CAS: 1210-33-9; 5-Chloro-10,11-Dihydro-5H-Dibenzo[a,D][7]Annulene

相似化合物

833-48-7 1729-63-1 1210-35-1

上下游产品

CAS号1210-34-0 5-羟基-10,11-二氢-5... | CAS号1210-35-1 二苯并环庚酮 | CAS号4890-85-1 邻苯乙基苯甲酸 | CAS号833-48-7 10,11-二氢-5H-二苯并... | CAS号7199-29-3 环庚米特 | CAS号69159-50-8 1-(二苯基环庚基)-哌嗪 | CAS号1210-34-0 5-羟基-10,11-二氢-5... | CAS号1210-35-1 二苯并环庚酮 | CAS号1729-63-1 10,11-二氢-5H-二苯并... | CAS号7005-53-0 5-氨基二苯并环庚烷

10,11-二氢二苯并[a,B]环庚烯-5-酮置于sodium Tetrahydroborate,氯化亚砜体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 3.0H,反应生成二苯并环庚烯酮基氯
参考文献:二苯并[b,F] [1,4]氮杂ze庚因和二苯并[b,E] Oxepinesine:在h1R,H4R,5-Ht2Ar和其他选定的gpcr中,氯取代方式对药理学的影响.
标题:二苯并[b,F] [1,4]氮杂ze庚因和二苯并[b,E] Oxepinesine:在h1R,H4R,5-Ht2Ar和其他选定的gpcr中,氯取代方式对药理学的影响.
摘要:受到vuf6884(7-Chloro-11-(4-Methylpiperazin-1-Yl)dibenzo [b,F] [1,4] Oxazepine的启发),报道为双重h1 / H4受体配体(pki:8.11(人h1R( Hh1R)),7.55(人h4R(hh4R))),四种已知的和28种新的奥氮平及其相关的奥西平衍生物已合成,并在组胺受体和选定的胺能gpcr上进行了药理学表征.与奥氮平系列相反,在奥西平系列中,新化合物显示出对hh1R的高亲和力(pki:6.8-8.7),但对hh4R的亲和力不高(pki:<=5.3).对于一种oxepine衍生物(1-(2-氯-6,11-二氢二苯并[b,E] Oxepin-11-基]-4-甲基哌嗪),对映体被分离,R-对映体被鉴定为是对映体. Hh1R(pki:8.83(R),7.63(S))和豚鼠h1R(gph1R)(pki:8.82(R),7.
Doi:10.1016/j.Phrs.2016.09.042

专利信息

专利号:EP-0946499-B1
优先权日:1996-11-22
标 题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK NORMAN; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R<1> is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R<2> is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R<3> and R<3'> are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R<7>)n(W)p, wherein R<7> is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH( phi )CH2C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R<1> to -CX'X''-, oxygen and sulfur.

专利号:US-6262302-B1
优先权日:1996-11-22
标题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK N; AUDIA JAMES E
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6153652-A
优先权日:1996-11-22
标 题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds

专利号:WO-9822433-A1
优先权日:1996-11-22
标题:N-(ARYL/HETEROARYL/ALKYLACETYL) AMINO ACID AMIDES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS

专利号:EP-0946499-A1
优先权日:1996-11-22
标题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds

专利号:CA-2272065-A1
优先权日:1996-11-22
标题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting .beta.-amyloid peptide release and/or its synthesis by use of such compounds