专利号:US-8487109-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; URMANN MATTHIAS; HALLAND NIS; ALONSO JORGE; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
专利号:US-8420812-B2 优先权日:2007-07-03 标题:Process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates 发明人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS 权利人:RKYEK OMAR; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; URMANN MATTHIAS; HALLAND NIS; SANOFI SA 摘要:A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates n The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), n nwherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:EP-1776333-B1 优先权日:2004-07-21 标 题:Ammonium salts and ammonium salt/mineral salt clathrate compounds for use as vehicle and effective form for pharmaco-medical applications and for use as phase transfer agents for chemical applications 发明人:REUTER UWE; OETTMEIER RALF; KASCH HELMUT 权利人:KASCH HELMUT 摘要:This invention relates to ammonium salts and stable storable ammonium salts and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues such as bicarbonate, to methods for producing them and to pharmaco-medical and chemical synthetic applications for said compounds. According to the invention, compounds for pharmaco-medical and chemical synthetic applications are produced which comprise the ammonium salt and ammonium salt/mineral salt clathrate compounds (inclusion compounds, clusters) having acid dibasic anionic acid residues of general formula I with R1, R2, R3 and R4=alkyl and substituted alkyl straight-chain or branched, optionally having an alcohol, ether, silyether, ester, amino or amide function, H or aryl-alkyl, with aryl being an aromatic or heteroaromatic ring having optionally additional substituents, such as alkyl having 1 to 4 C atoms, OH, NR*2 with R*2=O, alkyl with alkyl of between 1 and 4 C atoms or H, COOH, COOR, CN, NO2 and the cationic positive N+ is optionally part of an active agent, Y is a dibasic acid residue of an organic dicarboxylic acid or CO3-, corresponding to HY-=HCO3-, and x=0.5 to 30 represents the number of the mineral salt molecules for clathrate compound formation or 0. In pharmaco-medical applications applies the generalizable effectiveness principle according to which to ammonium salt/mineral salt cluster is used as vehicle and active agent for novel forms of application of nitrogen-containing active agent bases. In chemistry, these agents are used in the synthesis of active agents and valuable products, e.g. of cyclic carbonates.
专利号:WO-03061385-A1 优先权日:2002-01-17 标题:Tricyclic nucleoside library compounds, synthesis, and use as antiviral agents 发明人:AN HAOYUN; HONG ZHI; SMITH KENNETH; DING YILI; GIRARDET JEAN-LUC 权利人:RIBAPHARM INC; AN HAOYUN; HONG ZHI; SMITH KENNETH; DING YILI; GIRARDET JEAN-LUC 摘要:Tricyclic nucleoside libraries and library compounds are prepared using combinatorial chemistry and non-combinatorial chemistry methods. Contemplated library compounds are particularly useful in inhibition of viral propagation, and particularly of viral propagation of the HCV virus.
专利号:CN-102180798-A 优先权日:2011-03-18 标题 :Method for one-step catalytic synthesis of N,N-diethylpropynylamine