- Discovery and optimization of pyrazole amides as antagonists of CCR1
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A HTS screen for CCR1 antagonists afforded a novel sub-micromolar hit 5 containing a pyrazole core. In this report the design, optimization, and SAR of novel CCR1 antagonists based on a pyrazole core motif is presented. Optimization led to the advanced ca
- Harcken, Christian,Sarko, Christopher,Mao, Can,Lord, John,Raudenbush, Brian,Razavi, Hossein,Liu, Pingrong,Swinamer, Alan,Disalvo, Darren,Lee, Thomas,Lin, Siqi,Kukulka, Alison,Grbic, Heather,Patel, Mita,Patel, Monica,Fletcher, Kim,Joseph, David,White, Della,Amodeo, Laura,Berg, Karen,Brown, Maryanne,Thomson, David S.
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p. 435 - 440
(2018/11/23)
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- AMIDOPYRIDINE DERIVATIVE, AND USE THEREOF
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The present invention relates to novel amidopyridine derivatives. More specifically, the present invention provides a medicinal agent which is useful as a prophylactic or therapeutic agent for diseases based on the production of cytokines from T cells, comprising as the active ingredient an amidopyridine derivative or a pharmacologically acceptable salt thereof. Provided are an amidopyridine derivative of the following general formula (I): wherein each symbol has the same meaning as defined in the description, or a pharmacologically acceptable salt thereof.
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Paragraph 0338; 0341; 0342
(2016/10/08)
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- Rearrangements of N-heterocyclic carbenes of pyrazole to 4-aminoquinolines and benzoquinolines
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1-Phenyl-substituted pyrazolium salts, formed by quaternization of pyrazoles with benzyl halides or long-chain alkyl halides, deprotonate to pyrazol-3-ylidenes that undergo a sequence of ring-opening, ring-closure, and tautomerization to new substituted 4
- Dreger, Andrij,Cisneros Camuna, Rafael,Munster, Niels,Andras Rokob, Tibor,Papai, Imre,Schmidt, Andreas
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experimental part
p. 4296 - 4305
(2010/10/19)
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- Pyrazole-amides and sulfonamides as sodium channel modulators
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Compounds of the present invention modulate PN3 in mammals and are useful in treating pain in mammals.
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Page/Page column 15
(2010/02/10)
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- Pyrazole-amides and sulfonamides as sodium channel modulators
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Compounds of the present invention modulate PN3 in mammals and are useful in treating pain in mammals.
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- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
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The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
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