相似化合物
75680-92-1 35857-89-7 65202-50-8欧盟法规
ECHA物质C&L通报上下游产品
3-chloro-6-methylpyridazine 6-oxo-1,6-dihydropyridazine-3-carboxylic acid 6-Methylpyridazin-3(2H)-on sodium chlorite 3-aminopyridazine-6-carboxylic acid -quinazoline-2-carboxylic acid8-chloro-10-oxo-10H-pyridazino6,1-b-quinazoline-2-carboxylic acid 6-chloro-pyridazine-3-carbonyl chloride 3-aminopyridazine-6-carboxamide 6-氯哒嗪-3-甲酸甲酯置于lithium Hydroxide Monohydrate体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 1.0H,以75%的收率获得产物6-氯哒嗪-3-羧酸
参考文献: Compounds And Methods For The Targeted Degradation Of Androgen Receptor[fr] Composés Et Méthodes Pour La Dégradation Ciblée Du Récepteur Des Androgènes
标题: Compounds And Methods For The Targeted Degradation Of Androgen Receptor[fr] Composés Et Méthodes Pour La Dégradation Ciblée Du Récepteur Des Androgènes
摘要:这项披露涉及化合物,其制备以及在需要的受试者中治疗前列腺癌,包括转移性和/或去势抵抗性前列腺癌中使用这些化合物的用途.
专利信息
专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:WO-0107416-A1
优先权日:1999-07-28
标题 :Method of producing pyridazine carboxylic acid derivatives
发明人:BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
摘要:The invention relates to a method of producing pyridazine carboxylic acid derivatives of the general formulae (Ia) or (Ib), wherein R<1> represents a group of the formula -OR<3> or -NR<4>R<5>, R<2> represents hydrogen, chlorine, a group of the formula -OR<6> or a group of the formula -NR<7>R<8>, R<3> represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, R<4> represents C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl, R<5> represents hydrogen, C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl and R<6> represents C1-10 alkyl, C3-8 cycloalkyl, aryl-C1-4-alkyl or an optionally substituted aromatic or heteroaromatic rest and R<7> and R<8> represent independently C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl or together with the nitrogen atom form a saturated or aromatic heterocyclic ring. The inventive derivatives are obtained by reacting the corresponding 3-chloropyridazines or 3,6-dichloropyridazine with carbon monoxide and alcohols or amines H-R<1> in the presence of palladium-phosphin complexes and bases. The pyridazine carboxylic acid derivatives (Ia, Ib) are the intermediates for the synthesis of pharmaceutically active substances.
专利号:US-2009118296-A1
优先权日:2005-07-20
标 题:Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase
发明人:BLACK CAMERON; DESCHENES DENIS; GAGNON MARC; LACHANCE NICOLAS; LEBLANC YVES; LEGER SERGE; LI CHUN SING; OBALLA RENATA M
权利人:MERCK FROSST CANADA LTD
摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
专利号:US-2009170828-A1
优先权日:2006-06-12
标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (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:US-7799787-B2
优先权日:2005-12-20
标 题 :Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人:DESCHENES DENIS; FORTIN REJEAN; LI CHUN SING; OBALLA RENATA M; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; fatty liver disease and cancer.