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1. 发明授权

US6153634A 4,5-azolo-oxindoles 失效
标题翻译： 4,5-azo-oxindoles
公开(公告)号：US6153634A
公开(公告)日：2000-11-28
申请号：US464507
申请日：1999-12-15
申请人： Kin-Chun Luk , Christophe Michoud , Steven Gregory Mischke
发明人： Kin-Chun Luk , Christophe Michoud , Steven Gregory Mischke
IPC分类号： C07D403/06 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/4188 , A61K31/424 , A61K31/429
CPC分类号： C07D403/06 , C07D487/04 , C07D513/04 , C09B23/04
摘要： Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
摘要翻译：公开了具有下式的新的4,5-azo-oxindoles这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。因此，这些化合物及其药学上可接受的盐和所述化合物的前药是用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂。还公开了含有这些化合物的药物组合物，以及用于治疗和/或预防癌症的方法，特别是使用这些化合物治疗或控制实体瘤的方法，以及可用于制备式I化合物的中间体。

2. 发明申请

US20090318408A1 HALO-SUBSTITUTED PYRIMIDODIAZEPINES 失效
标题翻译： HALO取代的吡咯烷酮
公开(公告)号：US20090318408A1
公开(公告)日：2009-12-24
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： A61K31/551 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译：本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。还提供了可用于合成式I化合物的中间体化合物。

3. 发明授权

US06313310B1 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles 失效
标题翻译： 4-和5-炔氧基吲哚和4-和5-烯氧基吲哚
公开(公告)号：US06313310B1
公开(公告)日：2001-11-06
申请号：US09464238
申请日：1999-12-15
申请人： Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
发明人： Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
IPC分类号： C07D40302
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.
摘要翻译：公开了抑制或调节蛋白激酶，特别是JNK蛋白激酶的4-和5-炔氧基吲哚以及4-和5-链烯氧基吲哚。本发明的化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂，特别可用于治疗类风湿性关节炎。还公开了含有前述化合物的药物组合物，用于治疗和/或控制炎症的方法，特别是在使用这些化合物治疗或控制类风湿性关节炎的药物组合物中，以及可用于制备本发明化合物的中间体。

4. 发明授权

US06197804B1 4,5-azolo-oxindoles 失效
标题翻译： 4,5-azo-oxindoles
公开(公告)号：US06197804B1
公开(公告)日：2001-03-06
申请号：US09571541
申请日：2000-05-16
申请人： Kin-Chun Luk , Steven Gregory Mischke
发明人： Kin-Chun Luk , Steven Gregory Mischke
IPC分类号： A61K31424
CPC分类号： C07D403/06 , C07D487/04 , C07D513/04 , C09B23/04
摘要： Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
摘要翻译：公开了具有下式的新的4,5-azo-oxindoles这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。因此，这些化合物及其药学上可接受的盐和*所述化合物的前药是用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂。还公开了含有这些化合物的药物组合物，以及用于治疗和/或预防癌症的方法，特别是使用这些化合物治疗或控制实体瘤的方法，以及可用于制备式I化合物的中间体。

5. 发明授权

US08044213B2 Thiazolyl-benzimidazoles 失效
标题翻译：噻唑基 - 苯并咪唑
公开(公告)号：US08044213B2
公开(公告)日：2011-10-25
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/427 , C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译：本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其使用方法。

6. 发明授权

US08003785B2 Halo-substituted pyrimidodiazepines 失效
标题翻译：卤代取代的嘧啶并二氮杂
公开(公告)号：US08003785B2
公开(公告)日：2011-08-23
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译：本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。还提供了可用于合成式I化合物的中间体化合物。

7. 发明申请

US20100160308A1 Thiazolyl-Benzimidazoles 失效
标题翻译：噻唑基 - 苯并咪唑
公开(公告)号：US20100160308A1
公开(公告)日：2010-06-24
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/5377 , A61K31/496 , C07D413/14 , C07D417/14 , A61P35/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译：本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其用途。

8. 发明授权

US6130239A 4-Alkenyl- and 4-alkynyloxindoles 失效
标题翻译： 4-烯基和4-炔氧基吲哚
公开(公告)号：US6130239A
公开(公告)日：2000-10-10
申请号：US464502
申请日：1999-12-15
申请人： Yi Chen , Wendy Lea Corbett , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
发明人： Yi Chen , Wendy Lea Corbett , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
IPC分类号： A61K31/404 , A61K31/4178 , A61K31/4409 , A61K31/454 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D209/34
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.
摘要翻译：公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐，其中R1，R2，R3，a，b和X如本文所定义。这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。这些化合物及其药学上可接受的盐和所述化合物的前药是可用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂，更特别是乳腺癌和结肠肿瘤的治疗或控制。还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。

9. 发明授权

US07067529B2 Glutamine fructose-y-phosphate amidotransferase (GFAT) inhibitors 失效
标题翻译：谷氨酰胺果糖-γ-磷酸酰胺转移酶（GFAT）抑制剂
公开(公告)号：US07067529B2
公开(公告)日：2006-06-27
申请号：US10827514
申请日：2004-04-19
申请人： David Robert Bolin , Shoaqing Chen , Steven Gregory Mischke , Yimin Qian
发明人： David Robert Bolin , Shoaqing Chen , Steven Gregory Mischke , Yimin Qian
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D401/04 , C07D217/18 , C07D217/22 , C07D217/26 , C07D401/06 , C07D401/12 , C07D405/10 , C07D413/06 , C07D417/06 , C07D417/10
摘要： Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents are as disclosed in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.
摘要翻译：提供了式I化合物及其药学上可接受的盐和酯，其中取代基如说明书中所公开的。该化合物可用于治疗2型糖尿病。

10. 发明授权

US07803816B2 MCH receptor antagonists 失效
标题翻译： MCH受体拮抗剂
公开(公告)号：US07803816B2
公开(公告)日：2010-09-28
申请号：US11526523
申请日：2006-09-25
申请人： Steven Joseph Berthel , Shawn David Erickson , Nader Fotouhi , Robert Francis Kester , Kyungjin Kim , Steven Gregory Mischke , Yimin Qian , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley , Hong Wang
发明人： Steven Joseph Berthel , Shawn David Erickson , Nader Fotouhi , Robert Francis Kester , Kyungjin Kim , Steven Gregory Mischke , Yimin Qian , Kshitij Chhabilbhai Thakkar , Jefferson Wright Tilley , Hong Wang
IPC分类号： A61K31/454 , C07D403/02
CPC分类号： C07D401/04 , C07D401/14 , C07D471/04
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of obesity, hyperphagia, anxiety, depression and related disorders and diseases.
摘要翻译：本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗肥胖，食欲过盛，焦虑，抑郁和相关疾病和疾病。

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