CAS: 35373-63-8; 2-Amino-3-(4-Chlorophenyl)Propan-1-Ol

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CAS号7424-00-2 DL-4-氯苯基丙氨酸

📜Dl-4-氯苯丙氨酸置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,以40.8 %的收率获得产物dl-4-氯苯丙氨酸醇
参考文献:发现 (1R,3R)-1-(3-Chloro-5-Fluorophenyl)-3-(Hydroxymethyl)-1,2,3,4-Tetrahydroisoquinoline-6-Carbonitrile,一种有效的选择性人瞬时受体激动剂潜在阳离子通道亚家族 M 成员 5 (Trpm5) 和作为潜在胃肠促动力剂的评估
标题:发现 (1R,3R)-1-(3-Chloro-5-Fluorophenyl)-3-(Hydroxymethyl)-1,2,3,4-Tetrahydroisoquinoline-6-Carbonitrile,一种有效的选择性人瞬时受体激动剂潜在阳离子通道亚家族 M 成员 5 (Trpm5) 和作为潜在胃肠促动力剂的评估
摘要:该出版物详细介绍了一系列选择性瞬时受体电位阳离子通道亚家族 M 成员 5 (Trpm5) 激动剂的发现,最终鉴定出先导化合物 (1 R,3 R)-1-(3-Chloro-5-Fluorophenyl)-3-(羟甲基)-1,2,3,4-四氢异喹啉-6-腈(39).我们在此描述了我们对目标激动的生物学原理,对当时的文献工具分子的检查,以及最后我们的发现过程,从通过先导开发的高通量筛选命中开始.我们还详细介绍了先导化合物39相对于相关家族成员 Trpa1,Trpv1,Trpv4,Trpm4 和 Trpm8 的选择性,药物代谢和药代动力学 (Dmpk) 概况以及在小鼠胃肠运动模型中的体内功效.
DOI:10.1016/j.Bmc.2022.117084

专利信息

专利号:US-7645754-B2
优先权日:2001-12-20
标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

专利号:MX-PA04005861-A
优先权日:2001-12-20
标题:SELECTIVE ANTAGONIST COMPOUNDS OF PIRROLOPIRIMIDINA A2B, ITS SYNTHESIS AND USE.

专利号:US-6613942-B1
优先权日:1997-07-01
标题 :Glucagon antagonists/inverse agonists
发明人：LING ANTHONY; GREGOR VLAD; GONZALEZ JAVIER; HONG YUFENG; KIEL DAN; KUKI ATSUO; SHI SHENGHUA; NAERUM LARS; MADSEN PETER; SAMS CHRISTIAN; LAU JESPER; PLEWE MICHAEL BRUNO; FENG JUN; TENG MIN; JOHNSON MICHAEL DAVID; TESTON KIMBERLY ANN; SIDELMANN ULLA GROVE; KNUDSEN LOTTE BJERRE
权利人:NOVO NORDISK AS
摘要:Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.

专利号:EP-1467995-A4
优先权日:2001-12-20
标题:COMPOUNDS OF PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONISTS, THEIR SYNTHESIS AND USE THEREOF