HRP20211002T1 - 1,3-tiazol-2-il supstituirani benzamidi - Google Patents

1,3-tiazol-2-il supstituirani benzamidi Download PDF

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HRP20211002T1
HRP20211002T1 HRP20211002TT HRP20211002T HRP20211002T1 HR P20211002 T1 HRP20211002 T1 HR P20211002T1 HR P20211002T T HRP20211002T T HR P20211002TT HR P20211002 T HRP20211002 T HR P20211002T HR P20211002 T1 HRP20211002 T1 HR P20211002T1
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pain
compound according
disease
disorders
endometriosis
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HRP20211002TT
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Adam James Davenport
Nico Braeuer
Oliver Martin Fischer
Andrea Rotgeri
Antje Rottmann
Ioana NEAGOE
Jens Nagel
Anne-Marie GODINHO-COELHO
Juergen Klar
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Bayer Aktiengesellschaft
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Publication of HRP20211002T1 publication Critical patent/HRP20211002T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • 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
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/582Recycling of unreacted starting or intermediate materials

Claims (16)

1. Spoj opće formule (I): [image] u kojem R1 predstavlja C1-C4-alkil; R2 predstavlja nesupstituirani tetrahidrofuran-3-il, R3 predstavlja C1-C4-alkil; A predstavlja CF3-pirimidinil; ili njegov enantiomer, diastereomer, racemat, hidrat, solvat ili sol, ili njihova smjesa.
2. Spoj prema patentnom zahtjevu 1 opće formule (Ia): [image]
3. Spoj prema patentnom zahtjevu 2, naznačen time što R1 predstavlja metil ili etil.
4. Spoj prema bilo kojem od patentnih zahtjeva 2 do 3, naznačen time što R3 predstavlja metil.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što A predstavlja 2-CF3-pirimidin-5-il.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time što R2 predstavlja nesupstituirani (3R)-tetrahidrofuran-3-il, ili (3S)-tetrahidrofuran-3-il.
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 6, naznačen time što R2 predstavlja nesupstituirani (3R)-tetrahidrofuran-3-il.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, naime 3-(5-metil-1,3-tiazol-2-il)-5-[(3R)-tetrahidrofuran-3-iloksi]-N-{(1R)-1-[2-(trifluorometil)pirimidin-5-il]etil}benzamid; 3-(5-metil-1,3-tiazol-2-il)-5-[(3S)-tetrahidrofuran-3-iloksi]-N-{(1R)-1-[2-(trifluorometil)pirimidin-5-il]etil}benzamid.
9. Spoj prema patentnom zahtjevu 8, naime 3-(5-metil-1,3-tiazol-2-il)-5-[(3R)-tetrahidrofuran-3-iloksi]-N-{(1R)-1-[2-(trifluorometil)pirimidin-5-il]etil}benzamid.
10. Farmaceutski pripravak naznačen time što sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili enantiomer, dijastereomer, racemat, hidrat, solvat, njihovu farmaceutski prihvatljivu sol ili njihovu smjesu i farmaceutski prihvatljiv razrjeđivač ili nosač.
11. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1 do 9, ili enantiomera, dijastereomera, racemata, hidrata, solvata, njihove farmaceutski prihvatljive soli ili njihove smjese, za pripremu lijeka za profilaksu ili liječenje bolesti.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili enantiomer, dijastereomer, racemat, hidrat, solvat, ili njihova farmaceutski prihvatljiva sol, ili njihova smjesa, za uporabu u liječenju bolesti.
13. Spoj za uporabu prema patentnom zahtjevu 12, naznačen što je bolest, bolest odabrana iz skupine koju čine genitourinarni, gastrointestinalni, respiratorni ili s bolom povezane bolesti, stanja ili poremećaji; ginekološke bolesti, uključujući dismenoreju, dispareuniju i endometriozu; bol povezanu s endometriozom; simptome povezane s endometriozom, pri čemu su navedeni simptomi dismenoreja, dispareunija, disurija ili dishezija; tanja bolesti mokraćnog sustava povezana sa začepljenjem izlaza iz mokraćnog mjehura; stanja urinarne inkontinencije (smanjeni kapacitet mjehura, povećana učestalost mikcije, urgentna inkontinencija, stresna inkontinencija ili hiperreaktivnost mokraćnog mjehura); benigna hipertrofija prostate; hiperplazija prostate; prostatitis; hiperrefleksija detruzora; prekomjerno aktivni mokraćni mjehur i simptomi povezani s preaktivnim mokraćnim mjehurom, pri čemu su navedeni simptomi povećana učestalost mokrenja, nokturija, urinarna hitnost ili urgentna inkontinencija; zdjelična preosjetljivost; uretritis; prostatitis; prostatodinija; cistitis; idiopatska preosjetljivost mjehura; epilepsija; parcijalni i generalizirani napadaji; respiratorni poremećaji, uključujući kronični opstruktivni plućni poremećaj (KOPB), astmu, bronhospazam, kronični kašalj i slično; gastrointestinalni poremećaji, uključujući sindrom iritabilnog crijeva (IBS), upalnu bolest crijeva (IBD), bilijarne kolike i drugi žučni poremećaji, bubrežne kolike, IBS s dominantnim proljevom, gastroezofagealni refluks, gastrointestinalna distenzija, Crohnova bolest; Parkinsonova bolest; Alzheimerova bolest; infarkt miokarda; poremećaji lipida; i bolesti povezane s bolom odabrane iz skupine koju čine hiperalgezija, alodinija, funkcionalni poremećaji crijeva (sindrom iritabilnog crijeva), artritis (osteoartritis, reumatoidni artritis), opekline, migrena ili klaster glavobolje, ozljede živaca, neuritis, neuralgije, trovanje, ishemijska ozljeda, intersticijski cistitis, traumatska ozljeda živca, posttraumatske ozljede (uključujući prijelome i sportske ozljede), trigeminalna neuralgija, neuropatija malih vlakana, dijabetička neuropatija, kronični artritis i srodne neuralgije, neuropatija uzrokovana HIV-om i liječenjem HIV-a, pruritus.
14. Spoj za uporabu prema patentnom zahtjevu 12, naznačen time što je bolest povezana sa sindromima boli, uključujući akutnu, kroničnu, upalnu i neuropatsku bol.
15. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što je sindrom boli odabran iz skupine upalne boli, kirurške boli, visceralne boli, zubne boli, predmenstrualne boli, boli povezane s endometriozom, središnje boli, boli zbog sindroma peckanja usta, boli zbog opeklina, boli zbog migrene, klaster glavobolje, boli zbog ozljede živca, boli zbog neuritisa, neuralgije, boli zbog trovanja, boli zbog ishemijske ozljede, boli zbog intersticijskog cistitisa, boli zbog raka, boli zbog virusne, parazitske ili bakterijske infekcije, boli zbog traumatske ozljede živca, boli zbog posttraumatskih ozljeda, boli zbog prijeloma i sportskih ozljeda, boli zbog trigeminalne neuralgije, boli povezane s neuropatijom malih vlakana, boli povezane s dijabetičkom neuropatijom, kronične boli u donjem dijelu leđa, fantomske boli udova, sindroma boli u zdjelici, kronične boli u zdjelici, boli neuroma, složenog regionalnog sindroma boli, boli povezane s gastrointestinalnom distenzijom, kronične artritične boli i srodnih neuralgija, i boli povezane s rakom, boli povezane s kemoterapijom, neuropatije uzrokovane HIV-om i liječenjem HIV-a; i boli povezane s bolestima ili poremećajima odabranim iz skupine koju čine hiperalgezija, alodinija, funkcionalni poremećaji crijeva (sindrom iritabilnog crijeva) i artritis (osteoartritis, reumatoidni artritis).
16. Spoj za uporabu prema patentnom zahtjevu 13, naznačen time što je bolest bolest odabrana iz skupine ginekološke bolesti, dismenoreje, dispareunije, endometrioze, boli povezane s endometriozom, simptoma povezanih s endometriozom, disurije ili dishezije.
HRP20211002TT 2014-12-09 2021-06-24 1,3-tiazol-2-il supstituirani benzamidi HRP20211002T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14196954 2014-12-09
PCT/EP2015/078765 WO2016091776A1 (en) 2014-12-09 2015-12-07 1,3-thiazol-2-yl substituted benzamides
EP15804824.9A EP3230281B1 (en) 2014-12-09 2015-12-07 1,3-thiazol-2-yl substituted benzamides

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HRP20220371TT HRP20220371T1 (hr) 2014-12-09 2015-12-07 1,3-tiazol-2-il supstituirani benzamidi
HRP20211002TT HRP20211002T1 (hr) 2014-12-09 2021-06-24 1,3-tiazol-2-il supstituirani benzamidi

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US (5) US10174016B2 (hr)
EP (2) EP3230281B1 (hr)
JP (2) JP6544665B2 (hr)
KR (2) KR102548799B1 (hr)
CN (2) CN107207507B (hr)
AR (2) AR102948A1 (hr)
AU (1) AU2015359626B2 (hr)
BR (1) BR112017012327B1 (hr)
CA (1) CA2969952A1 (hr)
CL (1) CL2017001488A1 (hr)
CO (1) CO2017005742A2 (hr)
CR (2) CR20210108A (hr)
CU (1) CU24411B1 (hr)
CY (2) CY1124486T1 (hr)
DK (2) DK3587417T3 (hr)
DO (2) DOP2017000137A (hr)
EA (2) EA034273B1 (hr)
EC (1) ECSP17036253A (hr)
ES (2) ES2908822T3 (hr)
HR (2) HRP20220371T1 (hr)
HU (2) HUE055290T2 (hr)
IL (6) IL252665B (hr)
JO (1) JOP20150301B1 (hr)
LT (2) LT3230281T (hr)
MA (2) MA41135B1 (hr)
MX (2) MX2020005909A (hr)
MY (1) MY192690A (hr)
NI (1) NI201700073A (hr)
PE (2) PE20220253A1 (hr)
PH (1) PH12017501079A1 (hr)
PL (2) PL3587417T3 (hr)
PT (2) PT3587417T (hr)
RS (2) RS63014B1 (hr)
SG (2) SG10202012274RA (hr)
SI (2) SI3587417T1 (hr)
SV (1) SV2017005461A (hr)
TN (1) TN2017000244A1 (hr)
TW (2) TWI716371B (hr)
UA (1) UA120382C2 (hr)
UY (1) UY36422A (hr)
WO (1) WO2016091776A1 (hr)

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