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    • 2. 发明申请
    • Prostaglandin derivatives
    • 前列腺素衍生物
    • US20060270740A1
    • 2006-11-30
    • US10545785
    • 2004-02-19
    • Fumie SatoTohru TanamiNaoya OnoMakoto YagiTakayuki SekiMariko Sato
    • Fumie SatoTohru TanamiNaoya OnoMakoto YagiTakayuki SekiMariko Sato
    • A61K31/557
    • C07C405/0016
    • A prostaglandin derivative represented by the formula (wherein X is a halogen atom; Y is ethylene group, vinylene group or ethylylene group; Z is a group represented by —(CH2)m, —O(CH2)n— or —S(O)p—(CH2)n— (m is an integer of 0 to 3; n is an integer of 0 to 2; and p is an integer of 0 to 2); R1 is a hydrogen atom, a C1-5 alkyl group or a substituted C1-5 alkyl group; R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted by C1-4 alkyl group or C4-15 cycloalkylalkyl group; and R3 is a hydrogen atom, a halogen atom or a C1-5 alkyl group or a substituted C1-5 alkyl group), a pharmaceutically acceptable salt thereof 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 disorder of systemic mast cell activation.
    • 由式(其中X是卤素原子; Y是亚乙基,亚乙烯基或亚乙基)表示的前列腺素衍生物; Z是由 - (CH 2 CH 2)m表示的基团, (CH 2)n - 或 - (CH 2)n - (CH 2)n - )n(m为0〜3的整数,n为0〜2的整数,p为0〜2的整数),R 1〜 氢原子,C 1-5烷基或取代的C 1-5烷基; R 2是C 1 -C 6烷基, 3-10个环烷基,被C 1-4烷基取代的C 3-10环烷基或C 1-4 - >环烷基烷基; R 3是氢原子,卤素原子或C 1-5烷基或取代的C 1-5 - >烷基),其药学上可接受的盐或其水合物,其对前列腺素DP受体具有优异的拮抗作用,因此可用于治疗过敏性鼻炎,鼻塞 离子,哮喘,过敏性结膜炎,全身肥大细胞增多症和系统性肥大细胞活化紊乱。
    • 3. 发明授权
    • Prostaglandin E1 derivatives
    • 前列腺素E1衍生物
    • US06455584B1
    • 2002-09-24
    • US09937782
    • 2002-01-04
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto YagiHitomi Hirano
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto YagiHitomi Hirano
    • C07C17700
    • C07C405/00A61K31/5575C07C405/0033
    • To provide a prostaglandin derivative represented by the formula: wherein A is an ethylene group, a vinylene group, an ethynylene group, O(CH2)q or S(O)r(CH2)q, R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C1-10 alkyl group, a C1-10 alkyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkenyl group, a C2-10 alkenyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s), a C2-10 alkynyl group, a C2-10 alkynyl group substituted with hydroxyl group(s) or C1-4 alkoxy group(s) or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 1 to 5, n is an integer of 1 to 4, p is 0, 1 or 2, q is an integer of 1 to 5 and r is 0, 1 or 2; a pharmaceutically acceptable salt thereof or a hydrate thereof exhibit excellent action in inhibiting the growth of vascular smooth muscle and is useful as a drug for inhibition of restenosis after percutaneous transluminal coronary angioplasty.
    • 提供由下式表示的前列腺素衍生物:其中A是亚乙基,亚乙烯基,亚乙炔基,O(CH 2)q或S(O)r(CH 2)q,R 1是C 3-10环烷基, C 1-4烷基-C 3-10环烷基,C 3-10环烷基-C 1-4烷基,C 1-10烷基,被羟基或C 1-4烷氧基取代的C 1-10烷基 C2-10链烯基,被羟基或C1-4烷氧基取代的C2-10烯基,C2-10炔基,被羟基取代的C2-10炔基 基团或C 1-4烷氧基或桥连环烃基,R 2是氢原子,C 1-10烷基或C 3-10环烷基,m是1至5的整数,n 是1〜4的整数,p为0,1或2,q为1〜5的整数,r为0,1或2。 其药学上可接受的盐或其水合物在抑制血管平滑肌的生长中表现出优异的作用,并且可用作用于抑制经皮腔内冠状动脉成形术后再狭窄的药物。
    • 7. 发明授权
    • Prostaglandin derivatives
    • 前列腺素衍生物
    • US06613932B1
    • 2003-09-02
    • US10070752
    • 2002-03-11
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto YagiHitomi Hirano
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto YagiHitomi Hirano
    • C07C6974
    • C07C405/00
    • A prostaglandin derivative represented by the formula: [wherein X is CH2, O or S(O)q1, Y is an ethylene group, a vinylene group, an ethynylene group, O(CH2)t1 or S(O)q2(CH2)t1, Z is an ethylene group, a vinylene group or an ethynylene group, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, R2 is a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, a C3-10 cycloalkyl group, a C1-5 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-5 alkyl group, a hydroxy-C1-5 alkyl group, a halogeno-C1-5 alkyl group, a C1-5 alkoxy-C1-5 alkyl group, a C2-4 alkoxycarbonyl-C1-5 alkyl group, a carboxyl-C1-5 alkyl group, a cyano-C1-5 alkyl group, a C1-5 alkyl group substituted with a group represented by the formula: —NR7R8, an acyl group, a group represented by the formula: —(CH2)t2CH(NH2)COOR9, etc., and R3 is a hydrogen atom, a C1-10 alkyl group, etc.], a pharmaceutically acceptable salt thereof or a hydrate thereof. Novel prostaglandin derivatives of the present invention have an excellent action in inhibiting the growth of vascular smooth muscle, and are useful as drugs for prevention or treatment of the restenosis after PTCA, etc.
    • 由下式表示的前列腺素衍生物[其中X为CH 2,O或S(O)q1,Y为亚乙基,亚乙烯基,亚乙炔基,O(CH 2)t 1或S(O)q 2(CH 2) t1,Z是亚乙基,亚乙烯基或亚乙炔基,R1是氢原子,C1-10烷基或C3-10环烷基,R2是C1-10烷基,C2-10烯基 基团,C 2-10炔基,C 3-10环烷基,C 1-5烷基-C 3-10环烷基,C 3-10环烷基-C 1-5烷基,羟基-C 1-5烷基, 卤代C 1-5烷基,C 1-5烷氧基-C 1-5烷基,C 2-4烷氧基羰基-C 1-5烷基,羧基-C 1-5烷基,氰基-C 1-5烷基, 由下式表示的C1-5烷基:-NR7R8,酰基,由下式表示的基团: - (CH2)t2CH(NH2)COOR9等,R3为氢原子, C 1-10烷基等],其药学上可接受的盐或其水合物。本发明的新型前列腺素衍生物 在抑制血管平滑肌生长中具有优异的作用,可用作预防或治疗PTCA等后再狭窄的药物。
    • 8. 发明授权
    • Prostaglandin E analogues
    • 前列腺素E类似物
    • US06482990B1
    • 2002-11-19
    • US10070154
    • 2002-03-04
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto Yagi
    • Fumie SatoTohru TanamiHideo TanakaNaoya OnoMakoto Yagi
    • C07L40500
    • C07C405/00C07C405/0025
    • A prostaglandin analog represented by Formula (I): [wherein A is an ethylene group, a vinylene group or an ethynylene group, Y1 and Y2 are the same or different, and each a hydrogen atom, a halogen atom, a cyano group, —CONR3R4 (wherein R3 and R4 are the same or different, and each a hydrogen atom or a C1-6 alkyl group, or R3 and R4 together with the nitrogen atom to which they are attached form a C4-8 cyclic amine), a C1-3 aminoalkyl group, a C1-6 hydroxyalkyl group, NR5R6 (wherein R5 and R6 are the same or different, and each a hydrogen atom or a C1-6 alkyl group), a hydroxyl group, a C1-6 alkoxy group, a C1-9 alkyl group, a C1-6 alkyl group substituted with halogen(s), a C1-5 acyl group or COOR7 (wherein R7 is a hydrogen atom, a C1-6 alkyl group or a phenyl group), R1 and R2 are the same or different, and each a hydrogen atom, a halogen atom, a C1-9 alkyl group or a C1-6 alkyl group substituted with halogen(s), m is an integer of 0 to 6, and n is an integer of 0 to 3], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    • 由式(I)表示的前列腺素类似物:[其中A是亚乙基,亚乙烯基或亚乙炔基,Y1和Y2相同或不同,氢原子,卤素原子,氰基 - CONR 3 R 4(其中R 3和R 4相同或不同,并且各自为氢原子或C 1-6烷基,或者R 3和R 4与它们所连接的氮原子一起形成C 4-8环胺),C 1 -3氨基烷基,C1-6羟基烷基,NR5R6(其中R5和R6相同或不同,各自为氢原子或C1-6烷基),羟基,C1-6烷氧基, C1-9烷基,被卤素取代的C1-6烷基,C1-5酰基或COOR7(其中R7是氢原子,C1-6烷基或苯基),R1和R2 各自为氢原子,卤素原子,C1-9烷基或被卤素取代的C1-6烷基,m为0〜6的整数,n为整数 0〜3],药物 其可接受的盐或其水合物。
    • 10. 发明授权
    • Process for the preparation of E-prostaglandins
    • 前列腺素的制备方法
    • US5648526A
    • 1997-07-15
    • US256924
    • 1994-07-29
    • Fumie SatoTakehiro AmanoKazuya KameoTohru TanamiMasaru MutohNaoya OnoJun Goto
    • Fumie SatoTakehiro AmanoKazuya KameoTohru TanamiMasaru MutohNaoya OnoJun Goto
    • B01J31/22B01J31/24C07B61/00C07C405/00
    • B01J31/2404B01J31/0237B01J31/0267B01J31/04B01J31/223B01J31/2282B01J31/2291C07C405/00B01J2531/824Y02P20/55
    • Object: To produce E-prostaglandins in a high yield and in a short time with suppressed formation of isomers.Structure: A process for preparing E-prostaglandins represented by the formula: ##STR1## (wherein A, R.sup.6 and R.sup.7 represent respectively an arbitrary group which does not participate in the reaction; B represents a vinylene or ethynylene group; and R.sup.4 and R.sup.5 may be the same or different from each other and each represents a hydrogen atom or a protective group of the hydroxyl group) which comprises reacting allyl esters of E-prostaglandins represented by the formula: ##STR2## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, an alkenyl group or an aryl group; and A, B, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined above) with at least one substance selected from the group consisting of bases and formic acid in the presence of a zero- or divalent palladium complex or a salt thereof.
    • PCT No.PCT / JP93 / 00115 Sec。 371日期1994年7月29日第 102(e)日期1994年7月29日PCT提交1993年2月2日PCT公布。 公开号WO93 / 16041 日期1993年8月19日目的:以高产率和短时间产生E-前列腺素,抑制异构体的形成。 结构:由下式表示的E-前列腺素的制备方法:其中A,R6和R7分别表示不参与反应的任意基团; B表示亚乙烯基或亚乙炔基,R4和R5可以 彼此相同或不同,并且各自表示氢原子或羟基的保护基),其包括使由下式表示的E-前列腺素的烯丙基酯反应(其中R1和R2可以相同或相同) 彼此不同,各自表示氢原子或低级烷基; R 3表示氢原子,低级烷基,烯基或芳基; A,B,R 4,R 5,R 6和R 7如上所定义 上述)与至少一种选自碱或甲酸的物质在零或二价钯络合物或其盐的存在下反应。