- Novel biphenyl derivative as well as preparation method and medical application thereof
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The invention relates to the field of medicinal chemistry, and discloses biphenyl derivatives with PD-1/PD-L1 inhibitory activity as well as a preparation method and application of the biphenyl derivatives. The invention further discloses a composition containing the biphenyl derivative with the PD-1/PD-L1 inhibitory activity or the pharmaceutically acceptable salt of the biphenyl derivative and a pharmaceutically acceptable carrier of the biphenyl derivative, and application of the biphenyl derivative in preparation of a PD-1/PD-L1 inhibitor. The compound can be used for treating tumors.
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Paragraph 0065; 0085; 0097-0099
(2021/07/21)
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- SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS AND METHODS USING SAME
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The present invention includes substituted 1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same. In one aspect, the compounds contemplated in the invention can be used to treat, ameliorate, or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient. In another aspect, the compounds contemplated in the invention can be used to treat, ameliorate, and/or prevent cancer in a patient.
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Page/Page column 313-315
(2021/08/13)
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- Heterocycle-substituted styryl-4-phenylpyridine derivative as well as preparation method and medical application thereof
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The invention relates to a heterocycle-substituted styryl-4-phenylpyridine derivative, a preparation method thereof and an application of the heterocycle-substituted styryl-4-phenylpyridine derivativeas a PD-1/PD-L1 inhibitor. Specifically, the invention discloses a compound shown as a formula (I) or pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and application thereof, and the definition of each group in the formula is shown in the specification and claims in detail.
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Paragraph 0147-0149
(2020/11/02)
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- PYRIMIDINE DERIVATIVES AS INHIBITORS OF PD1/PD-L1 ACTIVATION
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The compounds of Formula Ib, Formula Ia, and Formula I are described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The process of preparation of the compounds of Formula Ib, Formula Ia, and Formula I is also described. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are 2-(benzyloxy)pyrimidine derivatives that are inhibitors of PD-1/PD-L1 activation.
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Paragraph 000172
(2019/05/22)
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- BICYCLIC COMPOUNDS AS INHIBITORS OF PD1/PD-L1 INTERACTION/ACTIVATION
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The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation.
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Paragraph 00098
(2019/10/04)
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- SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME
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The present invention includes substituted 3,3'-bis(phenoxymethyl)-1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.
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Page/Page column 77; 78
(2019/10/23)
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- UREA COMPOUND AND PREPARATION METHOD AND APPLICATION THEREOF
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The present invention relates to a urea compound and a preparation method and an application thereof. The structure of the present compound is represented by formula (I), the definition of each variable in the formula being as described in the description. The compound can block interaction between the PD-1/PD-L1 signalling pathways. The compound of the present invention can be used for treating or preventing diseases related to the signalling pathways, such as cancer, autoimmune disease, chronic infectious disease, and other diseases.
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Paragraph 0072; 0073
(2019/11/14)
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- IMMUNE CHECKPOINT INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, X1, Y1 and n are as defined in the specification. The inventive Formula (I) compounds are inhibitors of the PD-1/PD-L1 protein/protein binding or functional interaction and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer and infectious diseases.
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Paragraph 0377
(2018/03/25)
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- DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
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The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
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- Substituted 4-aryl-4h-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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Page/Page column 16
(2008/06/13)
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- CB1 MODULATOR COMPOUNDS
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Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.
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Page/Page column 66-67
(2008/06/13)
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- Synthesis and reactions of a chemical model of the urocanase reaction
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Using a convergent synthetic strategy starting from nicotinic acid and imidazole, we have prepared the (E) and (Z) isomers of 1-benzyl-3-carbamoyl-5-[2-(ethoxycarbonylmethylene)-2(1-(p-tolylsulfamoyl)i midazol-4-yl)ethyl]pyridinium bromide (21) as models
- Winter, Joachim,Rétey, János
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p. 410 - 416
(2007/10/03)
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- Pyridinecarboxyimidamide compounds and the use thereof
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Disclosed are pyridinecarboximidamides having a vasodilating effect (hypotensive activity or antianginal activity), and acid adduct salts thereof. STR1 wherein when R1 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group, R2 represents a hydrogen atom and R3 represents a nitroxyl, 2-chlorophenyl or phenyl group; and when R1 represents a hydrogen atom, R2 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group and R3 represents a nitroxyl, 2-chlorophenyl or phenyl group. There is also disclosed the use of the compounds represented by the formula (I) for antihypertensive or antianginal purpose.
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- 5-substituted-6-aminopyrimidine derivatives
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A compound of the formula: STR1 in which R1 is --OH or --NH2 ; R2 is a halogen or --CN; R3 is a halogen or --CN; and n is one of the integers 1, 2 or 3; or a pharmaceutically acceptable salt thereof, are useful as antithrombotic agents.
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