cas 106973-36-8, (R)-4-Benzyl-5-oxo-3-morpholinecarboxylic Acid

Articles about 106973-36-8Total 13 be found

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A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor
The mechanistic target of rapamycin (mTOR) plays a pivotal role in growth and tumor progression and is an attractive target for cancer treatment. ATP-competitive mTOR kinase inhibitors (TORKi) have the potential to overcome limitations of rapamycin derivatives in a wide range of malignancies. Herein, we exploit a conformational restriction approach to explore a novel chemical space for the generation of TORKi. Structure-activity relationship (SAR) studies led to the identification of compound 12b with a ～450-fold selectivity for mTOR over class I PI3K isoforms. Pharmacokinetic studies in male Sprague Dawley rats highlighted a good exposure after oral dosing and a minimum brain penetration. CYP450 reactive phenotyping pointed out the high metabolic stability of 12b. These results identify the tricyclic pyrimido-pyrrolo-oxazine moiety as a novel scaffold for the development of highly selective mTOR inhibitors for cancer treatment.
Borsari, Chiara,Rageot, Denise,Dall'Asen, Alix,Bohnacker, Thomas,Melone, Anna,Sele, Alexander M.,Jackson, Eileen,Langlois, Jean-Baptiste,Beaufils, Florent,Hebeisen, Paul,Fabbro, Doriano,Hillmann, Petra,Wymann, Matthias P.
p. 8609 - 8630
(2019/10/16)

PEPTIDE DEFORMYLASE INHIBITORS
The present invention relates to {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3- oxopropyl}hydroxyformamide compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, processes for making and use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity and in treatment methods for bacterial infections
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(2013/06/27)

ANHYDRATE FORMS OF A PYRIDINE DERIVATIVE
The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.
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Page/Page column 19-20

(2011/04/14)

Fused Thiazole Derivatives As Kinase Inhibitors
A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 11

(2011/01/12)

PEPTIDE DEFORMYLASE INHIBITORS
The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I), wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
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Page/Page column 85

(2009/06/27)

FUSED THIAZOLE AND THIOPHENE DERIVATIVES AS KINASE INHIBITORS
A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)
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Page/Page column 109-110

(2009/07/17)

2-AMINOBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS
Compounds of formulae I, II and III: are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.
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Page/Page column 31

(2008/12/04)

FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 28-29

(2009/03/07)

Imidazopyridine Kinase Inhibitors
The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 93

(2009/01/20)

THIAZOLE DERIVATIVES AS KINASE INHIBITORS
A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 40

(2008/12/05)

PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS
There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: X represents a nitrogen atom; Y represents -C(H2)-, (-C(H2)-)2, -S(O2)- or -C(=O)-; Z represents -C(H2)-, -S(O2)-, -N(Rz)-, or an oxygen or sulphur atom; A represents hydrogen or -CH2OH; Rz represents hydrogen, C1-6 alkyl, C1-6 alkoxy, -COR7 or -SO2R7; R1 represents halogen, C1-6 alkyl, C1-6 alkoxy, =O, haloC1-6 alkyl, haloC1-6 alkoxy, hydroxyl or -CH2OH; m represents an integer from 0 to 3; R2 represents halogen, =O, C1-6alkyl (optionally substituted by one or more hydroxyl groups), -COOR7, -CONR7R8, C1-6 alkoxy, haloC1-6 alkyl, haloC1-6alkoxy or C1-6 alkyloC1-6 alkyl; n represents an integer from 0 to 3; p and q independently represent an integer from 0 to 2; R3 represents an -aryl, -heteroaryl, -heterocyclyl, -aryl-aryl, -aryl-heteroaryl, -aryl-heterocyclyl, -heteroaryl-aryl, -heteroaryl-heteroaryl, -heteroaryl-heterocyclyl, -heterocyclyl-aryl, -heterocyclyl-heteroaryl or -heterocyclyl-heterocyclyl group, all of which may be optionally substituted by one or more (e.g. 1, 2 or 3) halogen, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), C3-8cycloalkyl, C1-6 alkoxy, hydroxyl, haloC1-6alkyl, haloC1-6 alkoxy, cyano, -S-C1-6 alkyl, -SO-C1-6 alkyl, -SO2-C1-6 alkyl, -COR7, -CONR7R8, -NR7R8, -NR7COC1-6 alkyl, -NR7SO2-C1-6alkyl, C1-6 alkyl-NR7R8, -OCONR7R8 , -NR7CO2R8 or -SO2NR7R8 groups; R4 and R5 independently represent C1-6 alkyl, or R4 and R5 together with the carbon atom to which they are attached may together form a C3-8cycloalkyl group; R6 represents halogen, C1-6 alkyl, C3-8cycloalkyl, C1-6 alkoxy, haloC1-6 alkyl or haloC1-6 alkoxy; s represents an integer from 0 to 4; R7 and R8 independently represent hydrogen, C1-6 alkyl or C3-8cycloalkyl; or solvates thereof.
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Page/Page column 64

(2010/11/26)

FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
A series of 5,6-dihydro-l,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of b.enefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 77

(2008/06/13)

Chiral Synthesis of 3-Substituted Morpholines via Serine Enantiomers and Reductions of 5-Oxomorpholine-3-carboxylates
The chiral synthesis of 3-hydroxymethyl- and 3-carboxy-morpholines from serine enantiomers is described.Chemoselective and total reductions of 5-oxomorpholine-3-carboxylates are key synthetic steps.
Brown, George R.,Foubister, Alan J.,Wright, Brian
p. 2577 - 2580
(2007/10/02)