3- 羟基-6-甲基(1h)吲唑 | 82722-05-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 中文名称: 3- 羟基-6-甲基(1h)吲唑
• 中文别名: 6-甲基-1H-吲唑-3-醇；3-羟基-6-甲基(1h)吲唑
• 英文名称: 6-Methylindazol-3(2H)-one
• 英文别名: 6-Methyl-1H-indazol-3-ol；6-methyl-1,2-dihydroindazol-3-one
• CAS: 82722-05-2
• 化学式: C₈H₈N₂O
• mdl: MFCD07781628
• 分子量: 148.164
• InChiKey: XAJGLOJSIXFHBC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为产物：
  描述：

  对甲苯甲酰肼 在 正丁基锂 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 1.5h， 以61%的产率得到3- 羟基-6-甲基(1h)吲唑
  参考文献：
  名称：

  酰肼和与正丁基锂的反应

  摘要：

  当用3当量的正丁基锂处理时，芳族酰肼以良好的收率得到吲哚-3（2 H）-酮；在相同条件下，脂族和杂环酰肼可提供相应的醛。

  DOI：

  10.1039/c39820000450

文献信息

• Sulfonamide Compound
  申请人：MITSUBISI TANABE PHARMA CORPORATION

  公开号：US20150307454A1

  公开（公告）日：2015-10-29

  The present invention provides novel sulfonamide compounds having TRPM8 antagonistic activity which are useful as medicaments. Specifically, the present invention provides a sulfonamide compound of the formula (I): wherein Ring A is the following formula (i), (ii), or (ix): R 4 is optionally substituted alkyl, X 1 and X 2 are each independently tetrazolyl, tetrazolinonyl, optionally substituted triazolyl, triazolinonyl, oxadiazolonyl, optionally substituted alkanoylaminomethyl, or optionally substituted alkylsulfonylaminomethyl, or R 4 and X 2 combine with each other at their terminals together with the adjacent benzene to form indazolinonyl or benzoisoxazolonyl, and the other symbols are the same as described in the specification, or a pharmaceutically acceptable salt thereof.

  本发明提供了具有TRPM8拮抗活性的新型磺胺类化合物，其作为药物是有用的。具体而言，本发明提供了式(I)的磺胺类化合物：其中环A为以下式(i)、(ii)或(ix)：R4为可选择地取代的烷基，X1和X2分别独立地为四唑基、四唑烯酮基、可选择地取代的三唑基、三唑烯酮基、噁二唑烯酮基、可选择地取代的烷酰氨基甲基或可选择地取代的烷基磺酰氨基甲基，或R4和X2在它们的末端与相邻的苯环一起结合形成吲哚啉基或苯并异噁唑啉基，其他符号与说明书中描述的相同，或其药学上可接受的盐。
• 3-oxo-1, 3-dihydro-indazole-2-carboxylic acid amide derivatives as phospholipase inhibitors
  申请人：Eacho Irving Patrick

  公开号：US20060211755A1

  公开（公告）日：2006-09-21

  The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C 5 -C 13 alkyl; C,—C, 2 haloalkyl, C 4 C,2alkenyl, C 4 -C 12 alkynyl, or C,—C5alkylcycloalkyl, C3-C8cycloalkyl, C, C 5 alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with one to three substituents independently selected from C,—C 8 a)kyl, C,—C 8 haloalkyl, ′C 2 -C B alkenyl, C2-C 8 a)kynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (C}12) m 000C,—Csalkyl, (CH2) m NR a R b , and C,C 4 alkylcycloalkyl; wherein W and R b are independently selected from hydrogen, C,C B alkyl, C 2 -C B alkenyl, C 2 -C B alkynyl, and C,—C5alkylcycloalkyl; R 2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,—C 12 alkyl, C 2 C,2haloalkyl, C2-C,2 alkenyl, C 2 -C 12 alkynyl, C,—C 12 alkylaryl, C,—C 12 alkylcyclohexyl, C, C 12 alkylcyclopentyl, C,—C 12 alkylheterocyclic, (CH2) m 000H, (CH2) m C0(C,—C,o)alkyl, (CH 2 ) m COO(C,—C ,o )alkyl, (CH2) m COO(C 1 -C ,o )alkylaryl, C,—C ,o alkylamino, halo, (CH 2 ) m CONH 2 , (CH 2 ) r CONRaR b , phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from C B alkyl, C,—C B haloalkyl, C 2 -C B alkenyl, C Z C B alkynyl, phenyl, benzyl, hydroxy, C,—C5 alkoxy, (CH2) m 000C,—Csalkyl, and C,—C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,—C lo alkyl, C,C ,o haloalkyl, C 2 -C ,o alkenyl, C 2 -C ,o alkynyl, C,—C 6 alkylaryl, C,—C 6 alkylcyclohexyl, C—C 6 aikylcyclopentyl, C,—C 6 alkylheterocyclic, or aryl; or a pharmaceutically acceptable sallvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.

  本发明提供一种公式I（1）的化合物，其中：R选自C5-C13烷基；C，C2卤代烷基，C4-C2烯基，C4-C12炔基，或C，C5烷基环烷基，C3-C8环烷基，C，C5烷基杂环基和芳基，其中环烷基，环烯基，杂环和芳基取代基可选地独立地被选自C，C8烷基，C，C8卤代烷基，C2-CB烯基，C2-C8炔基，苯基，苄基，羟基，C，C5烷氧基，（C}12）m000C，C5烷基，（CH2）mNRaRb和C，C4烷基环烷基的一个到三个取代基所取代；其中W和Rb独立地选自氢，C，C8烷基，C2-CB烯基，C2-CB炔基和C，C5烷基环烷基；R2为氢；R3，R4，R5和R6独立地选自氢，C，C12烷基，C2-C，2卤代烷基，C2-C，2烯基，C2-C12炔基，C，C12烷基芳基，C，C12烷基环己基，C，C12烷基环戊基，C，C12烷基杂环基，（CH2）m000H，（CH2）mC0（C，C，o）烷基，（CH2）mCOO（C，C，o）烷基，（CH2）mCOO（C1-C，o）烷基芳基，C，C，o烷基氨基，卤素，（CH2）mCONH2，（CH2）rCONRaRb，苯基或芳基，其中苯基或芳基中的每个苯基或芳基可选地独立地被选自C烷基，C，C卤代烷基，C2-CB烯基，CZCB炔基，苯基，苄基，羟基，C，C5烷氧基，（CH2）m000C，C5烷基和C，C4烷基环烷基的一个到三个基团所取代；其中m为0、1、2或3；R7选自氢，C，C6烷基，C，C6卤代烷基，C2-C，o烯基，C2-C，o炔基，C，C6烷基芳基，C，C6烷基环己基，C-C6烷基环戊基，C，C6烷基杂环基或芳基；或其药学上可接受的盐；以及使用这种化合物来抑制肝脏脂酶和/或内皮脂酶活性，用于治疗、改善或预防肝脏脂酶和/或内皮脂酶介导的疾病。
• INDAZOLE ANALOG
  申请人：Wada Yasuhiro

  公开号：US20120225909A1

  公开（公告）日：2012-09-06

  [Objective] To provide a drug that selectively stimulates the β3-adrenergic receptors, particularly a drug capable of preferentially stimulating the β3-adrenergic receptors over the α1-adrenergic receptors. This drug can be used in the treatment and prevention of diabetes, obesity, hyperlipidemia, depression, cholelithiasis, diseases caused by biliary hyperkinesia, diseases caused by hyperfunction of the gastrointestinal tract, interstitial cystitis, overactive bladder or urinary incontinence, diseases associated with decreased lacrimation, and the like. [Solution] Indazole analogs represented by the general formula (I) or a salt thereof. Drugs that contains these indazole analogs or a salt thereof as the active ingredient.

  【目的】提供一种选择性刺激β3-肾上腺素能受体的药物，特别是一种能够优先刺激β3-肾上腺素能受体而非α1-肾上腺素能受体的药物。该药可以用于糖尿病、肥胖症、高脂血症、抑郁症、胆石症、胆道高动力症引起的疾病、胃肠道高功能引起的疾病、间质性膀胱炎、过度活动的膀胱或尿失禁、伴有泪液减少的疾病等的治疗和预防。 【解决方案】一般式（I）所代表的吲唑类似物或其盐。包含这些吲唑类似物或其盐作为活性成分的药物。
• N-substituted indole derivatives as PGE2 receptor modulators
  申请人：Idorsia Pharmaceuticals Ltd

  公开号：US11241431B2

  公开（公告）日：2022-02-08

  The present invention relates to derivatives of formula (I) wherein (R1)n, R2, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

  本发明涉及式 (I) 的衍生物 其中 (R1)n、R2、R3、R4a、R4b、R5a、R5b 和 Ar1 如说明书所述，涉及它们的制备、它们的药学上可接受的盐，以及它们作为药物的用途、含有一种或多种式 (I) 化合物的药物组合物，特别是它们作为前列腺素 2 受体 EP2 和/或 EP4 的调节剂的用途。
• Benzofurane and benzothiophene derivatives as PGE2 receptor modulators
  申请人：IDORSIA PHARMACEUTICALS LTD

  公开号：US11325899B2

  公开（公告）日：2022-05-10

  The present invention relates to benzofurane and benzothiophene derivatives of formula (I) wherein (R1)n, R2, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

  本发明涉及式 (I) 的苯并呋喃和苯并噻吩衍生物 其中(R1)n、R2、R3、R4a、R4b、R5a、R5b 和 Ar1 如说明书所述，以及它们通过调节免疫反应（包括重新激活肿瘤中的免疫系统）治疗癌症的用途。本发明进一步涉及式(II)的新型苯并呋喃和苯并噻吩衍生物及其作为药物的用途、它们的制备、它们的药学上可接受的盐及其作为药物的用途、含有一种或多种式(I)化合物的药物组合物，特别是它们作为前列腺素2受体EP2和/或EP4的调节剂的用途。