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1. 发明申请

WO1994019351A1 2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM 审中-公开
标题翻译： 2-苄基 - 多环烷酸衍生物及其制备方法
公开(公告)号：WO1994019351A1
公开(公告)日：1994-09-01
申请号：PCT/US1994001728
申请日：1994-02-24
申请人： SCHERING CORPORATION , TULSHIAN, Deen , McKITTRICK, Brian, A. , XIA, Yan , CHACKALAMANNIL, Samuel , GALA, Dinesh , DIBENEDETTO, Donald, J. , KUGELMAN, Max
发明人： SCHERING CORPORATION
IPC分类号： C07D487/14
CPC分类号： C07D487/14 , C07D239/54 , C07D473/40
摘要： Antihypertensive and bronchodilating compounds of formula (I) or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R1, R2 and R3 are hydrogen, lower alkyl, lower alkoxy, halogeno, hydroxy, (di-lower alkyl)amino, 4-morpholinyl, 1-pyrrolidinyl, 1-pyrrolyl, -CF3, -OCF3, phenyl or methoxyphenyl; or R1 and R2 together are methylenedioxy; or R1 and R2 together with the carbon atoms to which they are attached form a benzene ring; and R is hydrogen and R and R , together with the carbon atoms to which they are attached, form a saturated ring of 5 carbons; or R is lower alkyl, R is hydrogen or lower alkyl, and R is hydrogen; or R , R and the carbon atom to which they are attached form a saturated ring of 5-7 carbons, and R is hydrogen; or R is hydrogen, and R , R and the carbon atoms to which they are attached form a tetrahydrofuran ring; or R and R , together with the carbon atom to which they are attached, and R and R , together with the carbon atoms to which they are attached, each form a saturated ring of 5-7 carbons; pharmaceutical compositions containing said compounds: methods of treatment using said compounds; and a process for preparing polycyclic guanines comprising a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.
摘要翻译：公开了式（I）的抗高血压药和支气管扩张剂化合物或其药学上可接受的盐及其制备方法，其中：R1，R2和R3为氢，低级烷基，低级烷氧基，卤代，羟基，（二低级烷基）氨基，4-吗啉基，1-吡咯烷基，1-吡咯基，-CF3，-OCF3，苯基或甲氧基苯基; 或R 1和R 2一起是亚甲二氧基; 或R 1和R 2与它们所连接的碳原子一起形成苯环; 和R a是氢，R和R c连同它们所连接的碳原子一起形成5个碳原子的饱和环; 或R a是低级烷基，R b是氢或低级烷基，R c是氢; 或R a，R b和它们所连接的碳原子形成5-7个碳原子的饱和环，R c是氢; 或R a是氢，R b，R c和它们所连接的碳原子形成四氢呋喃环; 或R a和R b与它们所连接的碳原子一起，和R和R c连同它们所连接的碳原子一起形成饱和的环 5-7个碳; 含有所述化合物的药物组合物：使用所述化合物的治疗方法; 以及制备多环鸟嘌呤的方法，包括a）还原亚硝基嘧啶，用酰化试剂处理还原的亚硝基嘧啶，得到酰胺嘧啶; b）使酰胺嘧啶与卤化/环化试剂反应得到卤代嘌呤; c）在碱的存在下使卤代嘌呤与胺反应，得到取代的氨基嘌呤; 和d）用合适的脱水剂封闭取代的氨基嘌呤的环。

2. 发明申请

WO1993007289A1 ENZYMATIC SYNTHESIS OF CHIRAL 'alpha'-HYDROXYKETONES AND DERIVATIVES 审中-公开
标题翻译：丙氨酸（ALPHA） - 羟基酮和衍生物的酶合成
公开(公告)号：WO1993007289A1
公开(公告)日：1993-04-15
申请号：PCT/US1992008168
申请日：1992-10-01
申请人： SCHERING CORPORATION , GALA, Dinesh
发明人： SCHERING CORPORATION
IPC分类号： C12P41/00
CPC分类号： C12P41/004 , C12P7/26 , C12P7/62
摘要： A process for the preparation of a chiral α-hydroxyketone, or ester thereof, comprising hydrolyzing an ester of said α-hydroxyketone with an enzyme that has a specificity for one enantiomer, or by esterifying said α-hydroxyketone with an esterifying agent in the presence of an enzyme that favors one enantiomer.

3. 发明申请

WO1992017433A1 PREPARATION OF CHIRAL HYDROXYKETONES 审中-公开
标题翻译：精制羟基酮的制备
公开(公告)号：WO1992017433A1
公开(公告)日：1992-10-15
申请号：PCT/US1992002231
申请日：1992-03-25
申请人： SCHERING CORPORATION , GALA, Dinesh
发明人： SCHERING CORPORATION
IPC分类号： C07C45/64
CPC分类号： C07D309/12 , C07C45/46 , C07C45/64 , C07C49/807 , C07C49/82
摘要： A process for preparing an hydroxyketone of formula (X); wherein Ar represents substituted phenyl, aromatic heterocyclic, or substituted aromatic heterocyclic; R and R independently represents hydrogen, C-1 to C-16 alkyl, aromatic, substituted aromatic, aromatic heterocyclic, substituted aromatic heterocyclic or C-1 to C-5 alkyl covalently bonded to Ar, with the provision that R and R are different. The process comprises contacting a compound of formula (V) with a solvent, a base and a chiral hydroxylating agent at a temperature of about -85 DEG C or less. Compounds of formulae (I) and (II) also are disclosed.
摘要翻译：制备式（X）的羟基酮的方法; 其中Ar表示取代的苯基，芳族杂环或取代的芳族杂环; R 1和R 2独立地表示氢，C 1至C 16烷基，芳族，取代的芳族，芳族杂环，取代的芳族杂环或与Ar共价结合的C-1至C-5烷基， R 1和R 2不同。该方法包括在约-85℃或更低的温度下使式（V）化合物与溶剂，碱和手性羟基化试剂接触。还公开了式（I）和（II）的化合物。

4. 发明申请

WO1996033178A1 PROCESS FOR THE PREPARATION OF TRIAZOLONES 审中-公开
标题翻译：制备三唑的方法
公开(公告)号：WO1996033178A1
公开(公告)日：1996-10-24
申请号：PCT/US1996005170
申请日：1996-04-17
申请人： SCHERING CORPORATION , ANDREWS, David, R. , GALA, Dinesh , GOSTELI, Jacques , GUENTER, Frank , LEONG, William , MERGELSBERG, Ingrid , SUDHAKAR, Anantha
发明人： SCHERING CORPORATION
IPC分类号： C07D249/12
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/12
摘要： A process for preparing triazolone compounds of formula (i) comprises heating a mixture of a compound of formula (ii) and a hydrazine derivative of the formula R -NH-NH-CHO, R -NH-NH-C(O)OC(CH3)3 or R -NH-NH-C(O)OCH2C6H5, optionally in the presence of an added base.
摘要翻译：制备式（i）的三唑酮化合物的方法包括加热式（ⅱ）化合物和式R 5 -NH-NH-CHO，R 5 -NH-NH- C（O）OC（CH 3）3或R 5 -NH-NH-C（O）OCH 2 C 6 H 5，任选地在加入的碱的存在下。

5. 发明申请

WO2020100011A1 IMPROVED SYNTHETIC METHODS OF MAKING FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2020100011A1
公开(公告)日：2020-05-22
申请号：PCT/IB2019/059677
申请日：2019-11-11
申请人： JANSSEN PHARMACEUTICA NV , GALA, Dinesh
发明人： GALA, Dinesh , DEPRÉ, Dominique Paul Michel , MATCHA, Kiran , HUYGAERTS, Andy Josephina Joannes , MOENS, Luc Jozef Raphael
IPC分类号： A61K31/506 , C07D263/08 , C07D487/04
摘要： Processes for preparing (((3a R ,6a S )-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1 H )-yl)(2-fluoro-6-(2 H -1,2,3-triazol-2-yl)phenyl)methanone are described, which are useful for commercial manufacturing. Said compound is an orexin receptor modulator and may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia and depression.

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