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1. 发明申请

US20200291041A1 PCSK9 Inhibitors and Methods of Use Thereof 审中-公开
公开(公告)号：US20200291041A1
公开(公告)日：2020-09-17
申请号：US16744929
申请日：2020-01-16
申请人： Michael H. Serrano-Wu , Mark Chambers , Erica Goldsmith , Jason Tierney , Karamjit Jandu , David Clark , Paul Hinchliffe
发明人： Michael H. Serrano-Wu , Mark Chambers , Erica Goldsmith , Jason Tierney , Karamjit Jandu , David Clark , Paul Hinchliffe
IPC分类号： C07D491/107 , C07D417/12 , C07D417/14 , C07D487/10 , C07D498/04 , C07D471/10 , C07D471/04 , C07D401/14 , C07D403/14 , C07D495/04 , A61P9/00 , A61P3/06
摘要： The invention relates to novel heteroaryl compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.

2. 发明授权

US09056874B2 Complement pathway modulators and uses thereof 有权
公开(公告)号：US09056874B2
公开(公告)日：2015-06-16
申请号：US13826725
申请日：2013-03-14
申请人： Christopher Michael Adams , Charles Babu , Michael Paul Capparelli , Jian Ding , Takeru Ehara , Keith Jendza , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Liang Xue , Nello Mainolfi , James J. Powers , Michael H. Serrano-Wu , Chun Zhang
发明人： Christopher Michael Adams , Charles Babu , Michael Paul Capparelli , Jian Ding , Takeru Ehara , Keith Jendza , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Liang Xue , Nello Mainolfi , James J. Powers , Michael H. Serrano-Wu , Chun Zhang
IPC分类号： C07D403/06 , C07D403/04 , C07D403/08 , C07D403/14 , C07D401/14 , C07D413/14 , C07D487/04 , C07D491/048 , A61K31/4184 , C07D413/06 , A61K31/423 , A61K31/4439 , A61K45/06
CPC分类号： A61K31/4184 , A61K31/423 , A61K31/4245 , A61K31/4439 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/14 , C07D413/06 , C07D413/14 , C07D487/04 , C07D491/048
摘要： The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

3. 发明授权

US08846656B2 Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators 有权
标题翻译：四氢吡啶 - 吡啶和四氢吡啶 - 嘧啶化合物及其作为C5a受体调节剂的用途
公开(公告)号：US08846656B2
公开(公告)日：2014-09-30
申请号：US13553120
申请日：2012-07-19
申请人： Christopher Michael Adams , Veronique Darsigny , Alec Nathanson Flyer , Christine Fang Gelin , Timothy Brian Hurley , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Erik Meredith , Chang Rao , Michael H. Serrano-Wu , Catherine Fooks Solovay
发明人： Christopher Michael Adams , Veronique Darsigny , Alec Nathanson Flyer , Christine Fang Gelin , Timothy Brian Hurley , Nan Ji , Rajeshri Ganesh Karki , Toshio Kawanami , Erik Meredith , Chang Rao , Michael H. Serrano-Wu , Catherine Fooks Solovay
IPC分类号： C07D471/04 , C07D491/107 , C07D491/044 , C07D471/10 , C07D471/08
CPC分类号： C07D471/04 , C07D471/08 , C07D471/10 , C07D491/044 , C07D491/107
摘要： The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供式I化合物：（I）制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

4. 发明授权

US08835451B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US08835451B2
公开(公告)日：2014-09-16
申请号：US12295534
申请日：2007-03-28
申请人： Michael H. Serrano-Wu , Young-Shin Kwak , Wenming Liu
发明人： Michael H. Serrano-Wu , Young-Shin Kwak , Wenming Liu
IPC分类号： A01N43/40 , A61K31/435 , C07D475/00
CPC分类号： C07D413/10 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/76 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
摘要翻译：本发明提供以下结构的有机化合物; A-L1-B-C-D-L2-E，其可用于治疗或预防动物，特别是人类中与DGAT1活性相关的病症或障碍。

5. 发明申请

US20090181928A1 ORGANIC COMPOUNDS 有权
标题翻译：有机化合物
公开(公告)号：US20090181928A1
公开(公告)日：2009-07-16
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/695 , C07D285/10 , A61K31/433 , A61K31/454 , C07D417/10 , C07D417/12 , A61K31/55 , C07F7/10 , A61P3/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

6. 发明申请

US20200231584A1 PCSK9 Inhibitors and Methods of Use Thereof 审中-公开
公开(公告)号：US20200231584A1
公开(公告)日：2020-07-23
申请号：US16744932
申请日：2020-01-16
申请人： Michael H. Serrano-Wu , Brian K. Hubbard , Virendar Kaushik , Doug Daniels
发明人： Michael H. Serrano-Wu , Brian K. Hubbard , Virendar Kaushik , Doug Daniels
IPC分类号： C07D417/12 , C07D413/12 , C07D417/14 , C07D403/12
摘要： The invention relates to a novel inhibitor pharmacophore of PCSK9 and heteroaryl compounds that bind the PCSK9 protein.

7. 发明授权

US09061012B2 Uses of DGAT1 inhibitors 有权
标题翻译： DGAT1抑制剂的用途
公开(公告)号：US09061012B2
公开(公告)日：2015-06-23
申请号：US13637372
申请日：2011-03-29
申请人： Charles Meyers , Michael H. Serrano-Wu , Tom Thuren
发明人： Charles Meyers , Michael H. Serrano-Wu , Tom Thuren
IPC分类号： A61K31/44 , A61K31/42
CPC分类号： A61K31/42
摘要： The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.
摘要翻译：本发明涉及DGAT1抑制剂或其药学上可接受的盐或酯的用途，用于预防，延缓进行或治疗选自乳糜微粒综合征，家族性乳糜微粒综合征和V型高脂蛋白血症的疾病或病症。本发明还涉及包含DGAT1抑制剂或其药学上可接受的盐或酯的药物组合物在预防，延缓进行或治疗选自乳糜微粒综合症，家族性乳糜微粒综合征的疾病或病症中的用途和V型高脂蛋白血症。

8. 发明申请

US20130023495A1 USES OF DGAT1 INHIBITORS 有权
标题翻译： DGAT1抑制剂的用途
公开(公告)号：US20130023495A1
公开(公告)日：2013-01-24
申请号：US13637372
申请日：2011-03-29
申请人： Charles Meyers , Michael H. Serrano-Wu , Tom Thuren
发明人： Charles Meyers , Michael H. Serrano-Wu , Tom Thuren
IPC分类号： C07F9/38 , A61K31/444 , C07D413/10 , A61K31/4245 , A61P25/00 , A61P3/06 , A61P17/00 , A61P1/16 , A61P27/02 , C07D401/12 , A61K31/675
CPC分类号： A61K31/42
摘要： The present invention relates to the use of a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia. The present invention further relates to the use of a pharmaceutical composition comprising a DGAT1 inhibitor, or a pharmaceutically acceptable salt or ester thereof, for the prevention, delay of progression or treatment of a disease or condition which is selected from chylomicronemia syndrome, familial chylomicronemia syndrome and Type V hyperlipoproteinemia.
摘要翻译：本发明涉及DGAT1抑制剂或其药学上可接受的盐或酯的用途，用于预防，延缓进行或治疗选自乳糜微粒综合征，家族性乳糜微粒综合征和V型高脂蛋白血症的疾病或病症。本发明还涉及包含DGAT1抑制剂或其药学上可接受的盐或酯的药物组合物在预防，延缓进行或治疗选自乳糜微粒综合症，家族性乳糜微粒综合征的疾病或病症中的用途和V型高脂蛋白血症。

9. 发明授权

US08912208B2 (4-{4-[5-(benzooxazol-2-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid useful for treating or preventing conditions or disorders associated with DGAT1 activity 有权
标题翻译：（4- {4- [5-（苯并恶唑-2-基氨基） - 吡啶-2-基] - 苯基} - 环己基） - 乙酸，用于治疗或预防与DGAT1活性相关的病症或障碍
公开(公告)号：US08912208B2
公开(公告)日：2014-12-16
申请号：US13614666
申请日：2012-09-13
申请人： Michael H. Serrano-Wu , Young-shin Kwak , Wenming Liu
发明人： Michael H. Serrano-Wu , Young-shin Kwak , Wenming Liu
IPC分类号： A01N43/40 , A61K31/435 , C07D401/00
CPC分类号： C07D413/10 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K45/06 , C07D213/72 , C07D213/73 , C07D213/74 , C07D213/76 , C07D237/20 , C07D239/42 , C07D263/48 , C07D277/42 , C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention provides (4-{4-[5-(Benzooxazol-2-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid which is useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
摘要翻译：本发明提供（4- {4- [5-（苯并恶唑-2-基氨基） - 吡啶-2-基] - 苯基} - 环己基） - 乙酸，其可用于治疗或预防与DGAT1活性相关的病症或障碍在动物，特别是人类。

10. 发明授权

US08084448B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08084448B2
公开(公告)日：2011-12-27
申请号：US12295545
申请日：2007-03-29
申请人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
发明人： Alan Neubert , David Barnes , Young-Shin Kwak , Katsumasa Nakajima , Gregory Raymond Bebernitz , Gary Mark Coppola , Louise Kirman , Michael H. Serrano-Wu , Travis Stams , Sidney Wolf Topiol , Thalaththani Ralalage Vedananda , James Richard Wareing
IPC分类号： A61K31/55 , A61K31/445 , A61K31/41 , C07D487/00 , C07D401/00 , C07D285/10
CPC分类号： C07D285/10 , C07D417/10
摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
摘要翻译：式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，肌肉骨骼，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。

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