JP2012525437A5 - - Google Patents
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- Publication number
- JP2012525437A5 JP2012525437A5 JP2012508764A JP2012508764A JP2012525437A5 JP 2012525437 A5 JP2012525437 A5 JP 2012525437A5 JP 2012508764 A JP2012508764 A JP 2012508764A JP 2012508764 A JP2012508764 A JP 2012508764A JP 2012525437 A5 JP2012525437 A5 JP 2012525437A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- purin
- dihydroxytetrahydrofuran
- formula
- bicyclic
- 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
- 150000001875 compounds Chemical class 0.000 claims 35
- LRMHVVPPGGOAJQ-UHFFFAOYSA-N methyl nitrate Chemical compound CO[N+]([O-])=O LRMHVVPPGGOAJQ-UHFFFAOYSA-N 0.000 claims 9
- 230000004410 intraocular pressure Effects 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 5
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- AQLVRTWKJDTWQQ-SDBHATRESA-N [(2r,3s,4r,5r)-5-[6-(cyclopentylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl nitrate Chemical compound O[C@@H]1[C@H](O)[C@@H](CO[N+]([O-])=O)O[C@H]1N1C2=NC=NC(NC3CCCC3)=C2N=C1 AQLVRTWKJDTWQQ-SDBHATRESA-N 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- DZXBHDRHRFLQCJ-UHFFFAOYSA-M sodium;methyl sulfate Chemical compound [Na+].COS([O-])(=O)=O DZXBHDRHRFLQCJ-UHFFFAOYSA-M 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- CHNUOJQWGUIOLD-NFZZJPOKSA-N epalrestat Chemical compound C=1C=CC=CC=1\C=C(/C)\C=C1/SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-NFZZJPOKSA-N 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 229940122072 Carbonic anhydrase inhibitor Drugs 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 102000004310 Ion Channels Human genes 0.000 claims 1
- 206010067013 Normal tension glaucoma Diseases 0.000 claims 1
- 206010030348 Open-Angle Glaucoma Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 229940097320 beta blocking agent Drugs 0.000 claims 1
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 claims 1
- JNGZXGGOCLZBFB-IVCQMTBJSA-N compound E Chemical compound N([C@@H](C)C(=O)N[C@@H]1C(N(C)C2=CC=CC=C2C(C=2C=CC=CC=2)=N1)=O)C(=O)CC1=CC(F)=CC(F)=C1 JNGZXGGOCLZBFB-IVCQMTBJSA-N 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 201000002978 low tension glaucoma Diseases 0.000 claims 1
- JZMJDSHXVKJFKW-UHFFFAOYSA-M methyl sulfate(1-) Chemical compound COS([O-])(=O)=O JZMJDSHXVKJFKW-UHFFFAOYSA-M 0.000 claims 1
- 239000003604 miotic agent Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 239000004090 neuroprotective agent Substances 0.000 claims 1
- 239000002504 physiological saline solution Substances 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims 1
- 239000003590 rho kinase inhibitor Substances 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17465509P | 2009-05-01 | 2009-05-01 | |
| US61/174,655 | 2009-05-01 | ||
| US21999009P | 2009-06-24 | 2009-06-24 | |
| US61/219,990 | 2009-06-24 | ||
| PCT/US2010/033112 WO2010127210A1 (en) | 2009-05-01 | 2010-04-30 | Method of reducing intraocular pressure in humans |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012525437A JP2012525437A (ja) | 2012-10-22 |
| JP2012525437A5 true JP2012525437A5 (enExample) | 2013-06-20 |
| JP5778663B2 JP5778663B2 (ja) | 2015-09-16 |
Family
ID=43030847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012508764A Expired - Fee Related JP5778663B2 (ja) | 2009-05-01 | 2010-04-30 | ヒトの眼圧を低下させるための医薬組成物 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US8470800B2 (enExample) |
| EP (1) | EP2424546B1 (enExample) |
| JP (1) | JP5778663B2 (enExample) |
| KR (1) | KR101757940B1 (enExample) |
| CN (1) | CN102413832B (enExample) |
| AU (1) | AU2010242943B2 (enExample) |
| BR (1) | BRPI1009971A2 (enExample) |
| CA (1) | CA2762064A1 (enExample) |
| CL (1) | CL2011002675A1 (enExample) |
| DK (1) | DK2424546T3 (enExample) |
| EA (1) | EA024042B1 (enExample) |
| ES (1) | ES2554684T3 (enExample) |
| HR (1) | HRP20151200T1 (enExample) |
| HU (1) | HUE028068T2 (enExample) |
| IL (1) | IL216081A (enExample) |
| MX (1) | MX2011011229A (enExample) |
| MY (1) | MY159244A (enExample) |
| NZ (1) | NZ596428A (enExample) |
| PL (1) | PL2424546T3 (enExample) |
| PT (1) | PT2424546E (enExample) |
| RS (1) | RS54378B1 (enExample) |
| SG (1) | SG175346A1 (enExample) |
| SI (1) | SI2424546T1 (enExample) |
| SM (1) | SMT201500295B (enExample) |
| WO (1) | WO2010127210A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102008062567A1 (de) | 2008-12-16 | 2010-06-17 | Bayer Schering Pharma Aktiengesellschaft | Dipeptoid-Prodrugs und ihre Verwendung |
| DE102009006602A1 (de) * | 2009-01-29 | 2010-08-05 | Bayer Schering Pharma Aktiengesellschaft | Alkylamino-substituierte Dicyanopyridine und deren Aminosäureester-Prodrugs |
| CN102665730A (zh) * | 2009-10-26 | 2012-09-12 | 伊诺泰克制药公司 | 眼用制剂及其制造方法 |
| BR112012017106A2 (pt) * | 2010-01-11 | 2018-05-29 | Inotek Pharmaceuticals Corp | combinação, kit e método de redução de pressão intraocular. |
| HUE031529T2 (en) * | 2010-03-19 | 2017-07-28 | Inotek Pharmaceuticals Corp | Combination compositions of adenosine a1 agonists and carbonic anhydrase inhibitors for reducing intraocular pressure |
| JP2013522323A (ja) * | 2010-03-19 | 2013-06-13 | イノテック ファーマシューティカルズ コーポレイション | 眼内圧を下げるためのアデノシンA1受容体アゴニストと非選択的β−アドレナリン受容体遮断薬との組合せ組成物 |
| JP2013523739A (ja) | 2010-03-26 | 2013-06-17 | イノテック ファーマシューティカルズ コーポレイション | N6−シクロペンチルアデノシン(cpa)、cpa誘導体またはそれらのプロドラッグを用いてヒトにおける眼内圧を低下させる方法 |
| DE102010030688A1 (de) | 2010-06-30 | 2012-01-05 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Dicyanopyridine und ihre Verwendung |
| US20120058983A1 (en) * | 2010-09-02 | 2012-03-08 | Bayer Pharma Aktiengesellschaft | Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension |
| NZ627778A (en) * | 2012-01-26 | 2017-01-27 | Inotek Pharmaceuticals Corp | Anhydrous polymorphs of (2r,3s,4r,5r)-5-(6-(cyclopentylamino)-9h-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)} methyl nitrate and processes of preparation thereof |
| AU2014239222A1 (en) | 2013-03-15 | 2015-10-01 | Inotek Pharmaceuticals Corporation | Ophthalmic formulations |
| JP2018501219A (ja) * | 2014-12-03 | 2018-01-18 | イノテック ファーマシューティカルズ コーポレイション | 黄斑変性の予防、軽減または治療方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101010085B (zh) * | 2004-05-26 | 2012-12-26 | 伊诺泰克制药公司 | 嘌呤衍生物作为腺苷a1受体激动剂及其用法 |
| PT1758596E (pt) * | 2004-05-26 | 2010-06-23 | Inotek Pharmaceuticals Corp | Derivados de purina como agonistas do receptor de adenosina a1 e processos para a sua utilização |
| AU2006320578B2 (en) * | 2005-11-30 | 2013-01-31 | Inotek Pharmaceuticals Corporation | Purine derivatives and methods of use thereof |
| CN102665730A (zh) * | 2009-10-26 | 2012-09-12 | 伊诺泰克制药公司 | 眼用制剂及其制造方法 |
| BR112012017106A2 (pt) * | 2010-01-11 | 2018-05-29 | Inotek Pharmaceuticals Corp | combinação, kit e método de redução de pressão intraocular. |
| HUE031529T2 (en) * | 2010-03-19 | 2017-07-28 | Inotek Pharmaceuticals Corp | Combination compositions of adenosine a1 agonists and carbonic anhydrase inhibitors for reducing intraocular pressure |
| JP2013522323A (ja) * | 2010-03-19 | 2013-06-13 | イノテック ファーマシューティカルズ コーポレイション | 眼内圧を下げるためのアデノシンA1受容体アゴニストと非選択的β−アドレナリン受容体遮断薬との組合せ組成物 |
-
2010
- 2010-04-30 KR KR1020117025057A patent/KR101757940B1/ko not_active Expired - Fee Related
- 2010-04-30 CA CA2762064A patent/CA2762064A1/en not_active Abandoned
- 2010-04-30 AU AU2010242943A patent/AU2010242943B2/en not_active Ceased
- 2010-04-30 WO PCT/US2010/033112 patent/WO2010127210A1/en not_active Ceased
- 2010-04-30 NZ NZ596428A patent/NZ596428A/en not_active IP Right Cessation
- 2010-04-30 RS RS20150782A patent/RS54378B1/sr unknown
- 2010-04-30 SI SI201031070T patent/SI2424546T1/sl unknown
- 2010-04-30 SG SG2011078151A patent/SG175346A1/en unknown
- 2010-04-30 US US12/771,289 patent/US8470800B2/en not_active Expired - Fee Related
- 2010-04-30 ES ES10770402.5T patent/ES2554684T3/es active Active
- 2010-04-30 JP JP2012508764A patent/JP5778663B2/ja not_active Expired - Fee Related
- 2010-04-30 BR BRPI1009971A patent/BRPI1009971A2/pt not_active IP Right Cessation
- 2010-04-30 MX MX2011011229A patent/MX2011011229A/es unknown
- 2010-04-30 CN CN201080018539.XA patent/CN102413832B/zh not_active Expired - Fee Related
- 2010-04-30 EA EA201171339A patent/EA024042B1/ru not_active IP Right Cessation
- 2010-04-30 HR HRP20151200TT patent/HRP20151200T1/hr unknown
- 2010-04-30 DK DK10770402.5T patent/DK2424546T3/en active
- 2010-04-30 MY MYPI2011004858A patent/MY159244A/en unknown
- 2010-04-30 HU HUE10770402A patent/HUE028068T2/en unknown
- 2010-04-30 PT PT107704025T patent/PT2424546E/pt unknown
- 2010-04-30 PL PL10770402T patent/PL2424546T3/pl unknown
- 2010-04-30 EP EP10770402.5A patent/EP2424546B1/en active Active
-
2011
- 2011-10-27 CL CL2011002675A patent/CL2011002675A1/es unknown
- 2011-11-01 IL IL216081A patent/IL216081A/en not_active IP Right Cessation
-
2013
- 2013-04-03 US US13/855,919 patent/US20130217643A1/en not_active Abandoned
-
2015
- 2015-11-30 SM SM201500295T patent/SMT201500295B/it unknown
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