- HETEROCYCLIC AMIDES AS KINASE INHIBITORS FOR USE IN THE TREATMENT CANCER
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Disclosed is a method of treating cancer in a human in need thereof, the method comprising administering to the human a RIP1 kinase inhibitor at a dose of about 50 mg to about 1600 mg. Also disclosed is a method of treating cancer in a human in need thereof, the method comprising administering to the human a RIP1 kinase inhibitor at a dose of about 50 mg to about 1600 mg, and administering to the human a PD1 antagonist thereof at a dose of about 200 mg.
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Page/Page column 82; 100
(2020/03/24)
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- HETEROCYCLIC AMIDES AS KINASE INHIBITORS
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Disclosed is a combination of a RIP1 kinase inhibitor compound and at least one other therapeutically active agent for use in the treatment of a RIP1 kinase mediated disease or disorder; particularly disclosed is a combination of a RIP1 kinase inhibitor compound and at least one other therapeutically active agent, wherein the at least one other therapeutically active agent is an immuno-modulator, for use in the treatment of cancer.
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Page/Page column 92
(2018/09/26)
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- INHIBITORS OF PI3 KINASE
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The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.
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Page/Page column 106
(2010/01/12)
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- HETEREOARYL NITRILE DERIVATIVES
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The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical con
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- Applications of ethyl carboethoxyformimidate to heterocyclic synthesis: Preparation of condensed pyrazinones and 1,4-oxazinones
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Aromatic and heteroaromatic 1,2-diamines, and o-aminophenols, condense smoothly with ethyl carboethoxyformimidate to give good yields of condensed pyrazinones and 1,4-oxazinones.
- McKillop, Alexander,Chattopadhyay, Shital K.,Henderson, Alan,Avendano, Carmen
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p. 301 - 304
(2007/10/03)
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- Synthesis of 4-Alkoxy-1,3-oxazol-5(2H)-ones, Precursors of 1-Alkoxy-Substituted Nitrile Ylides
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4-Alkoxy-1,3-oxazol-5(2H)-ones of type 4 and 7 were synthesized by two different methods: oxidation of the 4-(phenylthio)-1,3-oxazol-5(2H)-one 2a with m-chloroperbenzoic acid in the presence of an alcohol gave the corresponding 4-alkoxy derivatives 4, presumably via nucleophilic substitution of an intermediate sulfoxide (Scheme 2).The second approach is the BF3-catalyzed condensation of imino-acetates of type 6 and ketones (Scheme 3).The yields of this more straightforward method were modest due to the competitive formation of 1,3,5-triazine tricarboxylate 8.At 155 deg C, 1,3-oxazol-5(2H)-one 7b underwent decarboxylation leading to an alkoxy-substituted nitrile ylide which was trapped in a 1,3-dipolar cycloaddition by trifluoro-acetophenone to give the dihydro-oxazoles cis- and trans-9 (Scheme 4).In the absence of a dipolarophile, 1,5-dipolar cyclization of the intermediate nitrile ylide yielded isoindole derivatives 10 (Schemes 4 and 5).
- Bozhkova, Nina,Heimgartner, Heinz
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p. 825 - 837
(2007/10/02)
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- Cephem and cepham compounds
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This invention relates to new cephem and cepham compounds of high antimicrobial activity of the formula: STR1 wherein R1 is amino or a protected amino, R2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S or O containing 5-membered heterocyclic group substituted with oxo group(s), R3 is hydrogen or lower alkyl, R4 is hydrogen, acyloxy(lower)alkyl; acylthio(lower) alkyl; pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl;l halogen; hydroxy; thiazolium(lower)alkyl which may be substituted with suitable substituent(s); or lower alkoxy; R5 is carboxy or a protected carboxy, wherein R5 is COO- when R4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s) or thiazolium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond; and pharmaceutically acceptable salt thereof.
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- Cephem and cepham compounds
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This invention relates to novel 7-thiadiazol-oxyimino-3-cephem and cepham 4-carboxylic acid compounds of high antimicrobial activity.
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- Cephem and cepham compounds
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7-Substituted-3-cephem and cepham-4-carboxylic acids represented by the following formula (I): STR1 wherein R1 is amino or a protected amino, R2 is hydrogen, acyl, aryl which may be substituted with suitable substituent(s), lower alkyl substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cycloalkyl which may be substituted with suitable substituent(s), cyclo(lower)alkenyl, or S or O containing 5-membered heterocyclic group substituted with oxo group(s), R3 is hydrogen or lower alkyl, R4 is hydrogen; acyloxy(lower)alkyl); acylthio(lower)alkyl; pyridinium(lower)alkyl which may be substituted with suitable substituent(s); a heterocyclicthio(lower)alkyl which may be substituted with suitable substituent(s); lower alkyl; halogen; or hydroxy; and, R5 is carboxy or a protected carboxy, wherein R5 is COO- when R4 is pyridinium(lower)alkyl which may be substituted with suitable substituent(s), and the heavy solid line means single or double bond, are useful as antibiotics.
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