公开(公告)号：US20050009917A1

公开(公告)日：2005-01-13

申请号：US10493693

申请日：2003-08-07

申请人： Fumie Sato ,  Iwai Arai ,  Norikazu Takano ,  Tohru Tanami ,  Makoto Yagi

发明人： Fumie Sato ,  Iwai Arai ,  Norikazu Takano ,  Tohru Tanami ,  Makoto Yagi

IPC分类号： A61K31/5575 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P27/02 ,  A61P37/08 ,  A61K31/557

CPC分类号： A61K31/5575 ,  Y10S514/861 ,  Y10S514/887

摘要： A pharmaceutical preparation for preventing or treating pruritic symptoms which contains as an effective ingredient a prostaglandin derivative represented by formula [1] wherein X1 and X2 which are different from each other represent a hydrogen atom, a halogen atom or a hydroxyl group; Y is an ethylene group, a vinylene group or an ethynylene group; Z is the formula (CH2)kA(CH2)hB(CH2)q, (CH2)kA(CH2)rA′(CH2)t (CH2)kB(CH2)hB′(CH2)q or (CH2)k-1B′(CH2)q-1A′wherein k is an integer of 1 to 4, h is an integer of 0 to 4, q is an integer 1 to 4, r is an integer of 0 to 4, and t is an integer of 0 to 2; A and A′ which may be the same or different represent an ethylene group, a vinylene group or an ethynylene group; B and B′ which may be the same or different represent an oxygen atom or a group represented by the formula S(O)u wherein u is an integer of 0 to 2; W1 is a hydroxyl group, a C1-10 alkyloxy group, a C3-10 cycloalkyloxy group, an aryloxy group or an arylalkyloxy group; W2 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 group substituted by C3-10 cycloalkyl group(s), or a group represented by the formula wherein W4 is a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a C1-5 alkyl group substituted by C3-10 cycloalkyl group(s); v is an integer of 0 to 4; W3 is a hydrogen atom or a methyl group, or W3 when taken together with W2 and the adjacent carbon atom forms a C3-10 cycloalkyl group; m is 0 or 1, a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 用于预防或治疗瘙痒症状的药物制剂，其含有作为有效成分的由式[1]表示的前列腺素衍生物，其中X 1和X 2彼此不同，表示氢原子，卤素原子或 羟基; Y是亚乙基，亚乙烯基或亚乙炔基; Z是式（CH2）kA（CH2）hB（CH2）q，（CH2）kA（CH2）rA'（CH2）t（CH2）kB（CH2）hB'（CH2）q或（CH2） '（CH 2）q-1A'其中k为1〜4的整数，h为0〜4的整数，q为1〜4的整数，r为0〜4的整数，t为 0〜2; A和A'可以相同或不同，表示亚乙基，亚乙烯基或亚乙炔基; B和B'可以相同或不同，表示氧原子或由式S（O）u表示的基团，其中u为0-2的整数; W 1是羟基，C 1-10烷氧基，C 3-10环烷氧基，芳氧基或芳基烷氧基; W 2是C 1-10烷基，C 2-10烯基，C 2-10炔基，C 3-10环烷基，被C 3-10环烷基取代的C 1-5烷基， 或由下式表示的基团，其中W 4是C 1-10烷基，C 2-10烯基，C 2-10炔基或被C 3-10环烷基取代的C 1-5烷基， ; v为0〜4的整数; W 3为氢原子或甲基时，W 3与W 2一起形成，相邻碳原子形成C3-10环烷基; m为0或1，其药学上可接受的盐或其水合物。

公开(公告)号：US07718701B2

公开(公告)日：2010-05-18

申请号：US10493693

申请日：2003-08-07

申请人： Fumie Sato ,  Iwao Arai ,  Norikazu Takano ,  Tohru Tanami ,  Makoto Yagi

发明人： Fumie Sato ,  Iwao Arai ,  Norikazu Takano ,  Tohru Tanami ,  Makoto Yagi

IPC分类号： A01N53/00 ,  C07C59/00 ,  C07C69/74

CPC分类号： A61K31/5575 ,  Y10S514/861 ,  Y10S514/887

摘要： A method of treating atopy-evoked pruritic symptoms by administering a prostaglandin derivative.

摘要翻译： 通过施用前列腺素衍生物治疗特应性诱发的瘙痒症状的方法。

公开(公告)号：US06613932B1

公开(公告)日：2003-09-02

申请号：US10070752

申请日：2002-03-11

申请人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

发明人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

IPC分类号： C07C6974

CPC分类号： C07C405/00

摘要： 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.

摘要翻译： 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。

公开(公告)号：US06482990B1

公开(公告)日：2002-11-19

申请号：US10070154

申请日：2002-03-04

申请人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi

发明人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi

IPC分类号： C07L40500

CPC分类号： C07C405/00 ,  C07C405/0025

摘要： 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.

摘要翻译： 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。

公开(公告)号：US07763652B2

公开(公告)日：2010-07-27

申请号：US10521115

申请日：2003-07-11

申请人： Fumie Sato ,  Tohru Tanami ,  Makoto Yagi ,  Naoya Ono

发明人： Fumie Sato ,  Tohru Tanami ,  Makoto Yagi ,  Naoya Ono

IPC分类号： A61K31/215 ,  A61K31/557

CPC分类号： C07C405/0033

摘要： A prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 straight or branched chain alkyl group or a C4-13 cycloalkylalkyl group, R2 is a hydrogen atom or a CO2R3 group (R3 is a hydrogen atom, a C1-4 straight or branched chain alkyl group or a C2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 由式（I）表示的前列腺素衍生物：其中X是α-或/或b-取代基中的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，R 1是C 3-10环烷基， 被C 1-4直链或支链烷基或C4-13环烷基烷基取代的C3-10环烷基，R2是氢原子或CO2R3基（R3是氢原子，C1-4直链或支链烷基 基团或C2-4直链或支链烯基），n为1〜4的整数，p为0,1或2，其药学上可接受的盐或其水合物。

公开(公告)号：US20060094788A1

公开(公告)日：2006-05-04

申请号：US10521115

申请日：2003-07-11

申请人： Fumie Sato ,  Tohru Tanami ,  Makoto Yagi ,  Naoya Ono

发明人： Fumie Sato ,  Tohru Tanami ,  Makoto Yagi ,  Naoya Ono

IPC分类号： A61K31/557 ,  C07C317/20

CPC分类号： C07C405/0033

摘要： A prostaglandin derivative represented by Formula (I): wherein X is a halogen atom in the α- or β-substitution, Y is an ethylene group, a vinylene group or an ethynylene group, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with a C1-4 straight or branched chain alkyl group or a C4-13 cycloalkylalkyl group, R2 is a hydrogen atom or a CO2R3 group (R3 is a hydrogen atom, a C1-4 straight or branched chain alkyl group or a C2-4 straight or branched chain alkenyl group), n is an integer of 1 to 4 and p is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 由式（I）表示的前列腺素衍生物：其中X是α-取代或β-取代中的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，R 1是 C 3-10环烷基，被C 1-4直链或支链烷基取代的C 3-10环烷基或 C 4-13环烷基烷基，R 2是氢原子或CO 2 R 3 R 3基团（R 3是氢原子，C 1-4烷基直链或支链烷基或C 2-4直链或支链烯基 ），n为1〜4的整数，p为0,1或2，其药学上可接受的盐或其水合物。

公开(公告)号：US06822112B1

公开(公告)日：2004-11-23

申请号：US10048926

申请日：2002-02-05

申请人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi

发明人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi

IPC分类号： C07C6976

CPC分类号： C07C405/00

摘要： A prostaglandin derivative represented by the formula: wherein X is a halogen atom, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 0 to 5, and Y is a group represented by the formula: wherein R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C1-4 alkyl group substituted with C3-10 cycloalkyl group(s), a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a bridged cyclic hydrocarbon group, or a group represented by the formula: wherein n is an integer of 1 to 8; a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 由下式表示的前列腺素衍生物：其中X是卤素原子，R 1是氢原子，C 1-10烷基或C 3-10环烷基，m是0-5的整数，Y是 由下式表示的基团：其中R 2为C 3-10环烷基，被C 1-4烷基取代的C 3-10环烷基，被C 3-10环烷基取代的C 1-4烷基 C 1-10烷基，C 2-10烯基，C 2-10炔基或桥连环烃基，或由下式表示的基团：其中n为1至8的整数; 其药学上可接受的盐或其水合物。

公开(公告)号：US06740772B1

公开(公告)日：2004-05-25

申请号：US10070643

申请日：2002-03-11

申请人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

发明人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

IPC分类号： C07C17700

CPC分类号： C07C405/00 ,  C07C405/0016

摘要： A prostaglandin derivative represented by the formula: wherein X is a halogen atom in the &agr;- or &bgr;-position, Y is an ethylene group, a vinylene group or an ethynylene group, A is a group represented by the formula: 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), R1 is a C3-10 cycloalkyl group, a C1-4 alkyl-C3-10 cycloalkyl group, a C3-10 cycloalkyl-C1-4 alkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, and m is 0, 1 or 2], a pharmaceutically acceptable salt thereof or a hydrate thereof. The present invention is to provide novel PG derivatives having an excellent PGD2-like agonistic activity and a sleep-inducing action.

摘要翻译： 由下式表示的前列腺素衍生物：其中X是α-位或β-位的卤素原子，Y是亚乙基，亚乙烯基或亚乙炔基，A是由下式表示的基团：O（CH 2） （O）p（CH2）q（O）p（CH2）q（O）p（CH2）q（O）p（CH2） CH 2）r或S（O）p（CH 2）q O（CH 2）r（其中n为1〜5的整数，p为0,1或2，q为1〜3的整数，r为0或1 ），R 1为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 5-10烷基，C 5-10烯基 基团，C5-10炔基或桥连环烃基，R 2是氢原子，C 1-10烷基或C 3-10环烷基，m是0,1或2]，药学上可接受的 其盐或其水合物。本发明提供具有优异的PGD 2样激动活性和睡眠诱导作用的新型PG衍生物。

公开(公告)号：US20060270740A1

公开(公告)日：2006-11-30

申请号：US10545785

申请日：2004-02-19

申请人： Fumie Sato ,  Tohru Tanami ,  Naoya Ono ,  Makoto Yagi ,  Takayuki Seki ,  Mariko Sato

发明人： Fumie Sato ,  Tohru Tanami ,  Naoya Ono ,  Makoto Yagi ,  Takayuki Seki ,  Mariko Sato

IPC分类号： A61K31/557

CPC分类号： C07C405/0016

摘要： 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.

摘要翻译： 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。

公开(公告)号：US06455584B1

公开(公告)日：2002-09-24

申请号：US09937782

申请日：2002-01-04

申请人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

发明人： Fumie Sato ,  Tohru Tanami ,  Hideo Tanaka ,  Naoya Ono ,  Makoto Yagi ,  Hitomi Hirano

IPC分类号： C07C17700

CPC分类号： C07C405/00 ,  A61K31/5575 ,  C07C405/0033

摘要： 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.

摘要翻译： 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。