- CHEMICAL COMPOUNDS
-
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
- -
-
Paragraph 0185-0187
(2021/04/02)
-
- COMPOUND AS ACC INHIBITOR AND USE THEREOF
-
Disclosed are a class of compounds which are inhibitors of acetyl-CoA carboxylase (ACC) and the use thereof. In particular, provided are compounds as shown in formula I or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, and methods for preparing the same, and pharmaceutical compositions comprising the compounds and the use of the compounds or compositions for treating and/or preventing diseases associated with ACC expression, such as fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases. The compound has a good inhibitory activity against ACC and shows good promise to be a therapeutic drug for fibrotic diseases, metabolic diseases, cancers or tissue hyperplasia diseases.
- -
-
Paragraph 0343; 0344
(2020/06/15)
-
- ISOXAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF PULMONARY DISEASES AND DISORDERS
-
The present disclosure features disclosed method of treating disorders such as COPD, bronchitis and/or asthma using disclosed compounds, optionally together with one or more additional active agents. Contemplated methods include administrating orally or by inhalation to a patient one or more disclosed compounds.
- -
-
Paragraph 0293
(2017/03/21)
-
- COMPOUNDS, COMPOSITIONS, AND METHODS FOR INCREASING CFTR ACTIVITY
-
The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
- -
-
Paragraph 0129
(2016/07/27)
-
- DERIVATIVES OF 3-HETEROARYLISOXAZOL-5-CARBOXYLIC AMIDE USEFUL FOR THE TREATMENT OF INTER ALIA CYSTIC FIBROSIS
-
The present disclosure is based, in part, on the discovery that disclosed compounds can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
- -
-
Paragraph 0180
(2016/07/27)
-
- COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY
-
The present disclosure features compounds such as those having the Formulae (Ila), (lIb), (lIc), (Ild), (IlIa), and (Illb), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (Ila), (lIb), (lIc), (lId), (IlIa), or (Illb).
- -
-
Paragraph 0334
(2016/11/07)
-
- METALLO-BETA-LACTAMASE INHIBITORS
-
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
- -
-
Page/Page column 266
(2017/04/04)
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND USE THEREOF
-
Provided are therapeutically active compounds and the use in manufacture of medicaments for treating a cancer characterized by the presence of a mutant allele of IDH1.
- -
-
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
-
- COMPOUNDS, COMPOSITIONS AND METHODS OF INCREASING CFTR ACTIVITY
-
The present disclosure features disclosed compounds which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound.
- -
-
Paragraph 0341
(2016/02/24)
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
Page/Page column
(2015/03/31)
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
Page/Page column
(2015/02/19)
-
- AMINO PYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS
-
The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.
- -
-
Page/Page column 315
(2015/11/10)
-
- PYRROLOPYRIMIDINE AND PURINE DERIVATIVES
-
The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
- -
-
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
-
- THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
-
- HEPATITIS B ANTIVIRAL AGENTS
-
The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
- -
-
Page/Page column 221
(2013/07/05)
-
- THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
-
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
- -
-
Page/Page column
(2013/07/31)
-
- HETEROARYLOXYCARBOCYCLYL COMPOUNDS AS PDE10 INHIBITORS
-
Heteroaryloxycarbocyclyl compounds of formula (I), and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive -compulsive disorder, and the like. Formula (I)
- -
-
Page/Page column 47-48
(2011/12/02)
-
- CYCLOALKYLAMINE SUBSTITUTED ISOQUINOLONE DERIVATIVES
-
The invention relates to 6-substituted isoquinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and composit
- -
-
Page/Page column 70-71
(2008/12/06)
-
- 2, 4-DIAMINOPYRIMIDINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER
-
The present invention encompasses compounds of general formula (1) wherein Q and R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the
- -
-
Page/Page column 20
(2008/06/13)
-
- 2,4-DI(AMINOPHENYL) PYRIMIDINES AS PLK INHIBITORS
-
The invention relates to compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1, and R3 are defined as indicated in claim 1. Said compounds are used for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament having said properties.
- -
-
Page/Page column 48
(2008/06/13)
-