HRP20140724T1 - Modulatori masnih kiselina amid hidrolaze - Google Patents
Modulatori masnih kiselina amid hidrolaze Download PDFInfo
- Publication number
- HRP20140724T1 HRP20140724T1 HRP20140724AT HRP20140724T HRP20140724T1 HR P20140724 T1 HRP20140724 T1 HR P20140724T1 HR P20140724A T HRP20140724A T HR P20140724AT HR P20140724 T HRP20140724 T HR P20140724T HR P20140724 T1 HRP20140724 T1 HR P20140724T1
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- disease
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- pharmaceutically acceptable
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- 102100029111 Fatty-acid amide hydrolase 1 Human genes 0.000 title 1
- 108010046094 fatty-acid amide hydrolase Proteins 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 238000002360 preparation method Methods 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- YWGYNGCRVZLMCS-UHFFFAOYSA-N n-(4-chloropyridin-3-yl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]piperazine-1-carboxamide Chemical group C1=C2OC(F)(F)OC2=CC=C1CN(CC1)CCN1C(=O)NC1=CN=CC=C1Cl YWGYNGCRVZLMCS-UHFFFAOYSA-N 0.000 claims 5
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000016285 Movement disease Diseases 0.000 claims 2
- 206010029240 Neuritis Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 235000014632 disordered eating Nutrition 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000018652 Closed Head injury Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 102100027297 Fatty acid 2-hydroxylase Human genes 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000003577 HIV wasting syndrome Diseases 0.000 claims 1
- 101000937693 Homo sapiens Fatty acid 2-hydroxylase Proteins 0.000 claims 1
- 101000918494 Homo sapiens Fatty-acid amide hydrolase 1 Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010021333 Ileus paralytic Diseases 0.000 claims 1
- 206010062016 Immunosuppression Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 201000005081 Intestinal Pseudo-Obstruction Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028813 Nausea Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000014060 Niemann-Pick disease Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 201000001880 Sexual dysfunction Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 208000028004 allergic respiratory disease Diseases 0.000 claims 1
- 201000004982 autoimmune uveitis Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000037149 energy metabolism Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 230000013632 homeostatic process Effects 0.000 claims 1
- 238000005984 hydrogenation reaction Methods 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 claims 1
- 208000001286 intracranial vasospasm Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000008693 nausea Effects 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 201000007620 paralytic ileus Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000009881 secretory diarrhea Diseases 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 208000023516 stroke disease Diseases 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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 chain containing hetero atoms as chain links
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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Claims (12)
1. Spoj naznačen time da je 4-(2,2-difluoro-benzo[1,3]dioksol-5-ilmetil)-piperazin-1-karboksilna kiselina (4- kloro-piridin-3-il)-amid ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski prihvatljiva sol prema zahtjevu 1, naznačena time da je spomenuta sol hidrokloridna sol 4-(2,2-difluoro-benzo[1,3]dioksol-5-ilmetil)-piperazin-1-karboksilna kiselina(4-kloro-piridin-3-il)-amida.
3. Farmaceutski prihvatljiva sol prema zahtjevu 2, naznačena time da je hidrokloridna sol bis-hidroklorid.
4. Farmaceutski pripravak, naznačen time da sadrži:
(a) terapeutski efikasnu količinu bar jednog od 4-(2,2-difluorobenzo[1,3]dioksol-5-ilmetil)-piperazin-1-karboksilna kiselina(4-kloro-piridin-3-il)-amid i njegova farmaceutski prihvatljiva sol; i
(b) farmaceutski prihvatljivi ekscipijent.
5. Farmaceutski pripravak prema zahtjevu 4, naznačen time da sadrži: terapeutski efikasnu količinu 4-(2,2-difluoro-benzo[1,3]dioksol-5-ilmetil)-piperazin-1-karboksilna kiselina(4-kloro-piridin-3-il)-amida ili njegove farmaceutski prihvatljive soli.
6. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 3 ili pripravak prema zahtjevu 4 ili 5, naznačen time da je za upotrebu u terapiji.
7. Spoj ili pripravak za upotrebu prema zahtjevu 6, u postupku liječenja subjekta koji pati ili mu je dijagnosticirana bolest ili poremećaj, ili medicinsko stanje posredovano FAAH aktivnošću, naznačen time da je bolest, poremećaj ili medicinsko stanje izabrano iz grupe koju čine: anksioznost, depresija, bol, poremećaji spavanja, poremećaji ishrane, upala, poremećaji kretanja, HIV sindrom propadanja, zatvorena ozljeda glave, kap, poremećaj učenja i pamćenja, Alzheimerova bolest, epilepsija, Touretteov sindrom, Niemann-Pickova bolest, Parkinsonova bolest, Huntingtonova horeja, optički neuritis, autoimuni uveitis, odvikavanje od droga, mučnina, povraćanje, seksualna disfunkcija, posttraumatski stresni poremećaj, moždani vazospazam, glaukom, sindrom iritabilnog crijeva, upalna bolest crijeva, imunosupresija, bolest gastroezofagealnog refluksa, paralitički ileus, sekrecijska dijareja, čir želuca, reumatoidni artritis, hipertenzija, rak, hepatitis, alergijska bolest dišnih putova, autoimuni dijabetes, intraktabilni pruritis, neuritis, dijabetes, metabolički sindrom i osteoporoza.
8. Spoj ili pripravak za upotrebu prema zahtjevu 7, naznačen time da je bolest, poremećaj ili medicinsko stanje bol ili upala.
9. Spoj ili pripravak za upotrebu prema zahtjevu 7, naznačen time da je bolest, poremećaj ili medicinsko stanje anksioznost, poremećaj spavanja, poremećaj ishrane, ili poremećaj kretanja.
10. Spoj ili pripravak za upotrebu prema zahtjevu 7, naznačen time da je bolest, poremećaj ili medicinsko stanje multipla skleroza.
11. Spoj ili pripravak za upotrebu prema zahtjevu 6, naznačen time da za postupak liječenja energetskog metabolizma ili homeostaze kosti.
12. Postupak za sintezu 4-(2,2-difluoro-benzo[1,3]dioksol-5-ilmetil)-piperazin-1-karboksilna kiselina(4-kloro-piridin-3-il)-amida pomoću 2,2-difluorobenzo[1,3]dioksol-5-karbaldehida i piperazina u jednostupanjskoj reakciji hidrogenizacije.
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US33052210P | 2010-05-03 | 2010-05-03 | |
PCT/US2011/034755 WO2011139951A1 (en) | 2010-05-03 | 2011-05-02 | Modulators of fatty acid amide hydrolase |
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WO2017066747A1 (en) * | 2015-10-16 | 2017-04-20 | Scythian Biosciences Inc. | Methods and compositions for treating gastrointestinal inflammation |
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