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ME03744B - Spojevi 1-tetrahidropiranilkarbonil-2,3- dihidro-1h-indola, namijenjeni liječenju raka - Google Patents

Spojevi 1-tetrahidropiranilkarbonil-2,3- dihidro-1h-indola, namijenjeni liječenju raka

Info

Publication number
ME03744B
ME03744B MEP-2020-98A MEP202098A ME03744B ME 03744 B ME03744 B ME 03744B ME P202098 A MEP202098 A ME P202098A ME 03744 B ME03744 B ME 03744B
Authority
ME
Montenegro
Prior art keywords
cancer
compound according
hydrogen
dihydro
fluoro
Prior art date
Application number
MEP-2020-98A
Other languages
German (de)
English (en)
French (fr)
Inventor
Jolie Anne Bastian
Jiehao Chen
Jeffrey Daniel Cohen
James Robert Henry
William Thomas Mcmillen
Bradley Earl Reaman
Almudena Rubio
Daniel Jon Sall
Gaiying Zhao
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of ME03744B publication Critical patent/ME03744B/me

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/57Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (10)

1. Spoj formule: , naznačen time što: R1a je vodik, metil, etenil, cijano, fluor, klor, fluormetil ili difluormetil; R1b je vodik, fluor ili klor; R1c je vodik, hidroksi, fluor, benziloksi ili hidroksietilamino; R2 je vodik ili metil; R2a je vodik ili metil; i R3a je tetrahidropiranil.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je: .
3. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je: ,
4. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je: .
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je kristalni 4-fluor-N-{(1R)-1-[1-(tetrahidro-2H-piran-4-ilkarbonil)-2,3-dihidro-1H-indol-5-il]etil}benzamid.
6. Spoj u skladu s patentnim zahtjevom 5, koji je kristalni 4-fluor-N-{(1R)-1-[1-(tetrahidro-2H-piran-4-ilkarbonil)-2,3-dihidro-1H-indol-5-il]etil}benzamid, naznačen time što ima uzorak difrakcije rendgenskih zraka na prahu (zračenje Cu, λ-1,54060 Ǻ), koji sadrži najmanje jedan maksimum na 17,38°, u kombinaciji s jednim ili više maksimuma koje se bira iz skupine koju čine 12,51°, 15,65°, 16,37°, 17,56°, 21,48° i 25,23° (2θ ± 0,2°).
7. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-6, uz jedan ili više farmaceutski prihvatljivih pomoćnih tvari, nosača ili razrjeđivača.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time što je namijenjen upotrebi u terapiji.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-6, naznačen time što je namijenjen upotrebi u liječenju raka.
10. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 9, naznačen time što se rak bira iz skupine koju čine melanom, akutna mijeloidna leukemija, kronična limfocitna leukemija, kolorektalni rak, bubrežnih stanica karcinom, rak dojke, rak pluća, rak jajnika, karcinom jajovoda, primarni peritonealni karcinom, rak vrata maternice, želuca rak, jetre rak, rak gušterače, rak štitnjače, gliom, nehodgkinovski limfom, te Hodgkinov limfom.
MEP-2020-98A 2016-06-10 2017-05-31 Spojevi 1-tetrahidropiranilkarbonil-2,3- dihidro-1h-indola, namijenjeni liječenju raka ME03744B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662348457P 2016-06-10 2016-06-10
PCT/US2017/035097 WO2017213919A1 (en) 2016-06-10 2017-05-31 1-tetrahydropyranylcarbonyl-2,3-dihydro-1h-indole compounds for treating cancer
EP17728990.7A EP3468965B1 (en) 2016-06-10 2017-05-31 1-tetrahydropyranylcarbonyl-2,3-dihydro-1h-indole compounds for treating cancer

Publications (1)

Publication Number Publication Date
ME03744B true ME03744B (me) 2021-04-20

Family

ID=59031409

Family Applications (1)

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MEP-2020-98A ME03744B (me) 2016-06-10 2017-05-31 Spojevi 1-tetrahidropiranilkarbonil-2,3- dihidro-1h-indola, namijenjeni liječenju raka

Country Status (40)

Country Link
US (2) US10759786B2 (me)
EP (1) EP3468965B1 (me)
JP (1) JP6632746B2 (me)
KR (1) KR102241258B1 (me)
CN (1) CN109641881B (me)
AR (1) AR108586A1 (me)
AU (1) AU2017277833B2 (me)
BR (1) BR112018072872A2 (me)
CA (1) CA3027035C (me)
CL (1) CL2018003543A1 (me)
CO (1) CO2018013251A2 (me)
CR (1) CR20180579A (me)
CY (1) CY1123660T1 (me)
DK (1) DK3468965T3 (me)
DO (1) DOP2018000278A (me)
EA (1) EA037419B1 (me)
EC (1) ECSP19001734A (me)
ES (1) ES2797981T3 (me)
HR (1) HRP20200769T1 (me)
HU (1) HUE050155T2 (me)
IL (1) IL263497B (me)
JO (1) JOP20170131B1 (me)
LT (1) LT3468965T (me)
MA (1) MA45224B1 (me)
MD (1) MD3468965T2 (me)
ME (1) ME03744B (me)
MX (1) MX382877B (me)
MY (1) MY197462A (me)
NZ (1) NZ748500A (me)
PE (1) PE20190378A1 (me)
PH (1) PH12018502572A1 (me)
PL (1) PL3468965T3 (me)
PT (1) PT3468965T (me)
RS (1) RS60322B1 (me)
SG (1) SG11201809625RA (me)
SI (1) SI3468965T1 (me)
TW (1) TWI671294B (me)
UA (1) UA122526C2 (me)
WO (1) WO2017213919A1 (me)
ZA (1) ZA201807688B (me)

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MX384836B (es) 2016-03-07 2025-03-14 Enanta Pharm Inc Agentes antivirales contra la hepatitis b
NZ762994A (en) 2017-08-28 2025-11-28 Enanta Pharm Inc Hepatitis b antiviral agents
WO2019089412A1 (en) * 2017-11-01 2019-05-09 Merck Sharp & Dohme Corp. Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
US20210002371A1 (en) * 2017-12-21 2021-01-07 Brian A. Sherer Combination of an anti-pd-l1 antibody and ido1 inhibitor for the treatment of cancer
US11058678B2 (en) 2018-01-22 2021-07-13 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
US11992489B2 (en) 2018-08-17 2024-05-28 Merck Sharp & Dohme Llc Substituted tetrahydroquinoline compounds as indoleamine 2,3-dioxygenase inhibitors
AR116474A1 (es) 2018-09-21 2021-05-12 Enanta Pharm Inc DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV
EP3877366A4 (en) * 2018-11-06 2022-08-24 Merck Sharp & Dohme Corp. NOVEL SUBSTITUTED TRICYCLIC COMPOUNDS AS INDOLAMINE-2,3-DIOXYGENASE INHIBITORS
SG11202105007TA (en) 2018-11-21 2021-06-29 Enanta Pharm Inc Functionalized heterocycles as antiviral agents
US11236111B2 (en) 2019-06-03 2022-02-01 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US11760755B2 (en) 2019-06-04 2023-09-19 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
WO2021007488A1 (en) 2019-07-11 2021-01-14 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2021055425A2 (en) 2019-09-17 2021-03-25 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
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CN114213310B (zh) * 2021-12-31 2024-02-23 中国药科大学 吲哚啉化合物及其衍生物、制备方法、药物组合物和应用
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WO2025140363A1 (zh) * 2023-12-27 2025-07-03 海思科医药集团股份有限公司 一种苯基哌啶衍生物的制备方法

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Publication number Publication date
DK3468965T3 (da) 2020-06-15
CR20180579A (es) 2019-02-08
MA45224B1 (fr) 2020-06-30
MY197462A (en) 2023-06-19
PH12018502572A1 (en) 2019-10-28
HRP20200769T1 (hr) 2020-07-24
CO2018013251A2 (es) 2019-01-18
KR20190003750A (ko) 2019-01-09
ECSP19001734A (es) 2019-01-31
TW201806948A (zh) 2018-03-01
ZA201807688B (en) 2020-08-26
BR112018072872A2 (pt) 2019-03-06
UA122526C2 (uk) 2020-11-25
CY1123660T1 (el) 2022-03-24
EP3468965B1 (en) 2020-04-29
US9872853B2 (en) 2018-01-23
SG11201809625RA (en) 2018-11-29
EA037419B1 (ru) 2021-03-25
WO2017213919A1 (en) 2017-12-14
US10759786B2 (en) 2020-09-01
IL263497B (en) 2020-11-30
CA3027035C (en) 2021-05-04
JOP20170131B1 (ar) 2021-08-17
MD3468965T2 (ro) 2020-08-31
JP6632746B2 (ja) 2020-01-22
TWI671294B (zh) 2019-09-11
HUE050155T2 (hu) 2020-12-28
SI3468965T1 (sl) 2020-07-31
EP3468965A1 (en) 2019-04-17
PE20190378A1 (es) 2019-03-08
MX382877B (es) 2025-03-13
RS60322B1 (sr) 2020-07-31
KR102241258B1 (ko) 2021-04-16
NZ748500A (en) 2020-04-24
EA201892479A1 (ru) 2019-07-31
MX2018015275A (es) 2019-04-11
CN109641881B (zh) 2022-01-07
US20170354641A1 (en) 2017-12-14
US20190161477A1 (en) 2019-05-30
ES2797981T3 (es) 2020-12-04
DOP2018000278A (es) 2018-12-31
PL3468965T3 (pl) 2020-09-21
CN109641881A (zh) 2019-04-16
AR108586A1 (es) 2018-09-05
AU2017277833A1 (en) 2018-11-15
CA3027035A1 (en) 2017-12-14
JP2019518027A (ja) 2019-06-27
LT3468965T (lt) 2020-06-10
AU2017277833B2 (en) 2020-07-02
CL2018003543A1 (es) 2019-03-22
PT3468965T (pt) 2020-07-16
IL263497A (en) 2019-01-31

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