- TETRAHYDROQUINOLINO DERIVATIVES FOR THE TREATMENT OF METASTATIC AND CHEMORESISTANT CANCERS
-
Disclosed herein are compounds of Structural Formula I. Compounds of Structural Formula I inhibit aldehyde dehydrogenase isoform Ia3 (ALDHIa3) and are useful for treating cancer, for example, metastatic or chemoresistant cancer, such as metastatic cancer resistant to chemotherapy. Also disclosed herein are compositions comprising compounds of Structural Formula I and uses of compounds of Structural Formula I for treating cancer, for example, metastatic or chemoresistant cancer.
- -
-
Paragraph 00172
(2020/02/23)
-
- Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors
-
Protein arginine methyltransferase 5 (PRMT5) is an epigenetics related enzyme that has been validated as a promising therapeutic target for human cancer. Up to now, two small molecule PRMT5 inhibitors has been put into phase I clinical trial. In the prese
- Zhu, Kongkai,Song, Jia-Li,Tao, Hong-Rui,Cheng, Zhi-Qiang,Jiang, Cheng-Shi,Zhang, Hua
-
supporting information
p. 3693 - 3699
(2018/10/24)
-
- Triazole derivative having HSP90 (Heat Shock Protein) inhibiting activity, as well as preparation method and application of triazole derivative
-
The invention discloses a triazole derivative having an HSP90 (Heat Shock Protein) inhibiting activity, as well as a preparation method and an application of the triazole derivative. Specifically, the invention relates to the triazole derivative having a structure as shown in a formula (I), a stereisomer of the triazole derivative and a pharmaceutically acceptable salt, wherein the definition of each substituent group in the formula (I) and the definition in a description are the same. The compound with a novel structure has the HSP90 inhibiting activity, can be used to cure cancers, neurodegenerative disorders, inflammation diseases, autoimmune diseases, ischemic brain injuries and the like, and has a broad application prospect.
- -
-
Paragraph 0488; 0489; 0490; 0491
(2017/08/02)
-
- 4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS
-
The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 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 273
(2016/06/14)
-
- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R10, R11, R12, R13, R14, R15, R16, R17 and m are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
Page/Page column 32
(2016/05/19)
-
- NEW DIHYDROQUINOLINE PYRAZOLYL COMPOUNDS
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R15, R16, R17 and n are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
Page/Page column 38; 39
(2016/05/19)
-
- Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a ]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability
-
CYP11B2 inhibition is a promising treatment for diseases caused by excessive aldosterone. To improve the metabolic stability in human liver miscrosomes of previously reported CYP11B2 inhibitors, modifications were performed via a combination of ligand-and
- Hu, Qingzhong,Yin, Lina,Ali, Amjad,Cooke, Andrew J.,Bennett, Jonathan,Ratcliffe, Paul,Lo, Michael Man-Chu,Metzger, Edward,Hoyt, Scott,Hartmann, Rolf W.
-
supporting information
p. 2530 - 2537
(2015/03/30)
-
- DIHYDROQUINOLINE-2-ONE DERIVATIVES FOR USE AS ALDOSTERONE SYNTHASE INHIBITORS
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R9, R10 and R11 are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
Page/Page column 30; 31
(2014/09/29)
-
- Exploring DOXP-reductoisomerase binding limits using phosphonated N-aryl and N-heteroarylcarboxamides as DXR inhibitors
-
DOXP-reductoisomerase (DXR) is a validated target for the development of antimalarial drugs to address the increase in resistant strains of Plasmodium falciparum. Series of aryl- and heteroarylcarbamoylphosphonic acids, their diethyl esters and disodium salts have been prepared as analogues of the potent DXR inhibitor fosmidomycin. The effects of the carboxamide N-substituents and the length of the methylene linker have been explored using in silico docking studies, saturation transfer difference NMR spectroscopy and enzyme inhibition assays using both EcDXR and PfDXR. These studies indicate an optimal linker length of two methylene units and have confirmed the importance of an additional binding pocket in the PfDXR active site. Insights into the constraints of the PfDXR binding site provide additional scope for the rational design of DXR inhibitors with increased ligand-receptor interactions.
- Bodill, Taryn,Conibear, Anne C.,Mutorwa, Marius K.M.,Goble, Jessica L.,Blatch, Gregory L.,Lobb, Kevin A.,Klein, Rosalyn,Kaye, Perry T.
-
supporting information
p. 4332 - 4341
(2013/07/27)
-
- DIHYDROQUINOLINE-2-ONE DERIVATIVES
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
- -
-
Paragraph 0873; 0874
(2013/03/28)
-
- NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12/
- -
-
Paragraph 0391; 0392; 0393
(2013/04/10)
-
- NEW DIHYDROQUINOLINE-2-ONE DERIVATIVES
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds.
- -
-
Page/Page column 230; 231
(2013/03/28)
-
- NEW BICYCLIC DIHYDROQUINOLINE-2-ONE DERIVATIVES
-
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4? R5, R6, R7, R8, R9, R10, R11, R12/
- -
-
Page/Page column 78
(2013/04/10)
-
- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
-
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
- -
-
Page/Page column 86
(2012/07/27)
-
- ALDOSTERONE SYNTHASE INHIBITORS
-
This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
- -
-
Page/Page column 124
(2012/11/13)
-
- NOVEL HETEROCYCLIC CARBOXAMIDES AS M1 AGONISTS
-
The present invention relates to novel M1 agonistic compounds of formula (I) and their use in the treatment of cognitive impairment associated i.a. with schizophrenia and in the treatment of other diseases mediated by the muscarinic M1 receptor.
- -
-
Page/Page column 57
(2009/10/21)
-
- TETRAHYDROQUINOLINE, INDOLINE, AND RELATED ANILINE DERIVATIVES OF HETEROCYCLE-FUSED BENZODIOXAN METHYLAMINES
-
The present invention relates to a compound of the formula: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, useful as modulators of 5 -HTi A receptor activity and/or serotonin reuptake. These compounds are useful in treating nervous system disorders, such as anxiety-related disorders, cognition-related disorders, depression, schizophrenia, or sexual dysfunction and related illnesses.
- -
-
Page/Page column 59
(2008/06/13)
-