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1. 发明申请

US20060247178A1 Mitotic kinesin inhibitors and methods of use thereof 有权
公开(公告)号：US20060247178A1
公开(公告)日：2006-11-02
申请号：US11415455
申请日：2006-05-01
申请人： Jeremy Hans , Eli Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph Lyssikatos , John Robinson , Christopher Corrette , Robert Delisle
发明人： Jeremy Hans , Eli Wallace , Qian Zhao , Shelley Allen , Ellen Laird , Joseph Lyssikatos , John Robinson , Christopher Corrette , Robert Delisle
IPC分类号： A61K38/05 , A61K38/04 , A61K31/53 , A61K31/501 , A61K31/506 , A61K31/4745 , A61K31/4439 , A61K31/433 , C07D417/02 , C07D285/08
CPC分类号： C07D513/04 , C07D285/12 , C07D417/04 , C07D417/14 , C07D419/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D497/04 , C07F9/65395
摘要： This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

2. 发明申请

US20060079536A1 Calcium receptor modulating compound and use thereof 有权
标题翻译：钙受体调节化合物及其用途
公开(公告)号：US20060079536A1
公开(公告)日：2006-04-13
申请号：US10525158
申请日：2003-08-21
申请人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Gyorkos , Scott Pratt , Christopher Corrette
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Gyorkos , Scott Pratt , Christopher Corrette
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X 1是CR 1，CR 1，R 2，N或NR 13， ; X 2是N或NR 3; Y是C，CR 4或N，Z是CR 5，CR 5，R 6，N或NR 7 ; Ar是任选取代的环状基团; R为H，任选取代的烃基等; “img id =”custom-character-00001“he =”1.78mm“wi =”2.12mm“file =”US20060079536A1-20060413-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>是单键或双键; R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 13独立地是H，任选取代的烃基; 或其盐或其前药。式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q是C，CR 5或N; R 9，R 9，R 10，R 11和R 12都是还可以提供H，任选取代的烃基等，或其盐。还可以在式（II）中指定X 1，R 3，R 3，R 3，Y和X 3，和（ III）。

3. 发明申请

US20070135452A1 Nitrogen-containing fused heterocyclic compounds 失效
标题翻译：含氮稠合杂环化合物
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。}

4. 发明申请

US20070179165A1 Cyclic compounds 失效
标题翻译：环状化合物
公开(公告)号：US20070179165A1
公开(公告)日：2007-08-02
申请号：US10593891
申请日：2005-04-06
申请人： Albert Gyorkos , Christopher Corrette , Suk Cho , Timothy Turner , Kazuyoshi Aso , Masakuni Kori , Michiyo Mochizuki , Kevin Condroski , Christopher Siedem , Steven Boyd
发明人： Albert Gyorkos , Christopher Corrette , Suk Cho , Timothy Turner , Kazuyoshi Aso , Masakuni Kori , Michiyo Mochizuki , Kevin Condroski , Christopher Siedem , Steven Boyd
IPC分类号： A61K31/44 , A61K31/513 , C07D239/22
CPC分类号： C07D213/74 , C07C225/20 , C07C2602/08 , C07D215/233 , C07D215/56 , C07D231/56 , C07D237/28 , C07D239/46 , C07D239/47 , C07D239/56 , C07D239/94 , C07D239/95 , C07D239/96 , C07D265/36 , C07D455/02 , C07D471/04 , C07D487/04
摘要： There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W—Ar (I) wherein, A is a group represented by the formula (A1) or (A2): (wherein, ring Aa is a 5- or 6-membered ring which may be further substituted; ring Ab is a 5- or 6-membered ring which may be further substituted; ring Ac is a 5- or 6-membered ring which may be substituted; R1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, —O—, —S—, etc.; Y1, Y2 and Q are independently optionally substituted carbon or nitrogen; is a single or double bond); W is a bond, optionally substituted methylene, optionally substituted imino, —O—, —S—, etc.; Ar is optionally substituted aryl or optionally substituted heteroaryl; 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：<？in-line-formula description =“In-line Formulas”end =“lead”？> AW-Ar（I）式中，A为式（A1）或（A2）表示的基团：（其中，环Aa为5-或6-元环，其中，环Ab是可以被进一步取代的5-或6-元环;环Ac是可以被取代的5或6元环; R 1是任选取代的烷基，取代的氨基，取代的羟基等; X是羰基，-O-，-S-等; Y 1，Y 2和Q独立地是取代的碳或氮; 是单键或双键）; W是一个键，任意取代的亚甲基，任选取代的亚氨基，-O - ， - S-等; Ar是任选取代的芳基或任选取代的杂芳基; 或其盐或其前药。

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