HRP20211002T1 - 1,3-tiazol-2-il supstituirani benzamidi - Google Patents
1,3-tiazol-2-il supstituirani benzamidi Download PDFInfo
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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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- -1 1,3-thiazol-2-yl Chemical group 0.000 title claims 2
- 229940054066 benzamide antipsychotics Drugs 0.000 title 1
- 150000003936 benzamides Chemical class 0.000 title 1
- 208000002193 Pain Diseases 0.000 claims 33
- 230000036407 pain Effects 0.000 claims 31
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 16
- 201000010099 disease Diseases 0.000 claims 13
- 201000009273 Endometriosis Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- 230000001684 chronic effect Effects 0.000 claims 5
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 5
- 208000004296 neuralgia Diseases 0.000 claims 5
- 208000024891 symptom Diseases 0.000 claims 5
- 208000004454 Hyperalgesia Diseases 0.000 claims 4
- 208000028389 Nerve injury Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 230000008764 nerve damage Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 238000011282 treatment Methods 0.000 claims 4
- 208000005171 Dysmenorrhea Diseases 0.000 claims 3
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 3
- 208000004483 Dyspareunia Diseases 0.000 claims 3
- 206010020853 Hypertonic bladder Diseases 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 230000002496 gastric effect Effects 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- GTQPEQGDLVSFJO-CXAGYDPISA-N 3-(5-methyl-1,3-thiazol-2-yl)-5-[(3R)-oxolan-3-yl]oxy-N-[(1R)-1-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide Chemical compound CC1=CN=C(S1)C=1C=C(C(=O)N[C@H](C)C=2C=NC(=NC=2)C(F)(F)F)C=C(C=1)O[C@H]1COCC1 GTQPEQGDLVSFJO-CXAGYDPISA-N 0.000 claims 2
- 208000025978 Athletic injury Diseases 0.000 claims 2
- 208000006561 Cluster Headache Diseases 0.000 claims 2
- 206010010774 Constipation Diseases 0.000 claims 2
- 206010010904 Convulsion Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 206010051244 Dyschezia Diseases 0.000 claims 2
- 208000035154 Hyperesthesia Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 206010029240 Neuritis Diseases 0.000 claims 2
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 2
- 208000000450 Pelvic Pain Diseases 0.000 claims 2
- 208000005374 Poisoning Diseases 0.000 claims 2
- 208000010261 Small Fiber Neuropathy Diseases 0.000 claims 2
- 206010073928 Small fibre neuropathy Diseases 0.000 claims 2
- 208000000921 Urge Urinary Incontinence Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 206010053552 allodynia Diseases 0.000 claims 2
- 206010013990 dysuria Diseases 0.000 claims 2
- 230000009610 hypersensitivity Effects 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 208000037906 ischaemic injury Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 208000020629 overactive bladder Diseases 0.000 claims 2
- 231100000572 poisoning Toxicity 0.000 claims 2
- 230000000607 poisoning effect Effects 0.000 claims 2
- 208000017692 primary erythermalgia Diseases 0.000 claims 2
- 201000007094 prostatitis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 230000000472 traumatic effect Effects 0.000 claims 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- GTQPEQGDLVSFJO-DYVFJYSZSA-N 3-(5-methyl-1,3-thiazol-2-yl)-5-[(3S)-oxolan-3-yl]oxy-N-[(1R)-1-[2-(trifluoromethyl)pyrimidin-5-yl]ethyl]benzamide Chemical compound CC1=CN=C(S1)C=1C=C(C(=O)N[C@H](C)C=2C=NC(=NC=2)C(F)(F)F)C=C(C=1)O[C@@H]1COCC1 GTQPEQGDLVSFJO-DYVFJYSZSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010004663 Biliary colic Diseases 0.000 claims 1
- 206010071445 Bladder outlet obstruction Diseases 0.000 claims 1
- 208000009079 Bronchial Spasm Diseases 0.000 claims 1
- 208000014181 Bronchial disease Diseases 0.000 claims 1
- 206010006482 Bronchospasm Diseases 0.000 claims 1
- 206010068065 Burning mouth syndrome Diseases 0.000 claims 1
- 206010058019 Cancer Pain Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000023890 Complex Regional Pain Syndromes Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 206010017076 Fracture Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 208000008930 Low Back Pain Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010027566 Micturition urgency Diseases 0.000 claims 1
- 206010027603 Migraine headaches Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000005890 Neuroma Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010061334 Partial seizures Diseases 0.000 claims 1
- 208000004983 Phantom Limb Diseases 0.000 claims 1
- 206010056238 Phantom pain Diseases 0.000 claims 1
- 206010036018 Pollakiuria Diseases 0.000 claims 1
- 206010065347 Premenstrual pain Diseases 0.000 claims 1
- 206010036968 Prostatic pain Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 206010069645 Reduced bladder capacity Diseases 0.000 claims 1
- 206010038419 Renal colic Diseases 0.000 claims 1
- 206010066218 Stress Urinary Incontinence Diseases 0.000 claims 1
- 208000003800 Urinary Bladder Neck Obstruction Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 230000002917 arthritic effect Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000013116 chronic cough Diseases 0.000 claims 1
- 208000018912 cluster headache syndrome Diseases 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 230000035874 hyperreactivity Effects 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 230000027939 micturition Effects 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 206010029446 nocturia Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 230000003071 parasitic effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 208000022170 stress incontinence Diseases 0.000 claims 1
- 208000000143 urethritis Diseases 0.000 claims 1
- 206010046494 urge incontinence Diseases 0.000 claims 1
- 230000002485 urinary effect Effects 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non 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
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/495—Heterocyclic 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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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
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- A—HUMAN NECESSITIES
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- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic 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
- C07D498/08—Bridged systems
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling 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.
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| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| CN106588785A (zh) * | 2016-12-02 | 2017-04-26 | 山东吉田香料股份有限公司 | 一种乙酰基吡嗪的制备方法 |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
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| SG11202011018PA (en) * | 2018-05-15 | 2020-12-30 | Bayer Ag | 1,3-thiazol-2-yl substituted benzamides for the treatment of diseases associated with nerve fiber sensitization |
| BR112021005334A2 (pt) | 2018-10-05 | 2021-06-15 | Shionogi & Co., Ltd. | medicamento para tratamento de tosse crônica |
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