CO6440542A2 - Acido amida 4-(1,2,3,4-tetrahidroisoquinolina-2-il)-4- oxobutírico como moduladores de kcnq2/3 - Google Patents

Acido amida 4-(1,2,3,4-tetrahidroisoquinolina-2-il)-4- oxobutírico como moduladores de kcnq2/3

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Publication number
CO6440542A2
CO6440542A2 CO11069300A CO11069300A CO6440542A2 CO 6440542 A2 CO6440542 A2 CO 6440542A2 CO 11069300 A CO11069300 A CO 11069300A CO 11069300 A CO11069300 A CO 11069300A CO 6440542 A2 CO6440542 A2 CO 6440542A2
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Colombia
Prior art keywords
polysubstituted
unsubstituted
mono
unsaturated
saturated
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CO11069300A
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English (en)
Inventor
Sven Kuhnert
Gregor Bahrenberg
Beatrix Merla
Klaus Schiene
Wolfgang Schroder
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Gruenenthal Chemie
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Publication of CO6440542A2 publication Critical patent/CO6440542A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/06—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with the ring nitrogen atom acylated by carboxylic or carbonic acids, or with sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

La invención se refiere a ácido tetrahidroisoquinolinil-4-oxobutírico amidas sustituidos, métodos para la preparación de ellos, productos medicinales que contienen estos compuestos y el uso de éstos compuestos para la preparación de productos medicinales.Las amidas del ácido tetrahidroisoquinolinilo-4-oxobutírico que tienen la fórmula general (1) adecuadas para el tratamiento del dolor. Las amidas sustituidas del ácido tetrahidroisoquinolinilo-4-oxobutírico que tienen la fórmula general (1) con excelente afinidad por el canal KCNQ2/3 K+ adecuadas para el tratamiento de desórdenes o enfermedades que son parcialmente medidas por canales KCNQ2/3 K+. Las amidas sustituidas del ácido tetrahidroisoquinolinilo-4-oxobutírico actúan como moduladores, es decir, agonistas o antagonistas, del canalKCNQ2/3 K+.La invención provee amidas sustituidas del ácido tetrahidroisoquinolinilo-4-oxobutírico que tienen la fórmula general (1)En que R0 representa C1-10 alquilo o C2-10 heteroalquilo, cada uno saturado o no saturado, ramificado o no ramificado, no sustituido o mono o polisustituido; C3-7 cicloalquilo o heterociclilo, cada uno saturado o no saturado, no sustituido o mono o polisustituido; arilo o heteroarilo, cada uno no sustituido o mono o polisustituido; C1-8 unido-alquilo C3-7 cicloalquilo o heterociclilo, cada uno saturado o no saturado, no sustituido o mono o polisustituido, en que la cadena alquilo puede en cada caso ser ramificada o no ramificada, saturada o no saturada, no sustituida, mono o polisustituida; o C1-8 alquilo único arilo o heteroarilo, cada uno no sustituido o mono o polisustituido, en que la cadena alquilo puede ser en cada caso ramificada o no ramificada, saturada o no saturada, no sustituida, mono o polisustituida;R1 representa F; CI; Br; CN; C1-10 alquilo, de preferencia C1-6 alquilo, o C2-10 heteroalquilo, cada uno saturado o no saturado, ramificado o no ramificado, no sustituido o mono o polisustituido; C3-7 cicloalquilo, de preferencia C3-6 cicloalquilo, o heterociclilo, cada uno saturado o no saturado, no sustituido o mono o polisustituido; arilo o heteroarilo, cada uno no sustituido o mono o polisustituido; C1-8 alquilo unido C3-7 cicloalquilo, ...
CO11069300A 2008-12-17 2011-06-03 Acido amida 4-(1,2,3,4-tetrahidroisoquinolina-2-il)-4- oxobutírico como moduladores de kcnq2/3 CO6440542A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08021880 2008-12-17

Publications (1)

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CO6440542A2 true CO6440542A2 (es) 2012-05-15

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ID=40847003

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US (1) US8367700B2 (es)
EP (1) EP2358681A1 (es)
JP (1) JP2012512214A (es)
KR (1) KR20110100651A (es)
CN (1) CN102256947A (es)
AU (1) AU2009335340A1 (es)
BR (1) BRPI0922489A2 (es)
CA (1) CA2747094A1 (es)
CL (1) CL2011001428A1 (es)
CO (1) CO6440542A2 (es)
EC (1) ECSP11011095A (es)
IL (1) IL213565A0 (es)
MX (1) MX2011006384A (es)
NZ (1) NZ593994A (es)
PE (1) PE20120076A1 (es)
WO (1) WO2010075973A1 (es)
ZA (1) ZA201105262B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8367700B2 (en) 2008-12-17 2013-02-05 Gruenenthal Gmbh Substituted 4-(1.2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators
TWI475020B (zh) 2009-03-12 2015-03-01 The substituted nicotine amide as a KCNQ2 / 3 modifier
AR082733A1 (es) 2010-08-27 2012-12-26 Gruenenthal Gmbh 2-amino-quinolina-3-carboxamidas sustituidas como moduladores de kcnq2/3
PT2609083E (pt) 2010-08-27 2015-07-01 Gruenenthal Gmbh 2-oxi-quinolina-3-carboxamidas substituídas como moduladores de kcnq2/3
PE20140214A1 (es) 2010-08-27 2014-02-19 Gruenenthal Chemie 2-oxo- y 2-tioxo-dihidroquinolina-3-carboxamidas sustituidos como moduladores kcnq2/3
AU2011297937B2 (en) * 2010-09-01 2015-10-01 Grunenthal Gmbh Substituted 1-oxo-dihydroisoquinoline-3-carboxamides as KCNQ2/3 modulators
CN105461626B (zh) * 2015-12-17 2018-05-08 浙江工业大学 芳环或稠杂环联3,4-二氢异喹啉类共轭结构化合物及其应用
US10370355B2 (en) * 2016-04-13 2019-08-06 Ucb Biopharma Sprl Tetrahydroisoquinoline derivatives
AU2018336171B2 (en) 2017-09-22 2023-01-05 Jubilant Epipad LLC Heterocyclic compounds as PAD inhibitors
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
WO2019087214A1 (en) 2017-11-06 2019-05-09 Jubilant Biosys Limited Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
KR20200092346A (ko) 2017-11-24 2020-08-03 주빌런트 에피스크라이브 엘엘씨 Prmt5 억제제로서의 헤테로사이클릭 화합물
JP7279063B6 (ja) 2018-03-13 2024-02-15 ジュビラント プローデル エルエルシー Ｐｄ１／ｐｄ－ｌ１相互作用／活性化の阻害剤としての二環式化合物

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8916395D0 (en) * 1989-07-18 1989-09-06 Zambeletti Spa L Pharmaceuticals
US6855829B2 (en) 2001-02-20 2005-02-15 Bristol-Myers Squibb Company 3-fluoro-2-oxindole modulators of KCNQ potassium channels and use thereof in treating migraine and mechanistically related disease
DE102006049452A1 (de) 2006-10-17 2008-05-08 Grünenthal GmbH Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln
US8367700B2 (en) 2008-12-17 2013-02-05 Gruenenthal Gmbh Substituted 4-(1.2,3,4-tetrahydroisoquinolin-2-yl)-4-oxobutyric acid amide as KCNQ2/3 modulators

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WO2010075973A1 (de) 2010-07-08
KR20110100651A (ko) 2011-09-14
ZA201105262B (en) 2012-03-28
PE20120076A1 (es) 2012-02-06
MX2011006384A (es) 2011-07-13
JP2012512214A (ja) 2012-05-31
ECSP11011095A (es) 2011-07-29
CN102256947A (zh) 2011-11-23
CL2011001428A1 (es) 2011-11-18
CA2747094A1 (en) 2010-07-08
US20100152234A1 (en) 2010-06-17
IL213565A0 (en) 2011-07-31
BRPI0922489A2 (pt) 2015-12-15
US8367700B2 (en) 2013-02-05
EP2358681A1 (de) 2011-08-24
AU2009335340A1 (en) 2011-08-04
NZ593994A (en) 2012-08-31

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