公开(公告)号：US08053462B2

公开(公告)日：2011-11-08

申请号：US10591899

申请日：2005-03-04

申请人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

发明人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

IPC分类号： A01N43/38 ,  A61K31/405 ,  C07D209/16

CPC分类号： C07D209/30 ,  C07D209/14

摘要： This invention relates to a compound represented by formula (I) or a salt thereof, and a therapeutic agent for osteoporosis, an osteoblast activator, and an osteoclast suppressor comprising the same: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, a substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl, substituted or unsubstituted acyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted C1-6 alkylsulfonyl, or hydroxyl; R2 represents substituted or unsubstituted C1-21 alkyl; R3, R5 and R6, which may be the same or different, each represent a hydrogen atom or a halogen atom; and R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl.

摘要翻译： 本发明涉及由式（I）表示的化合物或其盐，以及骨质疏松症治疗剂，成骨细胞激活剂和破骨细胞抑制剂，其中X表示卤素原子; R 1表示氢原子，取代或未取代的C 1-6烷基，取代或未取代的C 2-6烯基，取代或未取代的C 2-6炔基，取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的酰基，取代或未取代的 取代或未取代的C 1-6烷基磺酰基或羟基; R2代表取代或未取代的C 1-12烷基; R 3，R 5和R 6可以相同或不同，各自表示氢原子或卤素原子; 并且R 4表示氢原子或取代或未取代的C 1-6烷基。

公开(公告)号：US07659304B2

公开(公告)日：2010-02-09

申请号：US12007992

申请日：2008-01-17

申请人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

发明人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

IPC分类号： A61K31/405 ,  C07D209/12

CPC分类号： C07D209/30

摘要： A compound represented by the following formula (I) or a salt thereof is provided: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group. Also provided is a therapeutic drug for osteoporosis and an osteoblast activator comprising the compound or a salt thereof.

摘要翻译： 提供由下式（I）表示的化合物或其盐：其中X表示卤素原子; R 1表示氢原子，取代或未取代的C 1-6烷基，取代或未取代的C 2-6烯基，取代或未取代的C 2-6炔基，取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的酰基 取代或未取代的芳基磺酰基，取代或未取代的C 1-6烷基磺酰基，取代或未取代的C 2-7烷氧基羰基或羟基; R2表示取代或未取代的C1〜21烷基; R3，R5和R6相同或不同，表示氢原子或卤素原子; R4表示氢原子或取代或未取代的C1-6烷基; 并且R 7表示氢原子或取代或未取代的C 1-11烃基。 还提供了用于骨质疏松症的治疗药物和包含该化合物或其盐的成骨细胞活化剂。

公开(公告)号：US20090054511A1

公开(公告)日：2009-02-26

申请号：US12007992

申请日：2008-01-17

申请人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

发明人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

IPC分类号： A61K31/404 ,  C07D209/20 ,  A61P19/10

CPC分类号： C07D209/30

摘要： It is intended to provide a tryptophan derivative that activates osteoblasts and to provide a therapeutic drug for osteoporosis and an osteoblast activator using this tryptophan derivative.This invention relates to a compound represented by the following formula (I) or a salt thereof: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl group, substituted or unsubstituted C2-6 alkenyl group, substituted or unsubstituted C2-6 alkynyl group, substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl group, substituted or unsubstituted acyl group, substituted or unsubstituted arylsulfonyl group, substituted or unsubstituted C1-6 alkylsulfonyl group, substituted or unsubstituted C2-7 alkoxycarbonyl group, or hydroxyl group; R2 represents a substituted or unsubstituted C1-21 alkyl group; R3, R5, and R6 are the same or different and represent a hydrogen atom or halogen atom; R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl group; and R7 represents a hydrogen atom or substituted or unsubstituted C1-21 hydrocarbon group, and to a therapeutic drug for osteoporosis and an osteoblast activator comprising the compound or a salt thereof.

摘要翻译： 旨在提供活化成骨细胞的色氨酸衍生物并提供用于骨质疏松症的治疗药物和使用该色氨酸衍生物的成骨细胞激活剂。 本发明涉及由下式（I）表示的化合物或其盐：其中X表示卤素原子; R 1表示氢原子，取代或未取代的C 1-6烷基，取代或未取代的C 2-6烯基，取代或未取代的C 2-6炔基，取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的酰基 取代或未取代的芳基磺酰基，取代或未取代的C 1-6烷基磺酰基，取代或未取代的C 2-7烷氧基羰基或羟基; R2表示取代或未取代的C1〜21烷基; R3，R5和R6相同或不同，表示氢原子或卤素原子; R4表示氢原子或取代或未取代的C1-6烷基; R7代表氢原子或取代或未取代的C1-21烃基，以及含有该化合物或其盐的骨质疏松症治疗药物和成骨细胞激活剂。

公开(公告)号：US20070197629A1

公开(公告)日：2007-08-23

申请号：US10591899

申请日：2005-03-04

申请人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

发明人： Masanori Somei ,  Atsuhiko Hattori ,  Nobuo Suzuki

IPC分类号： A61K31/405

CPC分类号： C07D209/30 ,  C07D209/14

摘要： This invention relates to a compound represented by formula (I) or a salt thereof, and a therapeutic agent for osteoporosis, an osteoblast activator, and an osteoclast suppressor comprising the same: wherein X represents a halogen atom; R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, a substituted or unsubstituted aromatic group, substituted or unsubstituted aralkyl, substituted or unsubstituted acyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted C1-6 alkylsulfonyl, or hydroxyl; R2 represents substituted or unsubstituted C1-21 alkyl; R3, R5 and R6, which may be the same or different, each represent a hydrogen atom or a halogen atom; and R4 represents a hydrogen atom or substituted or unsubstituted C1-6 alkyl.

摘要翻译： 本发明涉及由式（I）表示的化合物或其盐，骨质疏松症治疗剂，成骨细胞激活剂和破骨细胞抑制剂，其中X表示卤素原子; R 1表示氢原子，取代或未取代的C 1-6烷基，取代或未取代的C 2-6烯基，取代或未取代的C 取代或未取代的芳基，取代或未取代的芳烷基，取代或未取代的酰基，取代或未取代的芳基磺酰基，取代或未取代的C 1-6烷基磺酰基， 或羟基; R 2表示取代或未取代的C 1-12烷基; R 3，R 5和R 6可以相同或不同，各自表示氢原子或卤素原子; R 4表示氢原子或取代或未取代的C 1-6烷基。

公开(公告)号：US08258174B2

公开(公告)日：2012-09-04

申请号：US13059876

申请日：2009-08-19

申请人： Yoshikazu Mikami ,  Masanori Somei

发明人： Yoshikazu Mikami ,  Masanori Somei

IPC分类号： A61K315/4045 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D209/14 ,  A61K31/4045

摘要： The invention disclosed is drawn to a method of inhibiting apoptosis comprising administration an effective amount of an indole derivative represented by formula (1) as described herein.

摘要翻译： 所公开的本发明涉及一种抑制细胞凋亡的方法，包括给予本文所述的有效量的由式（1）表示的吲哚衍生物。

公开(公告)号：US20110306648A1

公开(公告)日：2011-12-15

申请号：US13059876

申请日：2009-08-19

申请人： Yoshikazu Mikami ,  Masanori Somei

发明人： Yoshikazu Mikami ,  Masanori Somei

IPC分类号： A61K31/4045 ,  A61P25/28 ,  A61P43/00

CPC分类号： C07D209/14 ,  A61K31/4045

摘要： Disclosed is an apoptosis inhibitor containing an indole derivative represented by the following formula (1) or a salt thereof as an active ingredient, wherein R1 represents a group selected from a hydrogen atom, an alkyl group having 1 to 6 carbon atoms which may have a substituent, an alkenyl group having 2 to 6 carbon atoms which may have a substituent, an alkynyl group having 2 to 6 carbon atoms which may have a substituent, an aromatic group which may have a substituent, an aralkyl group which may have a substituent, an acyl group which may have a substituent, an arylsulfonyl group which may have a substituent, an alkylsulfonyl group having 1 to 6 carbon atoms which may have a substituent, an alkoxy group having 1 to 6 carbon atoms which may have a substituent, an alkenyloxy group having 2 to 6 carbon atoms which may have a substituent, an alkynyloxy group having 2 to 6 carbon atoms which may have a substituent, an aryloxy group which may have a substituent, an aralkyloxy group which may have a substituent, and an acyloxy group which may have a substituent and a hydroxy group; and R2 represents a group selected from an alkyl group having 1 to 21 carbon atoms which may have a substituent, an alkenyl group having 2 to 6 carbon atoms which may have a substituent, an alkynyl group having 2 to 6 carbon atoms which may have a substituent, an aromatic group which may have a substituent, an aralkyl group which may have a substituent, an amino group which may have a substituent, an alkoxy group having 1 to 6 carbon atoms which may have a substituent, an alkenyloxy group having 2 to 6 carbon atoms which may have a substituent, an alkynyloxy group having 2 to 6 carbon atoms which may have a substituent, an aryloxy group which may have a substituent, an aralkyloxy group which may have a substituent, an acyloxy group which may have a substituent and a hydroxy group.

摘要翻译： 公开了含有下述式（1）所示的吲哚衍生物或其盐作为有效成分的凋亡抑制剂，其中，R1表示选自氢原子，可以具有碳原子数1〜6的烷基， 取代基，可以具有取代基的碳原子数2〜6的烯基，可以具有取代基的碳原子数2〜6的炔基，可以具有取代基的芳香族基，可以具有取代基的芳烷基， 可以具有取代基的酰基，可以具有取代基的芳基磺酰基，可以具有取代基的碳原子数1〜6的烷基磺酰基，可以具有取代基的碳原子数1〜6的烷氧基，烯氧基 可以具有取代基的碳原子数2〜6的烷基，可以具有取代基的碳原子数2〜6的炔氧基，可以具有取代基的芳氧基，芳烷氧基wh 可以具有取代基，可以具有取代基的酰氧基和羟基; R2表示可以具有取代基的碳原子数1〜21的烷基，可以具有取代基的碳原子数2〜6的烯基，可以具有取代基的碳原子数2〜6的炔基， 取代基，可以具有取代基的芳香族基团，可以具有取代基的芳烷基，可以具有取代基的氨基，可以具有取代基的碳原子数为1〜6的烷氧基，具有2〜 可以具有取代基的6个碳原子，可以具有取代基的碳原子数2〜6的炔氧基，可以具有取代基的芳氧基，可以具有取代基的芳烷氧基，可以具有取代基的酰氧基， 和羟基。

公开(公告)号：US20090005430A1

公开(公告)日：2009-01-01

申请号：US11663748

申请日：2005-09-16

申请人： Masanori Somei ,  Koki Shigenobu ,  Yoshio Tanaka

发明人： Masanori Somei ,  Koki Shigenobu ,  Yoshio Tanaka

IPC分类号： A61K31/404 ,  A61P7/00

CPC分类号： A61K31/4045 ,  A61K31/405 ,  Y10S514/88 ,  Y10S514/929

摘要： It is intended to find a compound that is structurally simpler than yohimbine, a pentacyclic condensed heterocyclic compound, and has an effect similar to that of yohimbine.The present invention relates to a pharmaceutical or food composition for α2 receptor blockage comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (wherein R1 represents a hydrogen, alkyl group, alkenyl group, alkynyl group, aromatic group, aralkyl group, acyl group, arylsulfonyl group, alkylsulfonyl group, or hydroxyl group; R2 represents a hydrocarbon group; R3, R4, R5, R6, and R7 are the same or different and represent a hydrogen, halogen, alkyl group, or alkoxy group; R8 represents a hydrogen or acyl group; n represents an integer of 1 to 6; and a and b are the same or different and represent 1 or 0).

摘要翻译： 旨在找到结构上比育亨宾简单的化合物，五环稠合杂环化合物，并且具有与育亨宾相似的效果。 本发明涉及用于α2受体阻断的药物或食品组合物，其包含由式（I）表示的化合物或其药学上可接受的盐：（其中R 1表示氢，烷基，烯基，炔基，芳族基团， 芳烷基，酰基，芳基磺酰基，烷基磺酰基或羟基; R 2表示烃基; R 3，R 4，R 5，R 6和R 7相同或不同，表示氢，卤素，烷基或烷氧基 ; R8表示氢或酰基; n表示1〜6的整数，a和b相同或不同，表示1或0）。

公开(公告)号：US11065229B2

公开(公告)日：2021-07-20

申请号：US16427266

申请日：2019-05-30

申请人： Masanori Somei ,  Kazuko Somei ,  Hiizu Somei

发明人： Masanori Somei

IPC分类号： A01N43/00 ,  A01N43/46 ,  A61K31/55 ,  A61K31/405 ,  A61P17/04 ,  A61K9/00

摘要： This invention relates to a method for treating atopic dermatitis, comprising administering an effective amount of N-acyltryptamine represented by Formula (I): wherein R represents a saturated aliphatic hydrocarbon group having 2 to 29 carbon atoms; or a pharmaceutically acceptable salt, hydrate or solvate thereof to a subject in need thereof.

公开(公告)号：US07872040B2

公开(公告)日：2011-01-18

申请号：US11663748

申请日：2005-09-16

申请人： Masanori Somei ,  Koki Shigenobu ,  Yoshio Tanaka

发明人： Masanori Somei ,  Koki Shigenobu ,  Yoshio Tanaka

IPC分类号： A61K31/405 ,  A61K31/40

CPC分类号： A61K31/4045 ,  A61K31/405 ,  Y10S514/88 ,  Y10S514/929

摘要： It is intended to find a compound that is structurally simpler than yohimbine, a pentacyclic condensed heterocyclic compound, and has an effect similar to that of yohimbine.The present invention relates to a pharmaceutical or food composition for α2 receptor blockage comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (wherein R1 represents a hydrogen, alkyl group, alkenyl group, alkynyl group, aromatic group, aralkyl group, acyl group, arylsulfonyl group, alkylsulfonyl group, or hydroxyl group; R2 represents a hydrocarbon group; R3, R4, R5, R6, and R7 are the same or different and represent a hydrogen, halogen, alkyl group, or alkoxy group; R8 represents a hydrogen or acyl group; n represents an integer of 1 to 6; and a and b are the same or different and represent 1 or 0).

摘要翻译： 旨在找到结构上比育亨宾简单的化合物，五环稠合杂环化合物，并且具有与育亨宾相似的效果。 本发明涉及一种α2受体阻断剂的药物或食品组合物，其包含式（I）表示的化合物或其药学上可接受的盐：（其中R 1表示氢，烷基，烯基，炔基，芳族基团， 芳烷基，酰基，芳基磺酰基，烷基磺酰基或羟基; R 2表示烃基; R 3，R 4，R 5，R 6和R 7相同或不同，表示氢，卤素，烷基或烷氧基 ; R8表示氢或酰基; n表示1〜6的整数，a和b相同或不同，表示1或0）。