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91. 发明申请

US20200207757A1 DERIVATIVES OF RESIQUIMOD 审中-公开
公开(公告)号：US20200207757A1
公开(公告)日：2020-07-02
申请号：US16612216
申请日：2018-05-18
申请人： Lihu YANG , Superb Wisdom Limited
发明人： Lihu Yang
IPC分类号： C07D471/04
摘要： A deuterated compound having structural formula I or a pharmaceutically acceptable salt thereof: Values and example values of the variable in formula (I) are disclosed herein. Also disclosed are the use of compounds of formula (I) in the methods of treating a disease selected from cancer, an autoimmune disease, and an infectious disease, and methods of enhancing an immune response to an antigen.

92. 发明申请

US20180141947A1 Purine Inhibitors of Human Phosphatidylinositol 3-Kinase Delta 审中-公开
公开(公告)号：US20180141947A1
公开(公告)日：2018-05-24
申请号：US15736510
申请日：2016-06-24
申请人： Meredeth Ann MCGOWAN , Hua ZHOU , Jason D. KATZ , Lihu YANG , Joey L. METHOT , Kathryn Ann LIPFORD , Shimin XU , Ning FU , Guoquan XU , Deqian BIAN , Jianmin FU , Yabin LI , kin Chiu FONG , MERCK SHARP & DOHME CORP.
发明人： Meredith Ann McGowan , Hua Zhou , Jason D. Katz , Lihu Yang , Joey L. Methot , Kathryn Ann Lipford , Shimin Xu , Ning Fu , Guoquan Xu , Deqian Bian , Jianmin Fu , Yabin Li , Kin Chiu Fong
IPC分类号： C07D473/30 , C07D473/34 , C07D519/00 , C07D471/04 , A61P35/00 , A61P19/02 , A61P11/06 , A61P11/00 , A61P37/00 , A61P17/06 , A61P11/08
CPC分类号： C07D473/30 , A61K45/06 , A61P11/00 , A61P11/06 , A61P11/08 , A61P17/06 , A61P19/02 , A61P35/00 , A61P37/00 , C07D471/04 , C07D473/34 , C07D519/00
摘要： The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

93. 发明申请

US20170114078A1 PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA 审中-公开
公开(公告)号：US20170114078A1
公开(公告)日：2017-04-27
申请号：US15318483
申请日：2015-06-09
申请人： Meredeth Ann MCGOWAN , Kin Chiu FONG , Neville John ANTHONY , Hua ZHOU , Jason D. KATZ , Lihu YANG , Chaomin LI , Yuan TIAN , Changwei MU , Baijun YE , Feng SHI , Xiaoli ZHAO , Jianmin FU , Yabin LI , Merck Sharp & Dohme Corp.
发明人： Meredeth Ann McGowan , Kin Chiu Fong , Neville John Anthony , Hua Zhou , Jason D. Katz , Lihu Yang , Chaomin Li , Yuan Tian , Changwei Mu , Baijun Ye , Feng Shi , Xiaoli Zhao , Jianmin Fu , Yabin Li
IPC分类号： C07D519/00 , C07D473/30 , C07D473/34 , A61K31/52
CPC分类号： C07D519/00 , A61K31/52 , C07D473/30 , C07D473/34
摘要： The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.

94. 发明授权

US09056859B2 Inhibitors of the renal outer medullary potassium channel 有权
标题翻译：肾外髓质钾通道抑制剂
公开(公告)号：US09056859B2
公开(公告)日：2015-06-16
申请号：US13881574
申请日：2011-10-24
申请人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
发明人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
IPC分类号： C07D257/04 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D495/04 , A61K31/496 , C07D311/76 , C07D311/80 , C07D403/10 , C07D307/88 , C07D311/02 , C07D405/06 , C07D471/08 , C07D487/08
CPC分类号： C07D405/12 , A61K31/496 , C07D257/04 , C07D307/88 , C07D311/02 , C07D311/76 , C07D311/80 , C07D403/10 , C07D405/06 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08 , C07D495/04
摘要： This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译：本发明涉及具有结构式（I）的化合物; 和它们的药学上可接受的盐，它们是肾外
膜髓质（ROMK）通道（Kir1.1）的抑制剂。式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水分滞留引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

95. 发明授权

US08759539B2 Substituted bicyclic amines for the treatment of diabetes 失效
标题翻译：用于治疗糖尿病的取代的双环胺
公开(公告)号：US08759539B2
公开(公告)日：2014-06-24
申请号：US13125088
申请日：2009-11-11
申请人： Jiafang He , John Bawiec , Weiguo Liu , Gui-Bai Liang , Lihu Yang
发明人： Jiafang He , John Bawiec , Weiguo Liu , Gui-Bai Liang , Lihu Yang
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D209/52 , C07D413/12 , C07D417/12 , A61K31/403 , A61K31/4184 , A61K31/4192 , A61K31/427 , A61K31/4709 , A61K31/4725 , A61K31/423
CPC分类号： C07D401/12 , C07D209/52 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
摘要翻译：本文描述的是取代的双环胺。特别地，本文描述的是作为SSTR5的拮抗剂有效的取代的双环胺，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍，肥胖，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。

96. 发明授权

US07935712B2 Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors 有权
标题翻译：螺吡色酮衍生物作为乙酰辅酶A羧化酶（ACC）抑制剂
公开(公告)号：US07935712B2
公开(公告)日：2011-05-03
申请号：US11988588
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A01N43/42 , A61K31/44 , A61K31/535
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

97. 发明申请

US20100216694A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 有权
标题翻译：抗菌三环化合物
公开(公告)号：US20100216694A1
公开(公告)日：2010-08-26
申请号：US12738857
申请日：2008-10-27
申请人： Gui-Bai Liang , Xibin Liao , Weiguo Liu , Paul E. Finke , Dooseop Kim , Lihu Yang , Songnian Lin
发明人： Gui-Bai Liang , Xibin Liao , Weiguo Liu , Paul E. Finke , Dooseop Kim , Lihu Yang , Songnian Lin
IPC分类号： A61K38/28 , C07C62/34 , A61K31/192 , C07D305/06 , A61K31/337 , A61K31/437 , C07D471/04 , A61P3/10 , A61K38/16
CPC分类号： C07D305/06 , C07B2200/07 , C07C62/34 , C07C2603/12 , C07D471/04
摘要： Tricyclic compounds containing a cyclopropanecarboxylic acid fused to a bicyclic ring, including pharmaceutically acceptable salts, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译：包含与双环稠合的环丙烷羧酸的三环化合物（包括药学上可接受的盐）是G蛋白偶联受体40（GPR40）的激动剂，并且可用作治疗化合物，特别是用于治疗2型糖尿病以及通常与该疾病有关，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

98. 发明申请

US20090270436A1 SPIROCHROMANON DERIVATIVES 有权
标题翻译：螺吡喃衍生物
公开(公告)号：US20090270436A1
公开(公告)日：2009-10-29
申请号：US12518466
申请日：2008-01-08
申请人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
发明人： Tomoharu Iino , Hideki Jona , Hideki Kurihara , Masayuki Nakamura , Kenji Niiyama , Jun Shibata , Tadashi Shimamura , Hitomi Watanabe , Takeru Yamakawa , Lihu Yang
IPC分类号： A61K31/438 , C07D401/14 , A61P3/00 , A61P35/00 , A61P31/00
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3: R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a machine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[ 3-c]吡唑，1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 具有Ar 2且任选具有一个或两个以上选自R 3：R 1和R 2的取代基的3,4-b]吡啶各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基， C1-C6烷氧基，C2-C7烷酰基，C2-C7烷氧基羰基，芳烷氧基羰基，氨基甲酰基C1-C6烷氧基，羧基-C2-C6链烯基或-Q1-N （Ra）-Q2-Rb; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; T和U各自独立地表示氮原子或机组; V表示氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

99. 发明授权

US07589085B2 Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃杂环环戊基杂芳基调节剂
公开(公告)号：US07589085B2
公开(公告)日：2009-09-15
申请号：US10567516
申请日：2004-08-06
申请人： Gabor Butora , Lihu Yang , Stephen D. Goble
发明人： Gabor Butora , Lihu Yang , Stephen D. Goble
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：本发明还涉及式（I）（II）（其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R15，R16，R17，R18，R19， R24和R25如本文所定义），其是趋化因子受体活性的调节剂，并且可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及作为自身免疫性病变如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

100. 发明授权

US07557124B2 Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂
公开(公告)号：US07557124B2
公开(公告)日：2009-07-07
申请号：US11587288
申请日：2005-04-22
申请人： Lihu Yang , Sander G. Mills , Richard Jiao
发明人： Lihu Yang , Sander G. Mills , Richard Jiao
IPC分类号： C07D405/02 , C07D309/14 , A61K31/47 , A61K31/351
CPC分类号： C07D309/14 , C07D405/12
摘要： Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：式I化合物（其中n，R 1，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 15，R 16，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

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