JP2016513677A5 - - Google Patents
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- JP2016513677A5 JP2016513677A5 JP2016502306A JP2016502306A JP2016513677A5 JP 2016513677 A5 JP2016513677 A5 JP 2016513677A5 JP 2016502306 A JP2016502306 A JP 2016502306A JP 2016502306 A JP2016502306 A JP 2016502306A JP 2016513677 A5 JP2016513677 A5 JP 2016513677A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- methylpropyl
- octane
- indazole
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 claims 8
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 claims 8
- -1 substituted Chemical class 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 208000010412 Glaucoma Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000005336 allyloxy group Chemical group 0.000 claims 4
- 208000010877 cognitive disease Diseases 0.000 claims 4
- 210000004087 cornea Anatomy 0.000 claims 4
- 206010023332 keratitis Diseases 0.000 claims 4
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 208000028698 Cognitive impairment Diseases 0.000 claims 3
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 3
- 206010013774 Dry eye Diseases 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims 3
- 125000001118 alkylidene group Chemical group 0.000 claims 3
- 125000005133 alkynyloxy group Chemical group 0.000 claims 3
- 208000010217 blepharitis Diseases 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 210000004175 meibomian gland Anatomy 0.000 claims 3
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 2
- 208000000044 Amnesia Diseases 0.000 claims 2
- 206010003645 Atopy Diseases 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 2
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 2
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 2
- 208000005100 Herpetic Keratitis Diseases 0.000 claims 2
- 206010022941 Iridocyclitis Diseases 0.000 claims 2
- 206010073938 Ophthalmic herpes simplex Diseases 0.000 claims 2
- 201000002154 Pterygium Diseases 0.000 claims 2
- 241001303601 Rosacea Species 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 2
- 201000004612 anterior uveitis Diseases 0.000 claims 2
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 2
- 206010069664 atopic keratoconjunctivitis Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000004406 elevated intraocular pressure Effects 0.000 claims 2
- 206010015907 eye allergy Diseases 0.000 claims 2
- 230000004410 intraocular pressure Effects 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 239000000472 muscarinic agonist Substances 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000008447 perception Effects 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 201000004700 rosacea Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 1
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000031091 Amnestic disease Diseases 0.000 claims 1
- 206010002650 Anorexia nervosa and bulimia Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010006542 Bulbar palsy Diseases 0.000 claims 1
- ITRXTZZBZSFHJX-SJFWKDOISA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=C(C1=CC=CC=C21)C)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=C(C1=CC=CC=C21)C)C ITRXTZZBZSFHJX-SJFWKDOISA-N 0.000 claims 1
- JRJZHTCPZCYIBW-LAQKFSSHSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC(=CC=C21)C)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC(=CC=C21)C)C JRJZHTCPZCYIBW-LAQKFSSHSA-N 0.000 claims 1
- XRUAMHUABWEBDK-FOZKEBTBSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)C(F)(F)F)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)C(F)(F)F)C XRUAMHUABWEBDK-FOZKEBTBSA-N 0.000 claims 1
- VMKXOJMOJZBXDN-LAQKFSSHSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)C)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)C)C VMKXOJMOJZBXDN-LAQKFSSHSA-N 0.000 claims 1
- JKEYKALOMMSCEY-FOZKEBTBSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)F)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)F)C JKEYKALOMMSCEY-FOZKEBTBSA-N 0.000 claims 1
- OHIAMUPUAFQXRN-UDNPVYIMSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)OC)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)OC)C OHIAMUPUAFQXRN-UDNPVYIMSA-N 0.000 claims 1
- SFDGDCVMPXBWNZ-ZYOXULSGSA-N C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=CC(=C21)C)C Chemical compound C1(CC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=CC(=C21)C)C SFDGDCVMPXBWNZ-ZYOXULSGSA-N 0.000 claims 1
- JDBGWWXCMUKFAZ-LAQKFSSHSA-N C1(CCC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=CC=C21)C Chemical compound C1(CCC1)COC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=CC=C21)C JDBGWWXCMUKFAZ-LAQKFSSHSA-N 0.000 claims 1
- YYECPNPFTGIKTR-NTSUVRSXSA-N COCCC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)F)C Chemical compound COCCC1CC2CCC(C1)N2C[C@H](CN2N=CC1=CC=C(C=C21)F)C YYECPNPFTGIKTR-NTSUVRSXSA-N 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 claims 1
- 208000011688 Generalised anxiety disease Diseases 0.000 claims 1
- 208000008069 Geographic Atrophy Diseases 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000004547 Hallucinations Diseases 0.000 claims 1
- 208000033463 Ischaemic neuropathy Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 229940121743 Muscarinic receptor agonist Drugs 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029240 Neuritis Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 206010061323 Optic neuropathy Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010033864 Paranoia Diseases 0.000 claims 1
- 208000027099 Paranoid disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 206010034912 Phobia Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000007014 Retinitis pigmentosa Diseases 0.000 claims 1
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 claims 1
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims 1
- 208000016807 X-linked intellectual disability-macrocephaly-macroorchidism syndrome Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 230000016571 aggressive behavior Effects 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000006986 amnesia Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 208000037765 diseases and disorders Diseases 0.000 claims 1
- 210000003372 endocrine gland Anatomy 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 208000027993 eye symptom Diseases 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 210000005095 gastrointestinal system Anatomy 0.000 claims 1
- 208000029364 generalized anxiety disease Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 210000002216 heart Anatomy 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000024714 major depressive disease Diseases 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000001328 optic nerve Anatomy 0.000 claims 1
- 208000020911 optic nerve disease Diseases 0.000 claims 1
- 208000019906 panic disease Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 201000002241 progressive bulbar palsy Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 231100000241 scar Toxicity 0.000 claims 1
- 230000037390 scarring Effects 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000000007 visual effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361790364P | 2013-03-15 | 2013-03-15 | |
| US61/790,364 | 2013-03-15 | ||
| PCT/US2014/026998 WO2014152144A1 (en) | 2013-03-15 | 2014-03-14 | Muscarinic agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016513677A JP2016513677A (ja) | 2016-05-16 |
| JP2016513677A5 true JP2016513677A5 (enExample) | 2017-04-13 |
Family
ID=50439523
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016502306A Pending JP2016513677A (ja) | 2013-03-15 | 2014-03-14 | ムスカリンアゴニスト |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9670209B2 (enExample) |
| EP (1) | EP2976079A1 (enExample) |
| JP (1) | JP2016513677A (enExample) |
| KR (1) | KR20150143439A (enExample) |
| CN (1) | CN105120865A (enExample) |
| AU (1) | AU2014240139A1 (enExample) |
| BR (1) | BR112015021271A2 (enExample) |
| CA (1) | CA2903276A1 (enExample) |
| IL (1) | IL241001A0 (enExample) |
| MX (1) | MX2015012043A (enExample) |
| RU (1) | RU2015144155A (enExample) |
| TW (1) | TW201446761A (enExample) |
| WO (1) | WO2014152144A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2015144155A (ru) | 2013-03-15 | 2017-04-24 | Акадиа Фармасьютикалз Инк. | Мускариновые агонисты |
| KR101613245B1 (ko) | 2015-04-27 | 2016-04-18 | 주식회사 대웅제약 | 신규의 4-메톡시 피롤 유도체 또는 이의 염 및 이를 포함하는 약학 조성물 |
| EP3436434B1 (en) | 2016-03-31 | 2020-07-08 | Oncternal Therapeutics, Inc. | Indoline analogs and uses thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5707798A (en) | 1993-07-13 | 1998-01-13 | Novo Nordisk A/S | Identification of ligands by selective amplification of cells transfected with receptors |
| JPH10152470A (ja) * | 1996-09-25 | 1998-06-09 | Yoshitomi Pharmaceut Ind Ltd | ピペラジン化合物 |
| EP1535912A1 (en) | 2000-04-28 | 2005-06-01 | Arcadia Pharmaceuticals Inc. | Muscarinic agonists |
| ES2238437T3 (es) | 2000-04-28 | 2005-09-01 | Acadia Pharmaceuticals Inc. | Agonistas muscarinicos. |
| US7550459B2 (en) * | 2001-12-28 | 2009-06-23 | Acadia Pharmaceuticals, Inc. | Tetrahydroquinoline analogues as muscarinic agonists |
| CA2520125A1 (en) * | 2003-03-28 | 2004-10-14 | Acadia Pharmaceuticals Inc. | Muscarinic m1 receptor agonists for pain management |
| US7931909B2 (en) | 2005-05-10 | 2011-04-26 | Allergan, Inc. | Ocular therapy using alpha-2 adrenergic receptor compounds having enhanced anterior clearance rates |
| RU2015144155A (ru) | 2013-03-15 | 2017-04-24 | Акадиа Фармасьютикалз Инк. | Мускариновые агонисты |
-
2014
- 2014-03-14 RU RU2015144155A patent/RU2015144155A/ru not_active Application Discontinuation
- 2014-03-14 AU AU2014240139A patent/AU2014240139A1/en not_active Abandoned
- 2014-03-14 WO PCT/US2014/026998 patent/WO2014152144A1/en not_active Ceased
- 2014-03-14 JP JP2016502306A patent/JP2016513677A/ja active Pending
- 2014-03-14 US US14/774,685 patent/US9670209B2/en not_active Expired - Fee Related
- 2014-03-14 MX MX2015012043A patent/MX2015012043A/es unknown
- 2014-03-14 CN CN201480015640.8A patent/CN105120865A/zh active Pending
- 2014-03-14 KR KR1020157025205A patent/KR20150143439A/ko not_active Withdrawn
- 2014-03-14 CA CA2903276A patent/CA2903276A1/en not_active Abandoned
- 2014-03-14 TW TW103109294A patent/TW201446761A/zh unknown
- 2014-03-14 BR BR112015021271A patent/BR112015021271A2/pt not_active IP Right Cessation
- 2014-03-14 EP EP14715518.8A patent/EP2976079A1/en not_active Withdrawn
-
2015
- 2015-09-01 IL IL241001A patent/IL241001A0/en unknown
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