摘要:
Drugs containing prostaglandins or pharmaceutically acceptable salts thereof as the active ingredient which have an antipruritic effect with little side effects and can efficaciously regulate, in particular, itching accompanying atopic syndromes.
摘要:
To provide a novel PG derivative with an excellent platelet aggregation inhibitor effect. A prostaglandin derivative represented by general formula (I) and a salt thereof.
摘要:
Prostaglandin analogues represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both: wherein A is ethylene, vinylene or ethynylene; Y and Y are each independently hydrogen, halogeno, cyano, CONR R (wherein R and R are each independently hydrogen or C1-6 alkyl, or R and R together with the nitrogen atom adjacent thereto may form C4-8 cyclic amine), C1-3 aminoalkyl, C1-6 hydroxyalkyl, NR R (wherein R and R are each independently hydrogen or C1-6 alkyl), hydroxyl, C1-6 alkoxy, C1-9 alkyl, C1-6 haloalkyl, C1-5 acyl, or COOR (wherein R is hydrogen, C1-6 alkyl, or phenyl); R and R are each independently hydrogen, halogeno, C1-9 alkyl, or C1-6 haloalkyl; m is an integer of 0 to 6; and n is an integer of 0 to 3.
摘要:
A prostaglandin derivative represented by the following general formula [I], its pharmaceutically acceptable salt or a hydrate thereof which has an excellent antagonism to prostaglandin DP receptor and, therefore, is useful against diseases such as allergic rhinitis, nasal obstruction, asthma, allergic conjunctivitis, systemic mastocytosis and systemic mast cell disease; [I] wherein X represents halogeno; Y represents ethylene, vinylene or ethynylene; Z represents -(CH2)m-, -O(CH2)n- or -S(O)p-(CH2)n- (wherein m is an integer of from 0 to 3; n is an integer of from 0 to 2; and p is an integer of from 0 to 2); R represents hydrogen or optionally substituted C1-5 alkyl; R represents C3-10 cycloalkyl optionally substituted by C1-4 alkyl or C4-15 cycloalkyl; and R represents hydrogen, halogeno or optionally substituted C1-5 alkyl.
摘要翻译:由以下通式[I]表示的前列腺素衍生物,其药学上可接受的盐或其水合物对前列腺素DP受体具有优良的拮抗作用,因此可用于治疗变应性鼻炎,鼻塞,哮喘,过敏性结膜炎 ,系统性肥大细胞增多症和系统性肥大细胞病; [I]其中X代表卤代; Y代表亚乙基,亚乙烯基或亚乙炔基; Z代表 - (CH2)m-,-O(CH2)n-或-S(O)p-(CH2)n-(其中m是0-3的整数; n是0-2的整数 ;并且p是0-2的整数); R 1代表氢或任选取代的C 1-5烷基; R 2表示任选被C 1-4烷基或C 4-15环烷基取代的C 3-10环烷基; 且R 3代表氢,卤代或任选取代的C 1-5烷基。
摘要:
Prostaglandin derivatives represented by the general formula (I), pharmaceutically acceptable salts thereof, or hydrates of the salts: (I) wherein X is halogeno of alpha or beta configuration; Y is ethylene, vinylene, or ethynylene; R is C3-10 cycloalkyl which may be substituted with a linear or branched C1-4 alkyl group, or C4-13 cycloalkylalkyl; R is hydrogen or CO2R ; R is hydrogen, linear or branched C1-4 alkyl, or linear or branched C2-4 alkenyl; n is an integer of 1 to 4; and p is 0, 1, or 2.
摘要:
Prostaglandin derivatives represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both wherein X is halogeno; R is hydrogen, C1-10 alkyl, or C3-10 cycloalkyl; m is an integer of 0 to 5; and Y is a group represented by formula (a) (wherein n is an integer of 1 to 8) or a group represented by general formula (b) (wherein R is C3-10 cycloalkyl, C3-10 cycloalkyl substituted with C1-4 alkyl, C1-4 alkyl substituted with C3-10 cycloalkyl, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, or a bridged cyclic hydrocarbon group).
摘要:
Novel prostaglandin derivatives represented by general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both, wherein X is CH2, O, S, or the like; Y is ethylene, vinylene, ethynylene, or the like; Z is ethylene, vinylene, or ethynylene; R is hydrogen, alkyl, or cycloalkyl; R is alkyl, alkenyl, alkynyl, cycloalkyl, or the like; and R is hydrogen, alkyl, or the like. The prostaglandin derivatives exhibit an excellent inhibitory activity against the proliferation of vascular smooth muscle and are useful as preventive or therapeutic drugs for post-PTCA restenosis and so on.
摘要:
A process for producing an intermediate for a 13,14-didehydroprostaglandin E, represented by general formula (I), (wherein R represents -COOR , cyano, hydroxy, -OCOR or -CONR R ; A represents vinylene, ethynylene, phenylene -C = C = C-; X represents oxygen or sulfur; m is 0 to 7; n, q and s are each 0 or 1; and p and r are each 0 to 5) by the free-radical reaction of a compound represented by general formula (II), with a compound represented by the following general formula: Y(CR R )mAn(CH2)pXq(CHR )rR , (wherein Y represents halogen or (a)) in the presence of a free-radical generator.
摘要翻译:(I)表示的13,14-二氢脯氨酸E的中间体的制备方法,其中R 6表示-COOR 9,氰基,羟基,-OCOR 10或-CONR 11 > R 12; A表示亚乙烯基,亚乙炔基,亚苯基-C = C = C-; X表示氧或硫; m为0至7; n,q和s各自为0或1; p和r各自为 (CR 3 R 4)mA n(CH 2)p X q(CHR 5)n表示的化合物与通式(II)所示的化合物进行自由基反应, (其中Y代表卤素或(a))在自由基生成剂存在下反应。
摘要:
Prostaglandin derivatives of general formula (I), pharmaceutically acceptable salts thereof, or hydrates of both: [wherein X is alpha a- or beta -substituent halogeno; Y is ethylene, vinylene, or ethynylene; A is O(CH2)n, S(O)p(CH2)n, O(CH2)qO(CH2)r, O(CH2)qS(O)p(CH2)r, S(O)p(CH2)qS(O)p(CH2)r, or S(O)p(CH2)qO(CH2)r (wherein n is an integer of 1 to 5; p is 0, 1 or 2; q is an integer of 1 to 3; and r is 0 or 1); R is C3-10 cycloalkyl, C1-4 alkyl C3-10 cycloalkyl, C3-10 cycloalkyl C1-4 alkyl, C5-10 alkyl, C5-10 alkenyl, C5-10 alkynyl, or a bridged cyclic hydrocarbon group; R is H, C1-10 alkyl, or C3-10 cycloalkyl; and m is 0, 1 or 2]. These compounds are novel and exhibit excellent prostaglandin D2-like agonism and a sleep-inducing effect.