SK278577B6 - Use of 6-(2-(4-(bis(4-fluorophenyl)methylene)-1- -piperidinyl)ethyl)-7-methyl-5h-thiazolo£3,2-a|pyrimidin-5-one - Google Patents

Use of 6-(2-(4-(bis(4-fluorophenyl)methylene)-1- -piperidinyl)ethyl)-7-methyl-5h-thiazolo£3,2-a|pyrimidin-5-one Download PDF

Info

Publication number: SK278577B6
Authority: SK; Slovakia
Prior art keywords: thiazolo; pyrimidin; piperidinyl; fluorophenyl; bis
Prior art date: 1990-06-13

Application number

SK1780-91A

Other languages

English (en)

Slovak (sk)

Inventor

Theo Frans Meert

Original Assignee

Theo Frans Meert

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.)

1990-06-13

Filing date

1991-06-11

Publication date

1997-10-08

1991-06-11 Application filed by Theo Frans Meert filed Critical Theo Frans Meert

1997-10-08 Publication of SK278577B6 publication Critical patent/SK278577B6/sk

Links

BDTRIDKONHOQQN-UHFFFAOYSA-N 4h-pyrimidin-5-one Chemical compound O=C1CN=CN=C1 BDTRIDKONHOQQN-UHFFFAOYSA-N 0.000 title abstract 2
239000003814 drug Substances 0.000 claims abstract description 25
229940079593 drug Drugs 0.000 claims abstract description 23
208000024891 symptom Diseases 0.000 claims abstract description 9
239000002253 acid Substances 0.000 claims abstract description 7
150000003839 salts Chemical class 0.000 claims abstract description 7
JUQLTPCYUFPYKE-UHFFFAOYSA-N ritanserin Chemical compound CC=1N=C2SC=CN2C(=O)C=1CCN(CC1)CCC1=C(C=1C=CC(F)=CC=1)C1=CC=C(F)C=C1 JUQLTPCYUFPYKE-UHFFFAOYSA-N 0.000 claims description 21
206010012335 Dependence Diseases 0.000 claims description 9
-1 (4-fluorophenyl) methylene Chemical group 0.000 claims description 8
208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 4
238000004519 manufacturing process Methods 0.000 claims description 2
239000000654 additive Substances 0.000 abstract 1
230000000996 additive effect Effects 0.000 abstract 1
ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 27
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 17
229950009626 ritanserin Drugs 0.000 description 17
229960003920 cocaine Drugs 0.000 description 13
229960002428 fentanyl Drugs 0.000 description 9
PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 description 9
230000037396 body weight Effects 0.000 description 8
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
241000700159 Rattus Species 0.000 description 6
150000001875 compounds Chemical class 0.000 description 4
206010013663 drug dependence Diseases 0.000 description 4
239000012530 fluid Substances 0.000 description 4
238000002360 preparation method Methods 0.000 description 4
239000000243 solution Substances 0.000 description 4
208000011117 substance-related disease Diseases 0.000 description 4
206010063659 Aversion Diseases 0.000 description 3
241001465754 Metazoa Species 0.000 description 3
239000004480 active ingredient Substances 0.000 description 3
239000003795 chemical substances by application Substances 0.000 description 3
230000007423 decrease Effects 0.000 description 3
239000012453 solvate Substances 0.000 description 3
239000000126 substance Substances 0.000 description 3
SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 2
244000025254 Cannabis sativa Species 0.000 description 2
235000012766 Cannabis sativa ssp. sativa var. sativa Nutrition 0.000 description 2
235000012765 Cannabis sativa ssp. sativa var. spontanea Nutrition 0.000 description 2
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
206010028813 Nausea Diseases 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
150000007513 acids Chemical class 0.000 description 2
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 2
230000003247 decreasing effect Effects 0.000 description 2
230000001419 dependent effect Effects 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000000380 hallucinogen Substances 0.000 description 2
239000000203 mixture Substances 0.000 description 2
230000008693 nausea Effects 0.000 description 2
229960002715 nicotine Drugs 0.000 description 2
SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 2
229940127240 opiate Drugs 0.000 description 2
WEXRUCMBJFQVBZ-UHFFFAOYSA-N pentobarbital Chemical compound CCCC(C)C1(CC)C(=O)NC(=O)NC1=O WEXRUCMBJFQVBZ-UHFFFAOYSA-N 0.000 description 2
239000000021 stimulant Substances 0.000 description 2
LODHFNUFVRVKTH-ZHACJKMWSA-N 2-hydroxy-n'-[(e)-3-phenylprop-2-enoyl]benzohydrazide Chemical compound OC1=CC=CC=C1C(=O)NNC(=O)\C=C\C1=CC=CC=C1 LODHFNUFVRVKTH-ZHACJKMWSA-N 0.000 description 1
BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 description 1
125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 1
208000019901 Anxiety disease Diseases 0.000 description 1
208000004547 Hallucinations Diseases 0.000 description 1
239000004866 Hashish Substances 0.000 description 1
206010019233 Headaches Diseases 0.000 description 1
GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 description 1
IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical group C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 description 1
241000208125 Nicotiana Species 0.000 description 1
235000002637 Nicotiana tabacum Nutrition 0.000 description 1
GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
239000008896 Opium Substances 0.000 description 1
YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Natural products OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 1
206010044565 Tremor Diseases 0.000 description 1
206010047700 Vomiting Diseases 0.000 description 1
235000013334 alcoholic beverage Nutrition 0.000 description 1
229960001391 alfentanil Drugs 0.000 description 1
229910000147 aluminium phosphate Inorganic materials 0.000 description 1
230000036506 anxiety Effects 0.000 description 1
230000004596 appetite loss Effects 0.000 description 1
229940125717 barbiturate Drugs 0.000 description 1
SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
229940092714 benzenesulfonic acid Drugs 0.000 description 1
229940049706 benzodiazepine Drugs 0.000 description 1
150000001557 benzodiazepines Chemical class 0.000 description 1
235000013361 beverage Nutrition 0.000 description 1
239000002775 capsule Substances 0.000 description 1
239000000969 carrier Substances 0.000 description 1
ANTSCNMPPGJYLG-UHFFFAOYSA-N chlordiazepoxide Chemical compound O=N=1CC(NC)=NC2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 ANTSCNMPPGJYLG-UHFFFAOYSA-N 0.000 description 1
ZHGASCUQXLPSDT-UHFFFAOYSA-N cyclohexanesulfonic acid Chemical compound OS(=O)(=O)C1CCCCC1 ZHGASCUQXLPSDT-UHFFFAOYSA-N 0.000 description 1
230000001627 detrimental effect Effects 0.000 description 1
229960002069 diamorphine Drugs 0.000 description 1
AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
208000035475 disorder Diseases 0.000 description 1
239000003937 drug carrier Substances 0.000 description 1
CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
231100000869 headache Toxicity 0.000 description 1
150000004677 hydrates Chemical class 0.000 description 1
235000021266 loss of appetite Nutrition 0.000 description 1
208000019017 loss of appetite Diseases 0.000 description 1
229940098779 methanesulfonic acid Drugs 0.000 description 1
238000000034 method Methods 0.000 description 1
150000007522 mineralic acids Chemical class 0.000 description 1
239000004081 narcotic agent Substances 0.000 description 1
229910017604 nitric acid Inorganic materials 0.000 description 1
229960001027 opium Drugs 0.000 description 1
150000007524 organic acids Chemical class 0.000 description 1
235000005985 organic acids Nutrition 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
229960001412 pentobarbital Drugs 0.000 description 1
239000008194 pharmaceutical composition Substances 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
239000000843 powder Substances 0.000 description 1
229960004889 salicylic acid Drugs 0.000 description 1
230000004936 stimulating effect Effects 0.000 description 1
239000000725 suspension Substances 0.000 description 1
230000009897 systematic effect Effects 0.000 description 1
238000010998 test method Methods 0.000 description 1
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
229940072690 valium Drugs 0.000 description 1
230000008673 vomiting 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence

Landscapes

Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Neurology (AREA)
Psychiatry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Addiction (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Hydrogenated Pyridines (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

SK1780-91A 1990-06-13 1991-06-11 Use of 6-(2-(4-(bis(4-fluorophenyl)methylene)-1- -piperidinyl)ethyl)-7-methyl-5h-thiazolo£3,2-a|pyrimidin-5-one SK278577B6 (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US53717590A	1990-06-13	1990-06-13

Publications (1)

Publication Number	Publication Date
SK278577B6 true SK278577B6 (en)	1997-10-08

Family

ID=24141527

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK1780-91A SK278577B6 (en)	1990-06-13	1991-06-11	Use of 6-(2-(4-(bis(4-fluorophenyl)methylene)-1- -piperidinyl)ethyl)-7-methyl-5h-thiazolo£3,2-a\|pyrimidin-5-one

Country Status (14)

Country	Link
EP (1)	EP0461705B1 (cs)
JP (1)	JPH04230218A (cs)
KR (1)	KR920000321A (cs)
AT (1)	ATE190488T1 (cs)
AU (1)	AU637502B2 (cs)
CA (1)	CA2044423A1 (cs)
CZ (1)	CZ279872B6 (cs)
DE (1)	DE69132036T2 (cs)
HU (1)	HU208080B (cs)
IE (1)	IE911996A1 (cs)
IL (1)	IL98444A (cs)
PT (1)	PT97961B (cs)
SK (1)	SK278577B6 (cs)
ZA (1)	ZA914501B (cs)

1991
- 1991-06-05 DE DE69132036T patent/DE69132036T2/de not_active Expired - Fee Related
- 1991-06-05 EP EP91201383A patent/EP0461705B1/en not_active Expired - Lifetime
- 1991-06-05 AT AT91201383T patent/ATE190488T1/de not_active IP Right Cessation
- 1991-06-11 JP JP3165147A patent/JPH04230218A/ja active Pending
- 1991-06-11 IL IL9844491A patent/IL98444A/en not_active IP Right Cessation
- 1991-06-11 CZ CS911780A patent/CZ279872B6/cs unknown
- 1991-06-11 AU AU78321/91A patent/AU637502B2/en not_active Ceased
- 1991-06-11 SK SK1780-91A patent/SK278577B6/sk unknown
- 1991-06-11 KR KR1019910009575A patent/KR920000321A/ko not_active Withdrawn
- 1991-06-12 IE IE199691A patent/IE911996A1/en unknown
- 1991-06-12 PT PT97961A patent/PT97961B/pt not_active IP Right Cessation
- 1991-06-12 ZA ZA914501A patent/ZA914501B/xx unknown
- 1991-06-12 CA CA002044423A patent/CA2044423A1/en not_active Abandoned
- 1991-06-13 HU HU911971A patent/HU208080B/hu not_active IP Right Cessation

Also Published As

Publication number	Publication date
DE69132036T2 (de)	2000-12-21
EP0461705A2 (en)	1991-12-18
HU208080B (en)	1993-08-30
IL98444A0 (en)	1992-07-15
PT97961B (pt)	1998-11-30
EP0461705B1 (en)	2000-03-15
AU637502B2 (en)	1993-05-27
ATE190488T1 (de)	2000-04-15
HUT60628A (en)	1992-10-28
CA2044423A1 (en)	1991-12-14
AU7832191A (en)	1991-12-19
PT97961A (pt)	1992-03-31
KR920000321A (ko)	1992-01-29
IE911996A1 (en)	1991-12-18
DE69132036D1 (de)	2000-04-20
HU911971D0 (en)	1991-12-30
CS178091A3 (en)	1992-02-19
ZA914501B (en)	1993-02-24
IL98444A (en)	1995-06-29
CZ279872B6 (cs)	1995-07-12
JPH04230218A (ja)	1992-08-19
EP0461705A3 (en)	1992-06-17

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EP0236684A2 (en)	1987-09-16	Galanthamine or analogues thereof for treating Alzheimer's disease
SK279237B6 (sk)	1998-08-05	Použitie amperozidu, 4-[4,4-bis(4-fluórfenyl)butyl
US5565455A (en)	1996-10-15	Method for treating substance abuse disorders
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US4978669A (en)	1990-12-18	Method of suppressing appetite by administration of tetrahydro-beta-carboline derivatives
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CH647515A5 (de)	1985-01-31	Substituierte s-triazinone bzw. thione.
US5397782A (en)	1995-03-14	Method of treating addiction to alcohol
US6221858B1 (en)	2001-04-24	Pyridyl-and pyrimidyl-piperazines in the treatment of substance abuse disorders
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AU626358B2 (en)	1992-07-30	Antiemesis ergoline derivatives
US5519044A (en)	1996-05-21	Use of 5HT-3 antagonists in preventing or reducing dependency on dependency-inducing agents
CZ217094A3 (en)	1995-03-15	Pharmaceutics which are antagonists of 5ht1a receptor for preparing a medicament for reducing symptoms caused by weaning or partial weaning of a person away from tobacco or nicotine use
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