- (PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
-
The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
- -
-
Paragraph 00350
(2020/07/15)
-
- THERAPEUTIC COMPOUNDS
-
The invention provides compounds of formula (I): wherein, A, C, D, X, and Y have any of the values defined in the specification, and salts thereof. The compounds are SIRT2 inhibitors and are useful for treating SIRT2 associated conditions.
- -
-
Sheet 0395; 0409
(2017/01/23)
-
- QUINOLINE DERIVATIVES
-
The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
- -
-
Page/Page column 41
(2009/04/24)
-
- QUINAZOLINE DERIVATIVES
-
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
- -
-
Page/Page column 112
(2008/06/13)
-
- NAPHTHYRIDINE DERIVATIVES AS ANTI-CANCER AGENTS
-
The invention concerns naphthyridine derivatives of Formula (I): or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, G1, G2, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders or disease states associated with angiogenesis and/or vascular permeability.
- -
-
Page/Page column 104
(2010/11/28)
-
- QUINOLINE DERIVATIVES
-
The invention concerns quinoline derivatives of Formula (I): or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
- -
-
Page/Page column 143
(2008/06/13)
-
- QUINOLINE DERIVATIVES FOR TREATING CANCER
-
The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
- -
-
Page/Page column 110
(2008/06/13)
-
- QUINAZOLINE DERIVATIVES
-
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
- -
-
Page/Page column 94
(2008/06/13)
-
- QUINOLINE DERIVATIVES
-
The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
- -
-
Page/Page column 89-90
(2008/06/13)
-
- NOVEL PHARMACEUTICAL COMPOSITIONS COMPRISING AGONISTS OF THE THYROID RECEPTOR
-
The invention provides compounds of formula I or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I) wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.
- -
-
Page/Page column 49
(2010/02/14)
-
- THYROID RECEPTOR AGONISTS
-
The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.
- -
-
Page/Page column 66
(2010/02/14)
-
- Substituted 4-phthalimidocarboxanilides as inhibitors of purine salvage phosphoribosyltransferases
-
The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
- -
-
-
- SPECIFIC ORTHO ORIENTATION IN THE VICARIOUS SUBSTITUTION OF HYDROGEN IN AROMATIC NITRO COMPOUNDS WITH CARBANION OF CHLOROMETHYL PHENYL SULFONE
-
Vicarious nucleophilic substitution of hydrogen atoms in nitroarenes with chloromethylphenyl sulfone proceeds selectively ortho to the nitro group when carried out in t-BuOK/THF base/solvent system.In the majority of 3-substituted nitrobenzene derivatives substitution occurs at the most hindered position 2.These conditions offer an efficient method of synthesis of 2,6 and 2,3-disubstituted nitrobenzene derivatives.
- Makosza, M.,Glinka, T.,Kinowski, A.
-
p. 1863 - 1868
(2007/10/02)
-