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公开(公告)号：US20240166675A1
公开(公告)日：2024-05-23
申请号：US18469393
申请日：2023-09-18
Inventor： Michael Anthony SCHMIDT , Michal OCIEPA , Martin D. EASTGATE , Bin ZHENG , Phil BARAN , Hai-Jun ZHANG , Molham NASER
IPC: C07F9/6578
CPC classification number: C07F9/6578 , C07B2200/07
Abstract: The present invention relates to novel phosphorous (V) (P(V)) reagents
methods for preparing thereof, and methods for preparing nucleoside phosphorothioate compounds by using the novel reagents.-
公开(公告)号：US20210079046A1
公开(公告)日：2021-03-18
申请号：US16618847
申请日：2018-06-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Gardner S. CREECH , Mahboubeh KHEIRABADI , Martin D. EASTGATE , David S. NIRSCHIL , Percy H. CARTER
IPC: C07K7/64 , C07K1/107 , C07K17/08 , C07C309/75 , C07C309/77 , C07D225/08 , C07K1/04
Abstract: The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using “catch-release” methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving said capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.
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公开(公告)号：US20170362259A1
公开(公告)日：2017-12-21
申请号：US15623570
申请日：2017-06-15
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Adrian ORTIZ , Carlos A. GUERRERO , Bin ZHENG , Jason J. ZHU , Michael Anthony SCHMIDT , Michael R. LUZUNG , Martin D. EASTGATE
IPC: C07F7/18 , C07D417/12
CPC classification number: C07F7/1804 , C07D211/28 , C07D417/12 , C07F7/081
Abstract: An improved process for making a compound B of the structure wherein n, R1, R2, and R3 are as defined in the specification. Compound B can be used to make tubulysin analogs that are, in turn, useful as anti-cancer agents, particularly when deployed in an antibody-drug conjugate.
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Patent Agency Ranking
公开(公告)号：US20240051996A1
公开(公告)日：2024-02-15
申请号：US17943532
申请日：2022-09-13
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Gardner S. CREECH , Mahboubeh KHEIRABADI , Martin D. EASTGATE , David S. NIRSCHL , Percy H. CARTER
IPC: C07K7/64 , C07C309/75 , C07C309/77 , C07D225/08 , C07K1/04 , C07K1/107 , C07K17/08
CPC classification number: C07K7/64 , C07C309/75 , C07C309/77 , C07D225/08 , C07K1/042 , C07K1/1077 , C07K17/08
Abstract: The disclosure is directed to the synthesis and improved methods for purifying macrocyclic peptides produced by solid phase peptide synthesis.
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公开(公告)号：US20190322694A1
公开(公告)日：2019-10-24
申请号：US16382692
申请日：2019-04-12
Inventor： Michael Anthony SCHMIDT , Bin ZHENG , Kyle KNOUSE , Justine deGRUYTER , Martin D. EASTGATE , Phil BARAN , William R. EWING , Richard E. OLSON , Ivar M. McDONALD
IPC: C07H21/00
Abstract: The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
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![PROCESS TOWARD THE MANUFACTURE OF (6R,10S)-10-{4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL)PHENYL]-6-OXO-1(6H)-PYRIMIDINYL}- 1-(DIFLUOROMETHYL)-6-METHYL-1,4,7,8,9,10-HEXAHYDRO-11,15-(METHENO)PYRAZOLO[4,3-B][1,7]DIAZACYCLOTETRADECIN-5(6H)-ONE](/abs-image/US/2023/12/28/US20230416252A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230416252A1
公开(公告)日：2023-12-28
申请号：US18031277
申请日：2021-10-11
Applicant: Bristol-Myers Squibb Company , Janssen Pharmaceutica NV
Inventor： Subha MUKHERJEE , William P. GALLAGHER , Christopher Robert JAMISON , Carolyn S. WEI , Sergei KOLOTUCHIN , Amarjit SINGH , Nicolas CUNIERE , Chris SFOUGGATAKIS , Adrian ORTIZ , Steven R. WISNIEWSKI , Bin ZHENG , Helen Y. LUO , Sébastien François Emmanuel LEMAIRE , Cyril BEN HAÏM , Kostiantyn CHERNICHENKO , Diego Fernando Domenico BROGGINI , Simon Albert WAGSCHAL , Duy Chi Trung CAO , Karl REUTER , Björn SCHMALZBAUER , Philipp KOSCHKER , Martin D. EASTGATE , Dimitri SKLIAR , Alexander ZHDANKO , Christos XIOURAS , Matthew Penfield MOWER , Ngoc Duc TRAN , Ramdane RAHMANI , Xavier Jean-Marie JUSSEAU , Kiran MATCHA , Luca Alessandro PEREGO
IPC: C07D471/16 , B01J23/72
CPC classification number: C07D471/16 , B01J23/72 , C07B2200/13
Abstract: The present application generally relates to several processes for the preparation of (6R,10S)-10-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6H)-pyrimidinyl}-1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6H)-one: Compound (I).
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公开(公告)号：US20230242569A1
公开(公告)日：2023-08-03
申请号：US18167772
申请日：2023-02-10
Inventor： Michael Anthony SCHMIDT , Bin ZHENG , Kyle KNOUSE , Justine deGRUYTER , Martin D. EASTGATE , Phil BARAN , William R. EWING , Richard E. OLSON , Ivar M. MCDONALD
IPC: C07H21/00
CPC classification number: C07H21/00
Abstract: The present invention relates to novel phosphorous (V) (P(V)) reagents, methods for preparing thereof, and methods for preparing organophosphorous (V) compounds by using the novel reagents.
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公开(公告)号：US20230212204A1
公开(公告)日：2023-07-06
申请号：US17758898
申请日：2021-01-14
Inventor： Dongmin XU , Nazaret RIVAS-BASCÓN , Kyle W. KNOUSE , Natalia PADIAL , Bin ZHENG , Julien VANTOUROUT , Michael SCHMIDT , Martin D. EASTGATE , Phi BARAN
CPC classification number: C07F9/65785 , C07F9/65515 , C07F17/02 , C07F9/653 , C07F9/3229 , C07F9/58
Abstract: The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
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