CAS: 446022-33-9; Ag 2037

专利信息

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:US-2005085492-A1
优先权日:2003-10-20
标 题:Stereoselective process for the synthesis of chiral garft compounds and intermediates
发明人：RAHMAN LEERA
权利人:AGOURON PHARMACEUTICALS MINC
摘要:The present invention describes a stereoselective preparation of derivatives and precursors of molecules having formula 1: n nMethod of preparing the compounds, intermediates and derivatives are described. The methods described herein allow the preparation of diastereomeric forms of compound having formula 1. The compounds of the invention are GARFT inhibitors.

专利号:US-2004266796-A1
优先权日:2003-06-25
标 题:Convergent processes for the synthesis of a GARFT inhibitor containing a methyl substituted thiophene core and intermediates therefor
发明人：DOVALSANTOS ELENA; FLAHIVE ERIK JON; HALDEN BRIAN JOHN; MITCHELL MARK BRYAN; NOTZ WOLFGANG REINHARD LUDWIG; O'NEILL-SLAWECKI STACY ANN; TIAN QINGPING
权利人:AGOURON PHARMA
摘要:The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: n n n wherein each of R 1 and R 2 are independently a hydrogen atom or a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; from an intermediate of the formula n n n wherein R 3 is a moiety that together with the attached CO 2 forms a readily hydrolyzable ester group; n Pg 1 is an amino protecting group; n R 4 is H; n or Pg 1 can optionally be taken together with R 4 and the nitrogen to which Pg 1 and R 4 are attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O) j wherein j is an integer from 0 to 2, and —NR 8 —, provided that two O atoms, two S(O) j moieties, or an O atom and a S(O) j moiety are not attached directly to each other; n R 5 is selected from the group consisting of —C≡C— and —CHâ•?CH—; and n R 8 is independently H or C 1 -C 6 alkyl; n to form the compound of the formula (I) that is optically pure; and to processesfor preparing intermediates thereof.

专利号:US-2023390297-A1
优先权日:2022-06-02
标 题:Use of nucleotide synthesis inhibitors for targeted therapy in mll3/4 compass mutant cancer
发明人：SHILATIFARD ALI; ZHAO ZIBO
权利人:UNIV NORTHWESTERN
摘要:Disclosed herein are methods and compositions for treating a subject comprising the administration of an effective amount of a nucleotide synthesis inhibitor to a subject in need of treatment for a MLL3/4 COMPASS deficient cancer or a MLL3/4 loss of function mutation.

专利号:US-10272065-B2
优先权日:2013-01-14
标题 :Gem-difluorinated C-glycoside compounds as anti-cancer agents
发明人：SLILATY STEVE N
权利人:ADVANOMICS CORP; BENOIT & COTE
摘要:The present document describes a synthesis of a class of gem-difluorinated C-glycoside compounds derived from podophyllotoxin, which may be used, but not exclusively, in oncology for the treatment of cancer. More particularly, the podophyllotoxin gem-difluorinated C-glycoconjugated derivatives display improved conformational and chemical stability, and improved cytotoxicity exhibited against drug-resistant cancer cell lines.

专利号:US-9295731-B2
优先权日:2013-04-01
标题 :Cleavable drug conjugates, compositions thereof and methods of use
发明人：NGUYEN MARK QUANG
权利人:NGUYEN MARK QUANG
摘要:Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.