1-(Methylsulfonyl)azepane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环庚烷
• 英文名称: 1-(Methylsulfonyl)azepane
• 英文别名: 1-methylsulfonylazepane
• 化学式: C₇H₁₅NO₂S
• mdl: MFCD00583963
• 分子量: 177.27
• InChiKey: KESCNDOJIXKQAV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：ALTENBURGER Jean-Michel

  公开号：US20110301148A1

  公开（公告）日：2011-12-08

  The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH 2 , —CH(R′)—, —NH(R′)— or a heteroatom chosen from O and S, it being understood that R′ represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH 2 -aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO 2 —NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH 2 -heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or (ii) form, together with the nitrogen atom that bears them, a heterocycloalkyl group optionally substituted with one or more groups chosen from the groups —(C1-C5)alkyl and —CH 2 -aryl; W is a group —(C1-C5)alkylene, optionally substituted with one or more hydroxyl groups; R5 and R6, which may be identical or different, represent, independently of each other, a hydrogen atom or a group chosen from the groups —(C1-C5)alkyl and the groups —(C3-C6)cycloalkyl, and also the process for preparing them and the therapeutic uses thereof.

  该发明涉及与化学式（I）对应的化合物，以其碱形式或酸盐形式存在： 其中n等于0、1、2、3或4；m等于0、1或2；o等于0或1；X代表一个基团—CH2、—CH(R′)—、—NH(R′)—或从O和S中选择的杂原子，其中R′代表一个基团—(C1-C5)烷基、—(C1-C5)烷氧基、—CH2-芳基、—C(O)R5或—COOR5；R1代表一个氧代基、—COOR5、—W—OH或—W—NR5R6；R2代表一个氢原子或从以下基团中选择的一个：(i) —(C1-C5)烷基、(ii) —(C1-C5)烷氧基、(iii) —COOR5、(iv) —NR5R6、(v) —C(O)—NR5R6、(vi) —SO2—NR3R4、(vii) 可选地被基团—(C1-C5)烷基取代的杂芳基、(viii) —W-芳基、(ix) —W-杂芳基、(x) —O—W-芳基、(xi) —O—W-杂芳基和(xii) —O—W—NR5R6；其中R3和R4，(i) 可能相同也可能不同，独立地代表一个氢原子、一个基团—(C1-C5)烷基、—(C3-C6)环烷基、芳基、杂芳基、—CH2-杂芳基、—(C1-C5)烷基-NR5R6、—W—OH或—W—NR5R6；或(ii) 与携带它们的氮原子一起形成一个杂环烷基基团，可选地取代一个或多个从以下基团中选择的基团：—(C1-C5)烷基和—CH2-芳基；W代表一个基团—(C1-C5)烷基，可选地取代一个或多个羟基；R5和R6，可能相同也可能不同，独立地代表一个氢原子或从以下基团中选择的一个：—(C1-C5)烷基和—(C3-C6)环烷基，以及其制备方法和治疗用途。
• Sulfonamide compounds as cysteine protease inhibitors
  申请人：Woo Soon H.

  公开号：US20090233909A1

  公开（公告）日：2009-09-17

  The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.

  本发明涉及式(I)的化合物，其为半胱氨酸蛋白酶的抑制剂，特别是对于B、K、L、F和S型的猫蛋白酶，因此可用于治疗这些蛋白酶介导的疾病。本发明涉及含有这些化合物的制药组合物以及制备这些化合物的过程。其中R3为-烷基-SO2NR5R6。
• LRRK2 INHIBITORS
  申请人：Bounaud Pierre-Yves

  公开号：US20140205537A1

  公开（公告）日：2014-07-24

  Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.

  本文提供了抑制或部分抑制富含亮氨酸重复激酶活性的化合物。本文还提供了治疗中枢神经系统疾病的方法，包括给予富含亮氨酸重复激酶抑制剂的治疗。
• PYRROLO CARBOXAMIDES AS MODULATORS OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORy, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES
  申请人：PHENEX PHARMACEUTICALS AG

  公开号：US20140349987A1

  公开（公告）日：2014-11-27

  The invention provides modulators for the orphan nuclear receptor ROR γ and methods for treating ROR γ mediated diseases by administrating these novel ROR γ modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.

  该发明提供了用于孤儿核受体RORγ的调节剂，并通过向需要此类治疗的人或哺乳动物中施用这些新型RORγ调节剂的方法来治疗RORγ介导的疾病。具体而言，本发明提供了公式（1）的吡咯羧酰胺化合物及其对映体、二对映异构体、N-氧化物、互变异构体、溶剂化物和药学上可接受的盐。
• Trk-INHIBITING COMPOUND
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US20160000783A1

  公开（公告）日：2016-01-07

  The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

  本发明提供了一种药物，其中包含具有Trk抑制活性的化合物作为预防和/或治疗Trk相关疾病的活性成分，例如疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或查加斯病。通式（I）所表示的化合物，其中所有符号都表示规范中描述的相同含义，其盐，N-氧化物，溶剂化物或前药是作为具有Trk抑制活性的药物成分在预防和/或治疗疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或查加斯病等疾病中有用的。