- BENZAMIDE CGRP RECEPTOR ANTAGONISTS
-
The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
- -
-
Page/Page column 103
(2015/11/09)
-
- ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
-
Compounds of formula (I) or (II) wherein Rx, Rz, R9, R10, R14, R14′, R15, R15′, A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
- -
-
Page/Page column
(2015/05/06)
-
- ANDROGEN RECEPTOR MODULATING CARBOXAMIDES
-
Compounds of formula (I) wherein Rx, Rz, R9, R10, R14, R14', R15, R15', A and B are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds possess utility as tissue-selective androgen receptor modulators (SARM) and are particularly useful as medicaments in the treatment of prostate cancer and other AR dependent conditions and diseases where AR antagonism is desired.
- -
-
Page/Page column 47-48
(2012/11/07)
-
- Direct C-2 arylation of alkyl 4-thiazolecarboxylates: New insights in synthesis of heterocyclic core of thiopeptide antibiotics
-
(Chemical Equation Presented) The Pd(0)-catalyzed regioselective C-2 (hetero)arylation of tert-butyl 4-thiazolecarboxylate with a broad (hetero)aryl halide is reported, including the direct coupling of pyridinyl halides. The process has allowed the preparation of valuable 2-pyridynyl-4- thiazolecarboxylates which are components of the complex heterocyclic core of thiopeptides antibiotics. As a first application, a synthesis of a tert-butyl sulfomycinamate thio-analogue from tert-butyl 4-thiazolecarboxylate is here described through a three-step direct pyridinylation, halogenation, and Stille cross-coupling sequence.
- Martin, Thibaut,Verrier, Cecile,Hoarau, Christophe,Marsais, Francis
-
supporting information; experimental part
p. 2909 - 2912
(2009/05/30)
-
- METHYLENE DIPIPERIDINE DERIVATIVES
-
The present invention relates to novel methylene dipiperidine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
- -
-
Page/Page column 16-17
(2010/11/30)
-
- Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
-
The invention relates to tetrahydronaphthyridine derivatives having formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said tetrahydronaphthyridine derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
- -
-
Page/Page column 62
(2008/06/13)
-
- SUBSTITUTED PIPERIDINES AS HISTAMINE H3 RECEPTOR LIGANDS
-
The present invention relates to novel piperidine ether derivatives having affinity for the histamine H3 receptor, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
- -
-
Page/Page column 27
(2010/02/10)
-