14383-51-8Relevant articles and documents
NOVEL PURINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 44, (2013/05/21)
The invention relates to PI3K inhibitors of the formula (I) ? in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS
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Page/Page column 35, (2012/03/12)
This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.
Amido compounds and their use as pharmaceuticals
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Page/Page column 30, (2010/11/26)
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
Phthalazine derivatives and remedies for erectile dysfunction
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, (2008/06/13)
The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1and R2are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1is a chlorine atom, R2is a methoxy group and Y is a 5- or 6-membered amine ring substituted with a hydroxyl group is excluded.
Manipulation of substituents at nitrogen in tropanes, homotropanes, and dehydro- derivatives
Howarth, Nicola M.,Malpass, John R.,Smith, Craig R.
, p. 10899 - 10914 (2007/10/03)
Trop-6-ene (8-methyl-8-azabicyclo[3.2.1]oct-6-ene) and substituted N- benzylnortrop-6-enes are synthesised. N-Debenzylation of tropanes fails using a wide variety of non-hydrogenolytic conditions despite effective application in model piperidine derivatives; debenzylation of homotropanes is more successful, giving norhomotropane and norhomotrop-7-ene. Bridged N-benzyl compounds react more slowly than N-methyl analogues with chloroformates; the resulting quaternary intermediates are more prone than the N-methyl analogues to suffer competitive reversion to the starting amine, especially in the tropanes, consistent with slower S(N)2 attack at the benzylic carbon during decomposition; the use of an N-p-methoxybenzyl group does allow partial debenzylation to nortrop-6-ene, suggesting greater S(N)1 character in the decomposition step in this case. 'Equatorial' attack is preferred in methylation of N-benzyl-nortrop-6-ene and -homotrop-7-ene with CH3I; subsequent reductive debenzylation of the quaternary salt achieves overall replacement of N-benzyl by N-methyl in both cases. VT NMR studies show the presence of a single 'equatorial' invertomer (CI syn- to the 2C-bridge) in N- chloro-norhomotropanes and -7-enes and by analogy, in the N-alkyl compounds.
Synthesis and pharmacology of N-isomeric quaternary tropane compounds
Nador,Scheiber,Karpati,Grober
, p. 1324 - 1327 (2007/10/02)
The synthesis of (8r)-8-(4-biphenylmethyl)-atropinium bromide (3) as N-isomeric form of xenytropium bromide, (8s)-8-(4-biphenylmethyl)-atropinium bromide (2), is reported. It was revealed, that the equatorial alkylation predominates in quaternization of tertiary tropane compounds. Furthermore, the preparation of other N-isomeric pairs of quaternary tropane derivatives in pure form is described. Xenytropium bromide is more active - 16 times on the parasympathetic end-plate and 8 times on the ganglion - than its N-isomer.
