AR068116A1 - Compuestos 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu, proceso de preparacion de los mismos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de disfunciones intestinales inducidas por opioides o ileo posquirurgico. - Google Patents

Compuestos 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu, proceso de preparacion de los mismos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de disfunciones intestinales inducidas por opioides o ileo posquirurgico.

Info

Publication number
AR068116A1
AR068116A1 ARP080103728A ARP080103728A AR068116A1 AR 068116 A1 AR068116 A1 AR 068116A1 AR P080103728 A ARP080103728 A AR P080103728A AR P080103728 A ARP080103728 A AR P080103728A AR 068116 A1 AR068116 A1 AR 068116A1
Authority
AR
Argentina
Prior art keywords
same
compounds
alkyl
pharmaceutical compositions
opioid receptors
Prior art date
Application number
ARP080103728A
Other languages
English (en)
Inventor
Priscila Vandyke
Timothy J Church
Bryan Frieman
Daniel D Long
Lan Jiang
Daisuke Roland Saito
Original Assignee
Theravance Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Theravance Inc filed Critical Theravance Inc
Publication of AR068116A1 publication Critical patent/AR068116A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Composiciones farmacéuticas que comprenden tales compuestos, uso de tales compuestos para tratar condiciones asociadas con la actividad de receptores opioides mu, y procesos e intermediarios utiles para preparar tales compuestos. Reivindicacion 1: Un compuesto de la formula (1): caracterizado porque: R7 es hidrogeno o -CH2-R1; R1 es alquilo C4-10, cicloalquilo C3-12, o fenilo, en donde cicloalquilo C3-12 y fenilo están cada uno opcionalmente sustituidos con uno o dos halo; R2 es seleccionado de -C(O)R3, -C(O)NHR4, -C(O)OR5, -S(O)2R6, y -C(O)R8; R3 es alquilo C1-6 sustituido con uno o dos sustituyentes seleccionados de -ORa, -S(O)2Rb, y -C(O)Rc; R4 y R5 son cada uno independientemente alquilo C1-6 sustituido con uno o dos sustituyentes seleccionados de -ORa y -S(O)2Rb; R6 es alquilo C1-3; R8 es fenilo, opcionalmente sustituido con uno o dos halo; Ra es H o alquilo C1-3; Rb es alquilo C1-3; Rc es seleccionado de hidrogeno, alquilo C1-3, y bencilo; y m es1 o 2; siempre que cuando R7 es hidrogeno, R2 es -C(O)R8, o una de sus sales farmacéuticamente aceptables.
ARP080103728A 2007-08-27 2008-08-27 Compuestos 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu, proceso de preparacion de los mismos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de disfunciones intestinales inducidas por opioides o ileo posquirurgico. AR068116A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US96636407P 2007-08-27 2007-08-27
US5106508P 2008-05-07 2008-05-07

Publications (1)

Publication Number Publication Date
AR068116A1 true AR068116A1 (es) 2009-11-04

Family

ID=40042620

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080103728A AR068116A1 (es) 2007-08-27 2008-08-27 Compuestos 8-azabiciclo[3.2.1]octil-2-hidroxibenzamida como antagonistas de receptores opioides mu, proceso de preparacion de los mismos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de disfunciones intestinales inducidas por opioides o ileo posquirurgico.

Country Status (13)

Country Link
US (4) US7902220B2 (es)
EP (1) EP2183249B1 (es)
JP (1) JP5296078B2 (es)
KR (1) KR101547214B1 (es)
CN (1) CN101790529B (es)
AR (1) AR068116A1 (es)
AU (1) AU2008293974B9 (es)
BR (1) BRPI0815797A2 (es)
CA (1) CA2695755C (es)
ES (1) ES2454648T3 (es)
MX (1) MX2010002171A (es)
TW (1) TWI423801B (es)
WO (1) WO2009029256A1 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY145633A (en) 2006-03-01 2012-03-15 Theravance Inc 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
TWI415850B (zh) * 2007-07-20 2013-11-21 Theravance Inc 製備ｍｕ類鴉片受體拮抗劑之中間物的方法
US7947710B2 (en) * 2007-08-27 2011-05-24 Theravance, Inc. Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
TWI423801B (zh) 2007-08-27 2014-01-21 Theravance Inc 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物
ES2390195T3 (es) * 2007-08-27 2012-11-07 Theravance, Inc. Compuestos de amidoalquil-8-azabiciclo(3,2,1)octano, como antagonistas del receptor opioide mu
US7691878B2 (en) * 2007-08-27 2010-04-06 Theravance, Inc. Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
US20120295942A1 (en) 2010-02-01 2012-11-22 Nicholas James Devereux Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Ｃｒｆ受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
CA3054122A1 (en) * 2017-03-02 2018-09-07 Sanwa Kagaku Kenkyusho Co., Ltd. Therapeutic agent for alcohol use disorders
JP7197880B2 (ja) * 2017-10-19 2022-12-28 学校法人 名城大学 エステル化剤及びその利用
JP2021512952A (ja) 2018-02-05 2021-05-20 アルカームス・インコーポレイテッド 疼痛の処置のための化合物
CN108732292B (zh) * 2018-04-27 2020-07-14 中国人民解放军第二军医大学 血浆中舒芬太尼的快速检测方法及装置

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TWI423801B (zh) 2007-08-27 2014-01-21 Theravance Inc 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物
US7947710B2 (en) * 2007-08-27 2011-05-24 Theravance, Inc. Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists

Also Published As

Publication number Publication date
CA2695755C (en) 2016-08-09
US20140080855A1 (en) 2014-03-20
MX2010002171A (es) 2010-04-30
US20150051243A1 (en) 2015-02-19
US20110118306A1 (en) 2011-05-19
US9199993B2 (en) 2015-12-01
WO2009029256A1 (en) 2009-03-05
TW200918057A (en) 2009-05-01
US7902220B2 (en) 2011-03-08
ES2454648T3 (es) 2014-04-11
BRPI0815797A2 (pt) 2015-06-16
CN101790529B (zh) 2012-09-05
AU2008293974A1 (en) 2009-03-05
US20090062333A1 (en) 2009-03-05
CA2695755A1 (en) 2009-03-05
JP5296078B2 (ja) 2013-09-25
US8802698B2 (en) 2014-08-12
KR101547214B1 (ko) 2015-08-25
TWI423801B (zh) 2014-01-21
JP2010537978A (ja) 2010-12-09
EP2183249B1 (en) 2014-02-26
AU2008293974B9 (en) 2013-10-31
EP2183249A1 (en) 2010-05-12
US8481563B2 (en) 2013-07-09
CN101790529A (zh) 2010-07-28
AU2008293974B2 (en) 2013-09-05
KR20100045524A (ko) 2010-05-03

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