CN101896455B - 作为mu阿片类受体拮抗剂的3-羧基丙基-氨基四氢萘衍生物 - Google Patents

作为mu阿片类受体拮抗剂的3-羧基丙基-氨基四氢萘衍生物 Download PDF

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Publication number
CN101896455B
CN101896455B CN200880119873.7A CN200880119873A CN101896455B CN 101896455 B CN101896455 B CN 101896455B CN 200880119873 A CN200880119873 A CN 200880119873A CN 101896455 B CN101896455 B CN 101896455B
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Prior art keywords
diethyl
naphthalene
amino
tetrahydrochysene
base
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Expired - Fee Related
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CN200880119873.7A
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English (en)
Chinese (zh)
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CN101896455A (zh
Inventor
肖恩·G·特拉普
迈克尔·R·利德贝特
丹尼尔·D·朗
约翰·R·雅各布森
普里西拉·范迪克
皮埃尔-让·科尔松
米罗斯拉夫·拉普塔
于颖
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Theravance Biopharma R&D IP LLC
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Shiwan Pharmaceutical
Theravance Biopharma R&D IP LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/48—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system of the same carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/28—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00—Chemistry: analytical and immunological testing
    • Y10T436/17—Nitrogen containing
    • Y10T436/173845—Amine and quaternary ammonium

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Otolaryngology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN200880119873.7A 2007-12-11 2008-12-10 作为mu阿片类受体拮抗剂的3-羧基丙基-氨基四氢萘衍生物 Expired - Fee Related CN101896455B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US722007P 2007-12-11 2007-12-11
US61/007,220 2007-12-11
US4921908P 2008-04-30 2008-04-30
US61/049,219 2008-04-30
PCT/US2008/086171 WO2009076408A2 (en) 2007-12-11 2008-12-10 3 -carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists

Publications (2)

Publication Number Publication Date
CN101896455A CN101896455A (zh) 2010-11-24
CN101896455B true CN101896455B (zh) 2015-04-29

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CN200880119873.7A Expired - Fee Related CN101896455B (zh) 2007-12-11 2008-12-10 作为mu阿片类受体拮抗剂的3-羧基丙基-氨基四氢萘衍生物

Country Status (18)

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US (5) US8106232B2 (enExample)
EP (1) EP2231585B1 (enExample)
JP (1) JP5403762B2 (enExample)
KR (1) KR101610165B1 (enExample)
CN (1) CN101896455B (enExample)
AR (1) AR072336A1 (enExample)
AU (1) AU2008335210B2 (enExample)
BR (1) BRPI0821611A8 (enExample)
CA (1) CA2707981C (enExample)
CL (1) CL2008003672A1 (enExample)
CO (1) CO6300937A2 (enExample)
ES (1) ES2402749T3 (enExample)
IL (1) IL205949A (enExample)
MY (1) MY149973A (enExample)
NZ (1) NZ586048A (enExample)
RU (1) RU2482107C2 (enExample)
TW (1) TWI412360B (enExample)
WO (1) WO2009076408A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7709517B2 (en) 2005-05-13 2010-05-04 The Regents Of The University Of California Diarylhydantoin compounds
NZ596260A (en) * 2006-03-29 2013-05-31 Univ California Diarylthiohydantoin compounds
TWI469971B (zh) 2007-10-26 2015-01-21 Univ California 二芳基乙內醯脲類化合物
EP2231589B1 (en) 2007-12-11 2013-02-13 Theravance, Inc. Aminotetralin compounds as mu opioid receptor antagonists
ES2431354T3 (es) * 2008-04-01 2013-11-26 Theravance, Inc. Derivados de 2-aminotetralina como antagonistas del receptor de opioide mu
RU2512390C2 (ru) * 2008-12-10 2014-04-10 Тереванс, Инк. Кристаллические формы соединения 3-карбоксипропил-аминотетралина
US20110071163A1 (en) * 2009-09-18 2011-03-24 Adolor Corporation Use of an opioid receptor antagonist for the treatment or prevention of gastrointestinal tract disorders
JP2024538727A (ja) * 2021-10-07 2024-10-23 エックス４ ファーマシューティカルズ， インコーポレイテッド マボリキサフォルの合成およびその中間体

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000037426A1 (en) * 1998-12-22 2000-06-29 Astrazeneca Ab Novel oxo-aminotetralin compounds useful in pain management
US6498196B1 (en) * 1998-12-22 2002-12-24 Edward Roberts Compounds useful in pain management

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JP2785879B2 (ja) * 1989-05-31 1998-08-13 ジ・アップジョン・カンパニー 治療学的に有用な２―アミノテトラリン誘導体
US6844368B1 (en) * 1998-12-22 2005-01-18 Edward Roberts Compounds useful in pain management
JP2003502277A (ja) * 1998-12-22 2003-01-21 アストラゼネカ・アクチエボラーグ 疼痛管理に有用な新規なチオ−アミノテトラリン化合物
US6231594B1 (en) * 1999-08-11 2001-05-15 Radiant Medical, Inc. Method of controlling body temperature while reducing shivering
JP2010509227A (ja) 2006-11-07 2010-03-25 ネクター セラピューティックス エイエル，コーポレイション オピオイド作動薬およびオピオイド拮抗薬の用量形態および同時投与
EP2231589B1 (en) * 2007-12-11 2013-02-13 Theravance, Inc. Aminotetralin compounds as mu opioid receptor antagonists
ES2431354T3 (es) 2008-04-01 2013-11-26 Theravance, Inc. Derivados de 2-aminotetralina como antagonistas del receptor de opioide mu
RU2512390C2 (ru) 2008-12-10 2014-04-10 Тереванс, Инк. Кристаллические формы соединения 3-карбоксипропил-аминотетралина

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000037426A1 (en) * 1998-12-22 2000-06-29 Astrazeneca Ab Novel oxo-aminotetralin compounds useful in pain management
US6498196B1 (en) * 1998-12-22 2002-12-24 Edward Roberts Compounds useful in pain management

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Identification of a New Scaffold for Opioid Receptor Antagonism Based on the 2-Amino-1,1-dimethyl-7-hydroxytetralin Pharmacophore;Peter Grundt等;《J. Med. Chem.》;20041231;第47卷(第21期);5069-5075 *
Synthesis and Structure–Activity Relationship of Novel Aminotetralin Derivatives with High u Selective Opioid Affinity;Caroline Roy等;《Bioorganic & Medicinal Chemistry Letters》;20021231;第12卷(第21期);3141–3143 *

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Publication number Publication date
IL205949A0 (en) 2010-11-30
TWI412360B (zh) 2013-10-21
US20140031380A1 (en) 2014-01-30
US8106232B2 (en) 2012-01-31
RU2482107C2 (ru) 2013-05-20
JP2011506463A (ja) 2011-03-03
US20120088787A1 (en) 2012-04-12
IL205949A (en) 2014-03-31
JP5403762B2 (ja) 2014-01-29
US8703791B2 (en) 2014-04-22
WO2009076408A2 (en) 2009-06-18
CA2707981A1 (en) 2009-06-18
CL2008003672A1 (es) 2009-05-29
BRPI0821611A8 (pt) 2016-12-13
US8969370B2 (en) 2015-03-03
CO6300937A2 (es) 2011-07-21
RU2010128542A (ru) 2012-01-27
ES2402749T3 (es) 2013-05-08
KR20100100939A (ko) 2010-09-15
CN101896455A (zh) 2010-11-24
MY149973A (en) 2013-11-15
TW200932211A (en) 2009-08-01
EP2231585B1 (en) 2013-02-13
AU2008335210B2 (en) 2013-10-10
US8318765B2 (en) 2012-11-27
AU2008335210A1 (en) 2009-06-18
US20140329845A1 (en) 2014-11-06
KR101610165B1 (ko) 2016-04-08
WO2009076408A3 (en) 2009-09-03
US20090149535A1 (en) 2009-06-11
CA2707981C (en) 2016-05-10
BRPI0821611A2 (pt) 2015-08-25
NZ586048A (en) 2012-06-29
AR072336A1 (es) 2010-08-25
US8492399B2 (en) 2013-07-23
US20130035510A1 (en) 2013-02-07
EP2231585A2 (en) 2010-09-29

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