2-Amino-6-anilino-purines and their use as medicaments
申请人:——
公开号:US20020016329A1
公开(公告)日:2002-02-07
2-Amino-6-anilino-purine derivatives of the formula I
1
in which the symbols are as defined in claim
1,
are described.
These compounds inhibit p34
cdc2
/cyclin B
cdc13
kinase and protein tyrosine kinase pp60
c-src
and can be used for treatment of hyperproliferative diseases, for example tumor diseases, and diseases which respond to inhibition of the activity of protein tyrosine kinase pp60
c-src
, in particular osteoporosis.
公式I中定义的符号如权利要求书1中所定义的那样,描述了1的2-氨基-6-苯胺基嘌呤衍生物。这些化合物抑制p34 cdc2/cyclin B cdc13激酶和蛋白酪氨酸激酶pp60 c-src,并可用于治疗过度增殖性疾病,例如肿瘤疾病,以及对蛋白酪氨酸激酶pp60 c-src活性抑制有反应的疾病,特别是骨质疏松症。
The instability of carbamate-protected alkyl imines has greatly hampered the development of catalytic asymmetric Mannich reactions suitable for the synthesis of optically active carbamate-protected chiral alkyl amines. A highly enantioselective Mannich reaction with in situ generation of carbamate-protected imines from stable α-amido sulfones catalyzed by an organic catalyst has been developed. This reaction provides a concise and highly enantioselective route converting aromatic and aliphatic aldehydes into optically active aryl and alkyl β-amino acids.
The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.
该发明描述了一种改进的合成方法,用于合成与烟酸和苄基衍生的哌嗪。产品化合物可用于治疗神经系统疾病。
[EN] PURINE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION<br/>[FR] DERIVES PURINES ET PROCEDES DE PREPARATION ASSOCIES
申请人:NOVARTIS AG
公开号:WO1997016452A1
公开(公告)日:1997-05-09
(EN) 2-Amino-6-anilino-purine derivatives of formula (1) in which the symbols are as defined in claim 1, are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.(FR) On décrit des dérivés 2-amino-6-anilino-purines de la formule 1 dans laquelle les symboles sont tels que définis dans la revendication 1. Ces composés inhibent la p34cdc2/cycline Bcdc13 kinase et on peut les utiliser dans le traitement de maladies à hyperprolifération, par exemple des tumeurs.
[EN] SYNTHESIS OF A NEUROSTIMULATIVE PIPERAZINE<br/>[FR] SYNTHÈSE D'UNE PIPÉRAZINE NEUROSTIMULATRICE
申请人:NEURALSTEM INC
公开号:WO2011028548A1
公开(公告)日:2011-03-10
The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.