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公开(公告)号：US20150239866A1
公开(公告)日：2015-08-27
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US09586931B2
公开(公告)日：2017-03-07
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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3.发明申请公开(公告)号：US20150299125A1
公开(公告)日：2015-10-22
申请号：US14440517
申请日：2013-11-04
申请人： Andrew M. HAIDLE , Brandon CASH , James P. JEWELL , Kerrie SPENCER , Michael D. ALTMAN , Ryan D. OTTE , Alan B. NORTHRUP , MERCK SHARP & DOHME CORP.
发明人： Andrew M. Haidle , Brandon Cash , James P. Jewell , Kerrie Spencer , Michael D. Altman , Ryan D. Otte , Alan B. Northrup
IPC分类号： C07D213/74 , C07D401/14 , C07D405/14
CPC分类号： C07D213/74 , C07D401/14 , C07D405/14 , C07D451/10 , C07H13/08
摘要： The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer.
摘要翻译： 本发明提供式（I）化合物，其为反式-4 - [（1R） - （6 - {[4-（二氟甲基）吡啶-2-基]氨基} -4-甲基-2,3 “ - 联吡啶-6'-基）-1-羟乙基]环己烷羧酸，Syk的有效抑制剂。 该化合物可用于治疗和预防由酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20100256097A1
公开(公告)日：2010-10-07
申请号：US12665045
申请日：2008-06-16
申请人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyan Chong Woo , Jonathan Young , Anna Zabierek
发明人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyan Chong Woo , Jonathan Young , Anna Zabierek
IPC分类号： A61K31/675 , C07D409/14 , A61K31/4439 , A61K31/4436 , C07D413/14 , A61K31/5377 , C07D409/12 , A61K31/501 , C07F9/28 , C07D417/14 , A61K31/541
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：US08367706B2
公开(公告)日：2013-02-05
申请号：US12665045
申请日：2008-06-16
申请人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
发明人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
IPC分类号： A61K31/4436 , C07D409/12
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：US10370368B2
公开(公告)日：2019-08-06
申请号：US15768097
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： A61K9/20 , A61P3/10 , C07D417/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US10450309B2
公开(公告)日：2019-10-22
申请号：US15769079
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Phieng Siliphaivanh , Kerrie Spencer , Satyanarayana Tummanapalli
IPC分类号： A61K31/35 , A61P3/10 , C07D311/22 , C07D311/58 , C07D405/14 , C07D417/14
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US20180291017A1
公开(公告)日：2018-10-11
申请号：US15768097
申请日：2016-11-28
申请人： Yongxin HAN , Phieng SILIPHAIVANH , Kerrie SPENCER , Satyanarayana TUMMANAPALLI , Merck Sharp & Dohme Corp.
IPC分类号： C07D417/14 , A61P3/10
CPC分类号： C07D417/14 , A61K9/2054 , A61P3/10
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatohepatitis, metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US20180305342A1
公开(公告)日：2018-10-25
申请号：US15767371
申请日：2016-11-28
申请人： Yongxin HAN , Jongwon LIM , Phieng SILIPHAIVANH , Kerrie SPENCER , Satyanarayana TUMMANAPALLI , Merck Sharp & Dohme Corp.
IPC分类号： C07D405/06 , C07D311/22 , C07D417/06 , C07D413/06
CPC分类号： C07D405/06 , A61K9/2054 , A61K31/353 , C07D311/22 , C07D413/06 , C07D417/06
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension. Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis metabolic syndrome, atherosclerosis, and cancer.
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公开(公告)号：US10336733B2
公开(公告)日：2019-07-02
申请号：US15767371
申请日：2016-11-28
申请人： Merck Sharp & Dohme Corp. , Yongxin Han , Jongwon Lim , Satyanarayana Tummanapalli , Phieng Siliphaivanh , Kerrie Spencer
IPC分类号： C07D417/06 , C07D413/06 , C07D311/22 , C07D405/06 , A61K31/353 , A61K9/20
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are antagonists of leukotriene B4 receptor 1 (BLT1) and may be useful in the treatment, prevention and suppression of diseases mediated by the leukotriene B4 receptor 1 (BLT1). The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, insulin resistance, hyperglycemia, dyslipidemia, lipid disorders, obesity, hypertension, Non-alcoholic fatty liver disease/nonalcoholic steatoepatitis, metabolic syndrome, atherosclerosis, and cancer.
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