JP2004520329A5 - - Google Patents
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- Publication number
- JP2004520329A5 JP2004520329A5 JP2002554108A JP2002554108A JP2004520329A5 JP 2004520329 A5 JP2004520329 A5 JP 2004520329A5 JP 2002554108 A JP2002554108 A JP 2002554108A JP 2002554108 A JP2002554108 A JP 2002554108A JP 2004520329 A5 JP2004520329 A5 JP 2004520329A5
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- JP
- Japan
- Prior art keywords
- alkyl
- ring
- group
- atoms
- formula
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 69
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 48
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 43
- 125000001072 heteroaryl group Chemical group 0.000 claims 39
- -1 alkylene sulfonic acid Chemical compound 0.000 claims 36
- 125000000623 heterocyclic group Chemical group 0.000 claims 36
- 229910052760 oxygen Inorganic materials 0.000 claims 35
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 33
- 125000006413 ring segment Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 28
- 150000002431 hydrogen Chemical class 0.000 claims 28
- 229910052717 sulfur Chemical group 0.000 claims 25
- 125000005843 halogen group Chemical group 0.000 claims 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 20
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052757 nitrogen Inorganic materials 0.000 claims 17
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 16
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 15
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 125000005041 acyloxyalkyl group Chemical group 0.000 claims 13
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 13
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 12
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 12
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 12
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 12
- 125000004442 acylamino group Chemical group 0.000 claims 12
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims 12
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 12
- 125000004414 alkyl thio group Chemical group 0.000 claims 12
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 12
- 125000001589 carboacyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 239000001301 oxygen Substances 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 239000011593 sulfur Chemical group 0.000 claims 12
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 claims 12
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 12
- 230000004308 accommodation Effects 0.000 claims 11
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 11
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 125000004430 oxygen atom Chemical group O* 0.000 claims 11
- 125000004434 sulfur atom Chemical group 0.000 claims 11
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 9
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 9
- 125000004663 dialkyl amino group Chemical group 0.000 claims 9
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 8
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 8
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- 230000004410 intraocular pressure Effects 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 7
- 238000007363 ring formation reaction Methods 0.000 claims 7
- 238000006467 substitution reaction Methods 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 4
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 4
- 150000001450 anions Chemical class 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 239000009937 cyclo 3 Substances 0.000 claims 4
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 4
- 229920002554 vinyl polymer Chemical group 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 125000006543 azetidinylalkyl group Chemical group 0.000 claims 3
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 241001465754 Metazoa Species 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229910021386 carbon form Inorganic materials 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001713 cholinergic effect Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000000542 sulfonic acid group Chemical group 0.000 claims 1
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25942600P | 2000-12-29 | 2000-12-29 | |
| US29625701P | 2001-06-06 | 2001-06-06 | |
| US30741801P | 2001-07-24 | 2001-07-24 | |
| PCT/US2001/049550 WO2002053158A1 (en) | 2000-12-29 | 2001-12-28 | Method for treating glaucoma ib |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004520329A JP2004520329A (ja) | 2004-07-08 |
| JP2004520329A5 true JP2004520329A5 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2005-12-22 |
Family
ID=27401231
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002554108A Pending JP2004520329A (ja) | 2000-12-29 | 2001-12-28 | 緑内障ｉｂの治療方法 |
Country Status (9)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU780205B2 (en) * | 2000-02-23 | 2005-03-10 | Alteon Inc. | Thiazolium compounds and treatments of disorders associated with protein aging |
| WO2002008210A1 (en) * | 2000-07-13 | 2002-01-31 | Alteon, Inc. | Cyanomethyl substituted thiazoliums and imidazoliums and treatments of disorders associated with protein aging |
| US7049333B2 (en) | 2002-06-04 | 2006-05-23 | Sanofi-Aventis Deutschland Gmbh | Substituted thiophenes: compositions, processes of making, and uses in disease treatment and diagnosis |
| CN100349881C (zh) * | 2003-04-02 | 2007-11-21 | 深圳市东阳光实业发展有限公司 | 取代五元氮杂环盐类化合物及其治疗蛋白老化相关疾病的用途 |
| US20050014747A1 (en) * | 2003-04-18 | 2005-01-20 | Emily Reinhard | Dihydrothiazine prodrugs of thiazolium agents |
| EP1660457B1 (en) * | 2003-08-26 | 2011-09-28 | Ecole Polytechnique Fédérale de Lausanne (EPFL) | Ionic liquids based on imidazolium salts incorporating a nitrile functionality |
| AU2005230846A1 (en) | 2004-03-31 | 2005-10-20 | Lexicon Pharmaceuticals, Inc. | 2-aminomethylthiazole-5-carboxamides as protein kinase modulators |
| NZ552751A (en) | 2004-07-16 | 2010-11-26 | Sunesis Pharmaceuticals Inc | Thienopyrimidines useful as aurora kinase inhibitors |
| EP2308852A1 (de) | 2005-08-21 | 2011-04-13 | Abbott GmbH & Co. KG | 5-Ring-Heteroaromaten-Verbindungen und ihre Verwendung als Bindungspartner für 5-HT5-Rezeptoren |
| US10206813B2 (en) | 2009-05-18 | 2019-02-19 | Dose Medical Corporation | Implants with controlled drug delivery features and methods of using same |
| JP5848332B2 (ja) | 2010-05-14 | 2016-01-27 | マリンクロッド エルエルシー | 光学造影および療法のタンデムのための官能性架橋型ナノ構造物 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ200429A (en) * | 1981-04-30 | 1984-10-19 | Smith & Nephew Ass | Applicator for placing pharmaceutically active agent in contact with moist surface,e.g.,eye |
| US5140048A (en) * | 1984-03-19 | 1992-08-18 | The Rockefeller University | Inhibitors of nonenzymatic cross-linking |
| US5017696A (en) * | 1987-09-17 | 1991-05-21 | The Rockefeller University | Advanced glycosylation end products and associated methods |
| DK0458589T3 (da) * | 1990-05-22 | 1995-04-03 | R Tech Ueno Ltd | Behandling af okulær hypertension med en okulær synergistisk kombination |
| NZ239161A (en) * | 1990-07-31 | 1994-01-26 | Smithkline Beecham Corp | Substituted [1h-imidazol-5-yl] alkanoic acid derivatives; medicaments, |
| US5153205A (en) * | 1990-10-01 | 1992-10-06 | Merck & Co., Inc. | Method to reduce introacular pressure without causing miosis |
| US5300031A (en) * | 1991-06-07 | 1994-04-05 | Liebel-Flarsheim Company | Apparatus for injecting fluid into animals and disposable front loadable syringe therefor |
| NO315930B1 (no) * | 1995-01-18 | 2003-11-17 | Picower Inst For Medical Res T | Anvendelse av tiazoliumforbindelser ved fremstilling av farmasöytiske preparater, preparater som inneholder forbindelsene, samt nyetiazoliumforbindelser |
| WO1996022095A2 (en) * | 1995-01-18 | 1996-07-25 | Alteon Inc. | Use of thiazolium compounds for preventing and reversing the formation of advanced glycosylation endproducts |
| US5656261A (en) | 1995-01-18 | 1997-08-12 | The Picower Institute For Medical Research | Preventing and reversing advanced glycosylation endproducts |
| US5744451A (en) * | 1995-09-12 | 1998-04-28 | Warner-Lambert Company | N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity |
| US5854000A (en) * | 1995-11-15 | 1998-12-29 | Alteon Inc. | Methods for measurement predicated on the presence of advanced glycosylation endproducts in tobacco and its combustion byproducts |
| US6121300A (en) * | 1998-11-10 | 2000-09-19 | Wagle; Dilip R. | Reversing advanced glycosylation cross-links using heterocyclic-substituted thiazolium salts |
| CA2448276A1 (en) * | 2001-05-30 | 2002-12-05 | Alteon Inc. | Method for treating glaucoma vi |
| JP2004536807A (ja) * | 2001-05-30 | 2004-12-09 | アルテオン インコーポレイテッド | 緑内障ｖの治療方法 |
| CA2448294A1 (en) * | 2001-05-30 | 2002-12-05 | Alteon Inc. | Method for treating fibrotic diseases or other indications vi |
-
2001
- 2001-12-28 CA CA002433346A patent/CA2433346A1/en not_active Abandoned
- 2001-12-28 EP EP01988353A patent/EP1353669B1/en not_active Expired - Lifetime
- 2001-12-28 AU AU2002241670A patent/AU2002241670B2/en not_active Ceased
- 2001-12-28 JP JP2002554108A patent/JP2004520329A/ja active Pending
- 2001-12-28 MX MXPA03005922A patent/MXPA03005922A/es active IP Right Grant
- 2001-12-28 AT AT01988353T patent/ATE369856T1/de not_active IP Right Cessation
- 2001-12-28 DE DE60130030T patent/DE60130030T2/de not_active Expired - Fee Related
- 2001-12-28 WO PCT/US2001/049550 patent/WO2002053158A1/en active IP Right Grant
- 2001-12-31 US US10/038,112 patent/US7432254B2/en not_active Expired - Fee Related
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