摘要:
Compositions containing adrenomedulin for inhibiting automatic uterine contraction or contraction caused by bradykinin. These compositions are usable for selectively inhibiting automatic uterine contraction or contraction caused by bradykinin, preventing premature birth, preventing abortion, ceasing delivery before cesarean section, or treating difficult menstruation.
a pharmaceutically acceptable salt or solvate thereof, wherein Ring Q is optionally substituted monocyclic aryl, optionally substituted monocyclic heteroaryl, optionally substituted fused aryl or optionally substituted fused heteroaryl, Y 1 is a bond or -NR 6 - or the like, Ring A is optionally substituted nonaromatic heterocyclediyl, a group of the formula: -Y 2 Z 1 - is a group of the formula:
or
R 7 are each independently hydrogen, optionally substituted lower alkyl or the like, R 8 and R 9 are each independently hydrogen or optionally substituted lower alkyl, n is an integer between 1 and 3, Z 1 is a bond, -O-, -S- or -NR 9 -, Ring B is optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl, Y 3 is a bond, optionally substituted lower alkylene optionally intervened by -O-, optionally substituted lower alkenylene or the like, and Z 2 is COOR 3 or the like.
摘要:
The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I)
wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.;R 1 , R 2 , R 3 , R 4 and R 5 are independently a hydrogen atom or a halogen atom etc.; R 6 is C2-C4 alkyloxy etc.; R 7 is independently a halogen atom etc.; R 8 is independently C1-C4 alkyl etc.; R 9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L 1 , L 2 and L 3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译:本发明产生具有DP受体拮抗活性的吲哚衍生物和包含所述化合物作为活性成分的药物组合物,还有用于治疗过敏性疾病的治疗剂。 通式(I)的化合物,其中环A是芳族碳环等; 环B为3〜8元含氮非芳香族杂环等; R 1,R 2,R 3,R 4和R 5独立地为氢原子或卤素原子等; R 6是C 2 -C 4烷氧基等。 R 7独立地为卤素原子等; R 8独立地为C 1 -C 4烷基等。 R 9为羧基等。 Y是单键等; M是磺酰基等。 L 1,L 2和L 3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q是0等 其药学上可接受的盐或水合物。
摘要:
Disclosed is a non-viral vector capable of delivering a given substance into the nucleus of a target cell effectively even when the target cells is a undividable cell such as a dendritic cell. A bilamellar liposome having a first lipid membrane and a second lipid membrane successively from the outside, the first lipid membrane having a membrane-fusing ability and the second lipid membrane having on its surface a nuclear transport peptide.
摘要:
An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).
摘要:
A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid µ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I):
(wherein R 1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R 2 and R 3 independently represent hydrogen, hydroxy or the like; R 4 is hydrogen, hydroxy or the like; R 5 is hydrogen; R 4 and R 5 may optionally form -O- or the like; R 6 represents hydrogen, lower alkyl or the like (wherein X represents -O- or -N(R 10 )-or the like; R 7 , R 8 , R 9a and R 9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents -CH- or the like; Z represents a crosslinkage composed of 2 to 5 atoms) or a pharmaceutically acceptable salt thereof or a solvate of either.
摘要翻译:一种由具有阿片样物质μ受体激动剂活性的化合物引起的便秘的治疗和/或预防剂,该药物包含作为有效成分的具有阿片受体拮抗剂活性的化合物,例如式(I)的化合物:(其中 R 1代表氢,低级烷基,环烷基低级烷基等; R 2和R 3独立地代表氢,羟基等; R 4是氢,羟基等; R 5是氢; R 4和R 5可以是 任选形成-O-等; R 6表示氢,低级烷基等(其中X表示-O-或-N(R 10) - 等; R 7,R 8,R 9a和R 9b独立地 表示氢,低级烷基,低级烷氧基羰基等; r表示0〜5的整数,Y表示-CH-等; Z表示2〜5个原子的交联键)或其药学上可接受的盐或溶剂合物 的任何一个。
摘要:
A CTGF expression inhibitor comprising a compound of the formula I:
a pharmaceutically acceptable salt or solvate thereof as an active ingredient, (wherein Y is hydroxy or a group of the formula: -NH-SO 2 -Y' (wherein Y' is optionally substituted aryl or optionally substituted alkyl), and R 1 to R 9 are each independently hydrogen, halogen, optionally substituted alkyl, optionally substituted alkoxy or the like).
摘要:
The present invention provides a process for the preparation of a bicyclic aminoalcohol which comprises reacting a starting compound, nopinone (I), with XCH 2 COOR 1 wherein X is halogen, and R 1 is alkyl, in the presence of an additive and a base to produce a compound (II), converting it to oxime derivative (III), and reducing it with an aluminum hydride.
摘要:
The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):
wherein R 1 is optionally substituted C1-C8 alkyl and the like; R 2 is C1-C6 alkyl; R 3 is C1-C6 alkyl and the like; or R 2 and R 3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R 4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like:
wherein R 5 is hydrogen and the like; X 1 is a single bond and the like; X 2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of -O-, or -N(R 6 )-, wherein R 6 is hydrogen and the like, and the like; X 3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
摘要翻译:本发明提供对大麻素受体具有激动作用的化合物,其由式(I)表示:其中R 1为任选取代的C 1 -C 8烷基等; R 2是C 1 -C 6烷基; R 3是C 1 -C 6烷基等; 或R 2和R 3可以一起形成任选取代的5至10元非芳族碳环; R 4是氢等; G为选自下式的基团:其中R 5为氢等; X 1是单键等; X 2是可以被一个或两个-O-或-N(R 6) - 基团取代的任选取代的C 1 -C 8亚烷基,其中R 6是氢等; X 3是单键等; 其药学上可接受的盐或溶剂合物,以及药物组合物,特应性皮炎治疗剂和抗瘙痒剂,特别是用于口服使用和外用的抗瘙痒剂,其各自含有所述化合物作为活性成分。
摘要:
A medical container comprising a body for containing a medicament, the body of the medical container being formed of a multilayered film comprising (i) a layer formed of a linear polyolefin and (ii) a layer formed of a cyclic polyolefin adjacent to the layer (i), and the layer (i) formed of the linear polyolefin satisfying the following conditions (a) and/or (b): Condition (a): an amount of a liquid component, which remains after Soxhlet's extraction with organic solvents followed by evaporation of the solvenst, is 0.2% by weight or less, and Condition (b): a branching degree of a component, which remains after Soxhlet's extraction with n-hexane followed by evaporation of n-hexane, is 50 or less per 1,000 carbon atoms.