CAS: 169590-41-4; 4-(3-(Difluoromethyl)-5-(3-Fluoro-4-Methoxyphenyl)-1H-Pyrazol-1-yl)Benzenesulfonamide

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CAS号170570-77-1 4,4-difluoro-1-... | CAS号17852-52-7 对氨磺酰基苯肼盐酸盐 | CAS号454-31-9 二氟乙酸乙酯 | CAS号455-91-4 3-氟-4-甲氧基苯乙酮

3-氟-4-甲氧基苯乙酮置于sodium Methylate体系中,用 甲醇,乙醇 用作溶剂,化学反应 44.0H,反应生成地拉考昔
参考文献:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
标题:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
摘要:A Series Of Sulfonamide-Containing 1,5-Diarylpyrazole Derivatives Were Prepared And Evaluated For Their Ability To Block Cyclooxygenase-2 (Cox-2) In Vitro And In Vivo. Extensive Structure-Activity Relationship (Sar) Work Was Carried Out Within This Series,And A Number Of Potent And Selective Inhibitors Of Cox-2 Were Identified. Since An Early Structural Lead (1F,Sc-236) Exhibited An Unacceptably Long Plasma Half-Life,A Number Of Pyrazole Analogs Containing Potential Metabolic Sites Were Evaluated Further In Vivo In An Effort To Identify Compounds With Acceptable Pharmacokinetic Profiles. This Work Led To The Identification Of Ii (4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide,Sc-58635,Celecoxib),Which Is Currently In Phase Iii Clinical Trials For The Treatment Of Rheumatoid Arthritis And Osteoarthritis.
Doi:10.1021/jm960803Q

专利信息

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

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-2003157061-A1
优先权日:2001-12-05
标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor
发明人：BENNETT DENNIS A
权利人:PHARMACIA CORP
摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.

专利号:US-2024287041-A1
优先权日:2021-05-20
标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
发明人：BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

专利号:EP-2054420-B1
优先权日:2006-08-02
标题:Benzimidazo[1,2-c][1,2,3]thiadiazol-7-sulfonamides as inhibitors of carbonic anhydrase and the intermediates for production thereof
发明人：MATULIS DAUMANTAS; DUDUTIENE VIRGINIJA; MATULIENE JURGITA; MISTINAITE LINA
权利人:BIOTECHNOLOGIJOS INST
摘要:The invention is related to novel compounds - benzimidazo[1,2-c][1,2,3]thiadiazole sulfonamides, corresponding to the general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression such as glaucome. The compounds of formula (I) inhibits enzymes such as carbonic anhydrases and metallo proteinases. This invention is also related to new intermediate compounds which are used for the synthesis of sulfonamides of formula (I).