Quinoline derivatives as nk-3 and nk-2 antagonists

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United States of America Patent

APP PUB NO 20040082589A1
SERIAL NO

10416596

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 1 wherein: R.sub.1 is H or alkyl; R.sub.2 is aryl, cycloalkyl or heteroaryl; R.sub.3 is H or C.sub.1-3 alkyl, optionally substituted by one or more fluorines; R.sub.4 is H, R.sub.8NR.sub.9R.sub.10, R.sub.11R.sub.13 or R.sub.11R.sub.12R.sub.13; R.sub.8 is a single bond or alkyl; R.sub.9 and R.sub.10 are selected independently from H, alkyl, cycloalkyl or cycloalkylC.sub.1-3alkyl, aryl or arylC.sub.1-3alkyl, or R.sub.9 and R.sub.10 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring which is optionally substituted by one or more fluorines; R.sub.11 is alkyl, alkenyl, aryl, heteroaryl, cycloalkyl, arylalkyl or cycloalkylalkyl, optionally substituted one or more times by C.sub.1-3 alkyl, phenyl and/or phenylC.sub.1-3alkyl; R.sub.12 is alkyl or alkoxy, optionally substituted one or more times by C.sub.1-3 alkyl and/or by phenyl; R.sub.13 is H or COO R.sub.14; R.sub.14 is H or alkyl; R.sub.5 is branched or linear alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, or a single or fused ring aromatic heterocyclic group; R.sub.6 represents H or up to three substituents independently selected from the list consisting of: alkyl, alkenyl, aryl, alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-alkylamino; R.sub.7 is H or halo; a is 1-6; and any of R.sub.2, R.sub.5, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12 and R.sub.14 may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

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Patent Owner(s)

Patent OwnerAddress
GLAXOSMITHKLINE S P AVIA ALESSANDRO FLEMING 2 VERONA 37135
LABORATOIRE GLAXOSMITHKLINE S A S78163 MARLY-LE-ROI CEDEX

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Farina, Carlo Baranzate di Bollate, IT 69 177
Gagliardi, Stefania Baranzate di Bollate, IT 44 143
Gerard, Guy Marguerite Marie Rennes, FR 3 14
Giardina, Giuseppe Baranzate di Bollate, IT 23 89
Grugni, Mario Baranzate di Bollate, IT 40 152
Martinelli, Marisa Baranzate di Bollate, IT 17 14

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