2-Pentylamino-Δ²-imidazolin | 98487-51-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑啉类
• 英文名称: 2-Pentylamino-Δ²-imidazolin
• 英文别名: (4,5-dihydro-1H-imidazol-2-yl)-pentyl-amine；N-pentyl-4,5-dihydro-1H-imidazol-2-amine
• CAS: 98487-51-5
• 化学式: C₈H₁₇N₃
• 分子量: 155.243
• InChiKey: OQIOPNMXGHTBJR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  36.4
• 氢给体数：
  2
• 氢受体数：
  1

文献信息

• GUANIDINE BASED COMPOUNDS
  申请人：Rozas Hernando Maria Isabel

  公开号：US20100331384A1

  公开（公告）日：2010-12-30

  The adrenergic receptors or adrenoceptors are a family of G-protein coupled receptors split into α and β subclasses. The adrenoceptors have important roles in regulating a myriad of physiological conditions and their malfunction has been implicated in the pathophysiology of a number of diseases. Disclosed herein are a series of novel guanidine and 2-aminoimidazoline compounds which are ligands of the alpha2-adrenoceptor (α2-ARs) subclass of adrenergic receptors. The invention also provides for pharmaceutical compositions comprising the novel compounds. The compounds are suitable for use in the manufacture of medicaments for the treatment of α2-ARs associated disorders, such as depression, schizophrenia, glaucoma and analgesia.

  肾上腺素受体或肾上腺素受体是一类G蛋白偶联受体家族，分为α和β亚类。肾上腺素受体在调节多种生理条件中起着重要作用，其功能失调已被认为与多种疾病的病理生理有关。本文披露了一系列新型胍啶和2-氨基咪唑啉化合物，它们是肾上腺素受体的α2-亚型（α2-ARs）亚类的配体。该发明还提供了包含这些新型化合物的药物组合物。这些化合物适用于制造用于治疗与α2-ARs相关疾病的药物，如抑郁症、精神分裂症、青光眼和镇痛的药物。
• [EN] OCULOSELECTIVE DRUGS AND PRODRUGS<br/>[FR] MEDICAMENTS ET PROMEDICAMENTS OCULOSELECTIFS
  申请人：OTHERA PHARMACEUTICALS INC

  公开号：WO2005115375A1

  公开（公告）日：2005-12-08

  Compounds of the following formula are disclosed: wherein R1 and R2 are each independently H, W, or a phenoxyl protecting group; and R4is H or W, provided that at least one of R1, R2, and R4 is W; R3 is hydrogen, straight chain or branched C1-C10 alkyl, cycloalkyl, amino, C1-C10 alkoxy, -NHC(=O)Ra, or -C(=O)N(H)Ra; Ra is alkyl, aryl, or heterocyclyl; Z is -0-, -O(C=O)-, or NH(C=O)-, wherein when Z is -0-, R5 is H, straight chain or branched C1-C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI-Clo alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolsdinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with CI-Clo alkyl, C1-C10 alkoxy, or halo; and W is:, wherein each R6 is independently H, straight chain or branched C1-C10 alkyl, or straight chain or branched Cl-C10 alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is -O(C=O)-, R5 is straight chain or branched C1-C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI-CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with Cl-C10 alkyl, C1-C10 alkoxy, or halo; and W is: , wherein each R6 is independently H, straight chain or branched CI-C to alkyl, or straight chain or branched C,-C to alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is-NH(C=O)-, R5 is straight chain or branched C1 -C10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C1-C10 alkyl, CI-CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, &oxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C1-C10 alkyl, C1-C10 alkoxy, or halo; and W is: ; wherein each R6 is independently H, straight chain or branched C1 -C to alkyl, or straight chain or branched C,-Clo alkoxyalkyl. Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions, are also disclosed.

  公开了以下式子的化合物：其中R1和R2分别独立地为H、W或苯氧基保护基；R4为H或W，但至少其中一个为W；R3为氢、直链或支链C1-C10烷基、环烷基、氨基、C1-C10烷氧基、-NHC（=O）Ra或-C（=O）N（H）Ra；Ra为烷基、芳基或杂环基；Z为-0-、-O（C=O）-或NH（C=O）-，其中当Z为-0-时，R5为H、直链或支链C1-C10烷基、环烷基、至少含有一个直链或支链C1-C10烷基的环烷基、CI-Clo烷氧基烷基、氨基、苯甲基、四氢呋喃基、二氢呋喃基、呋喃基、吗啉基、哌啶基、四氢吡喃基、二氢二氧杂环基、2,2-二甲基二氧杂环基、二氧杂环基、吡咯基、吡咯啉基、四氢噁唑基、二氢噁唑基、苯基或被CI-Clo烷基、C1-C10烷氧基或卤素取代的苯基；W为：其中每个R6独立地为H、直链或支链C1-C10烷基或直链或支链Cl-C10烷氧基烷基；R7为烷基、环烷基、芳基或芳烷基；当Z为-O（C=O）-时，R5为直链或支链C1-C10烷基、环烷基、至少含有一个直链或支链C1-C10烷基的环烷基、CI-CIO烷氧基烷基、氨基、苯甲基、四氢呋喃基、二氢呋喃基、呋喃基、吗啉基、哌啶基、四氢吡喃基、二氢二氧杂环基、2,2-二甲基二氧杂环基、二氧杂环基、吡咯基、吡咯啉基、四氢噁唑基、二氢噁唑基、苯基或被CI-C10烷基、C1-C10烷氧基或卤素取代的苯基；W为：其中每个R6独立地为H、直链或支链CI-C to烷基或直链或支链C,-C to烷氧基烷基；R7为烷基、环烷基、芳基或芳烷基；当Z为-NH（C=O）-时，R5为直链或支链C1-C10烷基、环烷基、至少含有一个直链或支链C1-C10烷基的环烷基、CI-CIO烷氧基烷基、氨基、苯甲基、四氢呋喃基、二氢呋喃基、呋喃基、吗啉基、哌啶基、四氢吡喃基、二氢二氧杂环基、2,2-二甲基二氧杂环基、二氧杂环基、吡咯基、吡咯啉基、四氢噁唑基、二氢噁唑基、苯基或被C1-C10烷基、C1-C10烷氧基或卤素取代的苯基；W为：其中每个R6独立地为H、直链或支链C1-C to烷基或直链或支链C,-Clo烷氧基烷基。还公开了制备这些化合物的方法、包含这些化合物的药物组成物以及通过给患者给药这些药物组成物的治疗方法。
• [EN] DERIVATIVES OF 1-[(IMIDAZOLIDIN-2-YL)IMINO)]INDAZOLE<br/>[FR] DÉRIVÉS DU 1-[(IMIDAZOLIDIN-2-YL)IMINO)]INDAZOLE
  申请人：IMP INNOVATIONS LTD

  公开号：WO2009071906A1

  公开（公告）日：2009-06-11

  The invention provides a compound of formula (I) wherein R1 denotes hydrogen, methyl or phenyl; R2, R3, R4 and R5 denote hydrogen, halogen, preferably a chlorine atom, alkyl, preferably methyl, alkoxyl, preferably methoxyl; m denotes a number 0 or 1; and HX denotes sulfuric, phosphoric, acetic, malonic, fumaric, oxalic, lactic, tartaric, citric, gluconic, p-toluenesulfonic, methanesulfonic acid, hydrogen bromide or hydrogen iodide, preferably hydrogen chloride. The use of the compounds as α2-adrenergic receptor agonists is also provided.

  本发明提供了一种式子为(I)的化合物，其中R1表示氢、甲基或苯基；R2、R3、R4和R5表示氢、卤素，优选为氯原子，烷基，优选为甲基，烷氧基，优选为甲氧基；m表示数字0或1；HX表示硫酸、磷酸、醋酸、马龙酸、富马酸、草酸、乳酸、酒石酸、柠檬酸、葡萄糖酸、对甲苯磺酸、甲磺酸、氢溴酸或氢碘酸，优选为氢氯酸。本发明还提供将该化合物用作α2肾上腺素受体激动剂的方法。
• SUBSTITUTED-PHENYL KETONE DERIVATIVES AS IP ANTAGONISTS
  申请人：——

  公开号：US20020091147A1

  公开（公告）日：2002-07-11

  This invention relates to compounds which are generally IP receptor modulators, particularly IP receptor antagonists, and which are represented by Formula I: 1 wherein A, R 1 and R 2 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

  本发明涉及一些化合物，通常是IP受体调节剂，特别是IP受体拮抗剂，其由公式I表示：其中A，R1和R2如说明书中所定义的那样；以及其各个异构体，外消旋或非外消旋异构体混合物和药学上可接受的盐或溶剂。本发明还涉及含有这样的化合物的制药组合物以及其作为治疗剂的使用方法。
• AMINO ACID LIPIDS AND USES THEREOF
  申请人：Quay Steven C.

  公开号：US20080317839A1

  公开（公告）日：2008-12-25

  This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.

  这份披露提供了一系列氨基酸脂类化合物和组合物，可用于药物传递、治疗、诊断和治疗疾病和病况。这些氨基酸脂类化合物和组合物可用于将各种药剂如核酸治疗剂传递到细胞、组织、器官和受试者中。