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公开(公告)号：EP0954526A2
公开(公告)日：1999-11-10
申请号：EP97952232.0
申请日：1997-12-05
Applicant: CORTECH, INC. , Gyorkos, Albert , Spruce, Lyle W.
Inventor： GYORKOS, Albert , SPRUCE, Lyle, W.
CPC classification number: C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/06156 , C07K5/06191 , C07K5/0806 , C07K5/12
Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases.
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2.发明公开COMPOUNDS HAVING BRADYKININ ANTAGONISTIC ACTIVITY AND MU-OPIOID AGONISTIC ACTIVITY 失效CONNECTIONS缓激肽拮抗活性和Mu阿片受体激动剂活动
公开(公告)号：EP0832106A2
公开(公告)日：1998-04-01
申请号：EP96918098.0
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.
Abstract: The present invention relates to pharmaceutically effective heterodimers comprising a bradykinin antagonist component covalently linked to a mu-opioid agonist component.
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公开(公告)号：WO2008051533A3
公开(公告)日：2008-06-12
申请号：PCT/US2007022472
申请日：2007-10-24
Applicant: TAKEDA PHARMACEUTICAL , 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: A01N43/52 , A61K31/415
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: 提供式（1）的化合物，其中R 1是任选取代的C 1-10烷基; R 2是H或可被1至3个取代基取代的C 1-6烷基; R 3是5或6元芳族基团，其可以被1至5个取代基取代，其中5或6元芳族基团可以与5-或6-元的 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。
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公开(公告)号：WO2006116412A8
公开(公告)日：2007-03-01
申请号：PCT/US2006015646
申请日：2006-04-26
Applicant: TAKEDA PHARMACEUTICAL , 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: 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。
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5.发明申请
公开(公告)号：WO9849190A9
公开(公告)日：1999-04-15
申请号：PCT/US9808259
申请日：1998-04-24
Applicant: CORTECH INC , SPRUCE LYLE W , GYORKOS ALBERT C , CHERONIS JOHN C , GOODFELLOW VAL S , LEIMER AXEL H , YOUNG JOHN M , GERRITY JAMES IVAN
Inventor： SPRUCE LYLE W , GYORKOS ALBERT C , CHERONIS JOHN C , GOODFELLOW VAL S , LEIMER AXEL H , YOUNG JOHN M , GERRITY JAMES IVAN
IPC: A61K38/00 , C07K5/06 , C07K5/062 , C07K5/087 , C07K5/093 , A61K31/41 , A61K38/05 , A61K38/06 , A61K38/07 , C07D271/06 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/08 , C07K5/10 , G01N33/52
CPC classification number: C07K5/06078 , A61K38/00 , C07K5/06043 , C07K5/06052 , C07K5/0812 , C07K5/0819
Abstract: The present invention relates to cystein protease inhibitors of general formula (I), wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R1 is optionally substituted alkyl or aryl.
Abstract translation: 本发明涉及通式（I）的半胱氨酸蛋白酶抑制剂，其中Z是半胱氨酸蛋白酶结合部分; X和Y是S，O或任选取代的N; 并且R 1是任选取代的烷基或芳基。
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Patent Agency Ranking
公开(公告)号：WO2008039640A2
公开(公告)日：2008-04-03
申请号：PCT/US2007/078144
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: A61K31/4365 , C07D471/04 , C07D215/18 , A61K31/4709
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型化合物。 还公开了它们的制备方法及其在作为抗菌剂的治疗中的用途，特别是其用于治疗艰难梭菌感染的用途。
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公开(公告)号：WO2005044793A2
公开(公告)日：2005-05-19
申请号：PCT/US2004/035648
申请日：2004-10-27
Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED , 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: C07D
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 1 is an oxygen, a sulfur or - NR 5 -, or formula (A"): wherein X is a nitrogen and R 6 is an optionally substituted hydrocarbyl, R 1 is an amino substituted by two optionally substituted hydrocarbyl groups, R 2 is an phenyl, Y 1 is CR 3a or a nitrogen, Y 2 is CR 3b or a nitrogen and Y 3 is CR 3C or a nitrogen, provided that one or less of Y 1 , Y 2 , and Y 3 is nitrogen, W is a bond, -(CH 2 )n-, and Z is a bond, -NR 4 -, etc.; 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：其中环A是由式（A'）表示的5元环：其中X是碳，X 1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是被两个任选取代的烃基取代的氨基， R 2是苯基，Y 1是CR 3a或氮，Y 2是CR 3b或氮和Y 3是CR 3或氮，条件是一个 或更少的Y 1，Y 2和Y 3是氮，W是键， - （CH 2）n - ，Z是键，-NR 4 - ， - 等。 ;或其盐或其前药。
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公开(公告)号：WO1998024806A3
公开(公告)日：1998-06-11
申请号：PCT/US1997021636
申请日：1997-12-05
Applicant: CORTECH, INC. , GYORKOS, Albert , SPRUCE, Lyle, W.
Inventor： CORTECH, INC.
IPC: C07K05/062
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公开(公告)号：WO9824806A2
公开(公告)日：1998-06-11
申请号：PCT/US9721636
申请日：1997-12-05
Applicant: CORTECH INC , GYORKOS ALBERT , SPRUCE LYLE W
Inventor： GYORKOS ALBERT , SPRUCE LYLE W
IPC: A61K38/55 , A61K31/41 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/495 , A61K31/513 , A61K38/00 , A61K38/05 , A61K38/06 , A61P43/00 , C07D271/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/02 , C07D491/02 , C07D495/04 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/12
CPC classification number: C07D271/10 , A61K38/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07K5/0202 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/06139 , C07K5/06156 , C07K5/06191 , C07K5/0806 , C07K5/12
Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases.
Abstract translation: 本发明涉及可用作丝氨酸蛋白酶抑制剂的某些取代的恶二唑，噻二唑和三唑拟肽。
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10.发明申请COMPOUNDS HAVING BRADYKININ ANTAGONISTIC ACTIVITY AND MU-OPIOID AGONISTIC ACTIVITY 审中-公开具有BRADYKININ拮抗活性和MU-OPIOID激活活性的化合物
公开(公告)号：WO1996039425A2
公开(公告)日：1996-12-12
申请号：PCT/US1996008923
申请日：1996-06-04
Applicant: CORTECH, INC. , CHERONIS, John, C. , GYORKOS, Albert , SPRUCE, Lyle, W. , WHALLEY, Eric, T.
Inventor： CORTECH, INC.
IPC: C07K07/18
Abstract: The present invention relates to pharmaceutically effective heterodimers comprising a bradykinin antagonist component covalently linked to a mu-opioid agonist component.
Abstract translation: 本发明涉及药物有效的异源二聚体，其包含与μ-阿片样物质激动剂组分共价连接的缓激肽拮抗剂组分。
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