CN115348962A - 作为GABAAα5受体调节剂的萘啶及吡啶并[3,4-c]哒嗪衍生物 - Google Patents

作为GABAAα5受体调节剂的萘啶及吡啶并[3,4-c]哒嗪衍生物 Download PDF

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Publication number
CN115348962A
CN115348962A CN202180023958.0A CN202180023958A CN115348962A CN 115348962 A CN115348962 A CN 115348962A CN 202180023958 A CN202180023958 A CN 202180023958A CN 115348962 A CN115348962 A CN 115348962A
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China
Prior art keywords
methyl
methoxy
methylpyridin
tetrahydro
alkyl
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CN202180023958.0A
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English (en)
Chinese (zh)
Inventor
G·斯扎博
A·波托尔
I·瓦格
G·I·图罗斯
O·埃利拉斯
G·L·卡普斯
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Richter Gedeon Nyrt
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Richter Gedeon Nyrt
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Publication of CN115348962A publication Critical patent/CN115348962A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202180023958.0A 2020-03-26 2021-03-25 作为GABAAα5受体调节剂的萘啶及吡啶并[3,4-c]哒嗪衍生物 Pending CN115348962A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
HUP2000113 2020-03-26
HUP2000113 2020-03-26
PCT/IB2021/052486 WO2021191838A1 (en) 2020-03-26 2021-03-25 NAPHTHYRIDINE AND PYRIDO[3,4-c]PYRIDAZINE DERIVATIVES AS GABAA α5 RECEPTOR MODULATORS

Publications (1)

Publication Number Publication Date
CN115348962A true CN115348962A (zh) 2022-11-15

Family

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CN202180023958.0A Pending CN115348962A (zh) 2020-03-26 2021-03-25 作为GABAAα5受体调节剂的萘啶及吡啶并[3,4-c]哒嗪衍生物

Country Status (22)

Country Link
US (1) US20240067637A1 (enExample)
EP (1) EP4126859A1 (enExample)
JP (1) JP7805946B2 (enExample)
KR (1) KR20220160061A (enExample)
CN (1) CN115348962A (enExample)
AR (1) AR121666A1 (enExample)
AU (1) AU2021244926A1 (enExample)
BR (1) BR112022019128A2 (enExample)
CA (1) CA3171441A1 (enExample)
CL (1) CL2022002568A1 (enExample)
CO (1) CO2022014877A2 (enExample)
CU (1) CU24714B1 (enExample)
EC (1) ECSP22082367A (enExample)
GE (2) GEAP202416066A (enExample)
IL (1) IL296716A (enExample)
JO (1) JOP20220219A1 (enExample)
MX (1) MX2022011933A (enExample)
PE (1) PE20221836A1 (enExample)
PH (1) PH12022552340A1 (enExample)
TW (1) TWI901650B (enExample)
WO (1) WO2021191838A1 (enExample)
ZA (1) ZA202211414B (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU231691B1 (hu) * 2021-09-29 2025-10-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102924452A (zh) * 2012-11-16 2013-02-13 苏州施亚生物科技有限公司 5,6,7,8-四氢-2H-吡啶并[3,4-c]哒嗪-3-酮的合成方法
CN103221402A (zh) * 2010-11-09 2013-07-24 霍夫曼-拉罗奇有限公司 三唑衍生物及其用于神经障碍的用途
CN103429582A (zh) * 2011-03-04 2013-12-04 莱西肯医药有限公司 Mst1激酶抑制剂及其用法
US20160102088A1 (en) * 2014-10-10 2016-04-14 Allergan, Inc. Piperidylpyrimidine derivatives as modulators of protein kinase inhibitors and of vascular endothelial growth factor receptor 2
WO2018104419A1 (en) * 2016-12-08 2018-06-14 F. Hoffmann-La Roche Ag New isoxazolyl ether derivatives as gaba a alpha5 pam
WO2018117196A1 (ja) * 2016-12-20 2018-06-28 大日本住友製薬株式会社 がん幹細胞を標的とする医薬
WO2020016443A1 (en) * 2018-07-20 2020-01-23 Boehringer Ingelheim International Gmbh Difluoromethyl-phenyl triazoles as gaba receptor modulators

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2728900B1 (fr) * 1994-12-29 1997-01-31 Synthelabo Derives de 3-phenylisoquinolein-1(2h)-one, leur preparation et leur application en therapeutique
SE0403085D0 (sv) * 2004-12-17 2004-12-17 Astrazeneca Ab Novel componds
BRPI0617306A2 (pt) * 2005-10-11 2011-07-19 Hoffmann La Roche derivados de isoxazol
BRPI0618383A2 (pt) * 2005-11-09 2011-08-30 Hoffmann La Roche derivados de 3-aril-isoxazol-4-carbonil-benzofurano
HU230518B1 (hu) 2005-12-20 2016-10-28 Richter Gedeon Nyrt. Bradykinin B1 receptor szelektív antagonista hatással rendelkező új fenatridin származékok, eljárás előállításukra, és az ezeket tartalmazó gyógyszerkészítmények
HUP0600808A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them
HUP0600809A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
HUP0600810A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
US7943619B2 (en) 2007-12-04 2011-05-17 Hoffmann-La Roche Inc. Isoxazolo-pyridazine derivatives
DK2937349T3 (en) 2011-03-23 2017-02-20 Amgen Inc CONDENSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3
CA2876778A1 (en) * 2012-06-26 2014-01-03 Saniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
KR20150033679A (ko) 2012-06-26 2015-04-01 사니오나 에이피에스 페닐 트리아졸 유도체 및 이의 gabaa 수용체 복합체 조절용 용도
WO2014001278A1 (en) * 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
WO2014001279A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
HUP1300139A2 (en) 2013-03-06 2014-09-29 Richter Gedeon Nyrt Phenoxypiperidine h3 antagonists
CN112409363B (zh) 2013-12-20 2023-11-14 艾吉因生物股份有限公司 用于治疗认知损害的苯并二氮杂䓬衍生物、组合物和方法
KR20180030545A (ko) * 2015-06-22 2018-03-23 다이닛본 스미토모 세이야꾸 가부시끼가이샤 바이사이클릭 헤테로사이클릭 아미드 유도체
JP2018525429A (ja) 2015-08-28 2018-09-06 アッヴィ・インコーポレイテッド S1p調節剤としての縮合複素環化合物
PT3439665T (pt) 2016-03-18 2022-09-27 Uwm Res Foundation Inc Tratamento de sintomas cognitivos e de humor em distúrbios neurodegenerativos e neuropsiquiátricos com gaba contendo agonistas de recetores de gabaa contendo alfa5
HU231057B1 (hu) 2017-03-13 2020-04-28 Richter Gedeon Nyrt Gyógyászatilag hatékony aril-szubsztituált pirazolo[1,5-a]pirimidin származékok
HU231058B1 (hu) 2017-03-13 2020-04-28 Richter Gedeon Nyrt. Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok
ES2902365T3 (es) 2017-11-27 2022-03-28 Dart Neuroscience Llc Compuestos de furanopirimidina sustituidos como inhibidores de PDE1
TW201938171A (zh) 2017-12-15 2019-10-01 匈牙利商羅特格登公司 作為血管升壓素V1a受體拮抗劑之三環化合物
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
AU2019286312B2 (en) 2018-06-13 2023-08-17 F. Hoffmann-La Roche Ag New isoxazolyl ether derivatives as GABA A alpha5 PAM
HU231414B1 (hu) 2018-07-13 2023-08-28 Richter Gedeon Nyrt. Tiadiazin származékok
HU231333B1 (hu) 2018-07-13 2023-01-28 Richter Gedeon Nyrt Spirokromán származékok
HU231478B1 (hu) 2018-07-13 2024-02-28 Richter Gedeon Nyrt. Szubsztituált (aza)indol származékok
HU231223B1 (hu) * 2018-09-28 2022-01-28 Richter Gedeon Nyrt. GABAA A5 receptor modulátor hatású biciklusos vegyületek

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103221402A (zh) * 2010-11-09 2013-07-24 霍夫曼-拉罗奇有限公司 三唑衍生物及其用于神经障碍的用途
CN103429582A (zh) * 2011-03-04 2013-12-04 莱西肯医药有限公司 Mst1激酶抑制剂及其用法
CN102924452A (zh) * 2012-11-16 2013-02-13 苏州施亚生物科技有限公司 5,6,7,8-四氢-2H-吡啶并[3,4-c]哒嗪-3-酮的合成方法
US20160102088A1 (en) * 2014-10-10 2016-04-14 Allergan, Inc. Piperidylpyrimidine derivatives as modulators of protein kinase inhibitors and of vascular endothelial growth factor receptor 2
WO2018104419A1 (en) * 2016-12-08 2018-06-14 F. Hoffmann-La Roche Ag New isoxazolyl ether derivatives as gaba a alpha5 pam
WO2018117196A1 (ja) * 2016-12-20 2018-06-28 大日本住友製薬株式会社 がん幹細胞を標的とする医薬
WO2020016443A1 (en) * 2018-07-20 2020-01-23 Boehringer Ingelheim International Gmbh Difluoromethyl-phenyl triazoles as gaba receptor modulators

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CAS: "RN 2094711-87-0", STN REGISTRY *
CAS: "RN 2331259-79-9", STN REGISTRY, 12 June 2019 (2019-06-12) *
CAS: "RN 2331259-96-0", STN REGISTRY *
CAS: "RN 2411227-75-1", STN REGISTRY, 5 March 2020 (2020-03-05) *

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BR112022019128A2 (pt) 2022-11-08
TW202202495A (zh) 2022-01-16
PH12022552340A1 (en) 2023-11-29
PE20221836A1 (es) 2022-11-29
AR121666A1 (es) 2022-06-29
US20240067637A1 (en) 2024-02-29
JOP20220219A1 (ar) 2022-09-13
CA3171441A1 (en) 2021-09-30
GEP20257761B (en) 2025-04-10
ZA202211414B (en) 2023-06-28
JP7805946B2 (ja) 2026-01-26
GEAP202416066A (en) 2024-12-10
KR20220160061A (ko) 2022-12-05
AU2021244926A1 (en) 2022-11-03
CU20220058A7 (es) 2023-05-11
TWI901650B (zh) 2025-10-21
EP4126859A1 (en) 2023-02-08
CO2022014877A2 (es) 2022-10-31
IL296716A (en) 2022-11-01
JP2023520647A (ja) 2023-05-18
ECSP22082367A (es) 2022-11-30
CU24714B1 (es) 2024-07-10
CL2022002568A1 (es) 2023-03-24
WO2021191838A1 (en) 2021-09-30
MX2022011933A (es) 2022-10-20

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