- SUBSTITUTED PYRROLOPYRIDINES AS JAK INHIBITORS
-
The present invention relates to new pyrrolopyridine compounds having the structures of Formula (I)-(IV), wherein the R groups, A, B, C, D and n are as defined in the detailed description, and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.
- -
-
Paragraph 0462; 0463
(2020/11/12)
-
- PROCESSES FOR THE PREPARATION OF FILGOTINIB
-
The present invention relates to processes for the preparation of Filgotinib. The present invention relates to novel processes for the preparation of filgotinib. The present invention also relates to novel intermediates for the preparation of filgotinib.
- -
-
Paragraph 0090-0091
(2020/03/09)
-
- THERAPEUTIC COMPOUNDS AND USES THEREOF
-
The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R5-R6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
- -
-
Page/Page column 193; 194
(2017/12/29)
-
- PROCESS FOR PREPARATION OF t-BUTOXYCARBONYLAMINE COMPOUNDS
-
Provided is a process for the preparation of t-butoxycarbonylamine compounds, which comprises using phosgene or a phosgene equivalent, t-butanol, and an organic base. Even when applied to a primary or secondary amine compound having low nucleophilicity, the process enables highly selective preparation of a t-butoxycarbonylamine compound at a low cost. In the process, a t-butoxycarbonylamine compound is prepared using: phosgene or a phosgene equivalent; t-butanol; an organic base; and either a primary or secondary amine compound or a primary or secondary ammonium salt.
- -
-
Page/Page column 6
(2013/02/28)
-
- PYRIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
-
The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
- -
-
Page/Page column 77
(2012/08/08)
-
- PYRIMIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
-
The present invention provides a pyrimidine compound of formula (I): wherein one of X and Y but not both is N, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tantomers, diastereomers, deuterated versions, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds
- -
-
Page/Page column 125
(2012/08/08)
-
- N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
-
The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
- -
-
Page/Page column 92
(2012/08/08)
-
- N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
-
The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
- -
-
Page/Page column 132
(2012/08/08)
-
- 2,6-Diaminopyridine compounds for treating diseases associated with amyloid proteins or for treating ocular diseases
-
The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compoun
- -
-
Page/Page column 31; 32
(2011/05/04)
-
- Heteroaryl Compounds and Their Uses
-
The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.
- -
-
Page/Page column 20-21
(2011/02/25)
-
- 2,6-Diaminopyridine Compounds Suitable For Treating Diseases Associated With Amyloid Or Amyloid-Like Proteins Or For Treating Or Preventing Ocular Diseases Or Conditions Associated With A Pathological Abnormality/Change In The Tissue Of The Visual System
-
The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
- -
-
Page/Page column 29-30
(2011/05/03)
-
- 2,6-DIAMINOPYRIDINE COMPOUNDS SUITABLE FOR TREATING DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS OR FOR TREATING OR PREVENTING OCULAR DISEASES OR CONDITIONS ASSOCIATED WITH A PATHOLOGICAL ABNORMALITY/CHANGE IN THE TISSUE OF THE VISUAL SYSTEM
-
The present invention relates to 2.6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compoun
- -
-
Page/Page column 65
(2011/05/05)
-
- Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2- ethanediones: Potent, selective carboxylesterase inhibitors
-
Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic,
- Young, Brandon M.,Hyatt, Janice L.,Bouck, David C.,Chen, Taosheng,Hanumesh, Parimala,Price, Jeanine,Boyd, Vincent A.,Potter, Philip M.,Webb, Thomas R.
-
supporting information; experimental part
p. 8709 - 8715
(2011/02/23)
-
- FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES
-
The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of p
- -
-
-
- NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel compounds corresponding to the general formula (I) below: and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also
- -
-
Page/Page column 39-40
(2010/11/08)
-
- INHIBITORS OF HEPATITIS C VIRUS PROTEASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
-
The present invention provides compounds of formula (I), (II) or (IV), or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of the Hepatitis C virus (HCV) protease enzyme and are also useful for the treatment of HCV infections in HCV--infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of formula (I), (II) or (IV), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formulas (I), (II) and (IV).
- -
-
Page/Page column 104
(2008/06/13)
-
- Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors
-
Pathological angiogenesis is associated with disease states such as cancer, diabetic retinopathy, rheumatoid arthritis, endometriosis, and psoriasis. There is much evidence that direct inhibition of the kinase activity of vascular endothelial growth facto
- Kuo, Gee-Hong,Wang, Aihua,Emanuel, Stuart,DeAngelis, Alan,Zhang, Rui,Connolly, Peter J.,Murray, William V.,Gruninger, Robert H.,Sechler, Jan,Fuentes-Pesquera, Angel,Johnson, Dana,Middleton, Steven A.,Jolliffe, Linda,Chen, Xin
-
p. 1886 - 1900
(2007/10/03)
-
- NOVEL COMPOUNDS THAT MODULATE PPARγ TYPE RECEPTORS, AND USE THEREOF IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
-
The invention relates to novel compounds corresponding to the general formula (I) below: (I) and also to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism),-or alternatively in cosmetic compositions.
- -
-
-
- Substituent Effects on the Isomer Ratios in the Rearrangement of Some 2- and 4-Nitraminopyridines
-
The preparation, and rearrangement in 92percent sulfuric acid, of 4-X-2-nitramino- (1), 2-X-4-nitramino- (2), and 6-X-2-nitramino-pyridines (3) is reported (X=H,Me,MeO,Br,Cl,CO2H).The product isomer ratios can be explained by differential electronic stabilization of the appropriate ? complexes for aromatic nitration and steric effects seem relatively unimportant.Deuteration had no effect on the product distribution
- Deady, Leslie W.,Korytsky, Olga L.,Rowe, Jeffrey E.
-
p. 2025 - 2034
(2007/10/02)
-