- TRIAZOLO-PYRIMIDINE COMPOUNDS AND USES THEREOF
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The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
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Page/Page column 107-108
(2020/05/07)
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- PYRIDINONE DERIVATIVES AND THEIR USE AS SELECTIVE ALK-2 INHIBITORS
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The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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Page/Page column 47-48; 56
(2019/06/11)
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- Substituted thiazole derivative and application thereof
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The invention provides a compound represented by a general formula (I), or a stereoisomer, pharmaceutically acceptable salt, solvate, hydrate, chemically protective form or prodrug thereof. The compound has an effect of inhibiting adenosine receptor 2a (A2a), and can be used as an antagonist of the adenosine receptor 2a (A2A) for treating tumors.
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Paragraph 0388-0392
(2019/02/13)
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- Synthesis and evaluation of thiomannosides, potent and orally active FimH inhibitors
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FimH is a type I fimbrial lectin located at the tip of type-1 pili of Gram-negative uropathogenic Escherichia coli (UPEC) guiding its ability to adhere and infect urothelial cells. Accordingly, blocking FimH with small molecule inhibitor is considered as a promising new therapeutic alternative to treat urinary tract infections caused by UPEC. Herein, we report that compounds having the S-glycosidic bond (thiomannosides) had improved metabolic stability and plasma exposures when dosed orally. Especially compound 5h showed the potential to inhibit biofilm formation and also to disrupt the preformed biofilm. And compound 5h showed prophylactic effect in UTI model in mice.
- Sattigeri, Jitendra A.,Garg, Malvika,Bhateja, Pragya,Soni, Ajay,Rauf, Abdul Rehman Abdul,Gupta, Mahendrakumar,Deshmukh, Mahesh S.,Jain, Tarun,Alekar, Nidhi,Barman, Tarani Kanta,Jha, Paras,Chaira, Tridib,Bambal, Ramesh B.,Upadhyay, Dilip J.,Nishi, Takahide
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p. 2993 - 2997
(2018/07/21)
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- DI-SUBSTITUTED PYRAZOLE COMPOUNDS FOR THE TREATMENT OF DISEASES
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Provided herein are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and compositions in treating a condition, disease, or disorder associated with abnormal activation of the SREBP pathway, including metabolic disorders such as obesity, cancer, cardiovascular disease, and nonalcoholic fatty liver disease (NAFLD) wherein the compound is according to Formula (I).
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Paragraph 00315
(2017/12/15)
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- 1-ALKYL-6-OXO-1,6-DIHYDROPYRIDIN-3-YL COMPOUNDS AND USE AS SGRM MODULATORS
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This specification generally relates to 1-alkyl-6-oxo-1,6-dihydropyridin-3-yl compounds (including salts thereof). This specification also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including treatment methods and medicament preparations), and processes for making such a compound.
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Paragraph 257
(2016/04/20)
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- Condensed derivatives of imidazole useful as pharmaceuticals
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The invention relates to the compounds (I) and their acids and bases salts: wherein: the dotted line indicates a double bond; X is N or C-R1 and Y is N or C-R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is Hydrogen or a substituent as defined in the application, or B is a (4-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, and possibly substituted as defined in the application; B not being Hydrogen when X is N and Y is C-R2; R1 is Hydrogen or a substituent as defined in the application; B and R1 cannot be simultaneously Hydrogen; R2 is Hydrogen or Halogen; their preparation, their use in the antibacterial prevention and therapy, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.
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Paragraph 0526
(2015/09/23)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
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Paragraph 0997; 0998
(2013/03/26)
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- BENZOTHIOPHENE SULFONAMIDES AND OTHER COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN
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The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
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Page/Page column 227
(2013/12/03)
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- SUBSTITUTED N-[1-CYANO-2-(PHENYL)ETHYL] 1-AMINOCYCLOALK-1-YLCARBOXAMIDE COMPOUNDS - 760
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The present invention provides compounds of formula (I) in which, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 111-112
(2012/01/05)
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- cMET INHIBITORS
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Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
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Page/Page column 214
(2010/04/03)
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- SUBSTITUTED PYRIDONE DERIVATIVE
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Compounds of the formula: (I) [wherein A is the formula: (III-1) R3 is a hydrogen atom, lower alkyl, etc.; m is 0 or 1; R1 is a hydrogen atom, halogen atom, etc.; R2 is a hydroxyl, etc.; p is 0 to 4; X is a carbon atom or
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Page/Page column 48
(2008/06/13)
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- BROMINATION OF 1-ALKYL-2-PYRIDONES
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The corresponding monobromides were obtained in the bromination of 1-alkyl-2-pyridones with bonded bromine (with N-bromosuccinimide and dioxane dibromide).The conditions under which the yields of the mixtures of isomers were 60-80percent, and almost no dibromides were obtained, were found.It was established that the ratios of the 3- and 5-bromo isomers depend on the character of the brominating agent.
- Shusherina, N.P.,Likhomanova, T.I.,Nikolaeva, S.N.
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p. 1284 - 1286
(2007/10/02)
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- CYCLOHEXYLATION OF N-ETHYL-2-PYRIDONE IN THE PRESENCE OF ALUMINIUM CHLORIDE
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The possibility of direct alkylation of N-ethyl-2-pyridone under Friedel-Crafts conditions was demonstrated.The reaction of N-ethyl-2-pyridone with cyclohexyl chloride in the presence of aluminium chloride took place at positions 3 and 5.
- Saidova, F. M.,Binchkauskas, V. Sh.,Khorev, S. G.,Enikeev, E. Ya.
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p. 353 - 357
(2007/10/02)
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