CAS: 153435-63-3; Tributyl(Pyrimidin-2-yl)Stannane

相似化合物

1277180-87-6 1447763-75-8 524019-27-0

上下游产品

tributylstannyllithium 2-bromopyrimidine 2-chloropyrimidine tri-n-butyl-tin hydride 2-phenylpyrimidine 2-(β-styryl)pyrimidine dimethyl(2-pyrimidyl)(vinyl)silane tert-butyl-diphenyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-4-pyrimidin-2-yl-pyrrole-2,5-dione3-{1-[3-(tert-butyl-diphenyl-silanyloxy)-propyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}-4-pyrimidin-2-yl-pyrrole-2,5-dione

专利信息

专利号:US-9295679-B2
优先权日:2008-03-25
标 题:Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity
发明人：NJAR VINCENT; BRODIE ANGELA; GEDIYA LALJI K
权利人:UNIV MARYLAND
摘要:Prodrugs of steroidal C-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at A ring portion of the ABC ring structure of the steroid. Suitable pro-drug groups include amino acid groups, succinate groups, phosphate groups, or sulfamate groups. The prodrugs of the disclosed compounds allow for improved oral bioavailability of the compounds that are inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds and the corresponding prodrugs are useful for the treatment of conditions such as human prostate cancer, breast cancer, and prostate hyperplasia.

专利号:US-10098896-B2
优先权日:2005-03-02
标 题:C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
发明人：BRODIE ANGELA; NJAR VINCENT C O
权利人:THE UNIV OF MARYLAND BALTIMORE; UNIV MARYLAND
摘要:Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-eliminationâ€? substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

专利号:WO-2010012637-A1
优先权日:2008-08-01
标题 :Process for the preparation of bosentan
发明人：RODRIGUEZ ROPERO SERGIO; HUGUET CLOTET JUAN
权利人:INKE SA; RODRIGUEZ ROPERO SERGIO; HUGUET CLOTET JUAN
摘要:The present invention provides a novel process for obtaining Bosentan, with few synthesis steps, by coupling the intermediate pyrimidine derivative of formula I with the sulfonamide derivative of formula II. The use of said process prevents the protection of the hydroxyl group of the sulfonamide II and thus is of considerable interest for obtaining Bosentan in a large industrial scale. The invention also refers to the intermediates of formula II and to a process for its production.

专利号:US-9018198-B2
优先权日:2008-03-25
标题 :Prodrugs of C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

专利号:US-7875599-B2
优先权日:2005-03-02
标题:C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
发明人：BRODIE ANGELA; NJAR VINCENT
权利人:UNIV MARYLAND
摘要:Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-eliminationâ€? substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

专利号:WO-2010039922-A1
优先权日:2008-10-03
标 题:Calcilytic compounds
发明人：CASILLAS LINDA N; CHARNLEY ADAM KENNETH; DEMARTINO MICHAEL P; DONG XIAOYANG; HARRIS PHILIP ANTHONY; MARQUIS ROBERT W JR; RAMANJULU JOSHI M; TROUT ROBERT
权利人:GLAXOSMITHKLINE LLC; CASILLAS LINDA N; CHARNLEY ADAM KENNETH; DEMARTINO MICHAEL P; DONG XIAOYANG; HARRIS PHILIP ANTHONY; MARQUIS ROBERT W JR; RAMANJULU JOSHI M; TROUT ROBERT
摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.