公开(公告)号：US20070135452A1

公开(公告)日：2007-06-14

申请号：US10577334

申请日：2004-10-27

申请人： Albert Gyorkos ,  Christopher Corrette ,  Suk Cho ,  Timothy Turner ,  Scott Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

发明人： Albert Gyorkos ,  Christopher Corrette ,  Suk Cho ,  Timothy Turner ,  Scott Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

IPC分类号： A61K31/519 ,  C07D471/02 ,  A61K31/4745 ,  C07D487/04

CPC分类号： C07D235/30 ,  C07D471/04

摘要： There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A′): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A″): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.

摘要翻译： 提供了包含式（I）化合物的CRF受体拮抗剂：其中环A是由式（A'）表示的5元环：其中X是碳，X 1 O >是氧，硫或-NR 5 - 或式（A“）：其中X是氮，R 6是任选取代的烃基，R 1是由两个任选取代的烃基取代的氨基，R 2是苯基，Y 1是H 3 S >或氮，Y 2是CR 3或氮和Y 3是C 3或N 3或N 3 条件是Y 1，Y 2和Y 3中的一个或多个为氮，W为键， - （CH _{2）n - ，Z为键，-NR 4 - 等; 或其盐或其前药。}

公开(公告)号：US07714009B2

公开(公告)日：2010-05-11

申请号：US10577334

申请日：2004-10-27

申请人： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

发明人： Albert Charles Gyorkos ,  Christopher Peter Corrette ,  Suk Young Cho ,  Timothy Mark Turner ,  Scott Alan Pratt ,  Kazuyoshi Aso ,  Masakuni Kori ,  Michiyo Gyoten

IPC分类号： A61K31/4168 ,  C07D403/12 ,  C07D403/14 ,  C07D235/30

CPC分类号： C07D235/30 ,  C07D471/04

摘要： There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A′): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A″): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.

摘要翻译： 提供了包含式（I）化合物的CRF受体拮抗剂：其中环A是由式（A'）表示的5元环：其中X是碳，X 1是氧，硫或 -NR5-或式（A“）：其中X是氮，R6是任选取代的烃基，R 1是被两个任选取代的烃基取代的氨基，R 2是苯基，Y 1是CR 3 a或氮，Y 2是 CR3b或氮，Y3为CR3c或氮，条件是Y1，Y2和Y3中的一个或多个为氮，W为键， - （CH2）n-，Z为键，-NR4-等 。 或其盐或其前药。

公开(公告)号：US06248740B1

公开(公告)日：2001-06-19

申请号：US09284362

申请日：1999-04-14

申请人： Yasuhiko Kawano ,  Hideaki Nagaya ,  Michiyo Gyoten

发明人： Yasuhiko Kawano ,  Hideaki Nagaya ,  Michiyo Gyoten

IPC分类号： C07D40304

CPC分类号： C07D487/04

摘要： The present invention provides a compound represented by the formula: wherein Ar1 and Ar2 are independently an aromatic group which may be substituted, and Ar1 and Ar2 may form a condensed cyclic group with an adjacent carbon atom; ring B is a nitrogen-containing heterocycle which may be substituted; X and Y are the same or different and are independently a bond, an oxygen atom, S(O)p (p is an integer of 0 ot 2), NR4 wherein R4 is a hydrogen atom or a lower alkyl group, or a bivalent linear lower hydrocarbon group which may contain 1 to 3 hetero atoms and the bivalent linear lower hydrocarbon group may be substituted; A is a nitrogen atom or CR7 wherein R7 is a hydrogen atom, a halogen atom, a hydrocarbon which may be substituted, an acyl group or a hydroxy group which may be substituted; R1, R2 and R3 are the same or different and are independently a hydrogen atom, a halogen atom, a hydrocarbon group which may be substituted, an acyl group or a hydroxy group which may be substituted; R8 is a hydrogen atom, a hydroxy group which may be substituted by a lower alkyl or a carboxyl group, or a salt thereof, which exhibits excellent anti-histaminic or eosinophil chemotaxis-inhibiting activities and is useful in treatment or prevention of asthma, allergic conjunctivitis, allergic rhinitis, chronic urticaria or atopic dermatitis.

摘要翻译： 本发明提供由下式表示的化合物：其中Ar1和Ar2独立地为可被取代的芳基，Ar1和Ar2可以与相邻的碳原子形成稠合的环状基团; 环B是可以被取代的含氮杂环; X和Y相同或不同，独立地为键，氧原子，S（O）p（p为0〜2的整数），NR4，其中R4为氢原子或低级烷基，或二价 可以含有1〜3个杂原子的直链低级烃基，二价直链低级烃基可以被取代; A是氮原子或CR 7，其中R7是氢原子，卤素原子，可被取代的烃基，酰基或可被取代的羟基; R1，R2和R3相同或不同，独立地为氢原子，卤素原子，可被取代的烃基，酰基或可被取代的羟基; R8是氢原子，可以被低级烷基或羧基取代的羟基或其盐，其表现出优异的抗组氨酸或嗜酸性粒细胞趋化性抑制活性，并且可用于治疗或预防哮喘，过敏 结膜炎，过敏性鼻炎，慢性荨麻疹或特应性皮炎。

公开(公告)号：US20060106048A1

公开(公告)日：2006-05-18

申请号：US10522119

申请日：2003-07-24

申请人： Yoshihisa Inoue ,  Nobuhiro Fujii ,  Michiyo Gyoten ,  Tatsumi Matsumoto

发明人： Yoshihisa Inoue ,  Nobuhiro Fujii ,  Michiyo Gyoten ,  Tatsumi Matsumoto

IPC分类号： A61K31/4741 ,  C07D491/02

CPC分类号： C07D491/04 ,  A61K31/4355 ,  A61K31/444 ,  A61K31/455 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/538 ,  A61K31/5513

摘要： The present invention provides a compound represented by the formula wherein A represents (1) a bond, (2) a group represented by the formula —CRa═CRb— (Ra and Rb each represent a hydrogen atom or C1-6 alkyl) and the like; R1 represents (1) cyano or (2) an optionally esterified or amidated carboxyl group; R2 represents (1) a hydrogen atom, (2) an optionally substituted hydroxy group, (3) an optionally substituted amino group and the like; R3 and R4 each represent a hydrogen atom and the like; R5 represents a hydrogen atom and the like; R6 represents an optionally substituted hydroxy group and the like; R7 and R8 each represent an optionally substituted hydrocarbon group and the like; R9 and R10 each represent (1) a hydrogen atom and the like; Y represents an optionally substituted methylene group; and n represents 0 or 1, or a salt thereof, which has an excellent phosphodiesterase IV inhibiting action.

摘要翻译： 本发明提供由下式表示的化合物：其中A表示（1）键，（2）由式-CR R a和R b各自表示氢原子或C 1-6烷基）等; R 1表示（1）氰基或（2）任选酯化或酰胺化的羧基; R 2表示（1）氢原子，（2）任选取代的羟基，（3）任选取代的氨基等; R 3和R 4各自表示氢原子等; R 5表示氢原子等; R 6表示任选取代的羟基等; R 7和R 8各自表示任选取代的烃基等; R 9和R 10各自表示（1）氢原子等; Y表示任选取代的亚甲基; n表示0或1，或其盐具有优异的磷酸二酯酶IV抑制作用。