658-89-9

Usage

InChI:InChI=1/C7H7F3N2O/c8-7(9,10)13-4-1-2-5(11)6(12)3-4/h1-3H,11-12H2

Upstream product

• 1351534-05-8 2-amino-4-trifluoromethoxy-N-acetylaniline 
• 461-82-5 4-(trifluoromethoxy)aniline 
• 1737-06-0 N-(4-(trifluoromethoxy)phenyl)acetamide 
• 787-57-5 2-nitro-4-trifluoromethoxy-N-acetylaniline 
• 69695-61-0 2-chloro-4-(trifluoromethoxy)aniline 
• 175278-17-8 2-bromo-4-trifluoromethoxyaniline 
• 123-30-8 4-amino-phenol 
• 2267-22-3 2-nitro-5-(trifluoromethoxy)aniline 
• 2267-23-4 2-nitro-4-trifluoromethoxyaniline 

Downstream Products

• 886465-13-0 1-(2-amino-4-trifluoromethoxy-phenyl)3-prop-2-ynyl-thiourea 
• 886465-12-9 1-(2-amino-5-trifluoromethoxy-phenyl)3-prop-2-ynyl-thiourea 
• 877681-12-4 5-(trifluoromethoxy)-1,3-dihydro-2H-benzo[d]imidazol-2-one 
• 1351534-24-1 (2R)-2-[2-chloro-5-[[3-(6-methoxybenzisoxazol-3-yl)-2-oxo-5-trifluoromethoxybenzimidazol-1-yl]methyl]phenoxy]propanoic acid 
• 114164-97-5 2-methyl-5-trifluoromethoxybenzimidazole 
• 919215-18-2 2-phenyl-5-trifluoromethoxybenzimidazole 

Relevant academic research and scientific papers

SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS

The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.

HMOX1 inducers

The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.

Synthesis method of 5-(trifluoromethoxy)-1H-benzo[d] imidazole-2-carboxylic acid

The invention belongs to the technical field of medical intermediates, and particularly relates to a synthesis method of 5-(trifluoromethoxy)-1H-benzo[d] imidazole-2-carboxylic acid. A compound A is used as an initial raw material, through the effect of i

Preparation method of 4- polyfluoro methoxy O-phenylenediamine (by machine translation)

The method disclosed by the invention 4 - is characterized in that the aminophenol, and the alkali :(1) are reacted at a mole ratio of the 1:0.8-1.5, 20-40 °C compound 0.1-24h with the halogen, and, the halogen compound in the solvent to 1:1.0-3.0,20-120 °C, 0.01-20Mpa react with 1-72h. 1-72h the 4 - 1:0.8-30.0 ammonia solution ;(2)4 - or the halogen compound at a mole ratio of the compound of the 1:0.2 - 2.5 amino phenol, 30-80 °C with 0.1-24h;(3)4 - the halogen and the halogen compound in the solvent 0.1-10%, 50-200 °C, 0.01-10Mpa: 4 . (by machine translation)

HETEROCYCLIC ACETAMIDE COMPOUND

[Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.

METALLOENZYME INHIBITOR COMPOUNDS

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Benzimidazolones: A new class of selective peroxisome proliferator- activated receptor γ (PPARγ) modulators

A series of benzimidazolone carboxylic acids and oxazolidinediones were designed and synthesized in search of selective PPARγ modulators (SPPARγMs) as potential therapeutic agents for the treatment of type II diabetes mellitus (T2DM) with improved safety profiles relative to rosiglitazone and pioglitazone, the currently marketed PPARγ full agonist drugs. Structure-activity relationships of these potent and highly selective SPPARγMs were studied with a focus on their unique profiles as partial agonists or modulators. A variety of methods, such as X-ray crystallographic analysis, PPARγ transactivation coactivator profiling, gene expression profiling, and mutagenesis studies, were employed to reveal the differential interactions of these new analogues with PPARγ receptor in comparison to full agonists. In rodent models of T2DM, benzimidazolone analogues such as (5R)-5-(3-{[3-(5-methoxybenzisoxazol-3-yl)benzimidazol-1-yl]methyl}phenyl) -5-methylox-azolidinedione (51) demonstrated efficacy equivalent to that of rosiglitazone. Side effects, such as fluid retention and heart weight gain associated with PPARγ full agonists, were diminished with 51 in comparison to rosiglitazone based on studies in two independent animal models. (Figure presented)

SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY

The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N- C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.

BENZIMIDAZOLES WITH A HETERO SPIRO-DECANE RESIDUE AS NPY-Y5 ANTAGONISTS

The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, formula (I), R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to -0-R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY- Y5 receptor antagonists.

PROPARGYL TRIFLUOROMETHOXY AMINOBENZIMIDAZOLE DERIVATIVES

Disclosed are compounds having the structure: wherein X is a) where R1 is H, C1-C6 alkyl, C3-C6 alkenyl, or C3-C6 alkynyl; R2 is H or C1-C4 alkyl