CAS: 7579-20-6; 3-Aminoisonicotinic Acid

相似化合物

179024-65-8 55279-29-3 55279-30-6

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CAS号4664-01-1 3,4-吡啶二甲酰亚胺 | CAS号179024-65-8 3-B°C-氨基异烟酸 | CAS号4664-08-8 吡啶-3,4-二羧酸酐 | CAS号490-11-9 吡啶-3,4-二羧酸 | CAS号4833-93-6 3-磺酸基异烟酸 | CAS号908240-50-6 2,4-二氯吡啶并[3,4-d]嘧啶 | CAS号462-08-8 3-氨基吡啶 | CAS号51752-67-1 4-氯-吡啶[3,4-D]嘧啶 | CAS号79612-46-7 3,3'-disulfaned... | CAS号18103-75-8 3-疏基吡啶-4-羧酸 | CAS号22378-50-3 2-Phenylpyrido[... | CAS号57842-10-1 3-碘异烟酸 | CAS号55279-29-3 3-氨基吡啶-4-醛 | CAS号64188-97-2 3-氨基异烟酸甲酯

3,4-吡啶二酰亚胺置于溴,Sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应 1.25H,以62%的收率获得产物3-氨基-4-吡啶羧酸
参考文献:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
标题:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
摘要:用于心力衰竭的一类新型治疗药物,高效和选择性的grk2抑制剂,在体外研究中表现出增强的β-肾上腺素信号传导能力.hts将衍生物5和1,2,4-三唑衍生物24A鉴定为命中化合物.新一代的脚手架和所有部分的sar研究都产生了带有n-苄基羧酰胺部分的4-甲基-1,2,4-三唑衍生物,对grk2的活性很高,对其他激酶的选择性更高.在亚型选择性方面,这些化合物对grk1,5,6和7表现出足够的选择性,并且对grk3具有几乎相同的抑制作用.我们的药物化学努力导致发现了115H(grk2 Ic 50= 18 Nm),获得了与人grk2和grk2抑制剂的共晶体结构,该抑制剂增强了β-肾上腺素能受体(βar)介导的camp积累,并防止了用异丙肾上腺素处理过的表达β2Ar的hek293细胞中βar的内在化.因此,115H似乎是心力衰竭治疗的一种新型疗法.
DOI:10.1021/acs.Jmedchem.7B00443

专利信息

专利号:US-6225329-B1
优先权日:1998-03-12
标 题 :Modulators of protein tyrosine phosphatases (PTPases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
权利人:NOVO NORDISK AS
摘要:The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, n wherein A, R 1 , R 2 , R 3 , R 4 , R 16 and R 17 are as defined in the specification. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

专利号:WO-9946236-A1
优先权日:1998-03-12
标题 :Modulators of protein tyrosine phosphatases (ptpases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOELLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
权利人:NOVO NORDISK AS; ONTOGEN CORP
摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

专利号:EP-1062199-A1
优先权日:1998-03-12
标题 :Modulators of protein tyrosine phosphatases (ptpases)
发明人：RICHTER LUTZ STEFAN; ANDERSEN HENRIK SUNE; VAGNER JOSEF; JEPPESEN CLAUS BEKKER; MOLLER NIELS PETER HUNDAHL; BRANNER SVEN; SU JING; BAKIR FARID; JUDGE LUKE MILBURN
权利人:NOVO NORDISK AS; ONTOGEN CORP
摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

专利号:US-2025304580-A1
优先权日:2021-11-09
标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

专利号:US-3950160-A
优先权日:1972-09-27
标题:Inhibiting the growth of weeds with 2-substituted pyrdidopyimidines and salts thereof
发明人：ABU EL-HAJ MARWAN J; DOMINY BERYL WILLIAM
权利人:PFIZER
摘要:2-Substituted pyridopyrimidines and their alkali and alkylamine salts as herbicides, and processes for the synthesis of starting materials leading to the preparation thereof.

专利号:US-9540371-B2
优先权日:2013-04-29
标 题:Substituted quinazolin-4(3H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, pyrido[3,2-d]pyrimidin-4(3H)-ones and pyrido[2,3-d]pyrimidin-4(3H)-ones as positive allosteric modulators of muscarinic acetycholine receptor M1
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; STAUFFER SHAUN R; PANARESE JOSEPH DAVID
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. Exemplary 3-benzylquinazolin-4(3H)-one compounds include compounds of formula (I):