ES8502977A1 - Un metodo de preparar profarmacos de pilocarpina - Google Patents
Un metodo de preparar profarmacos de pilocarpinaInfo
- Publication number
- ES8502977A1 ES8502977A1 ES525656A ES525656A ES8502977A1 ES 8502977 A1 ES8502977 A1 ES 8502977A1 ES 525656 A ES525656 A ES 525656A ES 525656 A ES525656 A ES 525656A ES 8502977 A1 ES8502977 A1 ES 8502977A1
- Authority
- ES
- Spain
- Prior art keywords
- group
- formula
- defined above
- image
- phenyl
- 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.)
- Expired
Links
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 title abstract 4
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 title abstract 4
- 229960001416 pilocarpine Drugs 0.000 title abstract 4
- 229940002612 prodrug Drugs 0.000 title abstract 2
- 239000000651 prodrug Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 239000001301 oxygen Substances 0.000 abstract 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 3
- 229910052717 sulfur Chemical group 0.000 abstract 3
- 239000011593 sulfur Chemical group 0.000 abstract 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005037 alkyl phenyl group Chemical group 0.000 abstract 1
- 210000004087 cornea Anatomy 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
METODO DE PREPARAR PROFARMACOS DE PILOCARPINA.CONSISTE EN HACER REACCIONAR UNA SAL DE ACIDO POLICARPICO, TAL COMO UNA SAL METALICA O UN COMPUESTO DE FORMULA (II) O UNA DE SUS SALES, CON UN COMPUESTO DE FORMULA (III), CON LA CONDICION DE QUE EN LA FORMULA (III) RA SEA DIFERENTE DE RK1 DE LA FORMULA (II), PARA OBTENER PROFARMACOS DE PILOCARPINA DE FORMULA (I), DONDE R1 ES UN GRUPO DE FORMULA (IV), (V) Y OTRAS; R3 ES ALQUILO, FENILO Y OTROS; R4 ES R3 Y OTROS; R5 Y R6 SON HIDROGENO O SIGNIFICAN IGUAL QUE R3; R2 ES H O R4; RA ES IGUAL QUE R3 Y OTRAS; ZA ES HIDROXI; H O UN GRUPO ELIMINABLE; RK1 ES OH O UN GRUPO R1; Y RK2 ES OH O UN GRUPO R2.TIENEN APLICACION PARA EL TRATAMIENTO DE GLAUCOMA.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK417082 | 1982-09-17 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES525656A0 ES525656A0 (es) | 1985-02-01 |
| ES8502977A1 true ES8502977A1 (es) | 1985-02-01 |
Family
ID=8130941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES525656A Expired ES8502977A1 (es) | 1982-09-17 | 1983-09-16 | Un metodo de preparar profarmacos de pilocarpina |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US4742073A (es) |
| EP (1) | EP0106541A3 (es) |
| JP (1) | JPS59130275A (es) |
| KR (1) | KR840006213A (es) |
| AU (1) | AU557083B2 (es) |
| CA (1) | CA1235416A (es) |
| ES (1) | ES8502977A1 (es) |
| IL (1) | IL69593A (es) |
| NZ (1) | NZ205617A (es) |
| PT (1) | PT77347B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU557083B2 (en) * | 1982-09-17 | 1986-12-04 | Hans Bundgaard | Pilocarpine prodrugs |
| DK406686D0 (da) * | 1986-08-26 | 1986-08-26 | Hans Bundgaard | Carboxylsyrederivater |
| US5066665A (en) * | 1990-05-21 | 1991-11-19 | Warner-Lambert Co. | Substituted isoxazolidin-3-ones and derivatives thereof acting at muscarinic receptors |
| US5066663A (en) * | 1990-05-21 | 1991-11-19 | Warner-Lambert Company | Substituted-hetero-cyclopentanones and cyclopentenones and derivatives thereof acting at muscarinic receptors |
| FI98815C (fi) | 1990-11-30 | 1997-08-25 | Santen Oy | Menetelmä uusien, farmakologisesti käyttökelpoisten bispilokarpiinihapon esterijohdannaisten valmistamiseksi |
| US5436350A (en) * | 1990-11-30 | 1995-07-25 | Jaervinen; Tomi | Bispilocarpic acid ester derivatives and process for their preparation |
| FI98910C (fi) | 1992-05-29 | 1997-09-10 | Santen Oy | Menetelmä farmaseuttisesti käyttökelpoisten pilokarpiinijohdannaisten valmistamiseksi |
| WO1993024466A1 (en) * | 1992-05-29 | 1993-12-09 | Leiras Oy | Novel pilocarpine derivatives and process for their preparation |
| US5521210A (en) * | 1993-04-13 | 1996-05-28 | Allergan, Inc. | Ophthalmic use of muscarinic agonists having increased duration of activity |
| CN115536641B (zh) * | 2022-09-29 | 2024-12-27 | 广州润尔眼科生物科技有限公司 | 一种内酯化合物及其制备方法与应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3470197A (en) * | 1967-08-30 | 1969-09-30 | Miles Lab | 1-substituted derivatives of 3-ethyl-4 - (1-methylimidazolyl-(5)-methyl)-2-pyrrolidinone |
| US3631059A (en) * | 1967-09-11 | 1971-12-28 | John T Goorley | Process for the extraction and purification of pilocarpine |
| US4045558A (en) * | 1975-10-08 | 1977-08-30 | Merck & Co., Inc. | Pilocarpine salts |
| US4061722A (en) * | 1976-04-26 | 1977-12-06 | Interx Research Corporation | Selected quaternary ammonium salts of pilocarpine useful in reducing intraocular pressure in warm-blooded animals |
| AU557083B2 (en) * | 1982-09-17 | 1986-12-04 | Hans Bundgaard | Pilocarpine prodrugs |
-
1983
- 1983-08-29 AU AU18494/83A patent/AU557083B2/en not_active Ceased
- 1983-08-29 IL IL69593A patent/IL69593A/xx unknown
- 1983-09-16 US US06/533,646 patent/US4742073A/en not_active Expired - Fee Related
- 1983-09-16 NZ NZ205617A patent/NZ205617A/en unknown
- 1983-09-16 ES ES525656A patent/ES8502977A1/es not_active Expired
- 1983-09-16 PT PT77347A patent/PT77347B/pt not_active IP Right Cessation
- 1983-09-16 JP JP58172052A patent/JPS59130275A/ja active Pending
- 1983-09-16 CA CA000436880A patent/CA1235416A/en not_active Expired
- 1983-09-16 EP EP83305437A patent/EP0106541A3/en not_active Withdrawn
- 1983-09-17 KR KR1019830004369A patent/KR840006213A/ko not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| AU1849483A (en) | 1984-03-22 |
| EP0106541A2 (en) | 1984-04-25 |
| IL69593A (en) | 1988-09-30 |
| CA1235416A (en) | 1988-04-19 |
| KR840006213A (ko) | 1984-11-22 |
| PT77347B (en) | 1986-03-11 |
| US4742073A (en) | 1988-05-03 |
| NZ205617A (en) | 1986-06-11 |
| JPS59130275A (ja) | 1984-07-26 |
| PT77347A (en) | 1983-10-01 |
| AU557083B2 (en) | 1986-12-04 |
| ES525656A0 (es) | 1985-02-01 |
| EP0106541A3 (en) | 1985-12-18 |
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