ES2234708T3 - Rivastigmina para el tratamiento de transtornos. - Google Patents
Rivastigmina para el tratamiento de transtornos.Info
- Publication number
- ES2234708T3 ES2234708T3 ES00992430T ES00992430T ES2234708T3 ES 2234708 T3 ES2234708 T3 ES 2234708T3 ES 00992430 T ES00992430 T ES 00992430T ES 00992430 T ES00992430 T ES 00992430T ES 2234708 T3 ES2234708 T3 ES 2234708T3
- Authority
- ES
- Spain
- Prior art keywords
- ethyl
- lower alkyl
- hydrogen
- rivastigmine
- 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.)
- Expired - Lifetime
Links
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 title description 24
- 229960004136 rivastigmine Drugs 0.000 title description 24
- 150000001875 compounds Chemical class 0.000 claims abstract description 15
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 13
- 150000003839 salts Chemical class 0.000 claims abstract description 11
- 206010067013 Normal tension glaucoma Diseases 0.000 claims abstract description 9
- 239000002253 acid Substances 0.000 claims abstract description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 9
- 239000001257 hydrogen Substances 0.000 claims abstract description 9
- 201000002978 low tension glaucoma Diseases 0.000 claims abstract description 9
- 239000012458 free base Substances 0.000 claims abstract description 7
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims abstract description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims abstract description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims abstract description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims abstract description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- CPEONABTMRSIKA-UHFFFAOYSA-N 1,4$l^{2}-oxazinane Chemical compound C1COCC[N]1 CPEONABTMRSIKA-UHFFFAOYSA-N 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-M L-tartrate(1-) Chemical compound OC(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-M 0.000 claims description 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 235000002906 tartaric acid Nutrition 0.000 claims description 2
- 239000011975 tartaric acid Substances 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract description 6
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical compound C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 230000004410 intraocular pressure Effects 0.000 description 22
- 239000003814 drug Substances 0.000 description 11
- 229940079593 drug Drugs 0.000 description 10
- 238000005259 measurement Methods 0.000 description 9
- 241001465754 Metazoa Species 0.000 description 6
- 239000000243 solution Substances 0.000 description 5
- 208000010412 Glaucoma Diseases 0.000 description 4
- 210000001747 pupil Anatomy 0.000 description 4
- 230000000699 topical effect Effects 0.000 description 4
- 210000004087 cornea Anatomy 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 150000002431 hydrogen Chemical group 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229940053973 novocaine Drugs 0.000 description 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 2
- PIJVFDBKTWXHHD-HIFRSBDPSA-N physostigmine Chemical class C12=CC(OC(=O)NC)=CC=C2N(C)[C@@H]2[C@@]1(C)CCN2C PIJVFDBKTWXHHD-HIFRSBDPSA-N 0.000 description 2
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 102100033639 Acetylcholinesterase Human genes 0.000 description 1
- 108010022752 Acetylcholinesterase Proteins 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 108010053652 Butyrylcholinesterase Proteins 0.000 description 1
- 102100032404 Cholinesterase Human genes 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- 206010030348 Open-Angle Glaucoma Diseases 0.000 description 1
- PIJVFDBKTWXHHD-UHFFFAOYSA-N Physostigmine Natural products C12=CC(OC(=O)NC)=CC=C2N(C)C2C1(C)CCN2C PIJVFDBKTWXHHD-UHFFFAOYSA-N 0.000 description 1
- 206010047163 Vasospasm Diseases 0.000 description 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 1
- 229960004373 acetylcholine Drugs 0.000 description 1
- 229940022698 acetylcholinesterase Drugs 0.000 description 1
- 210000001742 aqueous humor Anatomy 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 210000000795 conjunctiva Anatomy 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 210000003560 epithelium corneal Anatomy 0.000 description 1
- 230000036543 hypotension Effects 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000000626 neurodegenerative effect Effects 0.000 description 1
- 230000000324 neuroprotective effect Effects 0.000 description 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 210000001328 optic nerve Anatomy 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- PWXJULSLLONQHY-UHFFFAOYSA-N phenylcarbamic acid Chemical class OC(=O)NC1=CC=CC=C1 PWXJULSLLONQHY-UHFFFAOYSA-N 0.000 description 1
- 229960001697 physostigmine Drugs 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 210000001525 retina Anatomy 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 238000002691 topical anesthesia Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 125000002948 undecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
-
- 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
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99120678 | 1999-10-19 | ||
| EP99120678 | 1999-10-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2234708T3 true ES2234708T3 (es) | 2005-07-01 |
Family
ID=8239225
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES00992430T Expired - Lifetime ES2234708T3 (es) | 1999-10-19 | 2000-10-17 | Rivastigmina para el tratamiento de transtornos. |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US6534541B1 (enExample) |
| EP (1) | EP1225890B1 (enExample) |
| JP (1) | JP2003512324A (enExample) |
| AR (1) | AR026062A1 (enExample) |
| AT (1) | ATE285764T1 (enExample) |
| AU (1) | AU766001B2 (enExample) |
| CA (1) | CA2384690C (enExample) |
| DE (1) | DE60017174T2 (enExample) |
| DK (1) | DK1225890T3 (enExample) |
| ES (1) | ES2234708T3 (enExample) |
| NZ (1) | NZ518164A (enExample) |
| PT (1) | PT1225890E (enExample) |
| WO (1) | WO2001028553A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2237163T3 (es) | 1998-10-01 | 2005-07-16 | Novartis Ag | Nuevas formulaciones orales de revastigmina de liberacion controlada. |
| US9993558B2 (en) | 2004-10-01 | 2018-06-12 | Ramscor, Inc. | Sustained release eye drop formulations |
| US8541413B2 (en) * | 2004-10-01 | 2013-09-24 | Ramscor, Inc. | Sustained release eye drop formulations |
| WO2009022345A1 (en) * | 2007-08-14 | 2009-02-19 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Phenyl carbamates for the treatment of multiple sclerosis |
| US12478503B2 (en) | 2009-05-18 | 2025-11-25 | Glaukos Corporation | Implants with controlled drug delivery features and methods of using same |
| US10206813B2 (en) | 2009-05-18 | 2019-02-19 | Dose Medical Corporation | Implants with controlled drug delivery features and methods of using same |
| WO2011151359A1 (en) | 2010-06-02 | 2011-12-08 | Noscira, S.A. | Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative |
| CN107417574B (zh) * | 2017-03-21 | 2019-12-03 | 浙江省医学科学院 | 2,4-双取代苯乙酮化合物及其旋光异构体、药学上可接受的盐及应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL74497A (en) | 1985-03-05 | 1990-02-09 | Proterra Ag | Pharmaceutical compositions containing phenyl carbamate derivatives and certain phenyl carbamate derivatives |
| HU201906B (en) * | 1987-03-04 | 1991-01-28 | Sandoz Ag | Process for producing phenyl-carbamate derivative and acid additional salts and pharmaceutical compositions containing them |
| US4900748A (en) | 1988-03-04 | 1990-02-13 | The United States Of America As Represented By The Department Of Health And Human Services | Carbamates related to (-)-physostigmine as cholinergic agents |
| JP3708957B2 (ja) | 1991-09-26 | 2005-10-19 | アメリカ合衆国 | （−）−エゼロリン、（−）−ｎ１−ノルエゼロリンおよび（−）−ｎ１−ベンジルノルエゼロリンの置換フェンゼリンおよびフェニルカルバミン酸塩：特異的アセチルコリンエステラーゼ阻害薬としての使用 |
| ES2206449T3 (es) | 1991-09-26 | 2004-05-16 | The Government Of The Usa As Represented By The Secretary Of Department Of Health And Human Services | Inhibidores de colinesterasas, composiciones farmaceuticas y sus usos. |
| AU1138097A (en) * | 1995-12-22 | 1997-07-17 | Alcon Laboratories, Inc. | Combinations of prostaglandins and miotics for lowering intraocular pressure |
-
2000
- 2000-10-11 US US09/686,025 patent/US6534541B1/en not_active Expired - Fee Related
- 2000-10-17 ES ES00992430T patent/ES2234708T3/es not_active Expired - Lifetime
- 2000-10-17 PT PT00992430T patent/PT1225890E/pt unknown
- 2000-10-17 EP EP00992430A patent/EP1225890B1/en not_active Expired - Lifetime
- 2000-10-17 AU AU28349/01A patent/AU766001B2/en not_active Ceased
- 2000-10-17 JP JP2001531383A patent/JP2003512324A/ja active Pending
- 2000-10-17 DE DE60017174T patent/DE60017174T2/de not_active Expired - Lifetime
- 2000-10-17 AR ARP000105450A patent/AR026062A1/es unknown
- 2000-10-17 AT AT00992430T patent/ATE285764T1/de active
- 2000-10-17 WO PCT/EP2000/010234 patent/WO2001028553A1/en not_active Ceased
- 2000-10-17 NZ NZ518164A patent/NZ518164A/en not_active IP Right Cessation
- 2000-10-17 DK DK00992430T patent/DK1225890T3/da active
- 2000-10-17 CA CA2384690A patent/CA2384690C/en not_active Expired - Fee Related
-
2003
- 2003-01-23 US US10/349,718 patent/US6835748B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US6835748B2 (en) | 2004-12-28 |
| PT1225890E (pt) | 2005-05-31 |
| JP2003512324A (ja) | 2003-04-02 |
| AR026062A1 (es) | 2002-12-26 |
| NZ518164A (en) | 2003-10-31 |
| EP1225890B1 (en) | 2004-12-29 |
| DK1225890T3 (da) | 2005-04-04 |
| WO2001028553A1 (en) | 2001-04-26 |
| DE60017174T2 (de) | 2005-12-22 |
| US20030119832A1 (en) | 2003-06-26 |
| US6534541B1 (en) | 2003-03-18 |
| AU2834901A (en) | 2001-04-30 |
| CA2384690C (en) | 2010-08-17 |
| DE60017174D1 (de) | 2005-02-03 |
| ATE285764T1 (de) | 2005-01-15 |
| EP1225890A1 (en) | 2002-07-31 |
| AU766001B2 (en) | 2003-10-09 |
| CA2384690A1 (en) | 2001-04-26 |
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