- 9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS
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The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
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Paragraph 0555-0556
(2015/09/28)
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- JTE013 ANALOGS AND METHODS OF MAKING AND USING SAME
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JTE013 analogs having similar or greater stability relative to JTE013 are provided. Also provided are JTE013 analogs which can bind to both S1P2 and S IP5, some of which also have similar or greater stability relative to JTE013. In a
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Page/Page column 47-48
(2012/01/06)
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- Discovery of new orally active phosphodiesterase (PDE4) inhibitors
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A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.
- Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
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p. 1098 - 1104
(2007/10/03)
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- Method for inhibiting neoplastic cells and related conditions by exposure to substituted N- arylmethyl and heterocyclmethyl-1H-pyrazolo (3,4-B) quinolin-4-amines
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A method for inhibiting neoplastic cells and related conditions by exposing them to substituted N-arylmethyl and heterocyclmethyl-1H-pyrazolo?3,4-B!quinolin-4-amines.
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- Substituted N-arylmethyl and heterocyclmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines and compositions and methods of use thereof
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Substituted N-arylmethyl and heterocyclylmethyl-1H-pyrazolo[3,4-b]quinolin-4-amines, pharmaceutical compositions containing them and methods for a) effecting c-GMP-phosphodiesterase inhibition, b) treating heart failure and/or hypertension, c) reversing o
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- Synthesis of vicinal aminoiodo- and (acetylamino)iodo-1-alkylpyrazoles
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3- and 5-(Acetylamino)-4-iodo-1-alkylpyrazoles were obtained by successive acylation and iodination from 3- and 5-amino-1-alkylpyrazoles without isolating intermediate (acetylamino)pyrazoles. 3- and 5-Iodo- and 3,5-diiodo-4-amino-1-methylpyrazoles were synthesized from appropriate iodonitropyrazoles by reduction with SnCl2 in HCl.
- Tret'yakov,Vasilevsky
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p. 2585 - 2587
(2007/10/03)
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