TWI821321B - 唍衍生物 - Google Patents

唍衍生物 Download PDF

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Publication number
TWI821321B
TWI821321B TW108122548A TW108122548A TWI821321B TW I821321 B TWI821321 B TW I821321B TW 108122548 A TW108122548 A TW 108122548A TW 108122548 A TW108122548 A TW 108122548A TW I821321 B TWI821321 B TW I821321B
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TW
Taiwan
Prior art keywords
methyl
alkyl
formula
disorders
dihydrospiro
Prior art date
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TW108122548A
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English (en)
Chinese (zh)
Other versions
TW202035399A (zh
Inventor
傑諾斯 伊利斯
卡塔林 杜達斯尼
伊斯塔凡 萊涅斯基
帕爾 塔波桑義
艾妮塔 霍維斯
索特 涅莫斯
捷爾吉 李維
Original Assignee
匈牙利商羅特格登公司
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Publication of TW202035399A publication Critical patent/TW202035399A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
TW108122548A 2018-07-13 2019-06-27 唍衍生物 TWI821321B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HUP1800248A HU231333B1 (hu) 2018-07-13 2018-07-13 Spirokromán származékok
HUP1800248 2018-07-13

Publications (2)

Publication Number Publication Date
TW202035399A TW202035399A (zh) 2020-10-01
TWI821321B true TWI821321B (zh) 2023-11-11

Family

ID=89992725

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108122548A TWI821321B (zh) 2018-07-13 2019-06-27 唍衍生物

Country Status (24)

Country Link
US (1) US20210330650A1 (https=)
EP (1) EP3820869B1 (https=)
JP (1) JP7487167B2 (https=)
KR (1) KR20210033002A (https=)
CN (1) CN112823157B (https=)
AR (1) AR115782A1 (https=)
AU (1) AU2019300514B2 (https=)
BR (1) BR112020026996A2 (https=)
CA (1) CA3104258A1 (https=)
CL (1) CL2021000080A1 (https=)
CO (1) CO2021001216A2 (https=)
CU (1) CU24680B1 (https=)
EA (1) EA202190245A1 (https=)
ES (1) ES2964617T3 (https=)
GE (2) GEAP202315557A (https=)
HU (2) HU231333B1 (https=)
IL (1) IL279938B2 (https=)
MX (1) MX2021000460A (https=)
MY (1) MY206779A (https=)
PE (1) PE20211809A1 (https=)
PH (1) PH12020552183A1 (https=)
SG (1) SG11202012594RA (https=)
TW (1) TWI821321B (https=)
WO (1) WO2020012422A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU231414B1 (hu) 2018-07-13 2023-08-28 Richter Gedeon Nyrt. Tiadiazin származékok
TWI901650B (zh) 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔３，４－ｃ〕嗒衍生物
CN115403579A (zh) * 2021-05-27 2022-11-29 上海拓界生物医药科技有限公司 一种新的螺环衍生物及其用途
HU231691B1 (hu) 2021-09-29 2025-10-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok
WO2025175249A1 (en) 2024-02-14 2025-08-21 Olema Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2009127609A1 (en) * 2008-04-15 2009-10-22 Dac S.R.L. Spirocyclic derivatives as histone deacetylase inhibitors
TWI616438B (zh) * 2016-03-22 2018-03-01 默沙東藥廠 菸鹼乙醯膽鹼受體之異位調節劑

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NZ566036A (en) 2005-09-13 2010-06-25 Janssen Pharmaceutica Nv 2-Aniline-4-aryl substituted thiazole derivatives that modulate the alpha7 nicotinic receptor
CN101490056A (zh) * 2006-05-17 2009-07-22 阿斯利康(瑞典)有限公司 烟碱乙酰胆碱受体的配体101
TW200813067A (en) * 2006-05-17 2008-03-16 Astrazeneca Ab Nicotinic acetylcholine receptor ligands
US20100298314A1 (en) 2006-12-20 2010-11-25 Schering Corporation Novel jnk inhibitors
MX2010003156A (es) 2007-10-04 2010-04-01 Hoffmann La Roche Derivados de aril amida substituida con tetrazol y usos de los mismos.
MX2010003155A (es) 2007-10-04 2010-04-01 Hoffmann La Roche Derivados de ciclopropil aril amida y uso de los mismos.
KR20100124272A (ko) 2008-02-07 2010-11-26 아보트 러보러터리즈 양성 알로스테릭 조절제로서의 아미드 유도체 및 이의 사용방법
AR070936A1 (es) 2008-03-19 2010-05-12 Janssen Pharmaceutica Nv 1,2,4 -triazoles trisustituidos
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JP5486591B2 (ja) 2008-05-09 2014-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ アセチルコリン受容体モジュレーターとしての三置換ピラゾール
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WO2009127609A1 (en) * 2008-04-15 2009-10-22 Dac S.R.L. Spirocyclic derivatives as histone deacetylase inhibitors
TWI616438B (zh) * 2016-03-22 2018-03-01 默沙東藥廠 菸鹼乙醯膽鹼受體之異位調節劑

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網路文獻 STN CAS Registry Number:2224106-02-7、1953198-57-6、1947149-33-8、1944825-80-2, Date Entered STN: 2016.7.4-2018.5.20。

Also Published As

Publication number Publication date
KR20210033002A (ko) 2021-03-25
AU2019300514A1 (en) 2021-02-11
CU24680B1 (es) 2023-10-06
HUP1800248A2 (en) 2020-01-28
GEP20237534B (en) 2023-09-11
CO2021001216A2 (es) 2021-02-26
JP2021531260A (ja) 2021-11-18
AR115782A1 (es) 2021-02-24
AU2019300514B2 (en) 2023-02-02
GEAP202315557A (en) 2023-05-10
CN112823157A (zh) 2021-05-18
ES2964617T3 (es) 2024-04-08
EP3820869A1 (en) 2021-05-19
IL279938A (en) 2021-03-01
MX2021000460A (es) 2021-06-23
US20210330650A1 (en) 2021-10-28
PH12020552183A1 (en) 2021-06-21
IL279938B1 (en) 2024-09-01
SG11202012594RA (en) 2021-02-25
WO2020012422A1 (en) 2020-01-16
CL2021000080A1 (es) 2021-10-29
EA202190245A1 (ru) 2021-04-20
EP3820869B1 (en) 2023-08-30
PE20211809A1 (es) 2021-09-14
CU20200108A7 (es) 2021-07-02
IL279938B2 (en) 2025-01-01
HUE064417T2 (hu) 2024-03-28
BR112020026996A2 (pt) 2021-04-06
TW202035399A (zh) 2020-10-01
MY206779A (en) 2025-01-07
HU231333B1 (hu) 2023-01-28
CA3104258A1 (en) 2020-01-16
CN112823157B (zh) 2024-08-09
JP7487167B2 (ja) 2024-05-20

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