[EN] ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF [FR] CONJUGUÉS ANTICORPS-MÉDICAMENT COMPRENANT DES PEPTIDOMIMÉTIQUES DE GLP1 ET LEURS UTILISATIONS
SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
申请人:Dahmann Georg
公开号:US20130023502A1
公开(公告)日:2013-01-24
The invention relates to new substituted pyridinyl-pyrimidines of formula
1
wherein
ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O,
wherein R
1
, R
2
, R
4
, R
3
, R
5
and R
6
are defined as in claim
1
and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
[EN] SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS<br/>[FR] PYRIDINYL-PYRIMIDINES SUBSTITUÉES ET LEUR UTILISATION EN TANT QUE MÉDICAMENTS
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2012101013A1
公开(公告)日:2012-08-02
The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
申请人:Mueller Georg Stephan
公开号:US20070072847A1
公开(公告)日:2007-03-29
The present invention relates to the CGRP-antagonists of general formula I
wherein R
1
, R
2
, R
3
and R
4
are defined as in claim
1,
the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
Ring expansion by in situ tethering of hydroxy azides to ketones: The boyer reaction
作者:Vijaya Gracias、Kristine E. Frank、Gregory L. Milligan、Jeffrey Aubé
DOI:10.1016/s0040-4020(97)01012-0
日期:1997.12
under the action of protic or Lewis acids such as BF3·OEt2. The reaction appears to succeed due to the initial formation of a hemiketal, which then renders the attack of azide on an oxoniumion intramolecular. The scope of this reaction vis à vis ketone and hydroxyalkyl azide structure is discussed.
Compounds of Formula I:
and pharmaceutically acceptable salts and solvates thereof, wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, R
8
, R
9
, and R
10
have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.