公开(公告)号：WO2005099688A3

公开(公告)日：2007-05-31

申请号：PCT/US2005013583

申请日：2005-04-06

Applicant: TAKEDA PHARMACEUTICAL ,  GYORKOS ALBERT CHARLES ,  CORRETTE CHRISTOPHER PETER ,  CHO SUK YOUNG ,  TURNER TIMOTHY MARK ,  ASO KAZUYOSHI ,  KORI MASAKUNI ,  MOCHIZUKI MICHIYO ,  CONDROSKI KEVIN RONALD ,  SIEDEM CHRISTOPHER STEPHEN ,  BOYD STEVEN ARMEN

Inventor： GYORKOS ALBERT CHARLES ,  CORRETTE CHRISTOPHER PETER ,  CHO SUK YOUNG ,  TURNER TIMOTHY MARK ,  ASO KAZUYOSHI ,  KORI MASAKUNI ,  MOCHIZUKI MICHIYO ,  CONDROSKI KEVIN RONALD ,  SIEDEM CHRISTOPHER STEPHEN ,  BOYD STEVEN ARMEN

IPC: C07D487/04 ,  A61K31/407 ,  A61K31/4704 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5383 ,  C07C225/20 ,  C07D213/74 ,  C07D215/233 ,  C07D215/56 ,  C07D221/02 ,  C07D231/56 ,  C07D237/28 ,  C07D239/22 ,  C07D239/46 ,  C07D239/47 ,  C07D239/56 ,  C07D239/94 ,  C07D239/95 ,  C07D239/96 ,  C07D265/34 ,  C07D265/36 ,  C07D455/02 ,  C07D471/04

CPC classification number: 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

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W-Ar 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; R 1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, -O-, -S-, etc.; Y 1 , Y 2 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.

Abstract translation: 提供了包含式（I）的化合物的CRF受体拮抗剂：AW-Ar，其中A是由式（A1）或（A2）表示的基团（其中，环Aa是5-或6-元 环可以被进一步取代;环Ab是可以被进一步取代的5-或6-元环;环Ac是可被取代的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是 独立地任选取代的碳或氮;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。

公开(公告)号：WO2006116412A3

公开(公告)日：2006-11-02

申请号：PCT/US2006/015646

申请日：2006-04-26

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ASO, Kazuyoshi ,  GYOTEN, Michiyo ,  GYORKOS, Albert Charles ,  CORRETTE, Christopher Peter ,  CHO, Suk Young ,  PRATT, Scott Alan ,  SIEDEM, Christopher Stephen

Inventor： ASO, Kazuyoshi ,  GYOTEN, Michiyo ,  GYORKOS, Albert Charles ,  CORRETTE, Christopher Peter ,  CHO, Suk Young ,  PRATT, Scott Alan ,  SIEDEM, Christopher Stephen

IPC: C07D235/24 ,  C07D235/04 ,  C07D235/12 ,  C07D235/18 ,  C07D403/02

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I) : wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or -NR3- (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl) ; Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, -CO-, oxygen, sulfur, -SO-, -SO2-, -NR4-, -NR4-alk-, -CONR4- or -NR4CO- (wherein alk is an optionally substituted C3.-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl) ; or a salt thereof or a prodrug thereof .

公开(公告)号：WO2006116412A2

公开(公告)日：2006-11-02

申请号：PCT/US2006015646

申请日：2006-04-26

Applicant: TAKEDA PHARMACEUTICAL ,  GYORKOS ALBERT ,  CORRETTE CHRISTOPHER ,  CHO SUK ,  PRATT SCOTT ,  SIEDEM CHRISTOPHER ,  ASO KAZUYOSHI ,  GYOTEN MICHIYO

Inventor： GYORKOS ALBERT ,  CORRETTE CHRISTOPHER ,  CHO SUK ,  PRATT SCOTT ,  SIEDEM CHRISTOPHER ,  ASO KAZUYOSHI ,  GYOTEN MICHIYO

IPC: C07D487/02

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D235/30 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D417/10 ,  C07D471/04 ,  C07D471/06 ,  C07D495/04

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I) : wherein R1 is an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; R2 is an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or -NR3- (wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl) ; Y1, Y2 and Y3 are each an optionally substituted carbon or a nitrogen, provided that one or less of Y1, Y2 and Y3 is nitrogen; and Z is a bond, -CO-, oxygen, sulfur, -SO-, -SO2-, -NR4-, -NR4-alk-, -CONR4- or -NR4CO- (wherein alk is an optionally substituted C3.-4 alkylene and R4 is a hydrogen, an optionally substituted hydrocarbyl or an acyl) ; or a salt thereof or a prodrug thereof .

Abstract translation: 提供了包含式（I）化合物的CRF受体拮抗剂：其中R1是任选取代的烃基，任选取代的C连接的杂环基，任选取代的N-连接的杂芳基，氰基或酰基; R2是任选取代的环状烃基或任选取代的杂环基; X是氧，硫或-NR 3 - （其中R 3是氢，任选取代的烃基或酰基）; Y1，Y2和Y3各自为任选取代的碳或氮，条件是Y1，Y2和Y3中的一个或多个为氮; 并且Z是键，-CO-，氧，硫，-SO - ， - SO 2 - ， - NR 4 - ， - NR 4 - 烷 - ， - CONR 4 - 或-NR 4 CO-（其中alk是任选取代的C 3 -4 亚烷基和R 4是氢，任选取代的烃基或酰基）; 或其盐或其前药。

公开(公告)号：WO2004017908A3

公开(公告)日：2004-03-04

申请号：PCT/US2003/026317

申请日：2003-08-21

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  YASUMA, Tsuneo ,  MORI, Akira ,  KAWASE, Masahiro ,  KIMURA, Hiroyuki ,  YOSHIDA, Masato ,  GYORKOS, Albert, Charles ,  PRATT, Scott, Alan ,  CORRETTE, Christopher, Peter

Inventor： YASUMA, Tsuneo ,  MORI, Akira ,  KAWASE, Masahiro ,  KIMURA, Hiroyuki ,  YOSHIDA, Masato ,  GYORKOS, Albert, Charles ,  PRATT, Scott, Alan ,  CORRETTE, Christopher, Peter

IPC: C07D221/04

Abstract: 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; X 1 is CR 1 , CR 1 R 2 , N or NR 13 ; X 2 is N or NR 3 ; Y is C, CR 4 or N, Z is CR 5 , CR 5 R 6 , N or NR 7 ; 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; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 13 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, CR 5 or N; R 8 , R 9 ,R 10 , R 11 and R 12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X 1 , R 3 , R 1 , Y and X 3 in formula (II) and (III) as before.

公开(公告)号：WO9639425A3

公开(公告)日：1997-01-30

申请号：PCT/US9608923

申请日：1996-06-04

Applicant: CORTECH INC ,  CHERONIS JOHN C ,  GYORKOS ALBERT ,  SPRUCE LYLE W ,  WHALLEY ERIC T

Inventor： CHERONIS JOHN C ,  GYORKOS ALBERT ,  SPRUCE LYLE W ,  WHALLEY ERIC T

IPC: A61K38/00 ,  C07K7/18 ,  C07K19/00 ,  A61K38/08

CPC classification number: C07K19/00 ,  A61K38/00 ,  C07K7/18

Abstract: The present invention relates to pharmaceutically effective heterodimers comprising a bradykinin antagonist component covalently linked to a mu-opioid agonist component.

公开(公告)号：WO2008039640A3

公开(公告)日：2008-12-11

申请号：PCT/US2007078144

申请日：2007-09-11

Applicant: REPLIDYNE INC ,  GUILES JOSEPH ,  SUN XICHENG ,  JANJIC NEBOJSA ,  STRONG SARAH ,  GYORKOS ALBERT CHARLES

Inventor： GUILES JOSEPH ,  SUN XICHENG ,  JANJIC NEBOJSA ,  STRONG SARAH ,  GYORKOS ALBERT CHARLES

IPC: A61K31/4743 ,  C07D471/02

CPC classification number: C07D495/04 ,  C07D405/12

Abstract: Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy for Clostridium difficile infection.

Abstract translation: 公开了作为细菌甲硫氨酰合成酶（MetRS）抑制剂的对映体过量的新化合物。 还公开了它们的制备方法以及它们在治疗中作为抗菌剂的用途，特别是它们用于治疗艰难梭菌感染。

公开(公告)号：WO2008051533A2

公开(公告)日：2008-05-02

申请号：PCT/US2007/022472

申请日：2007-10-24

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ASO, Kazuyoshi ,  MOCHIZUKI, Michiyo ,  KOJIMA, Takuto ,  KOBAYASHI, Katsumi ,  PRATT, Scott, Alan ,  GYORKOS, Albert, Charles ,  CORRETTE, Christopher, Peter ,  CHO, Suk, Young

Inventor： ASO, Kazuyoshi ,  MOCHIZUKI, Michiyo ,  KOJIMA, Takuto ,  KOBAYASHI, Katsumi ,  PRATT, Scott, Alan ,  GYORKOS, Albert, Charles ,  CORRETTE, Christopher, Peter ,  CHO, Suk, Young

IPC: A61K31/4439

CPC classification number: C07D235/26 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

Abstract: There is provided a compound of the formula (1) wherein R 1 is an optionally substituted C 1-10 alkyl; R 2 is H, or a C 1-6 alkyl which may be substituted with 1 to 3 substituents; R 3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6- membered ring which may be substituted with 1 to 3 C 1-6 alkyls; R 4 is a hydrogen, a halogen, a hydroxy, a cyano, a C 1-6 alkyl or a C 1-6 alkoxy; Z is -O-, -S-, -SO-, -SO 2 -, or - NR 5 - wherein R 5 is a hydrogen or a C 1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.

Abstract translation: 本发明提供了式（1）的化合物，其中R 1是任选取代的C 1-10烷基; R 2是H或可以被1至3个取代基取代的C 1-6烷基; R 3是可以被1至5个取代基取代的5或6元芳族基团，其中5或6元芳族基团可以与5或6元环 可以被1至3个C 1-6烷基取代的环; R 4是氢，卤素，羟基，氰基，C 1-6烷基或C 1-6烷氧基; Z是-O - ， - S - ， - SO - ， - SO 2 - 或-NR 5 - ，其中R 5是 氢或C 1-6烷基; 或其盐或其前药，其具有CRF受体拮抗剂活性及其用途。

公开(公告)号：WO2005044793A3

公开(公告)日：2006-03-30

申请号：PCT/US2004035648

申请日：2004-10-27

Applicant: TAKEDA PHARMACEUTICAL ,  GYORKOS ALBERT CHARLES ,  CORRETTE CHRISTOPHER PETER ,  CHO SUK YOUNG ,  TURNER TIMOTHY MARK ,  PRATT SCOTT ALAN ,  ASO KAZUYOSHI ,  KORI MASAKUNI ,  GYOTEN MICHIYO

Inventor： GYORKOS ALBERT CHARLES ,  CORRETTE CHRISTOPHER PETER ,  CHO SUK YOUNG ,  TURNER TIMOTHY MARK ,  PRATT SCOTT ALAN ,  ASO KAZUYOSHI ,  KORI MASAKUNI ,  GYOTEN MICHIYO

IPC: C07D20060101 ,  C07D235/30 ,  C07D471/04 ,  A61K31/44 ,  A61K31/415 ,  C07D235/04 ,  C07D471/02

CPC classification number: C07D235/30 ,  C07D471/04

Abstract: 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 X

Abstract translation: 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

公开(公告)号：WO2005099688A2

公开(公告)日：2005-10-27

申请号：PCT/US2005/013583

申请日：2005-04-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  GYORKOS, Albert, Charles ,  CORRETTE, Christopher, Peter ,  CHO, Suk, Young ,  TURNER, Timothy, Mark ,  ASO, Kazuyoshi ,  KORI, Masakuni ,  GYOTEN, Michiyo ,  CONDROSKI, Kevin, Ronald ,  SIEDEM, Christopher, Stephen ,  BOYD, Steven, Armen

Inventor： GYORKOS, Albert, Charles ,  CORRETTE, Christopher, Peter ,  CHO, Suk, Young ,  TURNER, Timothy, Mark ,  ASO, Kazuyoshi ,  KORI, Masakuni ,  GYOTEN, Michiyo ,  CONDROSKI, Kevin, Ronald ,  SIEDEM, Christopher, Stephen ,  BOYD, Steven, Armen

IPC: A61K31/407

CPC classification number: 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

Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W-Ar 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; R 1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, -O-, -S-, etc.; Y 1 , Y 2 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.

Abstract translation: 提供了包含式（I）的化合物的CRF受体拮抗剂：AW-Ar，其中A是由式（A1）或（A2）表示的基团（其中，环Aa是5-或6-元 环可以被进一步取代;环Ab是可以被进一步取代的5-或6-元环;环Ac是可被取代的5-或6-元环; R 1是任选取代的烷基，被取代的 氨基，取代的羟基等; X是羰基，-O-，-S-等; Y 1，Y 2和Q独立地是任选取代的碳或氮; ...是单或双 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。

公开(公告)号：WO2004017908A2

公开(公告)日：2004-03-04

申请号：PCT/US0326317

申请日：2003-08-21

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD ,  YASUMA TSUNEO ,  MORI AKIRA ,  KAWASE MASAHIRO ,  KIMURA HIROYUKI ,  YOSHIDA MASATO ,  GYORKOS ALBERT CHARLES ,  PRATT SCOTT ALAN ,  CORRETTE CHRISTOPHER PETER

Inventor： YASUMA TSUNEO ,  MORI AKIRA ,  KAWASE MASAHIRO ,  KIMURA HIROYUKI ,  YOSHIDA MASATO ,  GYORKOS ALBERT CHARLES ,  PRATT SCOTT ALAN ,  CORRETTE CHRISTOPHER PETER

IPC: A61K31/00 ,  A61P19/08 ,  C07D487/04 ,  A61K

CPC classification number: C07D487/04

Abstract: 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; X is CR , CR R , N or NR ; X is N or NR ; Y is C, CR or N, Z is CR , CR R , N or NR ; 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; R , R , R , R , R , R , R and R 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, CR or N; R , R ,R , R and R are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X , R , R , Y and X in formula (II) and (III) as before.

Abstract translation: 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; ---是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为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为C，CR 5或N; R 8，R 9，R 10，R 11和R 12独立地是H，任选取代的烃基等，或其盐。 还如前所述地在式（II）和（III）中指定X 1，R 3，R 1，Y和X 3。