📜4,6-二甲基-5-硝基嘧啶-2-醇置于palladium 10% On Activated Carbon,氢气,三氯氧磷体系中,用 乙醇 作为反应溶剂,化学反应 10.0H,反应生成 5-氨基-4,6-二甲基嘧啶 参考文献: Pyrazolopyridines Useful In The Treatment Of Disorders Of The Central Nervous System[fr] Pyrazolopyridines Utiles Dans Le Traitement De Troubles Du Système Nerveux Central 标题: Pyrazolopyridines Useful In The Treatment Of Disorders Of The Central Nervous System[fr] Pyrazolopyridines Utiles Dans Le Traitement De Troubles Du Système Nerveux Central 摘要:本发明涉及在治疗中有用的化合物,包括含有这些化合物的组合物,以及治疗疾病的方法,包括给予这些化合物的管理.所指的化合物是尼古丁乙酰胆碱α7受体的正向变构调节剂(pams).
专利信息
专利号:US-4800207-A 优先权日:1987-11-02 标题:Hexahydropyrrolizine compounds useful as analgesics 发明人:CARMOSIN RICHARD J; CARSON JOHN R 权利人:MCNEILAB INC 摘要:Hexahydropyrrolizines of the formula (I): (I) wherein A is a 3-7 carbon or hetero-containing ring, R1 is a substituent, and x is 0-3. Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.
专利号:US-4716172-A 优先权日:1986-04-10 标 题 :4-substituted octahydroquinolizine analgesic compounds and octahydroquinolizinium intermediates 发明人:CARMOSIN RICHARD J; CARSON JOHN R 权利人:MCNEILAB INC 摘要:Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): where A is a 3 to 7 membered carbocyclic ring, R1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.
专利号:US-4689329-A 优先权日:1986-02-04 标 题:5-substituted octahydroindolizine analgesics compounds and 7-keto intermediates 发明人:CARMOSIN RICHARD J; CARSON JOHN R 权利人:MCNEILAB INC 摘要:Octahydroindolizidines and corresponding ketones of the formulae (I) and (II): (I) (II) where A is a 3-7 carbon or hetero-containing ring, R1 is a substituent, n is 0-6 and x is 0-3. Also, pharmaceutical compositions for treating pain containing (I) or (II) and methods for synthesis and use as well as novel intermediates in the synthesis.
专利号:US-4582836-A 优先权日:1985-01-09 标 题:Octahydroindolizine compounds useful as analgesics 发明人:CARMOSIN RICHARD J; CARSON JOHN R 权利人:MCNEILAB INC 摘要:Octahydroindolizidines of the formula (I): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R 1 is a substituent and x is 0-3. Also, pharmaceutical composition for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.
专利号:US-2004138238-A1 优先权日:2002-08-08 标题 :Substituted aminopyrimidine compounds as neurokinin antagonists 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY 摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:US-5728695-A 优先权日:1994-12-23 标题 :Spiroketal derivatives, compositions containing them and their use as therapeutic agents 发明人:HARRISON TIMOTHY; OWEN SIMON NEIL; SEWARD EILEEN MARY; SWAIN CHRISTOPHER JOHN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to spiroketal derivatives of formula (I) and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 9a , R 9b , m and n are as defined in the specification, and to processes for their preparation, to intermediates used in their synthesis, to pharmaceutical compositions containing them, and to their use in therapy. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia. ##STR1##
参考文献:10.1007/bf00742848 摘要:Dubovenko ZD, Mamaev VP. Pyrimidines. 72. Synthesis and some properties of 5-amino-2-r-4,6-diphenylpyrimidines and the products of their transformations. Chemistry of Heterocyclic Compounds. 1980 Sep;16(9):970–3. doi: 10.1007/bf00742848. 参考文献:10.1007/bf00742847 摘要:Kost AN, Terenin VI, Yudin LG, Sagitullin RS. Recyclization of 3-alkyl- and 1,3-dialkylisoquinolinium salts to naphthylamines. Chemistry of Heterocyclic Compounds. 1980 Sep;16(9):965–70. doi: 10.1007/bf00742847.