ME00459B - Aril fuzirana azapoliciklična jedinjenja - Google Patents
Aril fuzirana azapoliciklična jedinjenjaInfo
- Publication number
- ME00459B ME00459B MEP-2008-702A MEP70208A ME00459B ME 00459 B ME00459 B ME 00459B ME P70208 A MEP70208 A ME P70208A ME 00459 B ME00459 B ME 00459B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- disease
- compound according
- disorder
- optionally
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract 19
- 125000003118 aryl group Chemical group 0.000 title claims 6
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052717 sulfur Chemical group 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- -1 hydroxy, nitro, amino Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- 206010012335 Dependence Diseases 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 4
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- 208000018737 Parkinson disease Diseases 0.000 claims 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 4
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 230000009529 traumatic brain injury Effects 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 3
- 241000208125 Nicotiana Species 0.000 claims 3
- 235000002637 Nicotiana tabacum Nutrition 0.000 claims 3
- 206010057852 Nicotine dependence Diseases 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 208000025569 Tobacco Use disease Diseases 0.000 claims 3
- 125000005605 benzo group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 206010003805 Autism Diseases 0.000 claims 2
- 208000020706 Autistic disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000032841 Bulimia Diseases 0.000 claims 2
- 206010006550 Bulimia nervosa Diseases 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 2
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 2
- 208000015943 Coeliac disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 206010013530 Diverticula Diseases 0.000 claims 2
- 206010013554 Diverticulum Diseases 0.000 claims 2
- 208000014094 Dystonic disease Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 206010019233 Headaches Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010020651 Hyperkinesia Diseases 0.000 claims 2
- 208000000269 Hyperkinesis Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 208000005314 Multi-Infarct Dementia Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010033799 Paralysis Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 206010039966 Senile dementia Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims 2
- 208000016620 Tourette disease Diseases 0.000 claims 2
- 208000025865 Ulcer Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 201000004810 Vascular dementia Diseases 0.000 claims 2
- 206010047139 Vasoconstriction Diseases 0.000 claims 2
- 208000005298 acute pain Diseases 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 208000022531 anorexia Diseases 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 229940125717 barbiturate Drugs 0.000 claims 2
- 229940049706 benzodiazepine Drugs 0.000 claims 2
- 125000003310 benzodiazepinyl group Chemical class N1N=C(C=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229960003920 cocaine Drugs 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 206010061428 decreased appetite Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 206010013932 dyslexia Diseases 0.000 claims 2
- 208000010118 dystonia Diseases 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 210000004211 gastric acid Anatomy 0.000 claims 2
- 231100000869 headache Toxicity 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 2
- 201000010901 lateral sclerosis Diseases 0.000 claims 2
- 208000005264 motor neuron disease Diseases 0.000 claims 2
- 229960002715 nicotine Drugs 0.000 claims 2
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 229940005483 opioid analgesics Drugs 0.000 claims 2
- 208000019906 panic disease Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000028591 pheochromocytoma Diseases 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 230000001148 spastic effect Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical group C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 2
- 235000019505 tobacco product Nutrition 0.000 claims 2
- 231100000397 ulcer Toxicity 0.000 claims 2
- 230000025033 vasoconstriction Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 229910014585 C2-Ce Inorganic materials 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000006311 Pyoderma Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 208000035127 classic pyoderma gangrenosum Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000005004 perfluoroethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 1
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- 150000003462 sulfoxides Chemical class 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/22—Bridged ring systems
- C07D221/24—Camphidines
-
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- 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
- A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
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- 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
- A61P25/14—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
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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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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- A61P25/24—Antidepressants
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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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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/22—Bridged ring systems
-
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Traži se zaštita za jedinjenja formule I i njihovefarmaceutski prihvatljive soli, gde R 1 , R 2 , R 3 i n su kao što je definisano u specifikaciji, intermedijari u sintezi datihjedinjenja, farmaceutski preparati koji sadrže ova jedinjenja i postupciza upotrebu datih jedinjenja u lečenju neuroloških i fiziološkihporemećaja.
Claims (15)
1. Jedinjenje formule:R1 je vodonik, (C1-C6)alkil, nekonjugovan (C3-C6)alkenil, benzil, XC(=O)R13 ili -CH2CH2-O-(C1-C4)alkil;R2 I R3 su odabrani nezavisno od vodonika, (C2-C6)alkenila, (C2-C6)alkinila, hidroksi, nitro, amino, halo, cijano, -SOq(C1-C6)alkila gde q je nula, jedan ili dva, (C1-C6)alkilamino-, [(C1-C6)alkil]2amino-, -CO2R4, -CONR5R6, -S02NR7R8, -C(=O)R13, -XC(=O)R13, aril-(C0-C3)alkil- ili aril-( C0-C3)alkil-O-, gde je dati aril odabran od fenila i naftila, heteroaril-( C0-C3)alkil- ili heteroaril-( C0-C3)alkil-O-, gde dati je heteroaril odabran od peto- do sedmo-članih aromatičnih prstenova koji sadrže od jedan do četiri heteroatoma odabranih od kiseonika, azota i sumpora i X2 (C0-C6)alkoksi-( C0-C6)alkil-, gde X2 je odsutan ili X2 je (C1-C6)alkilamino- ili [(C1-C6)alkil]2amino-, i gde (C0-C6)alkoksi-( C0-C6)alkil- deo datog X2(C0-C6)alkoksi-( C0-C6)alkila- sadrži bar jedan atom ugljenika, i gde od jedan do tri atoma ugljenika grupe (C0-C6)alkoksi-( C0-C6)alkil- može po izboru da bude zamenjen(o) atomom kiseonika, azota ili sumpora, pod uslovom da bilo koja dva takva heteroatoma moraju da budu razdvojena sa najmanje dva atoma ugljenika, i gde neka od alkil grupa datog (C0-C6)alkoksi-( C0-C6)alkila- može po izboru da bude supstituisan sa od dva do sedam atoma fluora, i gde jedan od atoma ugljenika svake od alkil grupa datog aril-(C0-C3)alkila- i heteroaril-( C0-C3) alkila- može po izboru da bude zamenjen atomom kiseonika, azota ili sumpora, i gde svaka od gorenavedenih aril i heteroaril grupa može po izboru da bude supstituisana sa jednim ili više supstituenata, preferentno od nijednog do dva supstituenta koji su nezavisno odabrani od (C1-C6)alkila koji su po izboru supstituisani sa od jedan do sedam atoma fluora, (C1-C6)alkoksi koji je po izboru supstituisan sa od dva do sedam atoma fluora, halo, (C2-C6)alkenil, (C2-Ce)alkinil, hidroksi, nitro, cijano, amino, (C1-C6)alkilamino, [(C1-C6)alkil]2amino-, -CO2R4, -CONR5R6, -S02NR7R8, -C(=O)R13 I -XC(0)R13; iliR2 I R3 zajedno sa atomima ugljenika na koji su vezane grade četvoro- do sedmo-člani monociklični ili deseto- do 14-člani biciklični, karbociklični prsten koji može da bude zasićen ili nezasićen, gde jedan do tri nekondenzovana atoma ugljenika datih monocikličnih prstena I od jedan do pet atoma ugljenika datih bicikličnih prstena koji nisu deo benzo prstenova prikazanog u formuli I, može da bude po izboru I nezavisno zamenjeno atomom azota, kiseonika ili sumpora i gde dati monociklični i biciklični prstenovi mogu po izbom da budu supstituisani sa jednim ili više supstituenata, preferentno od nijednog do dva supstituenta za monociklične prstenove i od nijednog do tri supstituenata za biciklične prstenove, koji su odabrani, nezavisno od (C1-C6)alkila po izbom supstitisanog sa jedan do sedam atoma fluora, (C1-C6)alkoksi; nitro, cijano, halo, (C2-C6)alkenil, (C2-C6)alkinil, hidroksi, amino, (C1-C6)alkilamino, [(C1-C6)alkil]2amino-, -CO2R4, -CONR5R6, -S02NR7R8, -C(=O)R13 I -XC(=O)R13;svaki R4, R5, R6, R7, R8 i R13 su odabrani, nezavisno od vodonika i (C1-C6)alkila iliR5 i R6 ili R7 i R8 zajedno sa azotom na koji su vezani, grade pirolidin, piperidin, morfolin, azetidin, piperazin, -N-(C1-C6)alkilpiperazin ili tiomorfolinski prsten ili tiomorfolinski prsten gde sumpor iz prstena je zamnjen sa sulfoksidom ili sulfonom; i svaki X je nezavisno (C1-C6)alkilen;pod uslovom da: (a) bar jedan od R1, R2 I R3 ne može da bude vodonik i (b) gde R2 i R3 su vodonik, R1 ne može da bude vodonik, metil, fenetil, ciklopropilmetil, n-propil, alkil ili 3-metil-2-butenil; i njegova farmaceutski prihvatljiva so.
2. Jedinjenje prema zahtevu 1, naznačeno time, što R2 I R3, zajedno sa benzo prstenom formule I, grade biciklični prstenasti sistem koji je odabran od sledećih: gde R10 I R17 su odabrani nezavisno od (CO-C6)alkoksi-(CO-C6)alkila gde ukupan broj atoma ugljenika ne prelazi šest i gde bilo koja alkil grupa po izboru može da bude supstituisana sa od jednim do sedam atoma fluora; nitro, cijano, halo, cijano, halo, amino, (C1-C6)alkilamino, [((C1-C6)alkil]2amino-, -CO2R4, -CONR5R6, -S02NR7R8, -C(=O)R13 i -XC(=O)R13, fenil i monociklični heteraoaril, gde dati heteroaril je odabran od peto do sedmo članih aromatičnih prstena koji sadrže od jedan do četiri heteroatoma odabranih od kiseonika, azota I sumpora I gde su R4, R5, R6, R7, R8 I R13 kao što je definisano u zahtevu 1.
3. Jedinjenje prema zahtevu 1, naznačeno time, što R2 I R3, ne formiraju zajedno sa benzo prstenom formule I, biciklični ili triciklilčni prstenasti sistem..
4. Jedinjenje prema zahtevu 1, naznačeno time, što jedan ili oba R2 I R3 su -C(=O)R13 gde R13 je (C1-C6)alkil.
5. Jedinjenje prema zahtevu 1, naznačeno time, što jedan od R2 I R3 je -COR13 gde R13 je (C1-C6)alkil ili (C1-C3)alkil koji je po izboru supstituisan sa od jedan do sedam atoma fluora.
6. Jedinjenje prema zahtevu 1, naznačeno time, što jedan od R2 I R3 je CF3, fluoro, cijano ili C2F5.
7. Jedinjenje prema Zahtevu 1, naznačeno time, što je to 5, 8, 14-triazatetraciklo[10. 3. 1. 02,11. 04,9]heksadeka-2(l l), 3, 5, 7, 9-pentaen; ili njegova farmaceutski prihvatljiva so.
8. Farmaceutski preparat za upotrebu u smanjenju nikotinske zavisnosti ili smanjenju upotrebe duvana kod sisara, koji obuhvata količinu jedinjenja prema zahtevu 1 i farmaceutski prihvatljiv nosač.
9. Upotreba jedinjenja zahtevu 1 za dobijanje leka za smanjenje nikotinske zavisnosti ili kao pomoć za prestanak ili smanjenje upotrebe duvana kod sisara.
10. Upotreba jedinjenja zahtevu 1 za dobijanje leka za lečenje poremećaja ili stanja odabranog od inflamatornog obolenja creva (uključujući ali ne ograničavajući se na ulcerativni kolitis, pioderma gangrenoza i Crohn-ovo obolenje), sindrom nadraženih creva, spastična distonija, hronični bol, akutni bol, celijakija, inflamacije ielalne divertikule, vazokonstrukcije, anksioznosti, paničnog poremećaja, depresije, bipolamog poremećaja, autizam, poremećaji spavanja, poremećaja posle preletanja više vremenskih zona (Jet lag), amilotropne lateralne skleroze (ALS), kognitivne disfunkcije, hipertenzijae, bulimije, anoreksije, gojaznosti, srčane aritmije, hipersekrecije stomačne kiseline, čireva, feohromocitoma, progresivne supramuksulame paralize, hemijske zavisnosti I zloupotrebe (na primer, zavisnosti od ili zloupotreba nikotina (i/ili duvanskih proizvoda), alkohola, benzodiazepina, barbiturata, opoida ili kokaina), glavobolje, šloga, traumatske povrede mozga (TBI), opsesivno-kompulsivni poremećaj (OCD), psihoze, Huntington-ovog obolenja, tardivne diskinezije, hiperkinezije, disleksije, šizofrenije, multi-infarktne demencije, kongentivno slabljenje zbog starenja, epilepsije, senilne demencije Alzheime-ovog tipa (AD), Parkinson-ovog obolenja (PD), poremećaj hiperaktivnog deficita pažnje (ADHD) i Tourette'ov sindrom kod sisara.
11. Jedinjenje formule naznačeno time, što R2 i R3 su kao što je definisano u zahtevu 1; P’ je COOR16 gde R16 je alil, 2. 2. 2-trifluoroetil ili (C1-C6)alkil; -C(=O)NR5R6 gde R5 i R6 su kao što je definisano u zahtevu 2; -C(=O)H, -C(=O)(C1-C6)alkil gde alkil grupa može po izboru da bude supstituisana sa od 1 do 3 halo atoma, benzil ili t-butoksikarbonil (t-Boc).
12. Jedinjenje prema zahtevu 11, naznačeno time, što je formule R2 I R3 su nezavisno odabrani od vodonika, (C1-C6)alkila po izboru supstituisan sa jedan do sedam atoma fluora; -C(=O)(C1-C6)alkil, cijano, hidroksi, nitro, amino -0(C1-C6)alkil i halo.
13. Upotreba jedinjenja formule Ili njegove farmaceutski prihvatljive soli, za proizvodnju leka za smanjenje nikotinske zavisnosti ili kao pomoć za prestanak ili smanjenje upotrebe duvana.
14. Upotreba jedinejna formule ili njegove farmaceutski prihvatljive soli za proizvodnju leka za lečenje poremećaja ili stanja odabranog od od inflamatomog obolenja creva (uključujući ali ne ograničavajući se na ulcerativni kolitis, pioderma gangrenoza i Crohn-ovo obolenje), sindrom nadraženih creva, spastična distonija, hronični bol, akutni bol, celijakija, inflamacije ielalne divertikule, vazokonstrukcije, anksioznosti, paničnog poremećaja, depresije, bipolamog poremećaja, autizam, poremećaji spavanja, poremećaja posle preletanja više vremenskih zona (Jet lag), amilotropne lateralne skleroze (ALS), kognitivne disfunkcije, hipertenzijae, bulimije, anoreksije, gojaznosti, srčane aritmije, hipersekrecije stomačne kiseline, čireva, feohromocitoma, progresivne supramuksularne paralize, hemijske zavisnosti I zloupotrebe (na primer, zavisnosti od ili zloupotreba nikotina (i/ili duvanskih proizvoda), alkohola, benzodiazepina, barbiturata, opoida ili kokaina), glavobolje, šloga, traumatske povrede mozga (TBI), opsesivno-kompulsivni poremećaj (OCD), psihoze, Huntington-ovog obolenja, tardivne diskinezije, hiperkinezije, disleksije, šizofrenije, multi-infarktne demencije, kongentivno slabljenje zbog starenja, epilepsije, senilne demencije Alzheime-ovog tipa (AD), Parkinson-ovog obolenja (PD), poremećaj hiperaktivnog deficita pažnje (ADHD) I Tourette'ov sindrom kod sisara.
15. Jedinjenje ili njegova farmaceutski prihvatljiva so, kao što je definisano u jednom od zahteva 1 do 7 za upotrebu u medicini.
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| PCT/IB1998/001813 WO1999035131A1 (en) | 1997-12-31 | 1998-11-13 | Aryl fused azapolycyclic compounds |
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| ME00459B true ME00459B (me) | 2011-10-10 |
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| MEP-2008-702A ME00459B (me) | 1997-12-31 | 1998-11-13 | Aril fuzirana azapoliciklična jedinjenja |
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