cis-Bicyclo[3.3.0]octane-2-carboxylic acid | 7403-22-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: cis-Bicyclo[3.3.0]octane-2-carboxylic acid
• 英文别名: bicyclo[3.3.0]octane-2-carboxylic acid；Octahydropentalene-1-carboxylic acid；1,2,3,3a,4,5,6,6a-octahydropentalene-1-carboxylic acid
• CAS: 7403-22-7
• 化学式: C₉H₁₄O₂
• 分子量: 154.209
• InChiKey: AMDLMIANEBVNEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  cis-Bicyclo[3.3.0]octane-2-carboxylic acid 、 1,3-di-n-propyl-5,6-diamino-2-thiouracil 以to afford 1.70 g (overall yield: 57%) of the captioned Compound 24 as a white crystal的产率得到8-[(1R*,2R*,5R*)-Bicyclo[3.3.0]octan-2-yl]-1,3-dipropyl-2-thioxanthine
  参考文献：
  名称：

  Xanthine compounds

  摘要：

  以下式子所代表的新型黄嘌呤化合物：##STR1## 其中R.sup.1、R.sup.2和R.sup.3各自独立地代表氢或低碳基；X.sup.1和X.sup.2各自独立地代表氧或硫；Q代表：##STR2## 这些化合物可用作利尿剂、肾保护剂和支气管扩张剂。

  公开号：

  US05525607A1
• 作为产物：
  描述：

  1,5-cis,cis-cyclooctadiene 、 一氧化碳 在 氢氟酸 、 水 作用下， 45.0~50.0 ℃ 、8.96 MPa 条件下， 反应 3.0h， 生成 cis-Bicyclo[3.3.0]octane-2-carboxylic acid
  参考文献：
  名称：

  Organic reactions in liquid hydrogen fluoride. III. Carboxylic acids from olefins and carbon monoxide (hydrogen fluoride-Koch reaction)

  摘要：

  DOI：

  10.1021/jo00977a023

文献信息

• Substituted acrylamido-penicillanic acid derivatives
  申请人：Beecham Group p.l.c.

  公开号：EP0421752A3

  公开（公告）日：1992-01-22

  Compounds of formula (I) and their derivatives: wherein X is hydrogen or a group NHR¹, wherein R¹ is hydrogen or an amino protecting group, and R is an optionally substituted spiro, fused or bridged bicyclic group optionally containing one or more heteroatoms selected from oxygen, nitrogen and sulphur, are new and useful in the treatment of bacterial infections in humans and animals.

  式（I）及其衍生物的化合物：其中X为氢或基团NHR¹，其中R¹为氢或氨基保护基团，R为可选取代的螺环、融合或桥联的双环基团，可选含有一个或多个从氧、氮和硫中选择的杂原子，在人类和动物的细菌感染治疗中是新的且有用的。
• [EN] NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES<br/>[FR] NOUVEAUX COMPOSÉS TRICYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS D'ENZYMES IDH MUTANTES
  申请人：MERCK SHARP & DOHME

  公开号：WO2016089830A1

  公开（公告）日：2016-06-09

  The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

  本发明涉及式(I)的三环化合物，其为一种或多种突变IDH酶的抑制剂；其中A为-C(R1)=或-N=；X从以下组中选择：(II-i)和(II-ii)。本发明还涉及所述三环化合物在潜在治疗或预防涉及一种或多种突变IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗此类癌症中的用途。
• [EN] NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES<br/>[FR] NOUVEAUX COMPOSÉS TRICYCLIQUES COMME INHIBITEURS D'ENZYMES IDH MUTANTES
  申请人：MERCK SHARP & DOHME

  公开号：WO2016089833A1

  公开（公告）日：2016-06-09

  The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

  本发明涉及式(I)的三环化合物，这些化合物是一种或多种突变IDH酶的抑制剂：(I)；其中A为-C(R1)=或-N=；X选自以下组中的一种：(II-i)、(II-ii)、(II-iii)和(II-iv)。本发明还涉及所述三环化合物在潜在治疗或预防涉及一种或多种突变IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在潜在预防或治疗此类癌症中的用途。
• Bioactive peptides
  申请人：ALPHARMA AS

  公开号：US20030022821A1

  公开（公告）日：2003-01-30

  The present invention provides a modified lactoferrin peptide which is cytotoxic, 7 to 25 amino acids in length, with three or more cationic residues and which has one or more extra bulky and lipophilic amino acids as compared to the native lactoferrin sequence, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing such peptides, pharmaceutical compositions containing such peptides and use of the peptides as medicaments, particularly as antibacterials or anti-tumoural agents.

  本发明提供一种改性乳铁蛋白肽，其具有细胞毒性，长度为7至25个氨基酸，含有三个或更多阳离子残基，并且与天然乳铁蛋白序列相比，具有一个或多个额外的笨重和亲脂氨基酸，以及其酯、酰胺、盐和环状衍生物，以及制备这些肽的方法、含有这些肽的药物组合物和将这些肽用作药物的用途，特别是作为抗菌或抗肿瘤剂。
• Xanthine derivatives
  申请人：Kyowa Hakko Kogyo Co., Ltd.

  公开号：US05290782A1

  公开（公告）日：1994-03-01

  Novel xanthine compounds represented by the following formula: ##STR1## wherein each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents; ##STR2## where ----- represents a single bond or a double bond; Y represents a single bond or alkylene, n represents 0 or 1, each of W.sup.1 and W.sup.2 independently represents hydrogen, lower alkyl or amino, Z represents --CH.sub.2 -, --O--, --S-- or --NH--; represents ##STR3## each of R.sup.1 and R.sup.2 independently represents hydrogen, lower alkyl, allyl or propargyl; and R.sup.3 represents hydrogen or lower alkyl, and when Q represents the groups other than ##STR4## each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl; provided that when Q is ##STR5## then R.sup.1 R.sup.2 and R.sup.3 are not simultaneously methyl; and pharmaceutically acceptable salts thereof have a diuretic effect, a renal-protecting effect and a bronchodilatory effect.

  以下是由以下公式表示的新型黄嘌呤化合物：##STR1## 其中X.sup.1和X.sup.2各自独立地表示氧或硫; Q代表; ##STR2## 其中-----表示单键或双键; Y表示单键或烷基，n表示0或1，W.sup.1和W.sup.2各自独立地表示氢，低烷基或氨基，Z表示--CH.sub.2-，--O--，--S--或--NH--;表示##STR3## R.sup.1和R.sup.2各自独立地表示氢，低烷基，烯丙基或丙炔基; R.sup.3表示氢或低烷基，当Q表示除##STR4##以外的基团时，R.sup.1，R.sup.2和R.sup.3各自独立地表示氢或低烷基; 前提是当Q为##STR5##时，R.sup.1，R.sup.2和R.sup.3不能同时为甲基; 以及其药学上可接受的盐具有利尿作用，肾保护作用和支气管扩张作用。