ME02437B - Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora - Google Patents
Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptoraInfo
- Publication number
- ME02437B ME02437B MEP-2016-135A MEP13516A ME02437B ME 02437 B ME02437 B ME 02437B ME P13516 A MEP13516 A ME P13516A ME 02437 B ME02437 B ME 02437B
- Authority
- ME
- Montenegro
- Prior art keywords
- triazol
- pyrrol
- fenil
- karbonyl
- fluoro
- Prior art date
Links
- QFCMBRXRVQRSSF-UHFFFAOYSA-N 1,2,3,3a,4,5,6,6a-octahydropyrrolo[3,4-c]pyrrole Chemical class C1NCC2CNCC21 QFCMBRXRVQRSSF-UHFFFAOYSA-N 0.000 title claims 3
- 108050000742 Orexin Receptor Proteins 0.000 title claims 2
- 102000008834 Orexin receptor Human genes 0.000 title claims 2
- -1 -C1-4 alkoxy Chemical group 0.000 claims 286
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 255
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 163
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 81
- 150000005829 chemical entities Chemical class 0.000 claims 52
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 38
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 36
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 21
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 20
- 125000005843 halogen group Chemical group 0.000 claims 19
- XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical group N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims 18
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 16
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 13
- 239000000546 pharmaceutical excipient Substances 0.000 claims 10
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 10
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- MUDSDYNRBDKLGK-UHFFFAOYSA-N 4-methylquinoline Chemical group C1=CC=C2C(C)=CC=NC2=C1 MUDSDYNRBDKLGK-UHFFFAOYSA-N 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- NIHNNTQXNPWCJQ-UHFFFAOYSA-N fluorene Chemical compound C1=CC=C2CC3=CC=CC=C3C2=C1 NIHNNTQXNPWCJQ-UHFFFAOYSA-N 0.000 claims 7
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 7
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 125000004262 quinoxalin-2-yl group Chemical group [H]C1=NC2=C([H])C([H])=C([H])C([H])=C2N=C1* 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 5
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims 5
- SQOCEMCKYDVLMM-UHFFFAOYSA-N [2-(4,6-dimethylpyrimidin-2-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-[2-fluoro-6-(triazol-2-yl)phenyl]methanone Chemical group CC1=CC(C)=NC(N2CC3CN(CC3C2)C(=O)C=2C(=CC=CC=2F)N2N=CC=N2)=N1 SQOCEMCKYDVLMM-UHFFFAOYSA-N 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 5
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 4
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 4
- YIQVNKFWTSLVSA-UHFFFAOYSA-N 2-(trifluoromethyl)quinoxaline Chemical group C1=CC=CC2=NC(C(F)(F)F)=CN=C21 YIQVNKFWTSLVSA-UHFFFAOYSA-N 0.000 claims 4
- QWIDYOLZFAQBOB-UHFFFAOYSA-N 2-methyl-1h-pyrimidin-6-one Chemical compound CC1=NC=CC(=O)N1 QWIDYOLZFAQBOB-UHFFFAOYSA-N 0.000 claims 4
- HBAPRWLCCBZDNA-UHFFFAOYSA-N 4-methyl-6,7-dihydro-5h-cyclopenta[d]pyrimidine Chemical group CC1=NC=NC2=C1CCC2 HBAPRWLCCBZDNA-UHFFFAOYSA-N 0.000 claims 4
- ULXUMMWTPGKPRC-UHFFFAOYSA-N [2-(4,6-dimethylpyrimidin-2-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-[4-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical group N1=CC=NN1C1=CC(OC)=CC=C1C(=O)N(CC1C2)CC1CN2C1=NC(C)=CC(C)=N1 ULXUMMWTPGKPRC-UHFFFAOYSA-N 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- WCZVZNOTHYJIEI-UHFFFAOYSA-N cinnoline Chemical compound N1=NC=CC2=CC=CC=C21 WCZVZNOTHYJIEI-UHFFFAOYSA-N 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 4
- BGSRFMFTXMPTSC-UHFFFAOYSA-N 6-fluoro-1,3-benzothiazole Chemical group FC1=CC=C2N=CSC2=C1 BGSRFMFTXMPTSC-UHFFFAOYSA-N 0.000 claims 3
- AHOIGFLSEXUWNV-UHFFFAOYSA-N 6-methoxy-1,3-benzothiazole Chemical group COC1=CC=C2N=CSC2=C1 AHOIGFLSEXUWNV-UHFFFAOYSA-N 0.000 claims 3
- IVKILQAPNDCUNJ-UHFFFAOYSA-N 6-methyl-1,3-benzothiazole Chemical group CC1=CC=C2N=CSC2=C1 IVKILQAPNDCUNJ-UHFFFAOYSA-N 0.000 claims 3
- LHRIUKSRPHFASO-UHFFFAOYSA-N 6-methyl-1h-pyrimidin-4-one Chemical compound CC1=CC(=O)N=CN1 LHRIUKSRPHFASO-UHFFFAOYSA-N 0.000 claims 3
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical group C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims 3
- YEBKRKAIWOXVDB-UHFFFAOYSA-N n,n,6-trimethylpyrimidin-4-amine Chemical group CN(C)C1=CC(C)=NC=N1 YEBKRKAIWOXVDB-UHFFFAOYSA-N 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 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
- 206010002383 Angina Pectoris Diseases 0.000 claims 2
- 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 2
- 208000001871 Tachycardia Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 206010022437 insomnia Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003230 pyrimidines Chemical group 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 230000006794 tachycardia Effects 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical group C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 1
- 125000001401 1,2,4-triazol-4-yl group Chemical group N=1N=C([H])N([*])C=1[H] 0.000 claims 1
- 125000001414 1,2,4-triazol-5-yl group Chemical group [H]N1N=C([H])N=C1[*] 0.000 claims 1
- 125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical compound C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 claims 1
- CVEVUCIKZYPPRJ-UHFFFAOYSA-N 1h-indol-7-yl-(2-quinoxalin-2-yl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl)methanone Chemical compound C1C2CN(C=3N=C4C=CC=CC4=NC=3)CC2CN1C(=O)C1=CC=CC2=C1NC=C2 CVEVUCIKZYPPRJ-UHFFFAOYSA-N 0.000 claims 1
- CIVMONDHQUDUQU-UHFFFAOYSA-N 2-[5-[2-fluoro-6-(triazol-2-yl)benzoyl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl]-n,n-dimethyl-4-(trifluoromethyl)pyrimidine-5-carboxamide Chemical compound N1=C(C(F)(F)F)C(C(=O)N(C)C)=CN=C1N1CC2CN(C(=O)C=3C(=CC=CC=3F)N3N=CC=N3)CC2C1 CIVMONDHQUDUQU-UHFFFAOYSA-N 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- OQHVVOYDDRBQRI-UHFFFAOYSA-N 4-(trifluoromethyl)pyrimidine-5-carboxylic acid Chemical compound OC(=O)C1=CN=CN=C1C(F)(F)F OQHVVOYDDRBQRI-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- UQRONKZLYKUEMO-UHFFFAOYSA-N 4-methyl-1-(2,4,6-trimethylphenyl)pent-4-en-2-one Chemical group CC(=C)CC(=O)Cc1c(C)cc(C)cc1C UQRONKZLYKUEMO-UHFFFAOYSA-N 0.000 claims 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000006820 Arthralgia Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010012218 Delirium Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000000059 Dyspnea Diseases 0.000 claims 1
- 206010013975 Dyspnoeas Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 208000010496 Heart Arrest Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000001456 Jet Lag Syndrome Diseases 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 102000002512 Orexin Human genes 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Natural products C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 206010046996 Varicose vein Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 239000004305 biphenyl Substances 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 206010007776 catatonia Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 201000001883 cholelithiasis Diseases 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000001130 gallstones Diseases 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000033915 jet lag type circadian rhythm sleep disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- ROKXRIZJISDXOL-UHFFFAOYSA-N methyl 2-[5-[2-fluoro-6-(triazol-2-yl)benzoyl]-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-2-yl]-4-(trifluoromethyl)pyrimidine-5-carboxylate Chemical compound N1=C(C(F)(F)F)C(C(=O)OC)=CN=C1N1CC2CN(C(=O)C=3C(=CC=CC=3F)N3N=CC=N3)CC2C1 ROKXRIZJISDXOL-UHFFFAOYSA-N 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 108060005714 orexin Proteins 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000013220 shortness of breath Diseases 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- 208000022925 sleep disturbance Diseases 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 150000003852 triazoles Chemical group 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 208000027185 varicose disease Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/40—Heterocyclic 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
- A61K31/407—Heterocyclic 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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
- A61K31/41—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
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/41—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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic 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
- A61K31/435—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
- A61K31/435—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
- A61K31/4709—Non-condensed quinolines 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25450909P | 2009-10-23 | 2009-10-23 | |
| EP10773477.4A EP2491038B1 (en) | 2009-10-23 | 2010-10-21 | Disubstituted octahy - dropyrrolo [3,4-c]pyrroles as orexin receptor modulators |
| PCT/US2010/053606 WO2011050198A1 (en) | 2009-10-23 | 2010-10-21 | Disubstituted octahy - dropyrrolo [3,4-c] pyrroles as orexin receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02437B true ME02437B (me) | 2016-09-20 |
Family
ID=43385633
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-135A ME02437B (me) | 2009-10-23 | 2010-10-21 | Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora |
| MEP-2019-199A ME03452B (me) | 2009-10-23 | 2010-10-21 | Disupstituisani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2019-199A ME03452B (me) | 2009-10-23 | 2010-10-21 | Disupstituisani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora |
Country Status (38)
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2735411T3 (es) | 2009-10-23 | 2019-12-18 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina |
| US9586962B2 (en) | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
| US8501768B2 (en) * | 2011-05-17 | 2013-08-06 | Hoffmann-La Roche Inc. | Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds |
| EP2776430B1 (en) | 2011-11-08 | 2016-03-16 | Actelion Pharmaceuticals Ltd. | 2- (1,2,3-triazol-2-yl) benzamide and 3-(1,2,3-triazol-2-yl) picolinamide derivatives as orexin receptor antagonists |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| JP6346862B2 (ja) | 2012-02-07 | 2018-06-20 | エオラス セラピューティクス， インコーポレイテッド | オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン |
| KR101689093B1 (ko) | 2012-06-04 | 2016-12-22 | 액테리온 파마슈티칼 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| CA2882132C (en) * | 2012-08-16 | 2021-07-06 | The Scripps Research Institute | Kappa opioid ligands |
| WO2014057435A1 (en) | 2012-10-10 | 2014-04-17 | Actelion Pharmaceuticals Ltd | Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero )aryl)-pyrrolidin-1-yl]-methanone derivatives |
| CN103012293A (zh) * | 2012-12-13 | 2013-04-03 | 同济大学 | 一种抗失眠药物mk-4305中间体的合成方法 |
| WO2014141065A1 (en) | 2013-03-12 | 2014-09-18 | Actelion Pharmaceuticals Ltd | Azetidine amide derivatives as orexin receptor antagonists |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| WO2015003002A1 (en) * | 2013-07-03 | 2015-01-08 | Abide Therapeutics, Inc. | Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof |
| MY179605A (en) | 2013-12-04 | 2020-11-11 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
| WO2016020403A1 (en) * | 2014-08-04 | 2016-02-11 | Sandoz Ag | Preparation of a benzoic acid derivative and its use for the preparation of suvorexant |
| ES2901418T3 (es) | 2014-08-13 | 2022-03-22 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores del receptor de orexina |
| US9611262B2 (en) | 2014-09-11 | 2017-04-04 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| US10196383B2 (en) | 2015-07-17 | 2019-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| US10370380B2 (en) | 2015-11-23 | 2019-08-06 | Sunshine Lake Pharma Co., Ltd. | Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof |
| WO2017088731A1 (zh) * | 2015-11-24 | 2017-06-01 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| SI3414241T1 (sl) | 2016-02-12 | 2022-10-28 | Astrazeneca Ab | Halo-substituitani piperidini kot modulatorji receptorja oreksina |
| CA2960253A1 (en) | 2016-03-10 | 2017-09-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| WO2017197192A1 (en) | 2016-05-12 | 2017-11-16 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| CN105949203B (zh) * | 2016-05-24 | 2018-07-13 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途 |
| CN107759620B (zh) * | 2016-08-16 | 2021-11-12 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其使用方法和用途 |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| CN108299437B (zh) * | 2017-01-13 | 2022-07-08 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| GB201702174D0 (en) * | 2017-02-09 | 2017-03-29 | Benevolentai Bio Ltd | Orexin receptor antagonists |
| CA3059394C (en) | 2017-05-03 | 2023-09-12 | Idorsia Pharmaceuticals Ltd | Preparation of 2-([1,2,3]triazol-2-yl)-benzoic acid derivatives |
| GB201707499D0 (en) * | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
| GB201707504D0 (en) * | 2017-05-10 | 2017-06-21 | Benevolentai Bio Ltd | Orexin receptor antagonists |
| PE20200664A1 (es) | 2017-08-29 | 2020-06-11 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso |
| PE20200665A1 (es) | 2017-08-29 | 2020-06-11 | Lundbeck La Jolla Research Center Inc | Compuestos espirociclicos y sus metodos de preparacion y uso |
| US11324724B2 (en) | 2017-09-28 | 2022-05-10 | Boehringer Ingelheim International Gmbh | N-(2,2-difluoroethyl)-N-[(pyrimidinylamino)propanyl]arylcarboxamides |
| CN109988171A (zh) * | 2017-12-29 | 2019-07-09 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| CN109988169B (zh) * | 2017-12-29 | 2022-02-01 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| CN109988170B (zh) * | 2017-12-29 | 2022-04-26 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物及其用途 |
| GB201809295D0 (en) | 2018-06-06 | 2018-07-25 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| US20210169883A1 (en) * | 2018-07-27 | 2021-06-10 | Icahn School Of Medicine At Mount Sinai | Method of treating aggression with orexin receptor antagonists |
| WO2020100011A1 (en) * | 2018-11-14 | 2020-05-22 | Janssen Pharmaceutica Nv | Improved synthetic methods of making fused heterocyclic compounds as orexin receptor modulators |
| GB201818750D0 (en) | 2018-11-16 | 2019-01-02 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| CN112142713A (zh) * | 2019-06-27 | 2020-12-29 | 山东润博生物科技有限公司 | 一种咪草烟的合成方法 |
| JP7672386B2 (ja) * | 2019-08-07 | 2025-05-07 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節薬としての（２ｈ－１，２，３－トリアゾール－２－イル）フェニル化合物の改善された合成方法 |
| CN112876479B (zh) * | 2019-11-29 | 2022-07-26 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物的晶型 |
| WO2021104294A1 (en) * | 2019-11-29 | 2021-06-03 | Sunshine Lake Pharma Co., Ltd. | CRYSTAL FORMS OF OCTAHYDROPYRROLO [3,4-c] PYRROLE DERIVATIVES |
| CN112876481B (zh) * | 2019-11-29 | 2022-07-26 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物的晶型 |
| CN112876478B (zh) * | 2019-11-29 | 2022-07-26 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物的晶型 |
| CN112876480B (zh) * | 2019-11-29 | 2022-07-26 | 广东东阳光药业有限公司 | 八氢吡咯并[3,4-c]吡咯衍生物的晶型 |
| WO2022122009A1 (zh) * | 2020-12-11 | 2022-06-16 | 苏州晶云药物科技股份有限公司 | 吡咯类衍生化合物的晶型及其制备方法 |
| WO2022194122A1 (zh) * | 2021-03-16 | 2022-09-22 | 上海翰森生物医药科技有限公司 | 含氮杂环的多环化合物及其制备方法和应用 |
| CN114063673B (zh) * | 2021-11-09 | 2023-03-03 | 万华化学集团股份有限公司 | 一种反应釜温度控制方法、系统及存储介质 |
| CN116217593B (zh) * | 2021-12-02 | 2025-05-09 | 江苏恩华药业股份有限公司 | 一种八氢吡咯并[3,4-c]吡咯甲基酮衍生物及其应用 |
| WO2023163964A1 (en) | 2022-02-24 | 2023-08-31 | Teva Czech Industries S.R.O. | Solid state forms of seltorexant |
| WO2023180556A1 (en) | 2022-03-24 | 2023-09-28 | Janssen Pharmaceutica Nv | Methods for treating agitation in subjects with mild cognitive impairment or major neurocognition disorder |
| IL318368A (en) * | 2022-07-15 | 2025-03-01 | Biogen Ma Inc | Amofamyl-binding protein inhibitors and their uses |
| KR20250065855A (ko) * | 2022-09-14 | 2025-05-13 | 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 | 질소 함유 헤테로고리의 다환식 화합물의 유리 염기 결정형 및 이의 제조 방법 |
| CN120699043A (zh) * | 2022-11-23 | 2025-09-26 | 江苏恩华药业股份有限公司 | 一种二取代八氢吡咯并[3,4-c]吡咯甲基酮衍生物及其应用 |
| WO2024125395A1 (zh) * | 2022-12-12 | 2024-06-20 | 江苏恩华药业股份有限公司 | 一种取代四氢环戊基[c]吡咯衍生物、制备方法、中间体及其应用 |
| WO2024189472A1 (en) | 2023-03-14 | 2024-09-19 | Janssen Pharmaceutica Nv | Improved synthetic methods of making substituted pyrimidine intermediates for synthesis of orexin receptor modulators |
| WO2025003991A1 (en) | 2023-06-29 | 2025-01-02 | Janssen Pharmaceutica Nv | Method of treating depression using seltorexant |
| CN120383601A (zh) * | 2024-01-29 | 2025-07-29 | 成都康弘药业集团股份有限公司 | 食欲素受体调节剂及其制备方法和用途 |
| WO2025242852A1 (en) | 2024-05-24 | 2025-11-27 | Janssen Pharmaceutica Nv | Seltorexant for use in treating major depressive disorder with insomnia symptoms |
| CN118580243B (zh) * | 2024-08-07 | 2025-01-03 | 艾斯拓康生物医药(天津)有限公司 | 一类含氮并环化合物及其制备方法和应用 |
| CN119039301B (zh) * | 2024-10-31 | 2025-09-02 | 江苏豪森药业集团有限公司 | 一种含氮杂环的多环化合物晶型ⅰ的制备方法 |
Family Cites Families (152)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7503310A (nl) | 1975-03-20 | 1976-09-22 | Philips Nv | Verbindingen met antidepressieve werking. |
| GB1526331A (en) | 1976-01-14 | 1978-09-27 | Kefalas As | Phthalanes |
| EP0871628A1 (en) | 1995-06-06 | 1998-10-21 | Abbott Laboratories | Quinolizinone type compounds |
| GB9519563D0 (en) | 1995-09-26 | 1995-11-29 | Merck Sharp & Dohme | Therapeutic agents |
| AU3555200A (en) | 1999-03-17 | 2000-10-04 | F. Hoffmann-La Roche Ag | Oxazolone derivatives and their use as alpha-1 adrenoreceptor modulators |
| US6375897B1 (en) | 2000-02-14 | 2002-04-23 | Ansys Technologies, Inc. | Urine collection cup |
| MY145722A (en) | 2000-04-27 | 2012-03-30 | Abbott Lab | Diazabicyclic central nervous system active agents |
| US6809105B2 (en) | 2000-04-27 | 2004-10-26 | Abbott Laboratories | Diazabicyclic central nervous system active agents |
| CA2408343A1 (en) | 2000-05-11 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | N-acyltetrahydroisoquinoline derivatives |
| SE0100326D0 (sv) | 2001-02-02 | 2001-02-02 | Astrazeneca Ab | New compounds |
| WO2002070527A1 (en) | 2001-03-02 | 2002-09-12 | Akzo Nobel N.V. | Mass-selective purification of organometallics |
| WO2002070523A1 (en) | 2001-03-07 | 2002-09-12 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| WO2003002561A1 (en) | 2001-06-28 | 2003-01-09 | Smithkline Beecham P.L.C. | N-aroyl cyclic amine derivatives as orexin receptor antagonists |
| US6455722B1 (en) | 2001-06-29 | 2002-09-24 | Pabu Services, Inc. | Process for the production of pentaerythritol phosphate alcohol |
| GB2383315B (en) | 2001-12-18 | 2005-04-06 | Christopher Donald Clarke | Vehicle imaging system |
| GB0130341D0 (en) | 2001-12-19 | 2002-02-06 | Smithkline Beecham Plc | Compounds |
| DE10226943A1 (de) | 2002-06-17 | 2004-01-08 | Bayer Ag | Phenylaminopyrimidine und ihre Verwendung |
| NZ538029A (en) | 2002-07-09 | 2006-08-31 | Actelion Pharmaceuticals Ltd | 7,8,9,10-tetrahydro-6H-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-b]-quinazolinone derivatives |
| JP4528125B2 (ja) | 2002-10-11 | 2010-08-18 | アクテリオン ファーマシューティカルズ リミテッド | スルホニルアミノ−酢酸誘導体 |
| GB0225944D0 (en) | 2002-11-06 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| DE602004021786D1 (de) | 2003-03-26 | 2009-08-13 | Actelion Pharmaceuticals Ltd | Tetrahydroisochinolylacetamidderivate zur verwendung als orexinrezeptorantagonisten |
| JP2007523846A (ja) | 2003-04-28 | 2007-08-23 | アクテリオン ファマシューティカルズ リミテッド | キノキサリノン誘導体 |
| US20040242641A1 (en) | 2003-05-27 | 2004-12-02 | Buckley Michael J. | (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane is an effective analgesic agent |
| WO2005005439A1 (en) | 2003-07-09 | 2005-01-20 | Suven Life Sciences Limited | Benzothiazino indoles |
| TW200507850A (en) | 2003-07-25 | 2005-03-01 | Kyowa Hakko Kogyo Kk | Pharmaceutical composition |
| WO2005023231A1 (en) | 2003-09-10 | 2005-03-17 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Polypyrimidine tract binding protein promotes insulin secretory granule biogenesis |
| US7399765B2 (en) | 2003-09-19 | 2008-07-15 | Abbott Laboratories | Substituted diazabicycloalkane derivatives |
| US20050065178A1 (en) | 2003-09-19 | 2005-03-24 | Anwer Basha | Substituted diazabicycloakane derivatives |
| ES2515092T3 (es) | 2003-12-11 | 2014-10-29 | Sunovion Pharmaceuticals Inc. | Combinación de un sedante y un modulador neurotransmisor y métodos de mejorar la calidad del sueño y de tratar la depresión |
| HUP0400405A3 (en) | 2004-02-10 | 2009-03-30 | Sanofi Synthelabo | Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates |
| KR100848747B1 (ko) | 2004-03-01 | 2008-07-25 | 액테리온 파마슈티칼 리미티드 | 치환된 1,2,3,4-테트라하이드로이소퀴놀린 유도체 |
| US7435830B2 (en) | 2004-03-03 | 2008-10-14 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| US7435831B2 (en) | 2004-03-03 | 2008-10-14 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| US7226931B2 (en) | 2004-07-22 | 2007-06-05 | Cumbre Pharmaceuticals Inc. | (R/S) rifamycin derivatives, their preparations and pharmaceutical compositions |
| JP2008507543A (ja) | 2004-07-22 | 2008-03-13 | グラクソ グループ リミテッド | 抗細菌剤 |
| FR2874011B1 (fr) | 2004-08-03 | 2007-06-15 | Sanofi Synthelabo | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| CA2579227A1 (en) | 2004-11-04 | 2006-05-18 | Neurogen Corporation | Arylalkyl ureas as cb1 antagonists |
| WO2006056848A1 (en) | 2004-11-24 | 2006-06-01 | Pfizer Limited | Octahydropyrrolo[3,4-c]pyrrole derivatives |
| DE102004061344A1 (de) | 2004-12-20 | 2006-07-06 | Siemens Ag | Verfahren zur sicheren Auslegung eines Systems, zugehörige Systemkomponente und Software |
| WO2006124897A2 (en) | 2005-05-13 | 2006-11-23 | Lexicon Genetics Incorporated | Methods and compositions for improving cognition |
| ES2434467T3 (es) | 2005-05-13 | 2013-12-16 | Lexicon Pharmaceuticals, Inc. | Compuestos multicíclicos y métodos para su uso |
| GB0510204D0 (en) | 2005-05-19 | 2005-06-22 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| US20080175795A1 (en) | 2005-06-30 | 2008-07-24 | Bexel Pharmaceuticals, Inc. | Novel derivatives of amino acids for treatment of obesity and related disorders |
| GB0514018D0 (en) | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
| EP1922071A2 (en) | 2005-08-26 | 2008-05-21 | Merck & Co., Inc. | Diazaspirodecane orexin receptor antagonists |
| FR2896798A1 (fr) | 2006-01-27 | 2007-08-03 | Sanofi Aventis Sa | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| FR2896799B1 (fr) | 2006-02-02 | 2008-03-28 | Sanofi Aventis Sa | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| US7553836B2 (en) | 2006-02-06 | 2009-06-30 | Bristol-Myers Squibb Company | Melanin concentrating hormone receptor-1 antagonists |
| US20090105318A1 (en) | 2006-03-29 | 2009-04-23 | Coleman Paul J | Amidoethylthioether Orexin Receptor Antagonists |
| CA2647678A1 (en) | 2006-03-29 | 2007-11-08 | Merck & Co., Inc. | Diazepan orexin receptor antagonists |
| ATE496051T1 (de) | 2006-04-26 | 2011-02-15 | Actelion Pharmaceuticals Ltd | Pyrazolotetrahydropyridinderivate als orexinrezeptorantagonisten |
| WO2007146761A2 (en) | 2006-06-12 | 2007-12-21 | Neurogen Corporation | Diaryl pyrimidinones and related compounds |
| DK2049529T3 (da) | 2006-07-14 | 2010-11-29 | Merck Sharp & Dohme | Substituerede diazepan-orexin-receptor- antagonister |
| US20100029736A1 (en) | 2006-07-14 | 2010-02-04 | Merck & Co., Inc. | 2-substituted proline bis-amide orexin receptor antagonists |
| AU2007272854B2 (en) | 2006-07-14 | 2013-08-01 | Merck Sharp & Dohme Corp. | Bridged diazepan orexin receptor antagonists |
| US7994336B2 (en) | 2006-08-15 | 2011-08-09 | Actelion Pharmaceuticals Ltd. | Azetidine compounds as orexin receptor antagonists |
| ATE458740T1 (de) | 2006-08-28 | 2010-03-15 | Actelion Pharmaceuticals Ltd | 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulen- derivate als orexinrezeptor-antagonisten |
| JP2010503714A (ja) | 2006-09-18 | 2010-02-04 | エフ．ホフマン−ラ ロシュ アーゲー | オクタヒドロピロロ［３，４−ｃ］ピロール誘導体、抗ウイルス剤としてのそれらの使用 |
| CA2662612A1 (en) | 2006-09-29 | 2008-04-03 | Actelion Pharmaceuticals Ltd | 3-aza-bicyclo[3.1.0]hexane derivatives |
| WO2008052139A2 (en) | 2006-10-25 | 2008-05-02 | Somaxon Pharmaceuticals, Inc. | Ultra low dose doxepin and methods of using the same to treat sleep disorders |
| EP2089018A2 (en) | 2006-11-07 | 2009-08-19 | Lexicon Pharmaceuticals, Inc. | Methods of treating cognitive impairment and dementia |
| PE20081229A1 (es) | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| US20110077200A1 (en) | 2006-12-06 | 2011-03-31 | Somaxon Pharmaceuticals, Inc. | Combination therapy using low-dose doxepin for the improvement of sleep |
| EP2125823B1 (en) | 2006-12-22 | 2012-02-15 | Actelion Pharmaceuticals Ltd. | 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives |
| CL2008000836A1 (es) | 2007-03-26 | 2008-11-07 | Actelion Pharmaceuticals Ltd | Compuestos derivados de tiazolidina, antagonistas del receptor de orexina; composicion farmaceutica que los comprende; y su uso en el tratamiento de neurosis emocional, depresion grave, trastornos psicoticos, alzheimer, parkinson, dolor, entre otras. |
| JP2010525077A (ja) | 2007-04-25 | 2010-07-22 | ブリストル−マイヤーズ スクイブ カンパニー | 非塩基性メラニン凝集ホルモン受容体−１アンタゴニスト |
| AU2008255005B2 (en) | 2007-05-18 | 2013-05-02 | Merck Sharp & Dohme Corp. | OXO bridged diazepan orexin receptor antagonists |
| FR2918061B1 (fr) | 2007-06-28 | 2010-10-22 | Sanofi Aventis | Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique. |
| GB0712888D0 (en) | 2007-07-03 | 2007-08-15 | Glaxo Group Ltd | Novel compounds |
| TW200911242A (en) | 2007-07-03 | 2009-03-16 | Glaxo Group Ltd | Novel compounds |
| EP2164847B1 (en) | 2007-07-03 | 2011-09-14 | Actelion Pharmaceuticals Ltd. | 3-aza-bicyclo[3.3.0]octane compounds |
| US20090011994A1 (en) | 2007-07-06 | 2009-01-08 | Bristol-Myers Squibb Company | Non-basic melanin concentrating hormone receptor-1 antagonists and methods |
| WO2009011775A1 (en) | 2007-07-13 | 2009-01-22 | Merck & Co., Inc. | Amidoethyl alkylamino orexin receptor antagonists |
| FR2918986B1 (fr) * | 2007-07-19 | 2009-09-04 | Sanofi Aventis Sa | Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique |
| KR20100046047A (ko) | 2007-07-27 | 2010-05-04 | 액테리온 파마슈티칼 리미티드 | 2-아자-비시클로[3.3.0]옥탄 유도체 |
| CN101801918A (zh) | 2007-08-02 | 2010-08-11 | 弗·哈夫曼-拉罗切有限公司 | 作为食欲肽受体拮抗剂的单酰胺衍生物 |
| AU2008288151A1 (en) | 2007-08-15 | 2009-02-19 | Actelion Pharmaceuticals Ltd | 1,2-diamido-ethylene derivatives as orexin antagonists |
| CN101874030B (zh) | 2007-09-24 | 2012-11-14 | 埃科特莱茵药品有限公司 | 用作食欲素受体拮抗剂的吡咯烷和哌啶 |
| CA2703904A1 (en) | 2007-10-29 | 2009-05-07 | Merck Sharp & Dohme Corp. | Substituted diazepan orexin receptor antagonists |
| DE102007052177A1 (de) | 2007-10-30 | 2009-05-07 | Novega Produktionssysteme Gmbh | Ortungsbake |
| EP2058001A1 (en) | 2007-11-08 | 2009-05-13 | Crossbeta Biosciences B.V. | Enhancement of immunogenicity of antigens |
| CN101952286A (zh) | 2007-12-21 | 2011-01-19 | 阿斯利康(瑞典)有限公司 | 用于治疗和雄激素受体有关的病症的双环衍生物 |
| BRPI0821141A2 (pt) | 2007-12-21 | 2015-06-16 | Hoffmann La Roche | Derivados de heteroarila como antagonistas do receptor de orexina |
| GB0806536D0 (en) | 2008-04-10 | 2008-05-14 | Glaxo Group Ltd | Novel compounds |
| US8598119B2 (en) | 2008-05-27 | 2013-12-03 | Intra-Cellular Therapies, Inc. | Methods and compositions for sleep disorders and other disorders |
| EP2303871B1 (en) | 2008-07-29 | 2012-05-09 | F. Hoffmann-La Roche AG | Pyrrolidin-3-ylmethyl-amine as orexin antagonists |
| AR072899A1 (es) | 2008-08-07 | 2010-09-29 | Merck Sharp & Dohme | Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad. |
| US8129384B2 (en) | 2008-10-09 | 2012-03-06 | Glaxo Group Limited | Imidazo[1,2-a]pyrazines as orexin receptor antagonists |
| US8093255B2 (en) | 2008-10-09 | 2012-01-10 | Glaxo Group Limited | Imidazo[1,2-A]pyrimidines as orexin receptor antagonists |
| US20100267730A1 (en) | 2008-10-09 | 2010-10-21 | Giuseppe Alvaro | Novel compounds |
| CA2739915A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| US8466281B2 (en) | 2008-10-21 | 2013-06-18 | Merck Sharp & Dohme Corp. | 2,5-disubstituted morpholine orexin receptor antagonists |
| EP2350061B1 (en) | 2008-10-21 | 2013-08-14 | Merck Sharp & Dohme Corp. | 2,3-disubstituted piperidine orexin receptor antagonists |
| US8710076B2 (en) | 2008-10-21 | 2014-04-29 | Merck Sharp & Dohme Corp. | 2,5-disubstituted piperidine orexin receptor antagonists |
| CA2739927A1 (en) | 2008-10-21 | 2010-04-29 | Merck Sharp & Dohme Corp. | Disubstituted azepan orexin receptor antagonists |
| EP2348856B1 (en) | 2008-10-21 | 2013-08-14 | Merck Sharp & Dohme Corp. | 2,4-disubstituted pyrrolidine orexin receptor antagonists |
| EA201170624A1 (ru) | 2008-10-30 | 2011-12-30 | Мерк Шарп Энд Домэ Корп. | Изоникотинамидные антагонисты рецепторов орексинов |
| CA2741648A1 (en) | 2008-10-30 | 2010-05-06 | Merck Sharp & Dohme Corp. | 2,5-disubstituted phenyl carboxamide orexin receptor antagonists |
| JP2012507540A (ja) | 2008-10-30 | 2012-03-29 | メルク・シャープ・エンド・ドーム・コーポレイション | ピリダジンカルボキサミド・オレキシン受容体アンタゴニスト |
| JP2012509912A (ja) | 2008-11-26 | 2012-04-26 | グラクソ グループ リミテッド | 新規の化合物 |
| WO2010060470A1 (en) | 2008-11-26 | 2010-06-03 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| EP2358712A1 (en) | 2008-11-26 | 2011-08-24 | Glaxo Group Limited | Piperidine derivatives useful as orexin receptor antagonists |
| TW201033190A (en) | 2008-12-02 | 2010-09-16 | Glaxo Group Ltd | Novel compounds |
| AR074426A1 (es) | 2008-12-02 | 2011-01-19 | Glaxo Group Ltd | Compuesto de n-(((1s,4s,6s)-3-(2-piridinilcarbonil)3-azabiciclo (4,1.0)hept-4-il) metil)-2-heteroarilamina, su uso para la prepracion de un medicamento para el tratamiento de una enfermedad que requiere un antagonista de un receptor de orexina humana y composicion farmaceutica que lo comprende |
| GB0823467D0 (en) | 2008-12-23 | 2009-01-28 | Glaxo Group Ltd | Novel Compounds |
| US20100214135A1 (en) | 2009-02-26 | 2010-08-26 | Microsoft Corporation | Dynamic rear-projected user interface |
| KR20120007061A (ko) | 2009-04-24 | 2012-01-19 | 글락소 그룹 리미티드 | 오렉신 길항제로서 사용되는 3-아자비시클로［4.1.0］헵탄 |
| JP2013502448A (ja) | 2009-08-24 | 2013-01-24 | グラクソ グループ リミテッド | オレキシンアンタゴニストとして用いられるピペリジン誘導体 |
| WO2011023578A1 (en) | 2009-08-24 | 2011-03-03 | Glaxo Group Limited | 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder |
| JP5848251B2 (ja) | 2009-10-23 | 2016-01-27 | ヤンセン ファーマシューティカ エヌ．ベー． | オレキシン受容体調節因子としての縮合複素環式化合物 |
| ES2735411T3 (es) | 2009-10-23 | 2019-12-18 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirroles disustituidos como moduladores del receptor de orexina |
| WO2011050200A1 (en) | 2009-10-23 | 2011-04-28 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as orexin receptor modulators |
| AU2010310596B2 (en) | 2009-10-24 | 2014-11-13 | Indiana University Research And Technology Corporation | Methods and compositions for panic disorders |
| TWI410630B (zh) | 2009-11-10 | 2013-10-01 | Ct Lab Inc | 一種用以治療與食慾素受體１、食慾素受體２、體抑素受體２或多巴胺ｄ２ｌ受體相關之疾病的方法和組合物 |
| JP5793505B2 (ja) | 2009-12-23 | 2015-10-14 | ジャスコ ファーマシューティカルズ， エルエルシー | アミノピリミジンキナーゼ阻害薬 |
| TW201307320A (zh) | 2010-12-17 | 2013-02-16 | 大正製藥股份有限公司 | 吡唑衍生物 |
| WO2012089607A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Novel compounds with a 3a-azabicyclo [4.1.0] heptane core acting on orexin receptors |
| WO2012089606A1 (en) | 2010-12-28 | 2012-07-05 | Glaxo Group Limited | Azabicyclo [4.1.0] hept - 4 - yl derivatives as human orexin receptor antagonists |
| US9586962B2 (en) | 2011-04-20 | 2017-03-07 | Janssen Pharmaceutica Nv | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators |
| EP2708537A4 (en) | 2011-05-10 | 2014-10-01 | Taisho Pharmaceutical Co Ltd | HETEROAROMATIC RING DERIVATIVE |
| EP2730573A4 (en) | 2011-07-05 | 2014-12-03 | Taisho Pharmaceutical Co Ltd | METHYLPIPERIDINDERIVAT |
| US9029364B2 (en) | 2011-10-21 | 2015-05-12 | Merck Sharp & Dohme Corp. | 2,5-disubstituted thiomorpholine orexin receptor antagonists |
| US9440982B2 (en) | 2012-02-07 | 2016-09-13 | Eolas Therapeutics, Inc. | Substituted prolines/piperidines as orexin receptor antagonists |
| JP6346862B2 (ja) | 2012-02-07 | 2018-06-20 | エオラス セラピューティクス， インコーポレイテッド | オレキシンレセプターアンタゴニストとしての置換プロリン／ピペリジン |
| WO2013126856A1 (en) | 2012-02-23 | 2013-08-29 | Vanderbilt University | Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4 |
| HK1203197A1 (en) | 2012-06-15 | 2015-10-23 | Taisho Pharmaceutical Co., Ltd. | Branched chain alkyl heteroaromatic ring derivative |
| JP2014015452A (ja) | 2012-06-15 | 2014-01-30 | Taisho Pharmaceutical Co Ltd | ピラゾール誘導体を含有する医薬 |
| RS55675B1 (sr) | 2012-06-15 | 2017-06-30 | Taisho Pharmaceutical Co Ltd | Jedinjenja 1,3-oksazolidina ili 1,3-oksazinana kao antagonisti oreksinskog receptora |
| JP2014111586A (ja) | 2012-11-09 | 2014-06-19 | Taisho Pharmaceutical Co Ltd | ヘテロ芳香環誘導体を含有する医薬 |
| EP2925321A4 (en) | 2012-11-27 | 2016-04-27 | Merck Sharp & Dohme | 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists |
| JP2016028017A (ja) | 2012-12-13 | 2016-02-25 | 大正製薬株式会社 | フッ素置換ピペリジン化合物 |
| JP2014141480A (ja) | 2012-12-28 | 2014-08-07 | Taisho Pharmaceutical Co Ltd | メチルピペリジン誘導体を含有する医薬 |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| WO2015018027A1 (en) | 2013-08-08 | 2015-02-12 | Merck Sharp & Dohme Corp. | Thiazole orexin receptor antagonists |
| IL321987A (en) | 2013-12-03 | 2025-09-01 | Intra Cellular Therapies Inc | A long-acting injectable preparation containing polymeric microspheres of modified compressed gamma-carboline heterocyclic compounds or a sustained-release pharmaceutical preparation containing these compounds for use in the treatment of bipolar I and/or bipolar II disorders |
| US9586934B2 (en) | 2013-12-09 | 2017-03-07 | Merck Sharp & Dohme Corp. | 2-pyridyloxy-4-methyl orexin receptor antagonists |
| JP2015131802A (ja) | 2013-12-13 | 2015-07-23 | 大正製薬株式会社 | 分岐鎖アルキルヘテロ芳香環誘導体を含有する医薬 |
| JP5930010B2 (ja) | 2013-12-13 | 2016-06-08 | 大正製薬株式会社 | ヘテロ芳香環メチル環状アミン誘導体を含有する医薬 |
| WO2015095108A1 (en) | 2013-12-18 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thioether-piperidinyl orexin receptor antagonists |
| TW201613891A (en) | 2014-02-12 | 2016-04-16 | Eolas Therapeutics Inc | Substituted prolines / piperidines as orexin receptor antagonists |
| TW201613864A (en) | 2014-02-20 | 2016-04-16 | Takeda Pharmaceutical | Novel compounds |
| JP2017100950A (ja) | 2014-04-04 | 2017-06-08 | 大正製薬株式会社 | オキソ複素環誘導体 |
| JP2017100951A (ja) | 2014-04-04 | 2017-06-08 | 大正製薬株式会社 | オキサゾリジノン及びオキサジナノン誘導体 |
| WO2015180060A1 (zh) | 2014-05-28 | 2015-12-03 | 杭州普晒医药科技有限公司 | 一种二氮杂环庚烷化合物的盐及其晶型与无定型物 |
| ES2901418T3 (es) | 2014-08-13 | 2022-03-22 | Eolas Therapeutics Inc | Difluoropirrolidinas como moduladores del receptor de orexina |
| US20160051533A1 (en) | 2014-08-20 | 2016-02-25 | Ladd Research LLC | Diagnosis and pharmacological treatment of seasonal affective disorder and symptoms of seasonality |
| GB201415569D0 (en) | 2014-09-03 | 2014-10-15 | C4X Discovery Ltd | Therapeutic Compounds |
| US10196383B2 (en) | 2015-07-17 | 2019-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| GB201601703D0 (en) | 2016-01-29 | 2016-03-16 | C4X Discovery Ltd | Therapeutic compounds |
| CA2960253A1 (en) | 2016-03-10 | 2017-09-10 | Janssen Pharmaceutica Nv | Methods of treating depression using orexin-2 receptor antagonists |
| US20210169883A1 (en) | 2018-07-27 | 2021-06-10 | Icahn School Of Medicine At Mount Sinai | Method of treating aggression with orexin receptor antagonists |
| GB201820458D0 (en) | 2018-12-14 | 2019-01-30 | Heptares Therapeutics Ltd | Ox1 antagonists |
-
2010
- 2010-10-21 ES ES16163733T patent/ES2735411T3/es active Active
- 2010-10-21 JP JP2012535384A patent/JP5759470B2/ja active Active
- 2010-10-21 EP EP16163733.5A patent/EP3093291B1/en active Active
- 2010-10-21 US US16/391,791 patent/USRE48841E1/en active Active
- 2010-10-21 US US13/503,231 patent/US8653263B2/en not_active Ceased
- 2010-10-21 DK DK16163733.5T patent/DK3093291T3/da active
- 2010-10-21 EP EP10773477.4A patent/EP2491038B1/en active Active
- 2010-10-21 JO JOP/2010/0362A patent/JO3267B1/ar active
- 2010-10-21 PL PL10773477.4T patent/PL2491038T3/pl unknown
- 2010-10-21 ES ES10773477.4T patent/ES2585806T3/es active Active
- 2010-10-21 EA EA201270591A patent/EA022766B1/ru unknown
- 2010-10-21 PT PT107734774T patent/PT2491038T/pt unknown
- 2010-10-21 TR TR2019/10327T patent/TR201910327T4/tr unknown
- 2010-10-21 HR HRP20160781TT patent/HRP20160781T1/hr unknown
- 2010-10-21 KR KR1020177034279A patent/KR101859400B1/ko active Active
- 2010-10-21 CA CA2778484A patent/CA2778484C/en active Active
- 2010-10-21 EP EP19172579.5A patent/EP3581575A1/en active Pending
- 2010-10-21 HU HUE16163733A patent/HUE043962T2/hu unknown
- 2010-10-21 KR KR1020177034281A patent/KR101859409B1/ko active Active
- 2010-10-21 PL PL16163733T patent/PL3093291T3/pl unknown
- 2010-10-21 ME MEP-2016-135A patent/ME02437B/me unknown
- 2010-10-21 PT PT16163733T patent/PT3093291T/pt unknown
- 2010-10-21 AU AU2010310595A patent/AU2010310595B2/en active Active
- 2010-10-21 NZ NZ599629A patent/NZ599629A/en unknown
- 2010-10-21 SI SI201031898T patent/SI3093291T1/sl unknown
- 2010-10-21 LT LTEP16163733.5T patent/LT3093291T/lt unknown
- 2010-10-21 SM SM20190392T patent/SMT201900392T1/it unknown
- 2010-10-21 CN CN201080058816.XA patent/CN102781942B/zh active Active
- 2010-10-21 HU HUE10773477A patent/HUE028650T2/en unknown
- 2010-10-21 ME MEP-2019-199A patent/ME03452B/me unknown
- 2010-10-21 KR KR1020127013101A patent/KR20120105449A/ko not_active Withdrawn
- 2010-10-21 SI SI201031214A patent/SI2491038T1/sl unknown
- 2010-10-21 WO PCT/US2010/053606 patent/WO2011050198A1/en not_active Ceased
- 2010-10-21 PH PH1/2012/500796A patent/PH12012500796A1/en unknown
- 2010-10-21 BR BR112012010820-4A patent/BR112012010820B1/pt active IP Right Grant
- 2010-10-21 UA UAA201206182A patent/UA107812C2/ru unknown
- 2010-10-21 DK DK10773477.4T patent/DK2491038T3/da active
- 2010-10-21 RS RS20160501A patent/RS54945B1/sr unknown
- 2010-10-21 RS RS20190878A patent/RS59004B1/sr unknown
- 2010-10-21 MX MX2012004753A patent/MX2012004753A/es active IP Right Grant
- 2010-10-22 AR ARP100103874A patent/AR078731A1/es active IP Right Grant
- 2010-10-22 TW TW099136022A patent/TWI481613B/zh active
- 2010-10-22 CL CL2010001162A patent/CL2010001162A1/es unknown
- 2010-10-22 PE PE2010001000A patent/PE20110404A1/es active IP Right Grant
- 2010-10-25 UY UY0001032966A patent/UY32966A/es active IP Right Grant
-
2012
- 2012-04-17 IL IL219234A patent/IL219234A/en active IP Right Grant
- 2012-04-20 NI NI201200062A patent/NI201200062A/es unknown
- 2012-05-11 CO CO12077916A patent/CO6541572A2/es unknown
- 2012-05-17 EC ECSP12011908 patent/ECSP12011908A/es unknown
- 2012-05-23 CR CR20120273A patent/CR20120273A/es unknown
-
2013
- 2013-12-23 US US14/138,941 patent/US9079911B2/en active Active
-
2015
- 2015-06-09 US US14/734,225 patent/US20150335651A1/en not_active Abandoned
- 2015-10-13 AU AU2015242975A patent/AU2015242975B2/en active Active
-
2016
- 2016-07-05 SM SM201600216T patent/SMT201600216B/it unknown
- 2016-07-05 CY CY20161100629T patent/CY1117743T1/el unknown
-
2017
- 2017-01-24 US US15/413,965 patent/US20170129901A1/en not_active Abandoned
-
2018
- 2018-03-14 JO JOP/2018/0019A patent/JOP20180019B1/ar active
-
2019
- 2019-03-07 AR ARP190100557A patent/AR114667A2/es unknown
- 2019-07-05 HR HRP20191220TT patent/HRP20191220T1/hr unknown
- 2019-07-26 CY CY20191100794T patent/CY1121848T1/el unknown
- 2019-10-15 US US16/601,832 patent/US11059828B2/en active Active
-
2021
- 2021-07-09 US US17/372,168 patent/US11667644B2/en active Active
-
2023
- 2023-06-02 US US18/327,990 patent/US12378254B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME02437B (me) | Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora | |
| JP2013508403A5 (OSRAM) | ||
| JP2013508405A5 (OSRAM) | ||
| RU2015132181A (ru) | Фтор-[1,3]-оксазины в качестве ингибиторов васе1 | |
| JP2013508404A5 (OSRAM) | ||
| RU2396269C2 (ru) | Производные гетероарилзамещенного пиперидина в качестве ингибиторов печеночной карнитин пальмитоилтрансферазы (l-cpt1) | |
| RU2010137300A (ru) | Модуляторы бета-амилоида | |
| US9586962B2 (en) | Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators | |
| RU2424242C2 (ru) | Азолопиримидины в качестве ингибиторов активности каннабиноидного рецептора 1 | |
| HRP20231310T1 (hr) | Heteroarilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene | |
| JP2013545744A5 (OSRAM) | ||
| JP2020527560A5 (OSRAM) | ||
| JP2014517833A5 (OSRAM) | ||
| HRP20211262T1 (hr) | Supstituirani spojevi koji sadrže dušik | |
| JP2016512259A5 (OSRAM) | ||
| JP2011503166A5 (OSRAM) | ||
| RU2013124101A (ru) | Гетероциклические амины и их применения | |
| JP2014528446A5 (OSRAM) | ||
| RU2008141509A (ru) | Mglur5 модуляторы 1 | |
| JP2007523182A5 (OSRAM) | ||
| HRP20200440T1 (hr) | 1h-pirazolo[4,3-b]piridini kao pde1 inhibitori | |
| ME02100B (me) | Derivati 4-aminopirimidina i njihova primena kao antagonista adenozinskog a2a receptora | |
| RU2010130175A (ru) | Производные бензотиазола и бензоксазола и способы их применения | |
| RU2012154308A (ru) | Пиперидинил-замещенные лактамы как модуляторы gpr119 | |
| JP2010505809A5 (OSRAM) |