摘要:
A pyrrolidine derivative, which is an intermediate for a quinuclidine derivate side chain useful as a squalene synthase inhibitor, and producing method thereof are disclosed. A pyrrolidine derivative (X) represented by the following formula (X) (wherein R 1 and R 2 each represents a hydroxy group, C 1-6 alkoxy groups or the like; R 3 represents a hydrogen atom, a benzyl group or the like); or a salt thereof or a hydrate thereof:
an industrially-excellent and novel process for producing a basic antibiotic·inorganic acid salt, for example, an excellent production process for producing a hydrochloride thereof industrially, that is, a production process which comprises subjecting a basic antibiotic·oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: (wherein the ring A means the basic antibiotic; R 10 means a protected functional group used in organic synthesis; Ak-E means the alkali earth metal; and B means the inorganic acid, respectively); a novel oxalate useful as a production intermediate for producing an antibiotic·hydrochloride industrially, that is, an oxalate (II-I) of a carbapenem compound represented by the following formula: (wherein the ring A represents a 3- to 7-membered ring having at least one nitrogen atom, and the ring A may be substituted with other than R 6 ; R 1 represents hydrogen or methyl group; R 2 and R 5 are the same as or different form each other and each represents hydrogen or a hydroxyl-protecting group; R 3 represents a carboxyl-protecting group; R 4 represents hydrogen, a lower alkyl group or an amino-protecting group; R 6 represents (1) hydrogen, (2) an optionally protected hydroxyl group, carbamoyl, formimidoyl, acetoimidoyl or a lower alkyl group which may be substituted with a substituent represented by the formula: (wherein R 7 and R 8 are the same as or different from each other and each represents hydrogen, a lower alkyl group or an amino-protecting group) or (3) an amino-protecting group or an imino-protecting group; and m is 0 or 1); and a process for producing its.
摘要翻译:本发明提供:在工业上优和新方法用于生产基本antibiotic.inorganic酸的盐,例如,优良的生产过程用于制备盐酸盐在工业上,所做的是,一个生产过程,它包括使一个基本antibiotic.oxalate (II)盐交换与碱土金属盐(III)的无机酸的:(worin环的装置的基本抗生素; R <10>表示在有机合成中使用的保护的官能基团; AK- E表示碱土金属;且B是指无机酸,分别地); 一种新颖的草酸作为生产用于在antibiotic.hydrochloride生产工业上,做了中间有用是草酸盐(II-I)由下式表示的碳代青霉烯化合物:( worin环A darstellt 3-至7- 具有元环的至少一个氮原子,且环A可与其它除R <6> R上substituiertem <1> darstellt氢或甲基; R <2>和R <5>是相同的或不同 形成,且分别darstellt氢或羟基保护基; R <3>表示羧基保护基; R <4> darstellt氢,低级烷基或氨基保护基的; R <6> darstellt(1 )氢,(2)任选被保护的羟基,氨基甲酰基,亚胺甲基,acetoimidoyl或可被由下式表示的取代基所substituiertem的低级烷基:(worin - [R <7>和R <8>是 相同或彼此和各darstellt氢,低级烷基或氨基保护基),或者(3个不同的 )氨基保护基或亚氨基保护的基团; 且m是0或1); 和用于生产其的过程。
摘要:
Cephalosporin derivatives represented by general formula (I) [wherein R 1 represents a lower alkyl group, A represents (II) (wherein R 2 and R 3 may be the same or different and each represents a lower alkyl group, and R 4 represents a substituted lower alkyl group or an amino group), an optionally substituted group represented by formulae (III), (IV), (V) (wherein Rs represents a lower alkyl group] or a group of formula (VI) (wherein R 5 is the same as defined above and R 6 represents a hydroxy- lower alkyl group or a carboxyl group)] and pharmaceutically acceptable salts thereof, processes for their preparation, and antibacterial agents containing them.
摘要:
The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I): (wherein R 1 represents e.g. an amino group which may be substituted with an alkyl group; R 2 represents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; R 3 represents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.
摘要:
Cephalosporin derivatives represented by general formula (I), (wherein R1 represents a lower alkyl group, A represents (II) (wherein R2 and R3 may be the same or different and each represents a lower alkyl group, and R4 represents a substituted lower alkyl group or an amino group), an optionally substituted group represented by formulae (III), (IV), (V) (wherein R5 represents a lower alkyl group) or a group of formula (VI) (wherein R5 is the same as defined above and R6 represents a hydroxy-lower alkyl group or a carboxyl group)) and pharmaceutically acceptable salts thereof, processes for their preparation, and antibacterial agents containing them.
摘要:
An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein A is a basic antibiotic; R10 is a protected functional group to be used in organic synthesis; Ak-E is an alkaline earth metal; and B is an inorganic acid; carbapenem derivative-oxalic acid addition salts represented by general formula (II-I) and being useful as intermediates for the preparation of hydrochlorides of antimicrobial agents; and a process for preparing the same, (II-I) wherein A is a three- to seven-membered ring having at least one nitrogen atom; R1 is hydrogen or the like; R?2 and R5¿ are each hydrogen or a protecting group; R3 is a protecting group; R4 is hydrogen or the like; and R6 is hydrogen or the like.
摘要:
The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -D---E- represents a group represented by -CH 2 CH 2 - or -CH=CH-; W reprensents a group represented by -CH 2 -, - CH z CH 2 -, -CH=CH- or -CH=; the partial structure >X---Y- represents a group represented by >CH-(CH 2 ) n -, >C=CH-, >CH-CH 2 -CH(OH)-, >CH-CH 2 -C (=O) -, >CH-O- or >CH-O-CO-, provided that when W is -CH=, then X---Y- represents C-(CH 2 ) p -; Z represents a divalent aliphatic hydrocarbon group; R 1 and R 2 , which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1] .