ECSP961815A - (1S, 2S) -1 - (4-HYDROXYPHENYL) METHANOSULPHONATE -2- (4-HYDROXY-4-PHENYLPIPERIDIN- 1-IL) -1- PROPANOL TRIHYDRATE - Google Patents
(1S, 2S) -1 - (4-HYDROXYPHENYL) METHANOSULPHONATE -2- (4-HYDROXY-4-PHENYLPIPERIDIN- 1-IL) -1- PROPANOL TRIHYDRATEInfo
- Publication number
- ECSP961815A ECSP961815A ECSP961815A ECSP961815A EC SP961815 A ECSP961815 A EC SP961815A EC SP961815 A ECSP961815 A EC SP961815A EC SP961815 A ECSP961815 A EC SP961815A
- Authority
- EC
- Ecuador
- Prior art keywords
- trihydrate
- salt
- phenylpiperidin
- hydroxyphenyl
- propanol
- Prior art date
Links
- -1 4-HYDROXYPHENYL Chemical class 0.000 title abstract 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N 1-propanol Substances CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 title abstract 2
- 229940044613 1-propanol Drugs 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 2
- 210000003169 central nervous system Anatomy 0.000 abstract 2
- 239000012458 free base Substances 0.000 abstract 2
- QEMSVZNTSXPFJA-HNAYVOBHSA-N 1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol Chemical compound C1([C@H](O)[C@H](C)N2CCC(O)(CC2)C=2C=CC=CC=2)=CC=C(O)C=C1 QEMSVZNTSXPFJA-HNAYVOBHSA-N 0.000 abstract 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 206010065040 AIDS dementia complex Diseases 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 201000006474 Brain Ischemia Diseases 0.000 abstract 1
- 206010008120 Cerebral ischaemia Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 208000023105 Huntington disease Diseases 0.000 abstract 1
- 208000013016 Hypoglycemia Diseases 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 208000007101 Muscle Cramp Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 208000005392 Spasm Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 208000029650 alcohol withdrawal Diseases 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 206010008118 cerebral infarction Diseases 0.000 abstract 1
- YKGMKSIHIVVYKY-UHFFFAOYSA-N dabrafenib mesylate Chemical compound CS(O)(=O)=O.S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 YKGMKSIHIVVYKY-UHFFFAOYSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000002218 hypoglycaemic effect Effects 0.000 abstract 1
- LKGCPYOBWLSCTK-UHFFFAOYSA-N methanesulfonic acid;trihydrate Chemical compound O.O.O.CS(O)(=O)=O LKGCPYOBWLSCTK-UHFFFAOYSA-N 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 230000009529 traumatic brain injury Effects 0.000 abstract 1
- 150000004684 trihydrates Chemical class 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Esta invención se refiere al nuevo y clinicamente ventajoso trihidrato de la sal metanosulfonato de (1s,2s)-1-(4-hidroxifenil)-2-(4-hidroxi-4-fenilpiperidin-1-il)-1-propanol (denominado en lo sucesivo como "sal de mesilato trihidrato"). Esta sal de sal mesilato trihidrato, asi como la correswpondiente mesilato anhidra y la base libre del (1s,2s)-1-(4-hidroxifenil)-2-4 hidroxi-4-fenilpiperidin-1-il)-1-propanol (denominado en lo sucesivo como el "mesilato anhidro" y la "base libre") exhibe actividad como antagonistas de los receptores de NMDA (ácido N-metil-D aspártico) y son útiles en le tratamiento de la epilepsia, ansiedad, isquemia cerebral, espasmos musculares, demencia multinfirtica, lesión cerebral traumática dolor demencia relacionada con el SIDA, hipoglucemia, migraña, esclerosis amiotrófica lateral adición a las drogas y al alcohol, síntomas de abstinencia del alcohol y de las drogas, condiciones psicóticas, incontienecia urinaria y enfermedades degenerativas del SNC (sistema nervioso central), tales como aplopejía, enfermedad de Alzheimer, enfermedad de Parkinson y enfermedad de Huntington.This invention relates to the new and clinically advantageous trihydrate of the methanesulfonate salt of (1s, 2s) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4-phenylpiperidin-1-yl) -1-propanol (called hereinafter referred to as "mesylate trihydrate salt"). This salt of mesylate trihydrate salt, as well as the corresponding anhydrous mesylate and the free base of (1s, 2s) -1- (4-hydroxyphenyl) -2-4 hydroxy-4-phenylpiperidin-1-yl) -1-propanol ( hereinafter referred to as "anhydrous mesylate" and "free base") exhibits activity as antagonists of NMDA (N-methyl-D aspartic acid) receptors and are useful in the treatment of epilepsy, anxiety, cerebral ischemia, muscle spasms, multinfied dementia, traumatic brain injury, pain, AIDS-related dementia, hypoglycemia, migraine, amyotrophic lateral sclerosis, addition to drugs and alcohol, symptoms of alcohol and drug withdrawal, psychotic conditions, urinary incontinence and degenerative diseases of the CNS (central nervous system), such as stroke, Alzheimer's disease, Parkinson's disease, and Huntington's disease.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP961815 ECSP961815A (en) | 1996-07-05 | 1996-07-05 | (1S, 2S) -1 - (4-HYDROXYPHENYL) METHANOSULPHONATE -2- (4-HYDROXY-4-PHENYLPIPERIDIN- 1-IL) -1- PROPANOL TRIHYDRATE |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP961815 ECSP961815A (en) | 1996-07-05 | 1996-07-05 | (1S, 2S) -1 - (4-HYDROXYPHENYL) METHANOSULPHONATE -2- (4-HYDROXY-4-PHENYLPIPERIDIN- 1-IL) -1- PROPANOL TRIHYDRATE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP961815A true ECSP961815A (en) | 1997-11-04 |
Family
ID=42042545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP961815 ECSP961815A (en) | 1996-07-05 | 1996-07-05 | (1S, 2S) -1 - (4-HYDROXYPHENYL) METHANOSULPHONATE -2- (4-HYDROXY-4-PHENYLPIPERIDIN- 1-IL) -1- PROPANOL TRIHYDRATE |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP961815A (en) |
-
1996
- 1996-07-05 EC ECSP961815 patent/ECSP961815A/en unknown
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