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CAS号98-88-4 苯甲酰氯📜酮咯酸 反应生成 (S)-酮咯酸
参考文献:酮咯酸的活性对映异构体(-)-5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-α吡咯-1-羧酸]的绝对构型.
标题:酮咯酸的活性对映异构体(-)-5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-α吡咯-1-羧酸]的绝对构型.
摘要:5-苯甲酰基-1,2-二氢-3H-吡咯并[1,2-α-吡咯-1-羧酸的(-)-S异构体在其中的(+)-R异构体的效价约为其60倍.角叉菜胶水肿试验和ca.在小鼠苯醌扭曲试验中,其活性是(+)-R异构体的230倍.
DOI:10.1021/jm00154A027
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专利信息
专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-8546532-B2
优先权日:2008-04-17
标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-12264143-B2
优先权日:2020-12-17
标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
发明人:SAMMIS GLENN M; ROGGEN MARKUS
权利人:NALU BIO INC
摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.
专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
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 disgnostic and therapeutic uses.
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-2024082118-A1
优先权日:2021-05-19
标 题:Topical compositions and methods of preparing the same
发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION
权利人:LANDA LABS 2012 LTD
摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.