公开(公告)号：TW201613953A

公开(公告)日：2016-04-16

申请号：TW104117108

申请日：2015-05-27

Applicant: 美國科羅拉多州立大學 ,  THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE ,  匹斯可 安東尼D ,  PISCOPIO, ANTHONY D. ,  傅小勇 ,  FU, XIAOYONG ,  施峰 ,  SHI, FENG ,  劉華研 ,  LIU, HUAYAN ,  李志峰 ,  LI, ZHIFENG

Inventor： 匹斯可 安東尼D ,  PISCOPIO, ANTHONY D. ,  傅小勇 ,  FU, XIAOYONG ,  施峰 ,  SHI, FENG ,  劉華研 ,  LIU, HUAYAN ,  李志峰 ,  LI, ZHIFENG

IPC: C07K11/02 ,  A61K31/427

CPC classification number: C07K11/02 ,  C07D498/06 ,  C07D513/06 ,  C07D513/14 ,  C07K1/113 ,  C07K5/0821

Abstract: 本發明闡述用於製備式(1)及式(2)化合物之方法，其中X、Y、Z、R1-R7、L及n定義於本文中。本發明亦闡述可用於製備式(1)及式(2)化合物之中間體。

Abstract in simplified Chinese: 本发明阐述用于制备式(1)及式(2)化合物之方法，其中X、Y、Z、R1-R7、L及n定义于本文中。本发明亦阐述可用于制备式(1)及式(2)化合物之中间体。

公开(公告)号：IL263159D0

公开(公告)日：2018-12-31

申请号：IL26315918

申请日：2018-11-20

Applicant: ONKURE INC ,  PISCOPIO ANTHONY D

Inventor： PISCOPIO ANTHONY D

IPC: A61K20060101

Abstract: The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A and Z are defined herein.

公开(公告)号：IL263159A

公开(公告)日：2021-04-29

申请号：IL26315918

申请日：2018-11-20

Applicant: ONKURE INC ,  PISCOPIO ANTHONY D

Inventor： PISCOPIO ANTHONY D

IPC: A61K38/00 ,  A61K38/15 ,  A61K45/06 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07K5/097 ,  C07K11/02

Abstract: The present invention provides a novel macrocyclic prodrug compound of general Formula (I), a pharmaceutical composition comprising a compound of Formula (I), and a method for treating diseases mediated by HDAC enzymes by administering a compound of Formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, A and Z are defined herein.

公开(公告)号：IL223313A

公开(公告)日：2015-07-30

申请号：IL22331312

申请日：2012-11-28

Applicant: ASTRAZENECA AB ,  ARRAY BIOPHARMA INC ,  LEONARD JOHN ,  DEMATEI JOHN ,  SHAKYA SAGAR ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN

Inventor： LEONARD JOHN ,  DEMATEI JOHN ,  SHAKYA SAGAR ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN

IPC: C07D20060101

Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

公开(公告)号：IL188273A

公开(公告)日：2015-03-31

申请号：IL18827307

申请日：2007-12-19

Applicant: ASTRAZENECA AB ,  ARRAY BIOPHARMA INC ,  LEONARD JOHN ,  DEMATEI JOHN ,  SHAKYA SAGAR ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN

Inventor： LEONARD JOHN ,  DEMATEI JOHN ,  SHAKYA SAGAR ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN

IPC: C07D20060101

Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

公开(公告)号：WO1996033172A1

公开(公告)日：1996-10-24

申请号：PCT/IB1995000279

申请日：1995-04-20

Applicant: PFIZER INC. ,  PISCOPIO, Anthony, D. ,  RIZZI, James, P.

Inventor： PFIZER INC.

IPC: C07D211/96

CPC classification number: C07D295/24 ,  C07D211/96 ,  C07D241/04 ,  C07D241/08

Abstract: A compound of formula (I) wherein R , R , R , R , R , R , R , R , R and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, as well as AIDS, sepsis, septic shock and other diseases involving the production of TNF.

Abstract translation: 式（I）的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8， 9＆gt;和Ar如上所定义，可用于治疗选自关节炎，癌症，组织溃疡，再狭窄，牙周病，大疱性表皮松解症，巩膜炎和其他以基质金属蛋白酶活性为特征的疾病的病症，以及 艾滋病，败血症，败血性休克等涉及TNF产生的疾病。

公开(公告)号：WO2007002157A3

公开(公告)日：2007-01-04

申请号：PCT/US2006/024084

申请日：2006-06-21

Applicant: ARRAY BIOPHARMA INC. ,  ASTRAZENECA AB ,  DEMATTEI, John ,  SHAKYA, Sagar ,  PISCOPIO, Anthony, D. ,  HACHE, Bruno, P. ,  EVANS, Matthew, Charles ,  FORD, James, Gair ,  POINTON, Simon, Mark ,  PEETERS, Koen ,  LILLEY, Timothy, John ,  LEONARD, John

Inventor： DEMATTEI, John ,  SHAKYA, Sagar ,  PISCOPIO, Anthony, D. ,  HACHE, Bruno, P. ,  EVANS, Matthew, Charles ,  FORD, James, Gair ,  POINTON, Simon, Mark ,  PEETERS, Koen ,  LILLEY, Timothy, John ,  LEONARD, John

IPC: C07D403/02

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X 1 , X 2 , X 5 , R 2 and R 10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

公开(公告)号：WO2007002157A2

公开(公告)日：2007-01-04

申请号：PCT/US2006024084

申请日：2006-06-21

Applicant: ARRAY BIOPHARMA INC ,  ASTRAZENECA AB ,  DEMATTEI JOHN ,  SHAKYA SAGAR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN ,  LEONARD JOHN

Inventor： DEMATTEI JOHN ,  SHAKYA SAGAR ,  PISCOPIO ANTHONY D ,  HACHE BRUNO P ,  EVANS MATTHEW CHARLES ,  FORD JAMES GAIR ,  POINTON SIMON MARK ,  PEETERS KOEN ,  LILLEY TIMOTHY JOHN ,  LEONARD JOHN

IPC: A61K31/4184

CPC classification number: C07D235/06 ,  C07C201/08 ,  C07C205/58 ,  C07C227/04 ,  C07C227/08 ,  C07C227/18 ,  C07C229/60

Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X 1 , X 2 , X 5 , R 2 and R 10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Abstract translation: 提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X 1，X 2，X，X 如本文所定义，R 2和R 10分别如本文所定义。 式Ia-1化合物及其合成中间体可用于制备杂环衍生物如苯并咪唑衍生物。

公开(公告)号：WO0183432A3

公开(公告)日：2002-02-28

申请号：PCT/US0113627

申请日：2001-04-27

Applicant: ARRAY BIOPHARMA INC ,  HWANG CHANKOU ,  TARLTON EUGENE ,  PISCOPIO ANTHONY D

Inventor： HWANG CHANKOU ,  TARLTON EUGENE ,  PISCOPIO ANTHONY D

IPC: C07C315/04 ,  C07C317/28

CPC classification number: C07C315/04 ,  C07C317/28

Abstract: Disclosed is a process for selectively reducing a nitrile containing organic compound of formula (II) (in which R and R are independently lower alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and n is 0-6) that also contains a sulphone moiety, the nitrile being reduced to a primary amine by use of borane or a substituted borane at a temperature of about -10 DEG C to 60 DEG C.

Abstract translation: 公开了一种选择性还原含有式（II）有机化合物（其中R和R 1独立地为低级烷基，环烷基，芳基，杂芳基，芳基烷基或杂芳基烷基;且n为0-6）的腈的方法， 还含有砜部分，腈在约-10℃至60℃的温度下通过使用硼烷或取代的硼烷还原成伯胺。

公开(公告)号：WO1998011085A1

公开(公告)日：1998-03-19

申请号：PCT/IB1997001024

申请日：1997-08-25

Applicant: PFIZER INC. ,  PISCOPIO, Anthony, D. ,  HAWKINS, Joel, M. ,  CARON, Stephane ,  KELLY, Sarah, E. ,  RAGGON, Jeffrey, W. ,  CASTALDI, Michael, J. ,  DUGGER, Robert, W. ,  RUGGERI, Sally, G.

Inventor： PFIZER INC.

IPC: C07D311/22

CPC classification number: C07C33/50 ,  C07D311/22 ,  C07F5/025

Abstract: The invention relates to processes for preparing a compound of formula (X) and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R , R , and R are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula (X).

Abstract translation: 本发明涉及制备式（X）化合物和所述化合物的对映异构体的方法，其中苯甲酸部分连接于色满酮环的6或7位，R 1，R 2和 R 3如本文所定义。 本发明还涉及可用于制备式（X）化合物的中间体。