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公开(公告)号：US10738074B2
公开(公告)日：2020-08-11
申请号：US15752144
申请日：2016-08-11
申请人： Merck Sharp & Dohme Corp. , Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
发明人： Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong
IPC分类号： A01N43/04 , A61K31/70 , C07H21/04 , C07H21/02 , A61K39/39 , C07H19/20 , C07H19/23 , C07H21/00 , A61P35/00 , A61K31/7064 , A61K31/7084 , A61K31/708 , A61K31/706 , A61K31/7076
摘要： A class of polycyclic compounds of general formula (II), of general formula (II′), or of general formula (II″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
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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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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：US20120309735A1
公开(公告)日：2012-12-06
申请号：US13515941
申请日：2010-12-16
申请人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号： A61K31/506 , C07D417/12 , C07D417/14 , C07D471/04 , A61P19/02 , A61K31/551 , A61P11/06 , A61P11/00 , A61P29/00 , C07D471/10 , A61K31/5377
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎。
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公开(公告)号：US08101603B2
公开(公告)日：2012-01-24
申请号：US11827109
申请日：2007-07-09
IPC分类号： A61K31/535 , A61K31/44 , C07D221/00 , C07D471/04 , C07D413/14
CPC分类号： C07D221/16 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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6.发明授权Enantioselective transformation of α,β-unsaturated ketones using chiral organic catalysts 有权使用手性有机催化剂对α，β-不饱和酮的对映选择性转化公开(公告)号：US07592463B2
公开(公告)日：2009-09-22
申请号：US10313744
申请日：2002-12-05
IPC分类号： C07D233/28 , C07D235/02 , C07C45/69
CPC分类号： C07D405/04 , B01J31/0237 , B01J31/0247 , B01J2231/326 , C07B2200/07 , C07C45/69 , C07C49/543 , C07C49/553 , C07C49/557 , C07C49/577 , C07C49/643 , C07C269/06 , C07D233/32 , C07C271/24
摘要： Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of α,β-unsaturated ketones. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA) or (IIB) or are acid addition salts thereof, wherein, in one preferred embodiment, R1 is C1-C6 alkyl, R2 is phenyl or 2-methylfuryl, R3 and R4 are hydrogen, and R5 is phenyl optionally substituted with 1 or 2 substituents selected from the group consisting of halo, hydroxyl, and C1-C6 alkyl. The chiral imidazolidinones are useful in catalyzing a wide variety of reactions, including cycloaddition reactions, Friedel-Crafts alkylation reactions, and Michael additions.
摘要翻译： 提供了促进α，β-不饱和酮的对映选择性反应的非金属有机催化剂。 催化剂是具有式（IIA）或（IIB）结构的手性咪唑烷酮化合物或其酸加成盐，其中在一个优选的实施方案中，R 1是C 1 -C 6烷基，R 2是苯基或2-甲基呋喃基，R 3和R 4 是氢，R5是任选被1或2个选自卤素，羟基和C 1 -C 6烷基的取代基取代的苯基。 手性咪唑烷酮可用于催化多种反应，包括环加成反应，Friedel-Crafts烷基化反应和迈克尔加成。
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公开(公告)号：US20090012076A1
公开(公告)日：2009-01-08
申请号：US11827109
申请日：2007-07-09
IPC分类号： A61K31/5377 , C07D221/06 , A61K31/435 , C07D471/04 , A61P35/00 , A61K31/4375 , C07D413/14
CPC分类号： C07D221/16 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US06900357B2
公开(公告)日：2005-05-31
申请号：US10420339
申请日：2003-04-21
IPC分类号： C07C29/143 , C07C45/72 , C07D309/10
CPC分类号： C07D309/10 , C07B2200/07 , C07C29/143 , C07C45/72 , C07C2601/14 , C07C47/27 , C07C47/192 , C07C47/19 , C07C33/025 , C07C33/035 , C07C33/14 , C07C33/30
摘要： Nonmetallic, chiral organic catalysts are used to catalyze an enantioselective aldol coupling reaction between aldehyde substrates. The reaction may be carried out with a single enolizable aldehyde, resulting in dimerization to give a β-hydroxy aldehyde, or trimerization to give a dihydroxy tetrahydropyran. The reaction may also conducted with an enolizable aldehyde and a second aldehyde, which may or may not be enolizable, so that the coupling is a cross-aldol reaction in which the α-carbon of the enolizable aldehyde adds to the carbonyl carbon of the second aldehyde in an enantioselective fashion. Reaction systems composed of at least one enolizable aldehyde, an optional additional aldehyde, and the nonmetallic chiral organic catalyst are also provided, as are methods of implementing the enantioselective aldol reaction in the synthesis of sugars.
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公开(公告)号：US09822107B2
公开(公告)日：2017-11-21
申请号：US15105713
申请日：2014-12-18
申请人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier , MERCK SHARP & DOHME CORP.
发明人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier
IPC分类号： C07D417/12 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
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公开(公告)号：US20170217981A1
公开(公告)日：2017-08-03
申请号：US15515377
申请日：2015-09-25
申请人： Craig R. GIBEAU , Solomon D. KATTAR , Charles A. KATTAR , Jongwon LIM , John K. MACLEAN , Umar F. MANSOOR , Alan B. NORTHRUP , John M. SANDERS , Graham F. SMITH , MERCK SHARP & DOHME CORP.
发明人： MICHAEL D. ALTMAN , JASON D. BRUBAKER , MATTHEW L. CHILDERS , ANTHONY DONOFRIO , THIERRY FISCHMANN , CRAIG R. GIBEAU , SOLOMON D. KATTAR , CHARLES A. LESBURG , JONGWON LIM , JOHN K.F. MACLEAN , UMAR F. MANSOOR , ALAN B. NORTHRUP , JOHN M. SANDERS , GRAHAM F. SMITH
IPC分类号： C07D491/08 , A61K31/517 , A61K45/06 , C07D239/88 , A61K31/5377 , C07D403/12 , C07D401/12 , C07D413/12 , A61K31/538 , C07D491/052 , A61K31/5386 , C07D491/048 , A61K31/55 , C07D405/12 , C07D239/94
CPC分类号： C07D491/08 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D491/048 , C07D491/052 , C07D498/08 , A61K2300/00
摘要： The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibutors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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