专利号:US-7220858-B2 优先权日:2003-12-23 标 题 :Synthesis of hydrazine and chlorinated derivatives of bicyclic pyridazines 发明人:NELSON DEANNA J 权利人:BARBEAU PHARMA INC 摘要:The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.
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-8853410-B2 优先权日:2009-04-30 标 题:Process for preparing substituted isoxazoline compounds and their precursors 发明人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN 权利人:RACK MICHAEL; KOERBER KARSTEN; KAISER FLORIAN; BASF SE 摘要:The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) n nwhich are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I)n n nwherein R 1 to R 5 , R 8 and R 9 are described as in the description.n n The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.
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-RE42890-E 优先权日:2003-05-23 标题 :Furazanobenzimidazoles 发明人:EBERLE MARTIN; BACHMANN FELIX; STREBEL ALESSANDRO; ROY SUBHO; SRIVASTAVA SUDHIR; SAHA GOUTAM 权利人:BASILEA PHARMACEUTICA AG 摘要:The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R 1 to R 6 have the meanings given in the specification, for use as medicaments, to novel compounds of formula (I), to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same
专利号:US-2005137397-A1 优先权日:2003-12-23 标题:Synthesis of hydrazine derivatives of pyridazine