专利号:US-6492529-B1 优先权日:2000-01-18 标题 :Bis pyrazole-1H-pyrazole intermediates and their synthesis 发明人:KAPADIA SURESH R; SONG JINHUA J; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are aromatic heterocyclic compounds of the formula (I) wherein Ar 1 , Ar 2 , L, Q and X are described herein, and intermediate compounds useful for making such compounds. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. n Also disclosed are processes of making compounds of the formula (I), their intermediates and processes of making such intermediates, including bis pyrazole-1H-pyrazole intermediates of the formula: n wherein Alk, R x and R z are described herein.
专利号:US-9012445-B2 优先权日:2012-01-12 标题 :Substituted 4-(1H-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of mAChR M1 receptors 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; POSLUSNEY MICHAEL S; TARR JAMES C 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-6017926-A 优先权日:1997-12-17 标题 :Integrin receptor antagonists 发明人:ASKEW BEN C; COLEMAN PAUL J; DUGGAN MARK E; HALCZENKO WASYL; HUTCHINSON JOHN H; MEISSNER ROBERT S; PATANE MICHAEL A; WANG JIABING 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alpha v beta 3, alpha v beta 5 and/or alpha v beta 6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.
专利号:US-8962616-B2 优先权日:2012-05-04 标 题:Heterocyclic substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10316018-B2 优先权日:2015-08-27 标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators 发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG 权利人:PFIZER 摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9795613-B2 优先权日:2014-12-10 标题 :GLP-1 receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK 权利人:CELGENE INT II SÀRL 摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.
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