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) | CN109310692B (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) | TWI790997B (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 |
| SG10202011669PA (en) | 2014-10-20 | 2020-12-30 | Oyster Point Pharma Inc | Methods of treating ocular conditions |
| CN109310692B (zh) | 2016-04-07 | 2022-01-25 | 奥伊斯特普安生物制药公司 | 治疗眼部病状的方法 |
| TW202019417A (zh) | 2018-07-10 | 2020-06-01 | 美商奧伊斯特普安生物製藥公司 | 治療眼部症狀之正向異位調節劑與菸鹼乙醯膽鹼受體促效劑之組合 |
| TW202019424A (zh) | 2018-07-10 | 2020-06-01 | 美商奧伊斯特普安生物製藥公司 | 治療眼部症狀之方法 |
| 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 |
| CN117355307A (zh) * | 2021-05-07 | 2024-01-05 | 奥伊斯特普安生物制药公司 | 载体与烟碱激动剂的协同疗法 |
| 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 |
| WO2004039366A1 (en) | 2002-11-01 | 2004-05-13 | 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 |
| TWI405763B (zh) | 2006-11-02 | 2013-08-21 | 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 |
| AU2008211613B2 (en) | 2007-02-02 | 2013-05-23 | Pfizer Products Inc. | Tricyclic compounds and their use as glucocorticoid receptor modulators |
| 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 |
| WO2010028033A1 (en) | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclooctanes and uses thereof |
| WO2010028011A1 (en) | 2008-09-05 | 2010-03-11 | Targacept, Inc. | Amides of diazabicyclononanes and uses thereof |
| JP2012505834A (ja) * | 2008-10-14 | 2012-03-08 | サイコジェニックス・インコーポレーテッド | ニコチン性アセチルコリン受容体リガンドおよびその使用 |
| 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 |
| PL3279195T3 (pl) | 2008-12-01 | 2020-12-14 | Oyster Point Pharma, Inc. | Synteza i nowe postacie soli (R)-5-((E)-2-pirolidyn-3-ylowinylo)pirymidyny |
| US9145396B2 (en) * | 2008-12-01 | 2015-09-29 | Targacept, Inc. | Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine |
| CN102802630A (zh) * | 2009-06-17 | 2012-11-28 | 塔加西普特公司 | 通过神经元烟碱受体配体逆转左旋多巴诱导的运动障碍 |
| 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 |
| JP6162705B2 (ja) | 2011-10-20 | 2017-07-12 | ノバルティス アーゲー | アルファ７ニコチン性アセチルコリン受容体活性化剤による処置に対する応答性を予測するバイオマーカー |
| CN104094114A (zh) | 2011-11-30 | 2014-10-08 | 黛尔格诺斯蒂尔有限公司 | 干眼诊断 |
| SG10202011669PA (en) | 2014-10-20 | 2020-12-30 | Oyster Point Pharma Inc | Methods of treating ocular conditions |
| CN109310692B (zh) | 2016-04-07 | 2022-01-25 | 奥伊斯特普安生物制药公司 | 治疗眼部病状的方法 |
-
2017
- 2017-04-06 CN CN201780034734.3A patent/CN109310692B/zh active Active
- 2017-04-06 AU AU2017248276A patent/AU2017248276B2/en active Active
- 2017-04-06 MX MX2018012230A patent/MX385698B/es unknown
- 2017-04-06 SG SG11201808650QA patent/SG11201808650QA/en unknown
- 2017-04-06 US US16/091,830 patent/US10709707B2/en active Active
- 2017-04-06 DK DK17718304.3T patent/DK3439661T3/da active
- 2017-04-06 EP EP17718304.3A patent/EP3439661B1/en active Active
- 2017-04-06 IL IL299204A patent/IL299204A/en unknown
- 2017-04-06 PT PT177183043T patent/PT3439661T/pt unknown
- 2017-04-06 TW TW106111559A patent/TWI790997B/zh active
- 2017-04-06 TW TW112102845A patent/TWI876258B/zh active
- 2017-04-06 KR KR1020187032218A patent/KR102485299B1/ko active Active
- 2017-04-06 EP EP21189296.3A patent/EP3970724A1/en active Pending
- 2017-04-06 MY MYPI2018001700A patent/MY199237A/en unknown
- 2017-04-06 JP JP2018553080A patent/JP7090551B2/ja active Active
- 2017-04-06 NZ NZ746468A patent/NZ746468A/en unknown
- 2017-04-06 KR KR1020237000103A patent/KR102512777B1/ko active Active
- 2017-04-06 EA EA201892265A patent/EA201892265A1/ru unknown
- 2017-04-06 CN CN202210034408.5A patent/CN114533737B/zh 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 ES ES17718304T patent/ES2893126T3/es 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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