC分类号： C07D451/02 , A61K47/54 , C07D493/08
摘要： This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.
摘要翻译：本发明涉及抑制转运蛋白和受体的拮抗剂。本发明还涉及允许化合物部分转运或部分结合转运蛋白或受体的转运蛋白和受体的部分抑制剂。本发明还涉及差异阻止通过转运蛋白或受体的转运或结合的化合物。本发明还涉及这些化合物用于治疗某些疾病和病症的用途。

67. 发明申请

US20080009531A1 5-Anilino-4-Heteroarylpyrazole Derivatives Useful for the Treatment of Diabetes 审中-公开
标题翻译：可用于治疗糖尿病的5-苯胺基-4-杂芳基吡唑衍生物
公开(公告)号：US20080009531A1
公开(公告)日：2008-01-10
申请号：US11596959
申请日：2005-05-20
申请人： Louis Cantin , Xin Ma , Christiana Akuche , Sidney Liang
发明人： Louis Cantin , Xin Ma , Christiana Akuche , Sidney Liang
IPC分类号： A61K31/4155 , A61K31/4164 , A61K31/422 , A61K31/427 , A61P3/04 , A61P3/10 , A61P9/00 , C07D231/38 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D493/00 , C07D495/00
CPC分类号： C07D417/04 , A61K31/416 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D513/04
摘要： The present invention relates to 5-anilino-4-heteroarylpyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
摘要翻译：本发明涉及5-苯胺基-4-杂芳基吡唑化合物，药物组合物和治疗糖尿病及相关疾病的方法。

68. 发明授权

US06015912A Spirocyclic containing hydroxamic acids useful as metalloprotease inhibitors 失效
标题翻译：可用作金属蛋白酶抑制剂的含有螺环的异羟肟酸
公开(公告)号：US06015912A
公开(公告)日：2000-01-18
申请号：US918328
申请日：1997-08-26
申请人： Zhe Wang , Neil Gregory Almstead , Rimma Sandler Bradley , Michael George Natchus , Biswanath De , Stanislaw Pikul , Yetunde Olabisi Taiwo
发明人： Zhe Wang , Neil Gregory Almstead , Rimma Sandler Bradley , Michael George Natchus , Biswanath De , Stanislaw Pikul , Yetunde Olabisi Taiwo
IPC分类号： C07D487/10 , A61K31/40 , A61K31/403 , A61K31/407 , A61K31/435 , A61K31/438 , A61K31/527 , A61P1/02 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/06 , A61P15/08 , A61P15/18 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/04 , A61P21/00 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/02 , A61P33/06 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P39/02 , A61P41/00 , A61P43/00 , C07D207/48 , C07D209/54 , C07D209/96 , C07D471/10 , C07D491/10 , C07D491/113 , C07D491/20 , C07D493/20 , C07D495/10 , C07D491/00 , C07D495/00
CPC分类号： C07D471/10 , C07D209/96 , C07D491/10 , C07D495/10
摘要： The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译：本发明提供了权利要求中所述的式的化合物或其旋光异构体，非对映异构体或其对映异构体或其药学上可接受的盐或其可生物水解的酰胺，酯或酰亚胺可用作金属蛋白酶的抑制剂。还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病，病症和病症的药物组合物和方法。

69. 发明授权

US5789597A Process for the preparation of compounds having ACE inhibitory action and intermediates in said process 失效
标题翻译：用于制备具有ACE抑制作用的化合物的方法和所述方法中的中间体
公开(公告)号：US5789597A
公开(公告)日：1998-08-04
申请号：US596214
申请日：1996-02-15
申请人： Sonia Serra Mortes , Alberto Palomo Coll , Rok Zupet
发明人： Sonia Serra Mortes , Alberto Palomo Coll , Rok Zupet
IPC分类号： C07D521/00 , C07K5/02 , C07D211/30 , C07D233/26 , C07D487/02 , C07D495/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07K5/0222
摘要： There is disclosed a process for the preparation of compounds having ACE inhibitory action of the formula ##STR1## wherein R has the meanings as in claim 1, wherein the stereospecific amino acid N-�1-(S)-ethoxycarbonyl-3-phenylpropyl!-L-alanine is carboxylically activated with a thionyl chloride derivative wherein at least one chlorine atom is replaced by the residue of a heterocyclic ambident compound such as imidazole, benzimidazole, 2-methylimidazole or triazole, especially chlorothionylimidazole or thionyldiimidazole, in the presence of an organic solvent to the intermediate novel compound A or to the intermediate novel compound B and the obtained intermediate compound is reacted with an amino acid, preferably in the monosilylated form, most preferably in the disilylated form. Disclosed are also novel compounds useful as starting materials or intermediates in the present process.
摘要翻译： PCT No.PCT / SI95 / 00017 Sec。 371日期：1996年2月15日 102（e）日期1996年2月15日PCT提交1995年7月13日PCT公布。公开号WO96 / 02564 日期1996年2月1日公开了具有下式的化合物的具有ACE抑制作用的化合物的方法，其中R具有权利要求1所述的含义，其中立体定向氨基酸N- [1-（S） - 乙氧基羰基 -3-苯基丙基] -L-丙氨酸用亚硫酰氯衍生物进行羧基活化，其中至少一个氯原子被诸如咪唑，苯并咪唑，2-甲基咪唑或三唑的杂环环状化合物的残基替换，特别是氯代硫代酰基咪唑或亚硫酰基二咪唑，在中间体新化合物A或中间体新化合物B存在下，将有机溶剂与氨基酸反应，优选以单甲硅烷基化形式，最优选以二乙硅烷基化形式反应。本发明还公开了可用作原料或中间体的新化合物。

70. 发明授权

US5734049A Processes for preparing intermediates of inhibitors of enkephalinase and angiotensin converting enzyme and intermediates thereof 失效
公开(公告)号：US5734049A
公开(公告)日：1998-03-31
申请号：US743481
申请日：1996-11-04
申请人： Gary A. Flynn , Michael J. Genin , Douglas W. Beight
发明人： Gary A. Flynn , Michael J. Genin , Douglas W. Beight
IPC分类号： A61K38/00 , C07D20060101 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/00 , C07D405/14 , C07D409/00 , C07D409/14 , C07D471/04 , C07D471/14 , C07D491/00 , C07D491/14 , C07D491/147 , C07D495/00 , C07D495/14 , C07H19/16 , C07K5/06 , C07K5/078 , C07D417/04
CPC分类号： C07D401/06 , C07D471/04 , C07K5/06139 , A61K38/00
摘要： The present invention relates to novel processes for preparing intermediates of the formula I ##STR1## and to novel intermediates thereof which are useful in the preparation of inhibitors of enkephalinase and angiotensin converting enzyme.

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