摘要:
A microorganism resistant to a threonine analogue, which has a plasmid containing part or whole of a biotin operon; and a process for producing biotin, which comprises culturing a microorganism described above in a medium to produce and accumulate biotin in the medium, and collecting biotin.
摘要:
A microorganism resistant to a threonine analogue, which has a plasmid containing part or whole of a biotin operon; and a process for producing biotin, which comprises culturing a microorganism described above in a medium to produce and accumulate biotin in the medium, and collecting biotin.
摘要:
A microorganism resistant to a nicotinic acid analogue, which has a plasmid containing part or whole of a biotin operon; and a process for producing biotin, which comprises culturing a microorganism described above in a medium to produce and accumulate biotin in the medium, and collecting biotin.
摘要:
The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译:本发明提供具有CCR拮抗剂活性,特别是CCR5拮抗剂活性的新的环状化合物及其用途。 本发明化合物由下式表示:其中,R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基,可以被取代的含氮杂环基等,或其盐。
摘要:
Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要:
A compound of the formula: wherein R1 is a 5- or 6-membered ring; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; W is a group represented by wherein R3 and R3′ are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n′ are each an integer of 0 or 1 to 4; m and m′ are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.
摘要翻译:下式的化合物:其中R 1是5或6元环; Z 1是5或6元芳环; Z 2是基团-Z 2 O 2 -W 2 -Z 2b 2,其中Z 2a 和/或O 2各自为O,S(O)q q(其中q为0,1或2),亚氨基或键; 和W 2是亚烷基链; W是由R 3和R 3'表示的基团各自为氢原子,低级烷基或低级烷氧基; X是CH或N; n和n'各自为0或1〜4的整数; m和m'分别为1或2; Y是O,S(O)p(其中p是0,1或2),CH 2或NR 4(其中R' SUP> 4 SUP>是氢原子,低级烷基或低级酰基); R 2是(1)可以将氮原子转化为季铵或氧化物的氨基,或者(2)可含有硫原子的含氮杂环基 或氧原子作为构成环的原子,其中氮原子可以转化为季铵或氧化物; 或其盐。 该化合物对CCR5表现出优异的CCR拮抗剂活性,并且可用作人外周血单核细胞(特别是AIDS)中HIV感染的预防和/或治疗剂。
摘要:
An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要:
Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
摘要:
Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.
摘要翻译:通式(1)的化合物或其盐,表现出对HIV感染性疾病的预防和治疗作用,其中R 1为任选取代的五元或六元环基团; X 1是自由价或类似物; W是由e表示的二价基团。 例如通式(2)(其中A和B各自为任选取代的五至七元环; E1和E4各自为任选取代的碳等; E2和E3各自为氧等; 和b各自为单键或双键); X 2是构成直链部分的二价基团; Z 1是二价的环状基团等; Z 2是自由价或类似物; 和R 2是任选取代的氨基等。
摘要:
This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof.