Carbamic acid, phenyl-2-propenyl- | 57547-79-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Carbamic acid, phenyl-2-propenyl-
• 英文别名: phenyl(prop-2-enyl)carbamic acid
• CAS: 57547-79-2
• 化学式: C₁₀H₁₁NO₂
• 分子量: 177.2
• InChiKey: IELILUOKKWJXRN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• DERIVATIVES OF ALKYLPIPERAZINE AND ALKYLHOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
  申请人：Abouabdellah Ahmed

  公开号：US20070027141A1

  公开（公告）日：2007-02-01

  The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

  本发明涉及烷基哌嗪和烷基同源哌嗪羧酸盐及其衍生物，其制备方法以及作为脂肪酸酰胺水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和辣椒素受体等相互作用，发挥各种药理活性。通过抑制FAAH酶的代谢活性，通常导致疾病发作和其他病理状况的化合物不会生成，疾病的发生率大大降低。
• ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
  申请人：ABOUABDELLAH Ahmed

  公开号：US20070021405A1

  公开（公告）日：2007-01-25

  The present invention comprises compounds corresponding to the general formula (I): in which m, n=1 to 3 and m+n=2 to 5; p=1 to 7; A=single bond or X, Y and/or Z; X=optionally substituted methylene; Y=C 2 -alkenylene, which is optionally substituted, or C 2 -alkynylene; Z=C 3-7 -cycloalkyl; R 1 represents a group of aryl or heteroaryl type; R 2 represents a hydrogen or fluorine atom or a hydroxyl, C 1-6 -alkoxy or NR 8 R 9 group; R 3 represents a hydrogen atom or a C 1-6 -alkyl group; R 4 represents a hydrogen atom or a C 1-6 -alkyl, C 3-7 -cycloalkyl or C 3-7 -cycloalkyl-C 1-3 -alkyl group; in the base form or in the form of an addition salt with an acid, of a hydrate or of a solvate. The compounds are useful in the treatment of a number of diseases and/or pathological conditions such as chronic pain, dizziness, vomiting, nausea, eating disorders, neurological and psychiatric pathologies, acute or chronic neurodegenerative diseases, epilepsy, sleep disorders, cardiovascular diseases, renal ischaemia, cancers, disorders of the immune system, allergic diseases, parasitic, viral or bacterial infectious diseases, inflammatory diseases, osteoporosis, eye conditions, pulmonary conditions, gastrointestinal diseases or urinary incontinence.

  本发明包括符合一般式（I）的化合物： 其中m、n = 1至3，m+n = 2至5；p = 1至7；A = 单键或X、Y和/或Z；X = 可选择取代的亚甲基；Y = 可选择取代的C2-烯基或C2-炔基；Z = C3-7-环烷基；R1表示芳香族或杂环芳族基团；R2表示氢或氟原子或羟基、C1-6-烷氧基或NR8R9基团；R3表示氢原子或C1-6-烷基基团；R4表示氢原子或C1-6-烷基、C3-7-环烷基或C3-7-环烷基-C1-3-烷基基团；以碱形式或与酸的加合盐形式、水合物形式或溶剂合物形式存在。这些化合物可用于治疗多种疾病和/或病理情况，如慢性疼痛、头晕、呕吐、恶心、进食障碍、神经和精神病理、急性或慢性神经退行性疾病、癫痫、睡眠障碍、心血管疾病、肾脏缺血、癌症、免疫系统紊乱、过敏性疾病、寄生虫、病毒或细菌感染性疾病、炎症性疾病、骨质疏松症、眼部疾病、肺部疾病、胃肠疾病或尿失禁。
• PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
  申请人：ABOUABDELLAH Ahmed

  公开号：US20070021403A1

  公开（公告）日：2007-01-25

  The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

  本发明涵盖了吡啶基烷基氨基甲酸酯衍生物，其制备方法以及将其作为脂肪酸酰胺水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和辣椒素受体等相互作用，发挥各种药理活性。通过抑制FAAH酶的代谢活性，通常导致多种疾病和其他病理情况发生的化合物不会生成，疾病的发病率大大降低。
• DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
  申请人：ABOUABDELLAH Ahmed

  公开号：US20070021426A1

  公开（公告）日：2007-01-25

  The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula wherein A is selected from the group comprising X, Y or Z, and; X represents a methylene group optionally substituted by one or two C 1-6 -alkyl, C 3-7 -cycloalkyl or C 3-7 -cycloalkyl-C 1-3 -alkylene groups; Y represents either a C 2 -alkenylene group optionally substituted by one or two C 1-6 -alkyl, C 3-7 -cycloalkyl or C 3-7 -cycloalkyl-C 1-3 -alkylene groups; or a C 2 -alkynylene group; Z represents a group of formula: m represents an integer ranging from 1 to 5; p and q represent integers and are defined such that p+q is a number ranging from 1 to 5; n represents an integer ranging from 1 to 7; R 1 represents an R 2 group optionally substituted by one or more R 3 and/or R 4 groups; R 2 represents a group chosen from a pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, pyrrolyl, furyl, thienyl, imidazolyl, oxazolyl, thiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, naphthyl, quinolinyl, tetrahydroquinolinyl, isoquinolinyl, tetrahydroisoquinolinyl, 2-oxo-3,4-dihydroquinolinyl, 1-oxo-3,4-dihydroisoquinolinyl, quinazolinyl, quinoxalinyl, phthalazinyl, cinnolinyl, naphthyridinyl, benzofuranyl, dihydrobenzofuranyl, benzothienyl, dihydrobenzothienyl, indolyl, indolinyl, indazolyl, isoinR 5 R 6 , —O—(C 1-3 -alkylene)-O— or phenyl groups, the phenyl group optionally being substituted by one or more halogen atoms; R 3 represents a group chosen from halogen atoms or cyano, nitro, C 1-6 -alkyl, C 3-7 -cycloalkyl, C 1-6 -alkoxy, hydroxyl, C 1-6 -thioalkyl, C 1-6 -fluoroalkyl, C 1-6 -fluoroalkoxy, C 1-6 -fluorothioalkyl, NR 5 R 6 , NR 5 COR 6 , NR 5 CO 2 R 6 , NR 5 SO 2 R 6 , COR 5 , CO 2 R 5 , CONR 5 R 6 , SO 2 R 5 , SO 2 N. R 4 represents a group chosen from phenyl, phenyloxy, benzyloxy, naphthyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl groups; it being possible for the R 4 group or groups to be substituted by one or more R 3 groups which are identical to or different from one another; R 5 and R 6 represent, independently of one another, a hydrogen atom or a C 1-6 -alkyl group or form, with the atom or atoms which carry them, a ring chosen from an azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, azepine or piperazine ring, this ring optionally being substituted by a C 1-6 -alkyl or benzyl group; R 7 represents a hydrogen atom or a C 1-6 -alkyl group, and R 8 represents a hydrogen atom or a C 1-6 -alkyl, C 3-7 -cycloalkyl or C 3-7 -cycloalkyl-C 1-3 -alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt.

  本发明涉及化合物和组合物，用于治疗引起神经性和神经病理性疼痛、炎症性疾病、肾脏缺血、心血管疾病以及由内源性大麻素和/或脂肪酸酰胺水解酶（FAAH）代谢活动产生的其他底物引起的其他病理。这些化合物由以下式表示：其中A选自包括X、Y或Z的群组；X代表一个亚甲基基团，可选择地被一个或两个C1-6烷基、C3-7环烷基或C3-7环烷基-C1-3-烷基基团取代；Y代表一个C2-烯基基团，可选择地被一个或两个C1-6烷基、C3-7环烷基或C3-7环烷基-C1-3-烷基基团取代；或一个C2-炔基基团；Z代表一个以下式的基团：m代表一个范围从1到5的整数；p和q代表整数，并且定义为p+q为一个范围从1到5的数字；n代表一个范围从1到7的整数；R1代表一个R2基团，可选择地被一个或多个R3和/或R4基团取代；R2代表从吡啶基、嘧啶基、吡啶嗪基、吡嗪基、三嗪基、吡咯基、呋喃基、噻吩基、咪唑基、噁唑基、嘧唑基、异噁唑基、异噻唑基、噁二唑基、噻二唑基、三唑基、四唑基、萘基、喹啉基、四氢喹啉基、异喹啉基、四氢异喹啉基、2-氧代-3,4-二氢喹啉基、1-氧代-3,4-二氢异喹啉基、喹唑啉基、喹喹啉基、邻苯二嗪基、咪唑基、菲啉基、二氢菲啉基、苯并噻吩基、二氢苯并噻吩基、吲哚基、吲哚啉基、吲唑基、异吲哚基、—O—(C1-3-烷基)-O—或苯基，苯基可选择地被一个或多个卤素原子取代的基团；R3代表从卤素原子或氰基、硝基、C1-6烷基、C3-7环烷基、C1-6烷氧基、羟基、C1-6硫代烷基、C1-6氟烷基、C1-6氟烷氧基、C1-6氟硫代烷基、NR5R6、NR5COR6、NR5CO2R6、NR5SO2R6、COR5、CO2R5、CONR5R6、SO2R5、SO2N. R4代表从苯基、苯氧基、苄氧基、萘基、吡啶基、嘧啶基、吡啶嗪基或吡嗪基的基团；R4基团或基团可被一个或多个与之相同或不同的R3基团取代；R5和R6分别代表氢原子或C1-6烷基基团，或与携带它们的原子或原子形成的环中选择的一个环，该环可选择地被一个C1-6烷基或苄基团取代；R7代表氢原子或C1-6烷基基团，R8代表氢原子或C1-6烷基、C3-7环烷基或C3-7环烷基-C1-3-烷基基团；其盐，或所述化合物或所述盐的水合物或溶剂化合物。
• Carbamates derivatived from arylakylamines
  申请人：——

  公开号：US20040063950A1

  公开（公告）日：2004-04-01

  The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C 1 -C 4 )-alkylthio, (C 1 -C 4 )-alkoxyl, (C 1 -C 4 )-alkoxyl substituted by one or several F radicals, carbamoylamine, (C 1 -C 4 )-alkyl and (C 1 -C 4 )-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M 3 muscarinic receptor, and selectively, the M 2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.

  本发明涉及具有一般结构（I）的氨基甲酸酯，其中：R1、R2和R3分别为H、OH、SH、CN、F、Cl、Br、I、（C1-C4）-烷基硫醚、（C1-C4）-烷氧基、被一种或几种F基团取代的（C1-C4）-烷氧基、氨基甲酰胺、（C1-C4）-烷基和被一种或几种F或OH基团取代的（C1-C4）-烷基；R4代表取代或非取代的环烷基或环芳基基团（杂环烷基或非杂环烷基）。喹硷环的胺也可以形成季铵盐或氧化态（N-氧化物）。氨基甲酸酯（I）是M3胆碱能受体的拮抗剂，且具有选择性作用于M2受体。因此，它们可以用于治疗尿失禁（特别是由于膀胱不稳定引起的）、肠易激综合征、呼吸道疾病（特别是慢性阻塞性肺疾病、慢性支气管炎、哮喘、肺气肿和鼻炎）以及眼科手术。