[EN] BENZYL-, (PYRIDIN-3-YL)METHYL- OR (PYRIDIN-4-YL)METHYL-SUBSTITUTED OXADIAZOLOPYRIDINE DERIVATIVES AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS<br/>[FR] DÉRIVÉS D'OXADIAZOLOPYRIDINE À SUBSTITUTION BENZYLE, (PYRIDIN-3-YL)MÉTHYLE OU (PYRIDIN-4-YL)MÉTHYLE UTILISÉS EN TANT QU'INHIBITEURS DE LA GHRÉLINE O-ACYLTRANSFÉRASE (GOAT)
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2019149657A1
公开(公告)日:2019-08-08
The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
Methods and compositions for treating amyloid-related diseases
申请人:Kong Xianqi
公开号:US20060223855A1
公开(公告)日:2006-10-05
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
描述了用于治疗或预防与淀粉样蛋白相关疾病的方法、化合物、药物组合物和试剂盒。
Ruthenium‐Catalyzed Deaminative Hydrogenation of Amino Nitriles: Direct Access to 1,2‐Amino Alcohols
作者:Pilar Calleja、Martin Ernst、A. Stephen K. Hashmi、Thomas Schaub
DOI:10.1002/chem.201900531
日期:2019.7.17
approach for the efficient and highly selective synthesis of 1,2‐amino alcohols by direct reductive hydrolysis of N‐formyl‐protected α‐amino nitriles is reported. The commercially available RuHCl(CO)(PPh3)3 complex was found to be a suitable catalyst for this operationally simple protocol, in which no stoichiometric amounts of undesired metal waste are generated. The deaminative hydrogenation is performed
报道了一种通过N-甲酰基保护的α-氨基腈直接还原水解来高效,高选择性合成1,2-氨基醇的新方法。发现可商购获得的RuHCl(CO)(PPh 3)3络合物对于该操作简单的方案是合适的催化剂,其中不产生化学计量的不希望的金属废物。脱氨氢化反应在55 bar H 2下进行,使用1,4-二恶烷/水的6:1混合物作为溶剂。另外,在非常相似的条件下由氰基酮制备羟甲基醇。
[EN] GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME<br/>[FR] ANTAGONISTES DES RÉCEPTEURS DE L'HORMONE DE LIBÉRATION DES GONADOTROPHINES, LEUR PROCÉDÉ DE PRÉPARATION ET COMPOSITION PHARMACEUTIQUE LES COMPRENANT
申请人:SK CHEMICALS CO LTD
公开号:WO2013129879A1
公开(公告)日:2013-09-06
The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
The directamination of cyanohydrins with amines via a catalytic cyano-borrowing reaction was developed. The transformation features broad substrate scope, excellent functional group compatibility, and very mild and simple operations. Moreover, a titanium catalyst supported by quinine and (S)-BINOL ligands enabled an asymmetric cyano-borrowing reaction with moderate to high enantioselectivity.