JP2019513759A5 - - Google Patents
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- Publication number
- JP2019513759A5 JP2019513759A5 JP2018553080A JP2018553080A JP2019513759A5 JP 2019513759 A5 JP2019513759 A5 JP 2019513759A5 JP 2018553080 A JP2018553080 A JP 2018553080A JP 2018553080 A JP2018553080 A JP 2018553080A JP 2019513759 A5 JP2019513759 A5 JP 2019513759A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrimidine
- pyrrolidin
- pharmaceutically acceptable
- acceptable salt
- ylvinyl
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 76
- FNEHSHNEXMPCLJ-VWCDRPFISA-N 5-[(e)-2-[(3r)-pyrrolidin-3-yl]ethenyl]pyrimidine Chemical group C1NCC[C@@H]1\C=C\C1=CN=CN=C1 FNEHSHNEXMPCLJ-VWCDRPFISA-N 0.000 claims description 59
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 40
- 239000008194 pharmaceutical composition Substances 0.000 claims description 21
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 12
- 102000003923 Protein Kinase C Human genes 0.000 claims description 9
- 108090000315 Protein Kinase C Proteins 0.000 claims description 9
- 229940122739 Calcineurin inhibitor Drugs 0.000 claims description 6
- 101710192106 Calcineurin-binding protein cabin-1 Proteins 0.000 claims description 6
- 102100024123 Calcineurin-binding protein cabin-1 Human genes 0.000 claims description 6
- 102000001253 Protein Kinase Human genes 0.000 claims description 6
- 108060006633 protein kinase Proteins 0.000 claims description 6
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 5
- 206010013774 Dry eye Diseases 0.000 claims description 5
- DSLZVSRJTYRBFB-DUHBMQHGSA-N galactaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)C(O)=O DSLZVSRJTYRBFB-DUHBMQHGSA-N 0.000 claims description 5
- 239000007788 liquid Substances 0.000 claims description 5
- 239000000126 substance Substances 0.000 claims description 5
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 claims description 4
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 claims description 4
- 239000006210 lotion Substances 0.000 claims description 4
- 102000008130 Cyclic AMP-Dependent Protein Kinases Human genes 0.000 claims description 3
- 108010049894 Cyclic AMP-Dependent Protein Kinases Proteins 0.000 claims description 3
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical group CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims description 3
- 108010036949 Cyclosporine Proteins 0.000 claims description 3
- 241000021559 Dicerandra Species 0.000 claims description 3
- 235000010654 Melissa officinalis Nutrition 0.000 claims description 3
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims description 3
- 239000000443 aerosol Substances 0.000 claims description 3
- 229960001265 ciclosporin Drugs 0.000 claims description 3
- 239000006071 cream Substances 0.000 claims description 3
- 229930182912 cyclosporin Natural products 0.000 claims description 3
- 239000000499 gel Substances 0.000 claims description 3
- 239000000865 liniment Substances 0.000 claims description 3
- 239000002674 ointment Substances 0.000 claims description 3
- 239000006072 paste Substances 0.000 claims description 3
- KASDHRXLYQOAKZ-ZPSXYTITSA-N pimecrolimus Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](Cl)[C@H](OC)C1 KASDHRXLYQOAKZ-ZPSXYTITSA-N 0.000 claims description 3
- 229960005330 pimecrolimus Drugs 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 238000001356 surgical procedure Methods 0.000 claims description 3
- 239000000725 suspension Substances 0.000 claims description 3
- 229960001967 tacrolimus Drugs 0.000 claims description 3
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims description 3
- 238000011200 topical administration Methods 0.000 claims description 3
- 239000006199 nebulizer Substances 0.000 claims description 2
- 230000002093 peripheral effect Effects 0.000 claims description 2
- 229940098458 powder spray Drugs 0.000 claims description 2
- 238000011084 recovery Methods 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- 230000004489 tear production Effects 0.000 claims description 2
- 230000007704 transition Effects 0.000 claims description 2
- 239000006200 vaporizer Substances 0.000 claims description 2
- -1 2-pyrrolidin-3-ylvinyl Chemical group 0.000 claims 3
- PNLMJLLDHIESND-UHFFFAOYSA-N C(CC(O)(C(=O)O)CC(=O)O)(=O)O.N1=CN=CC=C1 Chemical compound C(CC(O)(C(=O)O)CC(=O)O)(=O)O.N1=CN=CC=C1 PNLMJLLDHIESND-UHFFFAOYSA-N 0.000 claims 2
- YJBSGPVXDGLMBC-SXKXKJGMSA-N O.O.O[C@@H]([C@@H](O)[C@H](O)C(O)=O)[C@@H](O)C(O)=O Chemical compound O.O.O[C@@H]([C@@H](O)[C@H](O)C(O)=O)[C@@H](O)C(O)=O YJBSGPVXDGLMBC-SXKXKJGMSA-N 0.000 claims 1
- 206010052143 Ocular discomfort Diseases 0.000 claims 1
- 150000004683 dihydrates Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 31
- 210000003928 nasal cavity Anatomy 0.000 description 8
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 4
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 2
- HVGZXVVUVQKTSC-OUCPDFHMSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid 5-[(E)-2-[(3R)-pyrrolidin-3-yl]ethenyl]pyrimidine Chemical group C1NCC[C@@H]1\C=C\C1=CN=CN=C1.OC(=O)CC(O)(C(O)=O)CC(O)=O HVGZXVVUVQKTSC-OUCPDFHMSA-N 0.000 description 2
- 239000012458 free base Substances 0.000 description 2
- 229960002715 nicotine Drugs 0.000 description 2
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000003442 weekly effect Effects 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022095460A JP2022120125A (ja) | 2016-04-07 | 2022-06-14 | 眼状態の治療方法 |
| JP2024086805A JP2024103594A (ja) | 2016-04-07 | 2024-05-29 | 眼状態の治療方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319648P | 2016-04-07 | 2016-04-07 | |
| US62/319,648 | 2016-04-07 | ||
| PCT/US2017/026385 WO2017177024A1 (en) | 2016-04-07 | 2017-04-06 | Methods of treating ocular conditions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022095460A Division JP2022120125A (ja) | 2016-04-07 | 2022-06-14 | 眼状態の治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019513759A JP2019513759A (ja) | 2019-05-30 |
| JP2019513759A5 true JP2019513759A5 (https=) | 2020-05-14 |
| JP7090551B2 JP7090551B2 (ja) | 2022-06-24 |
Family
ID=58549326
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553080A Active JP7090551B2 (ja) | 2016-04-07 | 2017-04-06 | 眼状態の治療方法 |
| JP2022095460A Pending JP2022120125A (ja) | 2016-04-07 | 2022-06-14 | 眼状態の治療方法 |
| JP2024086805A Pending JP2024103594A (ja) | 2016-04-07 | 2024-05-29 | 眼状態の治療方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022095460A Pending JP2022120125A (ja) | 2016-04-07 | 2022-06-14 | 眼状態の治療方法 |
| JP2024086805A Pending JP2024103594A (ja) | 2016-04-07 | 2024-05-29 | 眼状態の治療方法 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US10709707B2 (https=) |
| EP (2) | EP3439661B1 (https=) |
| JP (3) | JP7090551B2 (https=) |
| KR (2) | KR102485299B1 (https=) |
| CN (3) | CN114533737B (https=) |
| AU (1) | AU2017248276B2 (https=) |
| DK (1) | DK3439661T3 (https=) |
| EA (1) | EA201892265A1 (https=) |
| ES (1) | ES2893126T3 (https=) |
| IL (3) | IL299204A (https=) |
| MX (2) | MX385698B (https=) |
| MY (1) | MY199237A (https=) |
| NZ (1) | NZ746468A (https=) |
| PH (1) | PH12018502154A1 (https=) |
| PT (1) | PT3439661T (https=) |
| SG (1) | SG11201808650QA (https=) |
| TW (2) | TWI876258B (https=) |
| WO (1) | WO2017177024A1 (https=) |
| ZA (1) | ZA201807438B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9145396B2 (en) | 2008-12-01 | 2015-09-29 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine |
| EP3848028B9 (en) | 2014-10-20 | 2024-10-16 | Oyster Point Pharma, Inc. | Methods of treating ocular conditions |
| MX385698B (es) | 2016-04-07 | 2025-03-18 | Oyster Point Pharma Inc | Uso de un compuesto que comprende un grupo pirrolidinilo y pirimidinilo para tratar enfermedades oculares |
| EP3820443A1 (en) | 2018-07-10 | 2021-05-19 | Oyster Point Pharma, Inc. | Combinations of positive allosteric modulators and nicotinic acetylcholine receptor agonists for treating ocular conditions |
| WO2020014217A1 (en) | 2018-07-10 | 2020-01-16 | Oyster Point Pharma, Inc. | Methods of treating ocular conditions |
| ES3039903T3 (en) * | 2020-04-28 | 2025-10-27 | Oyster Point Pharma Inc | Local administration of nicotinic acetylcholine receptor agonists for the inhibition of coronavirus infections |
| KR20240021783A (ko) * | 2021-05-07 | 2024-02-19 | 오이스터 포인트 파마 인코포레이티드 | 벡터 및 니코틴 작용제 병용 요법 |
| WO2026080563A1 (en) | 2024-10-09 | 2026-04-16 | Oyster Point Pharma, Inc. | Simpinicline oral formations and use thereof |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6277855B1 (en) | 2000-04-21 | 2001-08-21 | Inspire Pharmaceuticals, Inc. | Method of treating dry eye disease with nicotinic acetylcholine receptor agonists |
| US20030008892A1 (en) | 2001-07-09 | 2003-01-09 | Pfizer Inc. | Pharmaceutical composition and method of modulating cholinergic function in a mammal |
| EP1461040B1 (en) | 2001-11-29 | 2006-03-15 | Pfizer Products Inc. | Succinic acid salts of 5,8,14-triazatetracyclo[10.3.1.0 2,11 .0 4,9 ]-hexadeca-2(11),3,5,7,9,-pentaene and pharmaceutical compositions thereof |
| AU2003269413A1 (en) | 2002-11-01 | 2004-05-25 | Pharmacia & Upjohn Company Llc | Nicotinic acetylcholine agonists in the treatment of glaucoma and retinal neuropathy |
| US7098331B2 (en) | 2003-03-05 | 2006-08-29 | Targacept, Inc. | Arylvinylazacycloalkane compounds and methods of preparation and use thereof |
| US20060270592A1 (en) | 2004-03-19 | 2006-11-30 | Ophthalmic Research Associates, Inc. | Use of neurotransmitters and neuropeptides for the treatment of dry eye diseases and related conditions |
| MX2007004495A (es) | 2004-10-15 | 2007-05-10 | Pfizer Prod Inc | Composiciones y procedimientos para la administracion intranasal, bucal, sublingual y pulmonar de vareniclina. |
| WO2006100075A2 (en) | 2005-03-22 | 2006-09-28 | Niconovum Ab | Use of an artificial sweetener to enhance absorption of nicotine |
| US20110086086A1 (en) | 2005-07-26 | 2011-04-14 | Pfizer Inc | Transdermal system for varenicline |
| TWI454262B (zh) | 2006-11-02 | 2014-10-01 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
| HRP20110702T1 (hr) | 2007-02-02 | 2011-10-31 | Pfizer Products Inc. | Triciklički spojevi i njihova uporaba kao modulatora glukokortikoidnih receptora |
| WO2008157365A2 (en) * | 2007-06-15 | 2008-12-24 | Targacept, Inc. | Vinylazacycloalkanes for treating neuropathic pain |
| US20090093446A1 (en) | 2007-10-05 | 2009-04-09 | Winston Laboratories, Inc. | Method for alleviating keratoconjunctivitis sicca |
| CL2008003507A1 (es) | 2007-11-26 | 2009-11-27 | Neuroderm Ltd | Composicion farmaceutica que comprende nicotina y un inhibidor de la desensibilizacion del receptor de acetilcolina nicotinico (nachr) opipramol; kit farmaceutico; dispositivo medico; y uso para tratar una enfermedad o trastorno del sistema nervioso central o periferico. |
| JP2011513421A (ja) | 2008-03-05 | 2011-04-28 | ターガセプト，インコーポレイテッド | サブタイプ選択的なジアザビシクロアルカンのアミド |
| WO2010028011A1 (en) | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclononanes and uses thereof |
| WO2010028033A1 (en) | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclooctanes and uses thereof |
| EP2342192A4 (en) * | 2008-10-14 | 2012-05-09 | Psychogenics Inc | NICOTINACETYLCHOLINE RECEPTOR LIGANDS AND THEIR USES |
| TW201024283A (en) | 2008-12-01 | 2010-07-01 | Targacept Inc | Synthesis and novel salt forms of (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine |
| WO2010065443A1 (en) * | 2008-12-01 | 2010-06-10 | Targacept, Inc. | Synthesis and novel salt forms of (r)-5-((e)-2-(pyrrolidin-3-ylvinyl)pyrimidine |
| US9145396B2 (en) | 2008-12-01 | 2015-09-29 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine |
| BRPI1014247A2 (pt) * | 2009-06-17 | 2016-04-12 | Targacept Inc | reversão da discinesia induzida pela l-dopa por ligantes de receptores nocotínicos neuronais. |
| US20110274628A1 (en) | 2010-05-07 | 2011-11-10 | Borschke August J | Nicotine-containing pharmaceutical compositions |
| US8821457B2 (en) | 2010-09-08 | 2014-09-02 | Johnson & Johnson Vision Care, Inc. | Punctal plug containing drug formulation |
| ES2776996T3 (es) | 2011-10-20 | 2020-08-03 | Novartis Ag | Biomarcadores predictivos de la sensibilidad al tratamiento por el activador del receptor de la acetilcolina nicotínico alfa 7 |
| EP2786142A4 (en) | 2011-11-30 | 2015-07-22 | Diagnostear Ltd | DIAGNOSIS OF THE DRY EYE |
| EP3848028B9 (en) | 2014-10-20 | 2024-10-16 | Oyster Point Pharma, Inc. | Methods of treating ocular conditions |
| MX385698B (es) | 2016-04-07 | 2025-03-18 | Oyster Point Pharma Inc | Uso de un compuesto que comprende un grupo pirrolidinilo y pirimidinilo para tratar enfermedades oculares |
-
2017
- 2017-04-06 MX MX2018012230A patent/MX385698B/es unknown
- 2017-04-06 CN CN202210034408.5A patent/CN114533737B/zh active Active
- 2017-04-06 TW TW112102845A patent/TWI876258B/zh active
- 2017-04-06 EP EP17718304.3A patent/EP3439661B1/en active Active
- 2017-04-06 JP JP2018553080A patent/JP7090551B2/ja active Active
- 2017-04-06 NZ NZ746468A patent/NZ746468A/en unknown
- 2017-04-06 TW TW106111559A patent/TWI790997B/zh active
- 2017-04-06 CN CN201780034734.3A patent/CN109310692B/zh active Active
- 2017-04-06 DK DK17718304.3T patent/DK3439661T3/da active
- 2017-04-06 SG SG11201808650QA patent/SG11201808650QA/en unknown
- 2017-04-06 EA EA201892265A patent/EA201892265A1/ru unknown
- 2017-04-06 AU AU2017248276A patent/AU2017248276B2/en active Active
- 2017-04-06 KR KR1020187032218A patent/KR102485299B1/ko active Active
- 2017-04-06 CN CN202210040168.XA patent/CN114432313A/zh active Pending
- 2017-04-06 WO PCT/US2017/026385 patent/WO2017177024A1/en not_active Ceased
- 2017-04-06 MY MYPI2018001700A patent/MY199237A/en unknown
- 2017-04-06 IL IL299204A patent/IL299204A/en unknown
- 2017-04-06 PT PT177183043T patent/PT3439661T/pt unknown
- 2017-04-06 ES ES17718304T patent/ES2893126T3/es active Active
- 2017-04-06 EP EP21189296.3A patent/EP3970724A1/en active Pending
- 2017-04-06 US US16/091,830 patent/US10709707B2/en active Active
- 2017-04-06 KR KR1020237000103A patent/KR102512777B1/ko active Active
-
2018
- 2018-10-03 IL IL262102A patent/IL262102B/en unknown
- 2018-10-05 PH PH12018502154A patent/PH12018502154A1/en unknown
- 2018-10-05 MX MX2021010399A patent/MX2021010399A/es unknown
- 2018-11-06 ZA ZA2018/07438A patent/ZA201807438B/en unknown
-
2020
- 2020-04-17 US US16/852,225 patent/US20200345734A1/en not_active Abandoned
-
2022
- 2022-01-24 IL IL290069A patent/IL290069B2/en unknown
- 2022-06-14 JP JP2022095460A patent/JP2022120125A/ja active Pending
-
2024
- 2024-05-29 JP JP2024086805A patent/JP2024103594A/ja active Pending
- 2024-09-05 US US18/825,758 patent/US20250000861A1/en active Pending
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