57012-20-1

Usage

Chemical Properties

Light yellow solid

InChI:InChI=1/C6H10N2O/c1-5-3-6(4-9)8(2)7-5/h3,9H,4H2,1-2H3

Upstream product

• 10250-59-6 1,3-dimethyl-1H-pyrazole-5-carboxylic acid methyl ester 
• 891273-63-5 1,3-dimethylpyrazole-5-carboxylic acid isopropyl ester 
• 5744-40-1 ethyl 1,3-dimethylpyrazole-5-carboxylate 

Downstream Products

• 1945950-21-9 PDD00017273 
• 1182280-64-3 N-(2,5-dimethyl-2H-pyrazol-3-ylmethyl)-4-(5-trifluormethyl-pyridin-2-yloxy)-benzenesulfonamide 
• 499770-63-7 1-(1,3-dimethyl-1H-pyrazol-5-yl)methanamine 
• 1374868-77-5 (4-bromo-1,3-dimethyl-1H-pyrazol-5-yl)methanol 
• 1356998-41-8 (4-iodo-1,3-dimethyl-1H-pyrazol-5-yl)methanol 

Relevant academic research and scientific papers

MACROCYCLIC COMPOUNDS

Disclosed are macrocyclic compounds of formula (I) comprising a 2-carboxy indole ring. Such compounds, and their pharmaceutically acceptable salts, are useful as Mcl-1 (myeloid cell leukemia-1) inhibitors. The compounds may be used in treating a disease o

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity

Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein we report a series of MCL-1 inhibitors that emanated from a high throughput screening (HTS) hit and progressed via iterative cycles of structure-guided design. Advanced compounds from this series exhibited subnanomolar affinity for MCL-1 and excellent selectivity over other BCL-2 family proteins as well as multiple kinases and GPCRs. In a MCL-1 dependent human tumor cell line, administration of compound 30b rapidly induced caspase activation with associated loss in cell viability. The small molecules described herein thus comprise effective tools for studying MCL-1 biology.

SUBSTITUTED SULFONIC ACID AMIDE COMPOUNDS

The present invention relates to the use of substituted sulfonic acid amide compounds of formula I, wherein Ra, n, Het, A, Y and D are as defined in the claims and the N-oxides and the salts thereof for combating phytopathogenic harmful fungi,

Novel bicyclic heterocyclic compounds, process for their preparation and compositions containing them

The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low expression of Perlecan.

FUSED PYRIMIDINE DERIVATIVES AND COMPOSITIONS THEREOF AS CXCR3 RECEPTOR MODULATORS, USEFUL IN PREVENTION AND TREATMENT OF INFLAMMATORY AND IMMUNOREGULATORY DISORDERS AND DISEASES

Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

TETRAHYDROQUINAZOLIN-4(3H)-ONE-RELATED AND TETRAHYDROPYRIDO[2,3-D]PYRIMIDIN-4(3H)-ONE-RELATED COMPOUNDS, COMPOSITIONS AND METHODS FOR THEIR USE

Compounds are provided having the formula (I) wherein variables A1, A2, A3, A4, R1, R2, R3, R4, Q and L are described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

INDANE DERIVATES AS MUSCARINIC RECEPTOR AGONISTS

The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptor.