Novel compounds

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United States of America Patent

APP PUB NO 20040102633A1
SERIAL NO

10433595

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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: wherein: R.sub.1 is H or alkyl; R.sub.2 is --R.sub.8R.sub.9; R.sub.8 is a single bond or alkyl, optionally substituted one or more times by hydroxy; R.sub.9 is aryl or cycloalkyl or heteroaryl, optionally substituted one or more times by hydroxy, alkoxy, or alkoxyalkyl; R.sub.3 is H or alkyl or cycloalkyl or cycloalkylalkyl, optionally substituted one or more times by hydroxy or by one or more fluorines; R.sub.4 is --NR.sub.10R.sub.11; R.sub.10 and R.sub.11 are independently selected from H or alkyl, or R.sub.10 and R.sub.11 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring comprising 3-8 ring members, which heterocyclic ring is unsubstituted or is substituted one or more times by one or more substituents R.sub.12; R.sub.12 is oxo or --R.sub.13 R.sub.14 R.sub.15, wherein R.sub.13 is a single bond or alkyl, R.sub.14 is OC(O) or C(O)O, and R.sub.15 is H or alkyl; R.sub.5 is an alkyl, cycloalkyl, cycloalkylalkyl, aryl, or single or fused ring aromatic heterocyclic group, which group is unsubstituted or is substituted one or more times by one or more substituents selected from halo such as fluoro, alkyl or haloalkyl such as fluoroalkyl; R.sub.6 represents H or up to three substituents independently selected from the list consisting of: alkyl, alkenyl, aryl, alkoxy or a hydroxylated derivative thereof, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, alkoxycarbonyl, haloalkyl such as trifluoromethyl, acyloxy, amino, mono- or di-alkylamino, alkoxyamido, alkoxycarboxylate or an esterified derivative thereof; R.sub.7 is H or halo; a is 1-6; and any of R.sub.1, R.sub.3, R.sub.5, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 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

International Classification(s)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Farina, Carlo Baranzate di Bollate, IT 69 177
Giardina, Giuseppe Baranzate di Bollate, IT 23 89
Grugni, Mario Baranzate di Bollate, IT 40 152
Nadler, Guy Marguerite Marie Gerard Rennes, FR 18 49

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