N-(cyclopropyl(5-naphtalen-1-yl-pyridin-3-yl)methyl)ethanesulfonamide | 1255870-09-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(cyclopropyl(5-naphtalen-1-yl-pyridin-3-yl)methyl)ethanesulfonamide
• 英文别名: N-[cyclopropyl-(5-naphthalen-1-ylpyridin-3-yl)methyl]ethanesulfonamide
• CAS: 1255870-09-7
• 化学式: C₂₁H₂₂N₂O₂S
• 分子量: 366.484
• InChiKey: LEDUQFBMAMLCIM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDERS
  申请人：NOVARTIS AG

  公开号：US20200164024A1

  公开（公告）日：2020-05-28

  The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , R 1 , X 1 , X 2 , and X 3 are described herein.

  该披露涉及对PCSK9的抑制剂，用于治疗胆固醇脂质代谢以及其他PCSK9发挥作用的疾病，其化学式为(I)： 或其药用可接受的盐、水合物、溶剂合物、前药、立体异构体、N-氧化物或互变异构体，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、X1、X2和X3如本文所述。
• SUBSTITUTED CARBAMOYLCYCLOALKYL ACETIC ACID DERIVATIVES AS NEP
  申请人：KARKI Rajeshri Ganesh

  公开号：US20120122764A1

  公开（公告）日：2012-05-17

  The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

  本发明提供了一种具有化学式I的化合物； 或其药学上可接受的盐，其中R 1 ，R 2 ，R 3 ，R 4 ，R 5 ，B，X，m和n在此处被定义。该发明还涉及制造该发明化合物的方法及其治疗用途。本发明进一步提供了该发明化合物的药物组合物，以及具有药理活性剂和该发明化合物的组合。
• CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
  申请人：ZECRI Frederic

  公开号：US20150031604A1

  公开（公告）日：2015-01-29

  The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13  I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  该发明提供了Formula I（序列ID号：1）的循环多肽：X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13，或者其酰胺、酯或盐，或其生物结合物，其中X1、X3、X4、X7、X8、X9、X10、X11、X12和X13在此有定义。这些多肽是APJ受体的激动剂。该发明还涉及一种制造该发明的多肽或其生物结合物的方法，以及它们的治疗用途，如治疗或预防急性失代偿性心力衰竭（ADHF）、慢性心力衰竭、肺动脉高压、心房颤动、布加达综合征、室性心动过速、动脉粥样硬化、高血压、再狭窄、缺血性心血管疾病、心肌病、心肌纤维化、心律失常、水潴留、糖尿病（包括妊娠糖尿病）、肥胖、周围动脉疾病、脑血管意外、短暂性脑缺血发作、创伤性脑损伤、肌萎缩侧索硬化、烧伤（包括晒伤）和子痫的组合。本发明还提供了药理活性剂的组合和制药组合。
• CYCLIC APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE
  申请人：ZECRI Frédéric

  公开号：US20160159871A1

  公开（公告）日：2016-06-09

  The invention provides a synthetic polypeptide of Formula I′: X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  该发明提供了式I′的合成多肽：X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13或其酰胺、酯、盐或生物结合物，其中X1、X3、X6、X7、X9、X11、X12和X13在此处定义。这些多肽和生物结合物是APJ受体的激动剂。该发明还涉及一种制造该发明的多肽和生物结合物的方法，以及其治疗用途，如治疗或预防急性失代偿性心力衰竭（ADHF）、慢性心力衰竭、肺动脉高压、心房颤动、布加达综合征、室性心动过速、动脉粥样硬化、高血压、再狭窄、缺血性心血管疾病、心肌病、心脏纤维化、心律失常、水潴留、糖尿病（包括妊娠期糖尿病）、肥胖、周围动脉疾病、脑血管意外、短暂性缺血性发作、创伤性脑损伤、肌萎缩侧索硬化、烧伤（包括晒伤）和子痫的组合。本发明还提供了药理活性剂的组合和制药组合物。
• DISULFIDE CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
  申请人：ZECRI Frédéric

  公开号：US20160145309A1

  公开（公告）日：2016-05-26

  The invention provides a synthetic polypeptide of Formula I′: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  该发明提供了公式I′的合成多肽：X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13或其酰胺、酯、盐或生物结合物，其中X1、X5、X6、X7、X9和X11至X13在此处定义。这些多肽和生物结合物是APJ受体的激动剂。该发明还涉及一种制造该发明的多肽或生物结合物的方法，以及其治疗用途，如治疗或预防急性失代偿性心力衰竭（ADHF）、慢性心力衰竭、肺动脉高压、心房颤动、布氏综合征、室性心动过速、动脉粥样硬化、高血压、再狭窄、缺血性心血管疾病、心肌病、心脏纤维化、心律失常、水潴留、糖尿病（包括妊娠期糖尿病）、肥胖、外周动脉疾病、脑血管意外、短暂性脑缺血发作、创伤性脑损伤、肌萎缩侧索硬化、烧伤（包括晒伤）和子痫前症。本发明进一步提供了药理活性剂的组合和制药组合物。