公开(公告)号：WO2020142547A8

公开(公告)日：2020-07-09

申请号：PCT/US2019/069145

申请日：2019-12-31

Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY ,  GREEN, Michael J. ,  JAHANGIR, Alam

Inventor： GREEN, Michael J. ,  JAHANGIR, Alam ,  MOORE, Tereza ,  COWAN, Tina, M. ,  ENNS, Gregory, M. ,  SHAMLOO, Mehrdad

IPC: A61K31/416

Abstract: Methods of treatment and pharmaceutical formulations configured to treat primary and secondary mitochondrial dysfunction are provided. The methods and treatments use an agonist of AMPK. The agonist activates AMPK to activate ATP-producing pathways and inhibiting ATP-consuming pathways, thus allowing for the alleviation of symptoms associated with mitochondrial dysfunctions.

公开(公告)号：WO2009138340A1

公开(公告)日：2009-11-19

申请号：PCT/EP2009/055443

申请日：2009-05-06

Applicant: F. HOFFMANN-LA ROCHE AG ,  ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

Inventor： ARZENO, Humberto Bartolome ,  DUNN, James Patrick ,  GOLDSTEIN, David Michael ,  GONG, Leyi ,  HAN, Xiaochun ,  HOGG, Joan Heather ,  JAHANGIR, Alam ,  PALMER, Wylie Solang ,  REUTER, Deborah Carol ,  SILVA, Tania ,  TIVITMAHAISOON, Parcharee ,  TREJO-MARTIN, Teresa Alejandra ,  WU, Shao-Yong

IPC: C07D401/14 ,  A61K31/506 ,  A61P29/00

CPC classification number: C07D401/14

Abstract: The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula (I), wherein m, n, p, q, Q, r, R 1 , R 2 , R 3 , X, X 1 , X 2 , X 3 , X 4 , X 5 , Y 1 , Y 2 , Z 1 , and Z 2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Abstract translation: 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法，制剂和组合物。 本申请公开了如下式（I）所述的JNK抑制剂的前药，其中m，n，p，q，Q，r，R1，R2，R3，X，X1，X2，X3，X4，X5， Y2，Z1和Z2如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂，以及本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

公开(公告)号：WO2005005394A3

公开(公告)日：2005-03-31

申请号：PCT/EP2004007405

申请日：2004-07-07

Applicant: HOFFMANN LA ROCHE ,  BLEY KEITH ROGER ,  CLARK ROBIN DOUGLAS ,  JAHANGIR ALAM

Inventor： BLEY KEITH ROGER ,  CLARK ROBIN DOUGLAS ,  JAHANGIR ALAM

IPC: C07D211/72 ,  C07D233/50 ,  C07D239/14 ,  C07D243/08 ,  C07D295/096 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04 ,  A61K31/4168 ,  C07D207/22 ,  C07D243/04 ,  C07D295/08

CPC classification number: C07D295/096 ,  C07D211/72 ,  C07D233/50 ,  C07D239/14 ,  C07D243/08 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04

Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R , R , A and X are as defined herein. Also disclosed are compounds and related compositions.

Abstract translation: 通过向有需要的受试者施用其中R 1，R 2，A和X如本文所定义的式（I）化合物来治疗IP拮抗剂介导的疾病或病症的方法。 还公开了化合物和相关组合物。

公开(公告)号：WO2008104472A1

公开(公告)日：2008-09-04

申请号：PCT/EP2008/051939

申请日：2008-02-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  DILLON, Michael, Patrick ,  JAHANGIR, Alam

Inventor： DILLON, Michael, Patrick ,  JAHANGIR, Alam

IPC: C07D239/46 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/505 ,  A61P15/00

CPC classification number: C07D413/12 ,  C07D239/46 ,  C07D239/48 ,  C07D403/12

Abstract: Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the compounds being of formula (I): wherein R 1 , R 2 , R 3 and R 4 are as defined herein.

Abstract translation: 用于治疗由P2X 3和/或P2X 2/3受体拮抗剂介导的疾病的化合物和方法，所述式（I）的化合物：其中R R 1，R 2，R 3和R 4如本文所定义。

公开(公告)号：WO2007025900A1

公开(公告)日：2007-03-08

申请号：PCT/EP2006/065525

申请日：2006-08-21

Applicant: F. HOFFMANN-LA ROCHE AG ,  DILLON, Michael Patrick ,  JAHANGIR, Alam ,  LUI, Alfred Sui-Ting ,  WILHELM, Robert Stephen

Inventor： DILLON, Michael Patrick ,  JAHANGIR, Alam ,  LUI, Alfred Sui-Ting ,  WILHELM, Robert Stephen

IPC: C07D239/48 ,  C07D401/12 ,  A61K31/506 ,  A61P11/00 ,  A61P13/00

CPC classification number: C07D401/12 ,  C07D239/48 ,  C07D471/04

Abstract: Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R 6 , R 7 and R 8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the compounds.

Abstract translation: 式（I）化合物或其药学上可接受的盐，其中A，D，E，G，J，X，Y，ZR 6，R 7和R 7， SUP> 8 如本文所定义。 还提供了使用该化合物治疗由P2X 3和/或P2X 3/3受体拮抗剂介导的疾病的方法和制备该化合物的方法。

公开(公告)号：WO2011033053A1

公开(公告)日：2011-03-24

申请号：PCT/EP2010/063682

申请日：2010-09-17

Applicant: F. HOFFMANN-LA ROCHE AG ,  JAHANGIR, Alam ,  SOTH, Michael ,  YANG, Hanbiao ,  LYNCH, Stephen, M.

Inventor： JAHANGIR, Alam ,  SOTH, Michael ,  YANG, Hanbiao ,  LYNCH, Stephen, M.

IPC: C07D487/18 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D487/18

Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula (I), wherein the variables Q, Q 1 , Q 2 , Q 3 , and Q 4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract translation: 本发明涉及式（I）的新型大环化合物的用途，其中变量Q，Q1，Q2，Q3和Q4定义如本文所述，其抑制JAK并且可用于治疗自身免疫和 炎性疾病。

公开(公告)号：WO2005005394A2

公开(公告)日：2005-01-20

申请号：PCT/EP2004/007405

申请日：2004-07-07

Applicant: F.HOFFMANN-LA ROCHE AG ,  BLEY, Keith, Roger ,  CLARK, Robin, Douglas ,  JAHANGIR, Alam

Inventor： BLEY, Keith, Roger ,  CLARK, Robin, Douglas ,  JAHANGIR, Alam

IPC: C07D233/00

CPC classification number: C07D295/096 ,  C07D211/72 ,  C07D233/50 ,  C07D239/14 ,  C07D243/08 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04

Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R 1 , R 2 , A and X are as defined herein. Also disclosed are compounds and related compositions.

Abstract translation: 通过向有需要的受试者施用其中R 1，R 2，A和X如本文所定义的式（I）化合物来治疗IP拮抗剂介导的疾病或病症的方法。 还公开了化合物和相关组合物。

公开(公告)号：WO2009106441A1

公开(公告)日：2009-09-03

申请号：PCT/EP2009/051755

申请日：2009-02-16

Applicant: F. HOFFMANN-LA ROCHE AG ,  BAMBERG, Joe, Timothy ,  DU BOIS, Daisy, Joe ,  ELWORTHY, Todd, Richard ,  HENDRICKS, Robert, Than ,  HERMANN, Johannes, Cornelius ,  JAHANGIR, Alam ,  KONDRU, Rama, K. ,  LEMOINE, Remy ,  LOU, Yan ,  OWENS, Timothy, D. ,  PARK, Jaehyeon ,  SMITH, David, Bernard ,  SOTH, Michael ,  YANG, Hanbiao

Inventor： BAMBERG, Joe, Timothy ,  DU BOIS, Daisy, Joe ,  ELWORTHY, Todd, Richard ,  HENDRICKS, Robert, Than ,  HERMANN, Johannes, Cornelius ,  JAHANGIR, Alam ,  KONDRU, Rama, K. ,  LEMOINE, Remy ,  LOU, Yan ,  OWENS, Timothy, D. ,  PARK, Jaehyeon ,  SMITH, David, Bernard ,  SOTH, Michael ,  YANG, Hanbiao

IPC: C07D487/04 ,  C07D519/00 ,  A61P29/00 ,  A61K31/5025

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q 1 , R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract translation: 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量Q1，R和X如本文所述定义，其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病。

公开(公告)号：WO2008104474A1

公开(公告)日：2008-09-04

申请号：PCT/EP2008/051944

申请日：2008-02-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  DILLON, Michael Patrick ,  DU BOIS, Daisy Joe ,  JAHANGIR, Alam

Inventor： DILLON, Michael Patrick ,  DU BOIS, Daisy Joe ,  JAHANGIR, Alam

IPC: C07D239/48 ,  A61K31/505 ,  A61P13/10

CPC classification number: C07D239/48

Abstract: Compounds of formula (I) wherein R 1 and R 2 are as defined herein. Also disclosed are methods of making and using the subject compounds.

Abstract translation: 其中R 1和R 2的式（I）化合物如本文所定义。 还公开了制备和使用本发明化合物的方法。

公开(公告)号：WO2007025925A1

公开(公告)日：2007-03-08

申请号：PCT/EP2006/065606

申请日：2006-08-23

Applicant: F. HOFFMANN-LA ROCHE AG ,  BROKA, Chris Allen ,  CARTER, David Scott ,  DILLON, Michael Patrick ,  FORD, Anthony P.D.W. ,  HAWLEY, Ronald Charles ,  JAHANGIR, Alam ,  MOORE, Amy Geraldine ,  PARISH, Daniel Warren

Inventor： BROKA, Chris Allen ,  CARTER, David Scott ,  DILLON, Michael Patrick ,  FORD, Anthony P.D.W. ,  HAWLEY, Ronald Charles ,  JAHANGIR, Alam ,  MOORE, Amy Geraldine ,  PARISH, Daniel Warren

IPC: A61K31/505 ,  A61K31/506 ,  A61P11/00 ,  A61P11/06 ,  A61P1/00

CPC classification number: A61K31/506 ,  A61K31/505 ,  A61K31/513 ,  A61K31/538 ,  Y10S514/826

Abstract: Methods for treating respiratory and gastrointestinal diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein D, X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined herein.

Abstract translation: 用于治疗由P2X 3和/或P2X 3/3受体拮抗剂介导的呼吸道和胃肠道疾病的方法，所述方法包括向有需要的受试者施用有效量 的式（I）化合物或其药学上可接受的盐，其中D，X，Y，R 1，R 2，R 3， R 4，R 5，R 6，R 7和R 8，R 8， >如本文所定义。