- NOVEL COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.5]undeca-1-ene structure represented by the following general formula (1):
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- Novel heterocyclic derivative capable of being used as SHP2 inhibitor
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The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.
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Paragraph 0396; 0398; 0400; 0401
(2019/08/30)
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- NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
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This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
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Page/Page column 80; 81
(2018/10/19)
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- Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2
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A series of spiropiperidine carbazoles were synthesized and evaluated as MCHR2 antagonists using a FLIPR assay. The pharmacokinetic properties of selected compounds have also been studied. This effort led to the discovery of potent and specific MCHR2 antagonists. Compound 38 demonstrated good pharmacokinetic properties across rat, beagle dog and rhesus monkey and had a favorable selectivity profile against a number of other receptors. These MCHR2 antagonists are considered appropriate tool compounds for study of the function of MCHR2 in vivo.
- Chen, Xiaoqi,Mihalic, Jeff,Fan, Pingchen,Liang, Lingming,Lindstrom, Michelle,Wong, Sylvia,Ye, Qiuping,Fu, Ying,Jaen, Juan,Chen, Jin-Long,Dai, Kang,Li, Leping
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scheme or table
p. 363 - 366
(2012/02/04)
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- NOVEL SPIRO COMPOUND AND MEDICINE COMPRISING THE SAME
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It is to provide a novel compound useful for preventing and/or treating diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. A spiro compound represented by the following general for
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Page/Page column 17-18
(2010/02/17)
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- ANTAGONISTS OF PGD2 RECEPTORS
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Described herein are compounds and pharmaceutical compositions containing such compounds that modulate the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.
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Page/Page column 65
(2009/06/27)
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- SPIRO-PIPERIDINE DERIVATIVES
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Present invention is concerned with novel indol- 2-yl-carbonyl-spiro-piperidine derivatives as Vla receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention andlor treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general Formula (I) wherein R1 to R 11 and X are as defined in the description
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Page/Page column 28; 30
(2008/12/06)
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- Modulators of muscarinic receptors
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 121
(2010/11/29)
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- MODULATORS OF MUSCARINIC RECEPTORS
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The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
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Page/Page column 84; 85
(2010/10/20)
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- Spiropiperidine derivatives
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A compound of the formula (I) wherein R1and R2is a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group. A is CH2, CO or SO2. B is a single bond, alkylene or alkenylene. D is O or S. E is alkylene or alkenylene. wherein G is a substituted or unsubstituted cycloalkene ring, or a substituted cycloalkane ring. Ar is a substituted or unsubstituted aryl ring, or a substituted or unsubstituted heteroaryl ring. R3is alkyl. n is 1-3. The invention includes a pharmacologically acceptable salt, ester or other derivative of a compound of the formula (I). The invention also provides pharmaceutical compositions and methods of treating specified diseases utilizing a compound of formula (I).
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- The synthesis and activity of spiroindane growth hormone secretagogues
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The synthesis and activities of a series of spiroindane growth hormone secretagogues is reported. Modification of the benzylic position of the spiroindane has resulted in a dramatic increase in potency resulting in subnanomolar peptidomimetic growth hormone secretagogues. In vivo data demonstrating the good oral activity of these analogs is reported.
- Tata, James R.,Nargund, Ravi P.,Murphy, Marcia M.,Johnston, David B. R.,Patchett, Arthur A.,Cheng, Kang,Wei, Liente,Chan, Wanda W.-S.,Butler, Bridget,Jacks, Thomas M.,Hickey, Gerard,Smith, Roy
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p. 663 - 668
(2007/10/03)
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