- AROMATIC COMPOUND
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Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.
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Paragraph 1232; 1233
(2016/05/19)
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- PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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- BRUTON'S TYROSINE KINASE INHIBITORS
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Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I)
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- ARYLALKYLAMINES AND PROCESS FOR PRODUCTION THEREOF
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The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensiing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc. The symbols in the formula represent the following meanings: Ar: optionally substituted aryl or optionally substituted heteroaryl here, the cyclic portion of the heteroaryl is bicyclic heterocyclic ring in which 5- to 6-membered monocyclic heterocyclic ring containing 1 or 2 hetero atom(s) and benzene ring are fused; R 1 : a group selected from the group consisting of optionally substituted cyclic hydrocarbon group, and optionally substituted heterocyclic group; n: an integer of 1 to 3; X: single bonding arm, -CH 2 -, -CO- , - (CH 2 ) m -CO- , -CH (R 2 ) -CO-, - (CH 2 ) p -Y-(C(R 3 ) (R 4 )) q -CO-, -NH-CO- or -N(R 5 ) -CO-; in the above-mentioned respective definitions of the X, the bonding arm described at the left end represents a bond with R 1 ; m is an integer of 1 to 3; p is an integer of 0 to 2; q is an integer of 0 to 2; Y: -O- or -SO 2 -; R 2 : phenyl or lower alkyl; R 3 , R 4 : each independently represents hydrogen atom or lower alkyl; R 5 : lower alkyl; provided that the ring portion of the group represented by R 1 is neither naphthylidine nor partially saturated group thereof, and, when X is -CH 2 - or -CO-, R 1 is not naphthyl.
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Page/Page column 35-36
(2010/11/25)
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- Piperididinyl and N-amidinopiperidinyl derivatives
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This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds
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- Intramolecular N-H insertion of α-diazocarbonyls catalyzed by Cu(acac)2: An efficient route to derivatives of 3-oxoazetidines, 3-oxopyrrolidines and 3-oxopiperidines
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Cu(acac)2 was found to be an efficient catalyst for the intramolecular N-H insertion by carbenoids. The competitive intramolecular C-H insertion by carbenoids is not a problem in the diazo decomposition reaction with Cu(acac)2 as catalyst. The reaction provided derivatives of 3-oxoazetidine, 3-oxopyrrolidine and 3-oxopiperidine in moderate to good yields.
- Wang, Jianbo,Hou, Yihua,Wu, Peng
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p. 2277 - 2280
(2007/10/03)
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- Piperidinyl-3-phosphinic acids as novel uptake inhibitors of the neurotransmitter γ-aminobutyric acid (GABA)
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Piperidinyl-3-phosphinic acid 2, piperidinyl-3-methylphosphinic acid 3 and N-(4,4-diphenyl-3-butenyl)-piperidinyl-3-phosphinic acid 4 have been synthesized as bioisosteres of the corresponding amino carboxylic acids, which are potent and specific GABA-uptake inhibitors. The novel amino phosphinic acids were tested for their GABA-uptake inhibitory activity and 2 and 4 were identified as the first phosphinic acid based GABA-uptake inhibitors. The methylphosphinic acid 3 was found to be inactive.
- Kehler, Jan,Stensbol, Tine B.,Krogsgaard-Larsen, Povl
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p. 811 - 814
(2007/10/03)
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- A CONVENIENT APPROACH TO THE N-SUBSTITUTED AMINO DIENES, N-BENZYL-5-ETHENYL-3,4-DIHYDROPYRIDIN-2-ONE AND N-CBZ-5-ETHENYL-1,2,3,4-TETRAHYDROPYRIDINE
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A synthesis of N-substituted amino dienes (1a) and (1b) is described according to two different approaches. 1a is obtained trough condensation of methyl 4-formyl-6-selenophenylhexanoate (4) with benzylamine followed by oxidation and elimination; 1b is for
- Bigogno, Chiara,Danieli, Bruno,Lesma, Giordano,Passarella, Daniele
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p. 973 - 982
(2007/10/02)
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- A convenient synthesis of functionalized 8- and 9-aza-1-oxaspiro[5.5]undecanes
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2-Hydroxy-8-(or 9-)aza-1-oxaspiro[5.5]undec-3-en-5-ones derived from their corresponding 2-furfuryl alcohols were used as key intermediates for the convenient synthesis of several novel 8- and 9-aza-1-oxaspiro[5.5]undecane derivatives.
- Apostolopoulos,Haroutounian
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p. 1843 - 1845
(2007/10/03)
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- Analogues of the low-efficacy partial GABAA agonist 4-PIOL. Syntheses and in vitro pharmacological studies
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4-PIOL (3-hydroxy-5-(4-piperidyl)isoxazole) is a low-efficacy GABAA agonist showing a dominating GABAA antagonist profile.Three dihydro analogues of 4-PIOL were synthesized, including (RS)-3-hydroxy-5-(4-piperidyl)-2-isoxazoline (1).The synthesis of 1 was based on a regioselective 1,3-dipolar cyclo-addition reaction between 1-benzyloxycarbonyl-4-vinylpiperidine (7) and bromonitrile oxide, prepared in situ from dibromoformoxime.Furthermore, the spiro analogues of 1 3-hydroxy-1-oxa-2,8-diazaspirodec-2-ene (2) and (RS)-3-hydroxy-1-oxa-2,7-diazaspirodec-2-ene (3) were synthesized regiospecifically via cycloaddition of bromonitrile oxide to the N-benzyloxycarbonyl-protected forms of 4-methylenepiperidine (11) and 3-methylenepiperidine (15) respectively.In contrast to 4-PIOL, none of the new compounds 1-3 showed detectable effects on the binding of 3H-GABAA or the subunit-selective GABAA agonist, 3H-THIP, to GABAA receptor sites, and they did not significantly affect the muscimol-stimulated binding of 3H-diazepam to the benzodiazepine site of the GABAA receptor complex.
- Amici, M De,Froelund, B,Hjeds, H,Krogsgaard-Larsen, P
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p. 625 - 631
(2007/10/02)
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