JP2016516792A - α−２アドレノレセプターおよびシグマレセプターリガンドの組み合わせ物 - Google Patents

α−２アドレノレセプターおよびシグマレセプターリガンドの組み合わせ物 Download PDF

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JP2016516792A
JP2016516792A JP2016508133A JP2016508133A JP2016516792A JP 2016516792 A JP2016516792 A JP 2016516792A JP 2016508133 A JP2016508133 A JP 2016508133A JP 2016508133 A JP2016508133 A JP 2016508133A JP 2016516792 A JP2016516792 A JP 2016516792A
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dichlorophenyl
pyrazol
yloxy
substituted
methyl
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JP2016508133A
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JP2016516792A5 (enExample
Inventor
ザマニロ−カスタネド、ダニエル
ミゲル ベラ−エルナンデス、ホセ
ミゲル ベラ−エルナンデス、ホセ
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Esteve Pharmaceuticals SA
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Esteve Pharmaceuticals SA
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Publication of JP2016516792A publication Critical patent/JP2016516792A/ja
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2016508133A 2013-04-16 2014-04-15 α−２アドレノレセプターおよびシグマレセプターリガンドの組み合わせ物 Pending JP2016516792A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13382140.5 2013-04-16
EP13382140.5A EP2792352A1 (en) 2013-04-16 2013-04-16 Alpha-2 adrenoreceptor and sigma receptor ligand combinations
PCT/EP2014/057608 WO2014170319A1 (en) 2013-04-16 2014-04-15 Alpha-2 adrenoceptor and sigma receptor ligand combinations

Publications (2)

Publication Number Publication Date
JP2016516792A true JP2016516792A (ja) 2016-06-09
JP2016516792A5 JP2016516792A5 (enExample) 2017-06-01

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JP2016508133A Pending JP2016516792A (ja) 2013-04-16 2014-04-15 α−２アドレノレセプターおよびシグマレセプターリガンドの組み合わせ物

Country Status (16)

Country Link
US (1) US20160058771A1 (enExample)
EP (2) EP2792352A1 (enExample)
JP (1) JP2016516792A (enExample)
KR (1) KR20150143754A (enExample)
CN (1) CN105228606A (enExample)
AR (1) AR095858A1 (enExample)
AU (1) AU2014255837A1 (enExample)
BR (1) BR112015026259A2 (enExample)
CA (1) CA2908926A1 (enExample)
HK (1) HK1219431A1 (enExample)
MX (1) MX2015014441A (enExample)
PH (1) PH12015502282A1 (enExample)
RU (1) RU2015148766A (enExample)
SG (1) SG11201508102XA (enExample)
TN (1) TN2015000440A1 (enExample)
WO (1) WO2014170319A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
SG11201604480PA (en) 2013-12-17 2016-07-28 Esteve Labor Dr SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011510096A (ja) * 2008-04-18 2011-03-31 ウォーソー・オーソペディック・インコーポレーテッド 疼痛および／または炎症の治療のためのαアドレナリン作動性受容体アゴニスト
JP2012526854A (ja) * 2009-05-15 2012-11-01 レクロ・ファーマ・インコーポレイテッド デクスメデトミジンの舌下組成物およびその使用方法
WO2012156497A1 (en) * 2011-05-19 2012-11-22 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003295491B2 (en) * 2002-11-15 2009-10-08 E.I. Du Pont De Nemours And Company Novel anthranilamide insecticides
KR101352012B1 (ko) 2004-08-27 2014-01-15 라보라토리오스 델 드라. 에스테브.에스.에이. 시그마 수용체 저해제
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
EP2292236A1 (en) 2009-08-14 2011-03-09 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention or treatment of pain induced by chemotherapy
DK2503993T3 (en) 2009-11-25 2016-08-22 Esteve Labor Dr Hydrochloridsalt af 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]-morpholin
EP2335688A1 (en) 2009-11-25 2011-06-22 Laboratorios Del. Dr. Esteve, S.A. Pharmaceutical compositions comprising sigma receptor ligands
MA34047B1 (fr) 2010-02-04 2013-03-05 Esteve Labor Dr Polymorphes et solvates de chlorhydrate de 4-[-2-[[5-méthyl-1-(2-naphtalényl)-1h-pyrazol-3-yl]oxy]éthyl]morpholine
US20110269727A1 (en) * 2010-04-29 2011-11-03 Toledano Annette C Composition to reduce allodynic back pain and related method of use
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
EP2426111A1 (en) 2010-08-09 2012-03-07 Laboratorios Del. Dr. Esteve, S.A. 4-[-2-[[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl]oxy]ethyl]morpholine hydrochloride amorphous solid forms
EP2460519A1 (en) 2010-12-03 2012-06-06 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in bone cancer pain

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011510096A (ja) * 2008-04-18 2011-03-31 ウォーソー・オーソペディック・インコーポレーテッド 疼痛および／または炎症の治療のためのαアドレナリン作動性受容体アゴニスト
JP2012526854A (ja) * 2009-05-15 2012-11-01 レクロ・ファーマ・インコーポレイテッド デクスメデトミジンの舌下組成物およびその使用方法
WO2012156497A1 (en) * 2011-05-19 2012-11-22 Laboratorios Del Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BERNHARD WUNSCH, JOURNAL OF MEDICINAL CHEMISTRY, vol. V55 N19, JPN5016005370, 11 October 2012 (2012-10-11), pages 8209 - 8210, ISSN: 0004052005 *

Also Published As

Publication number Publication date
PH12015502282A1 (en) 2016-02-01
EP2792352A1 (en) 2014-10-22
SG11201508102XA (en) 2015-11-27
US20160058771A1 (en) 2016-03-03
KR20150143754A (ko) 2015-12-23
MX2015014441A (es) 2016-06-21
RU2015148766A3 (enExample) 2018-03-29
EP2986284A1 (en) 2016-02-24
AR095858A1 (es) 2015-11-18
TN2015000440A1 (en) 2017-01-03
RU2015148766A (ru) 2017-05-18
HK1219431A1 (zh) 2017-04-07
BR112015026259A2 (pt) 2017-07-25
AU2014255837A1 (en) 2015-11-05
CN105228606A (zh) 2016-01-06
WO2014170319A1 (en) 2014-10-23
CA2908926A1 (en) 2014-10-23

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