hydron;5-methyl-2-[(Z)-2-naphthalen-1-ylethenyl]-4-piperidin-1-ylpyridine;chloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: hydron;5-methyl-2-[(Z)-2-naphthalen-1-ylethenyl]-4-piperidin-1-ylpyridine;chloride
• 化学式: C23H25ClN2
• 分子量: 364.9
• InChiKey: FIRAEJACZMKMQE-USGGBSEESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.82
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  16.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (1-萘甲基)三苯基氯化磷 、 正己烷 、 正丁基锂 、 5-methyl-4-piperidino-2-pyridinecarbaldehyde 、 在 氮气 、 水 、 四氢呋喃 、 乙醚 、 氯化钠 、 magnesium sulfate 、 正己烷 、 三苯基氧化膦 、 crude mixture 、 ethyl acetate n-hexane 、 乙醇 、 盐酸 、 methanol diethyl ether 作用下， 以 四氢呋喃 为溶剂， 反应 1.5h， 以to give 4.5 g (yield 41%) of the captioned compound (14-A) and 3.7 g (yield 37%) of the captioned compound (14-B) as crystals的产率得到(E)-5-methyl-2-[2-(1-naphthyl)-vinyl]-4-piperidinopyridine hydrochloride
  参考文献：
  名称：

  Anti-ulcer substituted pyridine derivatives

  摘要：

  一种被表示为通式##STR1##的取代吡啶衍生物，其中R.sup.1代表苯基或萘基，可选地被选自氢氧基、较低的烷基、较低的烷氧基、环烷基、较低的烷氧羰基、苯基和卤素原子的取代基取代; X代表氧原子、硫原子、羰基或式为--CH(OH)--或--N(R.sup.a)--的基团，其中R.sup.a是氢原子或较低的烷基; Y代表线性或支链较低的烷基或乙烯基，可选地被较低的烷基取代，但当X为氧或硫原子时，Y代表较低的烷基; R.sup.2和R.sup.3相同或不同，分别代表氢原子或较低的烷基; R.sup.4代表氢原子、较低的烷氧基、环烷氧基、较低的烷硫基、环烷硫基、芳氧基、芳基烷氧基或式为##STR2##的基团，其中R.sup.b和R.sup.c相同或不同，分别代表氢原子或较低的烷基。或R.sup.b和R.sup.c连同相邻的氮原子可以形成5-至7-成员饱和杂环环，该环可选地包含至少一种来自氧、硫和氮原子的其他杂原子，并可选地被较低的烷基取代; m和n分别为0或1，但m和n不能同时为0，或其酸加成盐。该化合物是一种抗溃疡剂。

  公开号：

  US04839353A1

文献信息

• [EN] 1, 3, 4-BENZOTRIAZEPIN-2-ONE SALTS AND THEIR USE AS CCK RECEPTOR LIGANDS<br/>[FR] SELS DE 1,3,4-BENZOTRIAZEPINE ET LEUR UTILISATION COMME LIGANDS DU RECEPTEUR DE CCK
  申请人：JOHNSON & JOHNSON

  公开号：WO2004101533A1

  公开（公告）日：2004-11-25

  This invention relates to pharmaceutically acceptable salts of compounds of formula (I) wherein: W is N or N+-O-; R2 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms. R3 is -(CR11R12)m-X-(CR13R14)p-R9; m is 0, 1, 2, 3 or 4; p is 0, 1 or 2; X is a bond, -CR15=CR16-, -C≡C-, C(O)NH, NHC(O), C(O)NMe, NMeC(O), C(O)O, NHC(O)NH, NHC(O)O, OC(O)NH, NH, O, CO, SO2, SO2NH, C(O)NHNH, R9 is H ; C1 to C6 alkyl ; or phenyl, naphthyl, pyridyl, benzimidazolyl, indazolyl, quinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, indolinyl, isoindolinyl, indolyl, isoindolyl or 2-pyridonyl substituted with -L-Q. R4 is an optionally substituted C1 to C18 hydrocarbyl group wherein up to three C atoms may optionally be replaced by N, O and/or S atoms ; and Such salts are useful, for example, for the treatment of gastrin related disorders.

  该发明涉及公式（I）化合物的药用可接受盐，其中：W为N或N+-O-；R2为可选择取代的C1至C18烃基团，其中最多三个C原子可选择地被N、O和/或S原子取代。R3为-(CR11R12)m-X-(CR13R14)p-R9；m为0、1、2、3或4；p为0、1或2；X为键、-CR15=CR16-、-C≡C-、C(O)NH、NHC(O)、C(O)NMe、NMeC(O)、C(O)O、NHC(O)NH、NHC(O)O、OC(O)NH、NH、O、CO、SO2、SO2NH、C(O)NHNH；R9为H、C1至C6烷基或苯基、萘基、吡啶基、苯并咪唑基、吲哚基、喹啉基、异喹啉基、四氢异喹啉基、吲哚啉基、异吲哚啉基、吲哚基、异吲哚基或2-吡啶酰基，取代为-L-Q。R4为可选择取代的C1至C18烃基团，其中最多三个C原子可选择地被N、O和/或S原子取代；这些盐可用于治疗胃泌素相关疾病。
• Gastrin and cholecystokinin receptor ligands (III)
  申请人：——

  公开号：US20030191116A1

  公开（公告）日：2003-10-09

  Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R 5 )—(R 5 being selected from H, Me, Et, Pr, Bn, OH and —CH 2 COOR 6 , wherein R 6 represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R 1 is H or C 1 to C 15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; R 2 is selected from H, Me, Et, Pr and OH, each R 2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R 3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R 3 is independently selected from H, Me, Et and Pr, or two R 3 groups on neighbouring carbn atoms are linked to form a C 3 to C 6 carbocylic ring, or two R 3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R 2 and R 3 on the same carbon atom together represent an ═O group; R 4 is C 1 to C 15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; V is —CO—NH—SO 2 —Ph, —SO 2 —NH—CO—Ph, —CH 2 OH, or a group of the formula —R 7 U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO 3 H; and R 7 is a bond; C 1 to C 6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C 1 to C 3 alkylene)—; —SO 2 NR 8 —CHR 9 —; —CO—NR 8 —CHR 9 —, R 8 and R 9 being independently selected from H and methyl; or —NH—(CO) c —CH 2 , c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described. 1

  公式（I）的化合物及其药学上可接受的盐是胃泌素和/或胆囊收缩素受体的配体。X和Y分别独立为═N—、—N(R5)—（R5选自H、Me、Et、Pr、Bn、OH和—CH2COOR6，其中R6代表H、Me、Et、Pr或Bn）、═CH—、—O—或—S—；n为1至4；A是一个可选择替代的5-或6-成员碳环，其中（a）1或2个C原子可选择替换为N、O和/或S原子，（b）A与公式（I）中的芳香基融合形成一个融合的双环，并且（c）含有X和Y的环与A的一个C原子连接；R1为H或C1至C15烃基，其中最多可有三个C原子可选择替换为N、O和/或S原子，最多可有三个H原子可选择替换为卤素原子；R2选自H、Me、Et、Pr和OH，当n大于1时，每个R2独立选择自H、Me、Et、Pr和OH；R3（当n为1时）选自H、Me、Et和Pr；或（当n大于1时）每个R3独立选择自H、Me、Et和Pr，或相邻碳原子上的两个R3基团连接形成一个C3到C6的碳环，或相邻碳原子上缺少两个R3基团，这两个基团由双键连接；或同一碳原子上的R2和R3共同表示一个═O基团；R4为C1至C15烃基，其中最多可有两个C原子可选择替换为N、O和/或S原子，最多可有三个H原子可选择替换为卤素原子；V为—CO—NH—SO2—Ph、—SO2—NH—CO—Ph、—CH2OH或式—R7U的基团（其中U为—COOH、四唑基、—CONHOH或—SO3H；而R7为键；C1至C6烃基亚烷，可选择地被羟基、氨基或乙酰胺基替代；—O—（C1至C3烷基）—；—SO2NR8—CHR9—；—CO—NR8—CHR9—，R8和R9独立选择自H和甲基；或—NH—（CO）c—CH2，c为0或1）；或其药学上可接受的盐。还描述了包含公式（I）化合物的组合物。
• Pharmaceutical compositions comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands
  申请人：——

  公开号：US20030195240A1

  公开（公告）日：2003-10-16

  Pharmaceutical compositions comprising a proton pump inhibitor and a compound of the formula (I) or its pharmaceutically acceptable salts, are useful in treating gastrointestinal disorders. X and Y are independently ═N—, —N(R 5 )— (R 5 being selected from H, Me, Et, Pr, Bn, —OH and —CH 2 COOR 6 , wherein R 6 represents H, Me, Et, Pr or Bn), ═CH—, S— or —O—; n is from 1 to 4; R 1 is H or C 1 to C 15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; R 2 is selected from H, Me, Et, Pr and OH, each R 2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R 3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R 3 is independently selected from H, Me, Et, and Pr, or two R 3 groups on neighbouring carbon atoms which are linked by a double bond; or R 2 and R 3 on the same carbon atom are linked to form a C 3 to C 6 carbocylic ring, or two R 3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R 2 and R 3 on the same carbon atom together represent an ═O group; R 4 is C 1 to C 15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to two H atoms may optionally be replaced by halogen atoms; Z is —(NR 7 ) a —CO—(NR 8 ) b — (wherein a is 0 or 1, b is 0 or 1, and R 7 and R 8 are independently selected from the groups recited above for R 6 ), —CO—NR 7 —CH 2 —CO—NR 8 —, —CO—O—, —CH 2 —CH 2 —, —CH═CH—, —CH 2 —NR— or a bond; Q is —R 9 V, or (II) (wherein R 9 is —CH 2 —; —CH 2 —CH 2 —; or (III) R 9 and R 8 , together with the nitrogen atom to which R 8 is attached, form a piperidine or pyrrolidine ring which is substitued by V; V is —CO—NH—SO 2 -Ph, SO 2 —NH—CO-Ph, —CH 2 OH, or a group of the formula —R 10 U, (wherein U is —COOH, tetrazolyl, —CONHOH— or —SO 3 H; and R 10 is a bond; C 1 to C 6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C 1 to C 3 alkylene)-; —SO 2 NR 11 —CHR 12 —; —CO—NR 11 —CHR 12 —, R 11 and R 12 being independently selected from H and methyl; or —NH—(CO), —CH 2 —, c being 0 or 1); T is C 1 to C 6 hydrocarbyl, —NR 6 R 7 (wherein R 6 and R 7 are as defined above), —OMe, —OH, —CH 2 OH, halogen or trihalomethyl; m is 1 or 2; p is from 0 to 3; and q is from 0 to 2, with the proviso that q is 1 or 2 when Z is a bond). 1

  含有质子泵抑制剂和公式（I）或其药学上可接受的盐的化合物的制剂，对治疗胃肠道疾病有用。其中，X和Y分别是═N—，—N（R5）—（其中R5选择自H，Me，Et，Pr，Bn，—OH和—CH2COOR6，其中R6代表H，Me，Et，Pr或Bn），═CH—，S—或—O—；n为1至4；R1为H或C1至C15的烃基，其中最多可有三个C原子被N，O和/或S原子取代，最多可有三个H原子被卤素原子取代；当n大于1时，R2选择自H，Me，Et，Pr和OH，每个R2独立选择自H，Me，Et，Pr和OH；当n为1时，R3选择自H，Me，Et和Pr；当n大于1时，每个R3独立选择自H，Me，Et和Pr，或被双键连接的相邻碳原子上的两个R3基团；或R2和R3在同一碳原子上连接形成C3到C6的环状碳基；或相邻碳原子上缺少两个R3基团，它们被双键连接；或R2和R3在同一碳原子上共同表示═O基团；R4为C1至C15的烃基，其中最多可有两个C原子被N，O和/或S原子取代，最多可有两个H原子被卤素原子取代；Z为—（NR7）a—CO—（NR8）b—（其中a为0或1，b为0或1，且R7和R8与上述R6中的基团独立选择），—CO—NR7—CH2—CO—NR8—，—CO—O—，—CH2—CH2—，—CH═CH—，—CH2—NR—或键；Q为—R9V，或（II）（其中R9为—CH2—；—CH2—CH2—；或（III）R9和R8与R8连接的氮原子一起形成被V取代的哌啶或吡咯烷环；V为—CO—NH—SO2-Ph，SO2—NH—CO-Ph，—CH2OH或公式—R10U的基团（其中U为—COOH，四唑基，—CONHOH—或—SO3H；R10为键；C1至C6的烃基，可选地被羟基，氨基或乙酰胺基取代；—O—（C1至C3的烷基）-；—SO2NR11—CHR12—；—CO—NR11—CHR12—，其中R11和R12独立选择自H和甲基；或—NH—（CO），—CH2—，其中c为0或1）；T为C1至C6的烃基，—NR6R7（其中R6和R7如上所定义），—OMe，—OH，—CH2OH，卤素或三卤甲基；m为1或2；p为0至3；q为0至2，但当Z为键时，q为1或2。
• Gastrin and cholecystokinin receptor lignads (iv)
  申请人：——

  公开号：US20030195237A1

  公开（公告）日：2003-10-16

  1 Compounds of the formula (I) or (II) and their pharmaceutically acceptable salts are ligands at gastrin and/or chole-cystokinin receptors. n is from 1 to 4; R 4 is C 1 to C 15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; Z is —(NR 5 ) a —CO—(NR 6 ) b -(wherein a is 0 or 1, b is 0 or 1, and R 5 and R 6 are independently selected from H, Me, Et, Pr, Bn), —CO—NR 5 —CH 2 —CO—NR 6 —, —CO—O—, —CH 2 —CH 2 —, —CH═CH—, CH 2 —NR 6 — or a bond; Q is R 7 V, or(a) wherein R 7 is —CH 2 —; —CH 2 —; or(b) R 7 and R 6 , together with the nitrogen atom to which R 6 is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is —CO—NH—SO 2 —Ph, —SO 2 —NH—CO—Ph, CH 2 OH, or a group of the formula —R 8 U, (wherein U is —COOH, tetrazolyl, —CONHOH— or —SO 3 H; and R 8 is a bond; C 1 to C 6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamino; —O-(C 1 to C 3 alkylene)-; —SO 2 NR 9 —CHR 10 —; —CO—NR 9 CHR 10 —, R 9 and R 10 being independently selected from H and methyl; or —NH—(CO) c —CH 2 —, c being 0 or 1); m is 1 or 2; q is from 0 to 2, with the proviso that q is 1 or 2 when Z is a bond); Compositions comprising a compound of formula (I) or (II) are also described.

  化合物(I)或(II)的配方及其药学上可接受的盐是胃泌素和/或胆囊肽受体的配体。其中n为1至4; R4为C1至C15烃基，其中最多可有两个C原子被N、O和/或S原子替换，最多可有三个H原子被卤素原子替换; Z为-(NR5)a-CO-(NR6)b-(其中a为0或1，b为0或1，R5和R6独立选择自H、Me、Et、Pr、Bn)、-CO-NR5-CH2-CO-NR6-、-CO-O-、-CH2-CH2-、-CH=CH-、CH2-NR6-或键; Q为R7V或(a)其中R7为-CH2-; -CH2-; 或(b) R7和R6与R6所连接的氮原子一起形成一个被V取代的哌啶或吡咯烷环; V为-CO-NH-SO2-Ph、-SO2-NH-CO-Ph、CH2OH或一个公式为-R8U的基团(其中U为-COOH、四唑基、-CONHOH-或-SO3H; R8为键; C1至C6烃基亚亚甲基，可选择地被羟基、氨基或乙酰氨基取代; -O-(C1至C3烷基)-; -SO2NR9-CHR10-; -CO-NR9CHR10-，其中R9和R10独立选择自H和甲基; 或-NH-(CO)c-CH2-，其中c为0或1); m为1或2; q为0至2，但当Z为键时，q为1或2。还描述了包含化合物(I)或(II)的组成物。
• Gastrin and cholecystokinin receptor ligands(II)
  申请人：——

  公开号：US20030199565A1

  公开（公告）日：2003-10-23

  Substituted imidazoles (1) are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure. Pharmaceutical compositions containing the novel imidazoles and pharmaceutical methods using them, alone and in conjunction with other drugs, especially diuretics and non-steroidal antiinflammatory drugs (NSAID's) are also described.

  取代咪唑（1）可作为血管紧张素II受体拮抗剂。这些化合物具有治疗高血压和充血性心力衰竭的活性。还描述了含有新型咪唑的药物组合物和使用它们的药物方法，单独或与其他药物一起使用，特别是利尿剂和非甾体抗炎药（NSAID）。