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610791-05-4 757239-60-4 36476-78-5欧盟法规
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CAS号53871-06-0 1-二苯甲基氮杂环丁烷-3-甲酸甲酯 | CAS号67-56-1 甲醇 | CAS号36476-78-5 3-吖丁啶羧酸 | CAS号610791-05-4 N-B°C-氮杂环丁烷-3-甲酸甲酯 | CAS号757239-60-4 1-Cbz-氮杂环丁烷-3-甲酸甲酯合成工艺路线路线简述
- 合成目标产物 3-Azetidinecarboxylic Acid, Methyl Ester, Hydrochloride 主要起始原料 Methanol And 3-Azetidinecarboxylic Acid
- (文献来源)合成步骤主要原料 Methanol 和 3-Azetidinecarboxylic Acid
3-吖丁啶羧酸置于三甲基氯硅烷体系中,用 甲醇 用作溶剂,以100%的收率获得氮杂环丁烷-3-甲酸甲酯盐酸盐
参考文献:Inhibitors Of Human Glycogen Phosphorylase
标题:Inhibitors Of Human Glycogen Phosphorylase
摘要:本发明涉及一种在糖原磷酸化酶酶内发现的新型糖原磷酸化酶抑制剂结合位点.该新型结合位点使得能够设计新型的糖原磷酸化酶抑制剂.
专利信息
专利号:WO-2018108954-A1
优先权日:2016-12-12
标题 :Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol
发明人:GOSSELIN FRANCIS; LINGHU XIN
权利人:HOFFMANN LA ROCHE; GENENTECH INC
摘要:Methods of making 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 9, an intermediate useful for the synthesis of estrogen receptor modulating compounds are described.
专利号:US-7816375-B2
优先权日:2000-09-11
标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof
发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-11066395-B2
优先权日:2016-09-30
标题:Dimethylaminoethanol salt of a GLP-1 receptor modulator
发明人:VIDAL EPHRAIM; BAKALE ROGER; TURNBULL PHILIP; MOSER DAVID; ROBBINS ANDREW; GRANT CRAIG
权利人:RECEPTOS LLC
摘要:Crystalline 2-hydroxy-N,N-dimethylethanaminium 1-(2-(5-(tert-butyl)-thiophene-2-carboxamido)-3-(4-(5-(4′-ethyl-[1,1′-bi(cyclohexan)]-3-en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same.
专利号:US-9839664-B2
优先权日:2014-07-25
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
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), GLP-1(9-36), and oxyntomodulin, 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, R 1 , R 2 , R 3 , R 4 , R 5 , n, p and q are as defined herein.
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.
专利号:US-9428490-B2
优先权日:2011-07-29
标 题 :Nuclear transport modulators and uses thereof
发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD
权利人:SANDANAYAKA VINCENT P; SHACHAM SHARON; KAUFFMAN MICHAEL; SHECHTER SHARON; MCCAULEY DILARA; LANDESMAN YOSEF; SENAPEDIS WILLIAM; SAINT-MARTIN JEAN-RICHARD; KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.