JPH0132806B2 - - Google Patents
Info
- Publication number
- JPH0132806B2 JPH0132806B2 JP55045784A JP4578480A JPH0132806B2 JP H0132806 B2 JPH0132806 B2 JP H0132806B2 JP 55045784 A JP55045784 A JP 55045784A JP 4578480 A JP4578480 A JP 4578480A JP H0132806 B2 JPH0132806 B2 JP H0132806B2
- Authority
- JP
- Japan
- Prior art keywords
- quinazolinone
- active
- isopropyl
- chloro
- muscle
- 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
- 239000013543 active substance Substances 0.000 claims description 36
- 206010052904 Musculoskeletal stiffness Diseases 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 13
- ZWOUXWWGKJBAHQ-UHFFFAOYSA-N fluproquazone Chemical compound N=1C(=O)N(C(C)C)C2=CC(C)=CC=C2C=1C1=CC=C(F)C=C1 ZWOUXWWGKJBAHQ-UHFFFAOYSA-N 0.000 claims description 12
- 238000002360 preparation method Methods 0.000 claims description 8
- 230000036592 analgesia Effects 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 239000002552 dosage form Substances 0.000 claims description 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- XFYDIVBRZNQMJC-UHFFFAOYSA-N tizanidine Chemical compound ClC=1C=CC2=NSN=C2C=1NC1=NCCN1 XFYDIVBRZNQMJC-UHFFFAOYSA-N 0.000 claims description 3
- VAFNJIFAZJWWNI-UHFFFAOYSA-N 1-(cyclopropylmethyl)-6-methoxy-4-phenylquinazolin-2-one Chemical compound O=C1N=C(C=2C=CC=CC=2)C2=CC(OC)=CC=C2N1CC1CC1 VAFNJIFAZJWWNI-UHFFFAOYSA-N 0.000 claims description 2
- HJICZLOIHNWNNY-UHFFFAOYSA-N 8-(4-fluorophenyl)-5-propan-2-yl-[1,3]dioxolo[4,5-g]quinazolin-6-one Chemical compound N=1C(=O)N(C(C)C)C2=CC=3OCOC=3C=C2C=1C1=CC=C(F)C=C1 HJICZLOIHNWNNY-UHFFFAOYSA-N 0.000 claims description 2
- FITUMOSFDCKONA-UHFFFAOYSA-N 8-phenyl-5-propan-2-yl-[1,3]dioxolo[4,5-g]quinazolin-6-one Chemical compound N=1C(=O)N(C(C)C)C2=CC=3OCOC=3C=C2C=1C1=CC=CC=C1 FITUMOSFDCKONA-UHFFFAOYSA-N 0.000 claims description 2
- 239000005964 Acibenzolar-S-methyl Substances 0.000 claims description 2
- JTIGKVIOEQASGT-UHFFFAOYSA-N proquazone Chemical compound N=1C(=O)N(C(C)C)C2=CC(C)=CC=C2C=1C1=CC=CC=C1 JTIGKVIOEQASGT-UHFFFAOYSA-N 0.000 claims description 2
- PDQRQJVPEFGVRK-UHFFFAOYSA-N 2,1,3-benzothiadiazole Chemical compound C1=CC=CC2=NSN=C21 PDQRQJVPEFGVRK-UHFFFAOYSA-N 0.000 claims 1
- SNEPLIKPVRZUFP-UHFFFAOYSA-N 5-chloro-n-(4,5-dihydro-1h-imidazol-2-yl)-7-methyl-2,1,3-benzothiadiazol-4-amine Chemical compound C12=NSN=C2C(C)=CC(Cl)=C1NC1=NCCN1 SNEPLIKPVRZUFP-UHFFFAOYSA-N 0.000 claims 1
- OAIZNWQBWDHNIH-UHFFFAOYSA-N 6-chloro-4-phenyl-1-(2,2,2-trifluoroethyl)quinazolin-2-one Chemical compound N=1C(=O)N(CC(F)(F)F)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 OAIZNWQBWDHNIH-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 description 19
- 238000012360 testing method Methods 0.000 description 14
- 208000002193 Pain Diseases 0.000 description 11
- 239000012190 activator Substances 0.000 description 11
- 230000036407 pain Effects 0.000 description 11
- AVRPFRMDMNDIDH-UHFFFAOYSA-N 1h-quinazolin-2-one Chemical compound C1=CC=CC2=NC(O)=NC=C21 AVRPFRMDMNDIDH-UHFFFAOYSA-N 0.000 description 10
- 230000000202 analgesic effect Effects 0.000 description 10
- 210000003205 muscle Anatomy 0.000 description 9
- 239000000203 mixture Substances 0.000 description 8
- 239000003826 tablet Substances 0.000 description 8
- 238000011260 co-administration Methods 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 208000007101 Muscle Cramp Diseases 0.000 description 5
- 208000005392 Spasm Diseases 0.000 description 5
- 230000001154 acute effect Effects 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- -1 quinazolinone compound Chemical class 0.000 description 5
- 241000700159 Rattus Species 0.000 description 4
- 239000000730 antalgic agent Substances 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- FNQJDLTXOVEEFB-UHFFFAOYSA-N 1,2,3-benzothiadiazole Chemical compound C1=CC=C2SN=NC2=C1 FNQJDLTXOVEEFB-UHFFFAOYSA-N 0.000 description 3
- 206010019233 Headaches Diseases 0.000 description 3
- 208000019695 Migraine disease Diseases 0.000 description 3
- 230000000996 additive effect Effects 0.000 description 3
- 229940035676 analgesics Drugs 0.000 description 3
- 238000013461 design Methods 0.000 description 3
- 231100000869 headache Toxicity 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 206010027599 migraine Diseases 0.000 description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- 206010021118 Hypotonia Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 208000004550 Postoperative Pain Diseases 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- HQPMKSGTIOYHJT-UHFFFAOYSA-N ethane-1,2-diol;propane-1,2-diol Chemical compound OCCO.CC(O)CO HQPMKSGTIOYHJT-UHFFFAOYSA-N 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 230000004118 muscle contraction Effects 0.000 description 2
- 230000036640 muscle relaxation Effects 0.000 description 2
- 229920001993 poloxamer 188 Polymers 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 239000000932 sedative agent Substances 0.000 description 2
- 229940125723 sedative agent Drugs 0.000 description 2
- 230000001755 vocal effect Effects 0.000 description 2
- BTCRLDWAIABUCZ-UHFFFAOYSA-N 4-(4-fluorophenyl)-7-methyl-1-propan-2-ylquinazolin-2-one;1h-quinazolin-2-one Chemical compound C1=CC=C2NC(=O)N=CC2=C1.N=1C(=O)N(C(C)C)C2=CC(C)=CC=C2C=1C1=CC=C(F)C=C1 BTCRLDWAIABUCZ-UHFFFAOYSA-N 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000000060 Migraine with aura Diseases 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 206010043269 Tension headache Diseases 0.000 description 1
- 208000008548 Tension-Type Headache Diseases 0.000 description 1
- ZWUKMNZJRDGCTQ-UHFFFAOYSA-N Tizanidine hydrochloride Chemical compound Cl.ClC=1C=CC2=NSN=C2C=1NC1=NCCN1 ZWUKMNZJRDGCTQ-UHFFFAOYSA-N 0.000 description 1
- 208000025865 Ulcer Diseases 0.000 description 1
- 208000001407 Vascular Headaches Diseases 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 229960004977 anhydrous lactose Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 230000002917 arthritic effect Effects 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 206010013663 drug dependence Diseases 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 208000013465 muscle pain Diseases 0.000 description 1
- 239000003158 myorelaxant agent Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 210000005227 renal system Anatomy 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 208000018316 severe headache Diseases 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 230000001550 time effect Effects 0.000 description 1
- 231100000048 toxicity data Toxicity 0.000 description 1
- 231100000397 ulcer Toxicity 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 239000000080 wetting agent Substances 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
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH341179A CH640415A5 (en) | 1979-04-10 | 1979-04-10 | Therapeutic preparations for the treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS55141413A JPS55141413A (en) | 1980-11-05 |
| JPH0132806B2 true JPH0132806B2 (cg-RX-API-DMAC7.html) | 1989-07-10 |
Family
ID=4255400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP4578480A Granted JPS55141413A (en) | 1979-04-10 | 1980-04-09 | Analgesic and muscle stiffness relaxing medicine |
Country Status (3)
| Country | Link |
|---|---|
| JP (1) | JPS55141413A (cg-RX-API-DMAC7.html) |
| AT (1) | AT378916B (cg-RX-API-DMAC7.html) |
| CH (1) | CH640415A5 (cg-RX-API-DMAC7.html) |
-
1979
- 1979-04-10 CH CH341179A patent/CH640415A5/de not_active IP Right Cessation
-
1980
- 1980-04-09 AT AT0191680A patent/AT378916B/de not_active IP Right Cessation
- 1980-04-09 JP JP4578480A patent/JPS55141413A/ja active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| AT378916B (de) | 1985-10-25 |
| CH640415A5 (en) | 1984-01-13 |
| ATA191680A (de) | 1985-03-15 |
| JPS55141413A (en) | 1980-11-05 |
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