IL118328A - Use of a combination of a selective antagonist for N-methyl-D-aspartate in the forebrain and an amplifier for re-stimulation to stimulate, in order to prepare a pharmaceutical preparation for the treatment of Parkinson's disease - Google Patents

Use of a combination of a selective antagonist for N-methyl-D-aspartate in the forebrain and an amplifier for re-stimulation to stimulate, in order to prepare a pharmaceutical preparation for the treatment of Parkinson's disease

Info

Publication number: IL118328A
Authority: IL; Israel
Prior art keywords: mmol; pharmaceutical composition; hydroxy; ethyl acetate; hexane
Prior art date: 1995-05-26

Application number

IL11832896A

Other languages

English (en)

Hebrew (he)

Other versions

IL118328A0 (en

Original Assignee

Pfizer

Priority date (The priority date 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 date listed.)

1995-05-26

Filing date

1996-05-20

Publication date

2001-06-14

1996-05-20 Application filed by Pfizer filed Critical Pfizer

1996-09-12 Publication of IL118328A0 publication Critical patent/IL118328A0/xx

2001-06-14 Publication of IL118328A publication Critical patent/IL118328A/en

Links

238000002360 preparation method Methods 0.000 title claims abstract description 111
239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 89
210000004129 prosencephalon Anatomy 0.000 title claims abstract description 77
239000003795 chemical substances by application Substances 0.000 title claims abstract description 55
230000002964 excitative effect Effects 0.000 title claims abstract description 54
208000018737 Parkinson disease Diseases 0.000 title claims abstract description 34
239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 title claims description 66
230000002708 enhancing effect Effects 0.000 title claims description 44
239000005557 antagonist Substances 0.000 claims abstract description 29
HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims abstract description 27
210000001103 thalamus Anatomy 0.000 claims abstract description 11
230000001965 increasing effect Effects 0.000 claims abstract description 9
210000002071 ventral thalamic nuclei Anatomy 0.000 claims abstract description 9
239000000203 mixture Substances 0.000 claims description 182
150000001875 compounds Chemical class 0.000 claims description 96
VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 60
WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 50
WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 50
230000000694 effects Effects 0.000 claims description 49
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239000003085 diluting agent Substances 0.000 claims description 33
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230000000648 anti-parkinson Effects 0.000 claims description 29
239000000939 antiparkinson agent Substances 0.000 claims description 29
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239000000556 agonist Substances 0.000 claims description 20
241000124008 Mammalia Species 0.000 claims description 19
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TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical group NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims description 15
239000003954 decarboxylase inhibitor Substances 0.000 claims description 15
-1 (1S,2S)-1-(4-hydroxy-3- methoxyphenyl)-2-(4- hydroxy- -phenylpiperidino)-1-propanol Chemical group 0.000 claims description 14
239000003814 drug Substances 0.000 claims description 14
101710096582 L-tyrosine decarboxylase Proteins 0.000 claims description 13
239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 13
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 claims description 12
CAGLIAGCBUSTQI-MGPUTAFESA-N 1-[(1s,2s)-1-hydroxy-1-(4-hydroxy-3-methoxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol Chemical group C1=C(O)C(OC)=CC([C@H](O)[C@H](C)N2CCC(O)(CC2)C=2C=CC=CC=2)=C1 CAGLIAGCBUSTQI-MGPUTAFESA-N 0.000 claims description 11
229910052739 hydrogen Inorganic materials 0.000 claims description 11
239000001257 hydrogen Substances 0.000 claims description 11
230000001225 therapeutic effect Effects 0.000 claims description 10
JGYVZUCCBOVDJE-MJGOQNOKSA-N (3r,4s)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]-3,4-dihydro-2h-chromene-4,7-diol Chemical group C1CN([C@H]2[C@H](C3=CC=C(O)C=C3OC2)O)CCC1(O)C1=CC=C(F)C=C1 JGYVZUCCBOVDJE-MJGOQNOKSA-N 0.000 claims description 9
150000003839 salts Chemical class 0.000 claims description 9
229940124597 therapeutic agent Drugs 0.000 claims description 9
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230000002195 synergetic effect Effects 0.000 claims description 7
125000000217 alkyl group Chemical group 0.000 claims description 6
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 6
239000003112 inhibitor Substances 0.000 claims description 6
239000003543 catechol methyltransferase inhibitor Substances 0.000 claims description 5
239000000221 dopamine uptake inhibitor Substances 0.000 claims description 5
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125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 5
BDERNNFJNOPAEC-UHFFFAOYSA-N 1-propanol Substances CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 4
229940044613 1-propanol Drugs 0.000 claims description 4
239000000048 adrenergic agonist Substances 0.000 claims description 4
229940126157 adrenergic receptor agonist Drugs 0.000 claims description 4
230000028436 dopamine uptake Effects 0.000 claims description 4
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
125000001475 halogen functional group Chemical group 0.000 claims description 4
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
239000003402 opiate agonist Substances 0.000 claims description 4
230000013275 serotonin uptake Effects 0.000 claims description 4
239000000674 adrenergic antagonist Substances 0.000 claims description 3
230000002301 combined effect Effects 0.000 claims description 3
229940123685 Monoamine oxidase inhibitor Drugs 0.000 claims description 2
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
239000002899 monoamine oxidase inhibitor Substances 0.000 claims description 2
125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
229910052760 oxygen Inorganic materials 0.000 claims description 2
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
125000001424 substituent group Chemical group 0.000 claims description 2
229910052717 sulfur Inorganic materials 0.000 claims description 2
PYRPUIOAVUHMPL-XLDGYAMZSA-N 4-[1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]piperidin-2-yl]phenol Chemical group C1([C@H](O)[C@H](C)N2C(CCCC2)C=2C=CC(O)=CC=2)=CC=C(O)C=C1 PYRPUIOAVUHMPL-XLDGYAMZSA-N 0.000 claims 2
102000034527 Retinoid X Receptors Human genes 0.000 claims 2
SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 2
FVOOPOSZDXPIMS-UHFFFAOYSA-N 3,4-dihydro-2h-chromen-2-ol Chemical group C1=CC=C2OC(O)CCC2=C1 FVOOPOSZDXPIMS-UHFFFAOYSA-N 0.000 claims 1
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XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 799
VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 774
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WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 122
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RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 107
CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 104
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HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 100
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YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 84
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OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 62
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VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 54
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238000000034 method Methods 0.000 description 41
FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 38
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Classifications

- G—PHYSICS
- G10—MUSICAL INSTRUMENTS; ACOUSTICS
- G10H—ELECTROPHONIC MUSICAL INSTRUMENTS; INSTRUMENTS IN WHICH THE TONES ARE GENERATED BY ELECTROMECHANICAL MEANS OR ELECTRONIC GENERATORS, OR IN WHICH THE TONES ARE SYNTHESISED FROM A DATA STORE
- G10H5/00—Instruments in which the tones are generated by means of electronic generators
- G10H5/10—Instruments in which the tones are generated by means of electronic generators using generation of non-sinusoidal basic tones, e.g. saw-tooth
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/582—Recycling of unreacted starting or intermediate materials

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Engineering & Computer Science (AREA)
Chemical & Material Sciences (AREA)
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Pharmacology & Pharmacy (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Organic Chemistry (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Multimedia (AREA)
Acoustics & Sound (AREA)
Physics & Mathematics (AREA)
Psychology (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicines Containing Plant Substances (AREA)
Hydrogenated Pyridines (AREA)
Orthopedics, Nursing, And Contraception (AREA)

IL11832896A 1995-05-26 1996-05-20 Use of a combination of a selective antagonist for N-methyl-D-aspartate in the forebrain and an amplifier for re-stimulation to stimulate, in order to prepare a pharmaceutical preparation for the treatment of Parkinson's disease IL118328A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
PCT/IB1995/000398 WO1996037226A2 (en)	1995-05-26	1995-05-26	Combinations for the treatment of parkinsonism containing selective nmda antagonists
HU9601419A HUP9601419A3 (en)	1995-05-26	1996-05-24	Synergetic pharmaceutical compositions for treating parkinson-disease

Publications (2)

Publication Number	Publication Date
IL118328A0 IL118328A0 (en)	1996-09-12
IL118328A true IL118328A (en)	2001-06-14

Family

ID=89994003

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL11832896A IL118328A (en)	1995-05-26	1996-05-20	Use of a combination of a selective antagonist for N-methyl-D-aspartate in the forebrain and an amplifier for re-stimulation to stimulate, in order to prepare a pharmaceutical preparation for the treatment of Parkinson's disease

Country Status (26)

Country	Link
US (1)	US6258827B1 (da)
EP (1)	EP0828513B1 (da)
JP (1)	JPH11505828A (da)
CN (1)	CN1159325A (da)
AT (1)	ATE258067T1 (da)
AU (1)	AU696258B2 (da)
BR (1)	BR9602485A (da)
CA (1)	CA2219911C (da)
CO (1)	CO4700422A1 (da)
CZ (1)	CZ283979B6 (da)
DE (1)	DE69532482T2 (da)
DK (1)	DK0828513T3 (da)
ES (1)	ES2211904T3 (da)
FI (1)	FI974323A (da)
HU (1)	HUP9601419A3 (da)
IL (1)	IL118328A (da)
MX (1)	MX9709112A (da)
NO (1)	NO962130L (da)
NZ (1)	NZ286656A (da)
PL (1)	PL314413A1 (da)
PT (1)	PT828513E (da)
RU (1)	RU2176145C2 (da)
SG (1)	SG45479A1 (da)
TR (1)	TR199600436A2 (da)
TW (1)	TW470740B (da)
WO (1)	WO1996037226A2 (da)

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GB2321190B (en) *	1997-01-16	2000-09-20	Britannia Pharmaceuticals Ltd	Pharmaceutical composition
IL134363A0 (en) *	1997-10-24	2001-04-30	Warner Lambert Co	Method for treating disease-related or drug-induced dyskinesias
US6362196B1 (en)	1999-10-29	2002-03-26	Merck & Co., Inc.	Method to treat pain utilizing benzimidazole NMDA/NR2B antagonists
US6432976B1 (en)	1999-10-29	2002-08-13	Merck & Co., Inc.	8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
US6291499B1 (en)	1999-10-29	2001-09-18	Merck & Co., Inc.	2-cyclohexyl benzimidazole NMDA/NR2B antagonists
US6380205B1 (en)	1999-10-29	2002-04-30	Merck & Co., Inc.	2-cyclohexyl quinazoline NMDA/NR2B antagonists
US6369076B1 (en)	1999-10-29	2002-04-09	Merck & Co. Inc.	5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
US6489477B1 (en)	1999-10-29	2002-12-03	Merck & Co., Inc.	2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists
US6476041B1 (en)	1999-10-29	2002-11-05	Merck & Co., Inc.	1,4 substituted piperidinyl NMDA/NR2B antagonists
US6495561B2 (en)	1999-10-29	2002-12-17	Merck & Co., Inc.	2-cyclohexyl imidazopyridine NMDA/NR2B antagonists
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1995
- 1995-05-26 WO PCT/IB1995/000398 patent/WO1996037226A2/en active IP Right Grant
- 1995-05-26 RU RU96109832/14A patent/RU2176145C2/ru not_active IP Right Cessation
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1996
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CO4700422A1 (es)	1998-12-29
CA2219911A1 (en)	1996-11-28
PL314413A1 (en)	1996-12-09
CZ152496A3 (cs)	1998-04-15
WO1996037226A2 (en)	1996-11-28
CN1159325A (zh)	1997-09-17
HU9601419D0 (en)	1996-07-29
US6258827B1 (en)	2001-07-10
WO1996037226A3 (en)	1996-12-27
JPH11505828A (ja)	1999-05-25
NO962130L (no)	1996-11-27
IL118328A0 (en)	1996-09-12
DE69532482D1 (de)	2004-02-26
MX9709112A (es)	1998-02-28
DE69532482T2 (de)	2004-11-25
DK0828513T3 (da)	2004-04-13
ES2211904T3 (es)	2004-07-16
PT828513E (pt)	2004-05-31
CA2219911C (en)	2004-07-27
FI974323A0 (fi)	1997-11-25
BR9602485A (pt)	1998-04-22
HUP9601419A3 (en)	1998-01-28
ATE258067T1 (de)	2004-02-15
EP0828513A2 (en)	1998-03-18
AU5451996A (en)	1996-12-05
NZ286656A (en)	2001-03-30
NO962130D0 (no)	1996-05-24
CZ283979B6 (cs)	1998-07-15
RU2176145C2 (ru)	2001-11-27
SG45479A1 (en)	1998-01-16
TR199600436A2 (tr)	1996-12-21
TW470740B (en)	2002-01-01
EP0828513B1 (en)	2004-01-21
HUP9601419A2 (en)	1997-09-29
FI974323A (fi)	1997-11-25
AU696258B2 (en)	1998-09-03

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2001-11-25	FF	Patent granted
2002-02-10	KB	Patent renewed
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