KR860009012A - 벤조티아진 디옥사이드 유도체의 제조방법 - Google Patents
벤조티아진 디옥사이드 유도체의 제조방법 Download PDFInfo
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- KR860009012A KR860009012A KR1019860004181A KR860004181A KR860009012A KR 860009012 A KR860009012 A KR 860009012A KR 1019860004181 A KR1019860004181 A KR 1019860004181A KR 860004181 A KR860004181 A KR 860004181A KR 860009012 A KR860009012 A KR 860009012A
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- South Korea
- Prior art keywords
- methyl
- ethyl
- compound
- amino
- methylpyridinium
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
- C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
- C07D213/20—Quaternary compounds thereof
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/38—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pain & Pain Management (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Dental Preparations (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 일반식(Ⅱ)의 옥시캄 화합물을 일반식(Ⅲ) 또는 (Ⅲ')의 아실할라이드 화합물 또는 그의 하이드로클로라이드 산부가염과 반응시킴을 특징으로 하여 일반식(Ⅰ) 또는 (Ⅰ')의 화합물 또는 그의 약제학적으로 허용되는 산부가염을 제조하는 방법.상기식에서, R은 2-피리딜, 6-메틸-2-피리딜, 6-플루오로-2-피리딜, 6-클로로-2-피리딜, 5-메틸-3-이속사졸릴 또는 2-티아졸릴이고; Y는 각 알킬부위에 3개까지의 탄소원자를 갖는 N, N-디알킬아미노이거나, N-메틸-N-벤질아미노, N-에틸-N-벤질아미노, N-메틸-N-(β-페닐에틸)아미노 또는 N-에틸-N-(β-페닐에틸)아미노이거나, 또는 각각 사이클로알킬 부위에 6개까지의 탄소원자를 갖는 N-메틸-N-사이클로알킬아미노 또는 N-에틸-N-사이클로알킬아미노이거나, 또는 N-메틸-N-페닐아미노, N-에틸-N-페닐아미노, N-메틸-N-(p-클롤로페닐)아미노, N-에틸-N-(p-클롤로페닐)아미노, N-메틸-N-(N', N'-디메킬카바밀메틸)아미노, N-메틸-N-(N, N'-디메킬카바밀메틸)아미노,피롤리디노, 피페리디노, 2-메틸피페리미노, 2-에틸피레리미노, 호모페리디노, 1-아자-사이클로옥틸, N-메틸피페라지노, 모르폴리노 또는 티오모르폴리노이고; Z는 피리디늄, 2-메틸피리디늄, 3-메틸피리디늄,4-메틸피리디늄, 2,6디메틸피리디늄, 2,4,6-트리메틸피리디늄, 3-에틸피리디늄, 4-에틸피리디늄, 3-에틸-4-메틸피리디늄, 4-에틸-2-메틸피리디늄 또는 5-에틸-2-메틸피리디늄이고; A는 약리학적으로 혀용되는 음이온이고; X는 염소 또는 브롬이다.
- 제1항에 있어서, 모화합물인 옥시캄 출발물질에 대하여 적어도 등가몰량의 아실할라이드를 사용하는 방법.
- 제1항에 있어서, 적어도 등가량의 적절한 표준염기의 존재하에 거의 무수상태의 조건하에 반응불활성 유기용매중에서 반응을 수행하는 방법.
- 제3항에 있어서, 약 0 내지 약 50℃의 온도하에서 약 30분 내지 약 125시간동안 반응을 수행하는 방법.
- 제3항에 있어서, 용매가 할로겐화 저급탄화수소이고, 표준염기가 3급 아민인 방법.
- 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(모르폴리노메틸)-벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
- 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(피페리디노메틸)-벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
- 제1항에 있어서, 제조된 화합물이 2-메틸-N-(6-메틸-2-피리디닐)-4-[피페리디노메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
- 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(메틸피레라지노메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
- 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(피리디늄메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드 클로라이드인 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US06/738,805 US4623486A (en) | 1985-05-29 | 1985-05-29 | [4-substituted benzoyloxy]-N-substituted-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides having anti-arthritic activity |
US738,805 | 1985-05-29 | ||
US738805 | 1985-05-29 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR860009012A true KR860009012A (ko) | 1986-12-19 |
KR870000913B1 KR870000913B1 (ko) | 1987-05-06 |
Family
ID=24969564
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019860004181A KR870000913B1 (ko) | 1985-05-29 | 1986-05-28 | 벤조티아진 디옥사이드 유도체의 제조방법 |
Country Status (25)
Country | Link |
---|---|
US (1) | US4623486A (ko) |
EP (1) | EP0208404B1 (ko) |
JP (1) | JPS61277683A (ko) |
KR (1) | KR870000913B1 (ko) |
CN (1) | CN1004628B (ko) |
AT (1) | ATE56010T1 (ko) |
AU (1) | AU557396B1 (ko) |
CA (1) | CA1270485A (ko) |
DD (1) | DD247451A5 (ko) |
DE (1) | DE3673710D1 (ko) |
DK (1) | DK249086A (ko) |
EG (1) | EG17811A (ko) |
ES (1) | ES8707211A1 (ko) |
FI (1) | FI86065C (ko) |
GR (1) | GR861389B (ko) |
HU (2) | HU200178B (ko) |
IL (1) | IL78912A (ko) |
NO (1) | NO165240C (ko) |
NZ (1) | NZ216310A (ko) |
PH (1) | PH23146A (ko) |
PL (1) | PL147843B1 (ko) |
PT (1) | PT82649B (ko) |
SU (2) | SU1538896A3 (ko) |
YU (1) | YU44576B (ko) |
ZA (1) | ZA863986B (ko) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2650589A1 (fr) * | 1989-08-04 | 1991-02-08 | Esteve Labor Dr | Derives benzothiaziniques, leur preparation et leurs applications comme medicaments ou comme intermediaires de synthese de medicaments |
JPH069600A (ja) * | 1992-05-06 | 1994-01-18 | Bristol Myers Squibb Co | タクソールのベンゾエート誘導体 |
FR2795412B1 (fr) * | 1999-06-23 | 2001-07-13 | Adir | Nouveaux derives d'ammonium quaternaire, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
GB0031107D0 (en) * | 2000-12-20 | 2001-01-31 | Glaxo Group Ltd | Chemical compounds |
FR2818641B1 (fr) * | 2000-12-21 | 2004-03-05 | Servier Lab | Nouveaux derives de 1,1-dioxo-2h-1,2-benzothiazine 3-carboxamides, leur procede de preparation et les compositions pharmaceutiques que les contiennent |
GB0202873D0 (en) * | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
US20090238763A1 (en) | 2006-07-09 | 2009-09-24 | Chongxi Yu | High penetration compositions and uses thereof |
US20090221703A1 (en) | 2006-07-09 | 2009-09-03 | Chongxi Yu | High penetration composition and uses thereof |
WO2008024829A2 (en) * | 2006-08-23 | 2008-02-28 | Board Of Regents, The University Of Texas System | Radiohaloimatinibs and methods of their synthesis and use in pet imaging of cancers |
CN101522692A (zh) | 2006-10-11 | 2009-09-02 | 于崇曦 | 具有快速皮肤穿透速度的带正电荷的水溶性的昔康及其相关化合物的前药 |
CN103980228B (zh) * | 2006-10-11 | 2020-03-17 | 于崇曦 | 具有快速皮肤穿透速度的带正电荷的水溶性的昔康及其相关化合物的前药 |
JP2009514988A (ja) * | 2006-10-26 | 2009-04-09 | シコール インコーポレイティド | イマチニブ塩基及びイマチニブメシレート、及びそれらの調製方法 |
WO2008070350A2 (en) | 2006-10-27 | 2008-06-12 | The Board Of Regents Of The University Of Texas System | Methods and compositions related to wrapping of dehydrons |
JP5235423B2 (ja) | 2007-01-25 | 2013-07-10 | 株式会社 資生堂 | 皮膚外用組成物 |
WO2008149181A1 (en) | 2007-06-04 | 2008-12-11 | Techfields Inc | Pro-drugs of nsaias with very high skin and membranes penetration rates and their new medicinal uses |
WO2010065936A1 (en) | 2008-12-04 | 2010-06-10 | Chongxi Yu | High penetration compositions and their applications |
CN101665472B (zh) * | 2009-06-15 | 2011-08-24 | 威海迪素制药有限公司 | 2-甲基-3,4-二氢-4-氧代-2h-1,2-苯并噻嗪-3-羧酸乙酯-1,1-二氧化物的制备方法 |
US8609842B2 (en) | 2010-04-23 | 2013-12-17 | Fujian South Pharmaceutical Co., Ltd. | Method for synthesizing Imatinib |
WO2013008242A1 (en) | 2011-07-12 | 2013-01-17 | Natco Pharma Limited | A process for the preparation of highly pure 4-(4-methyl piperazinomethyl) benzoic acid dihydrochloride |
WO2013035102A1 (en) | 2011-09-05 | 2013-03-14 | Natco Pharma Limited | Processes for the preparation of imatinib base and intermediates thereof |
Family Cites Families (21)
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CH93751A (de) * | 1921-02-24 | 1922-04-01 | Hoffmann La Roche | Verfahren zur Darstellung des p-Diäthylaminomethylbenzoesäurebenzylesters. |
CH93438A (de) * | 1921-02-24 | 1922-04-01 | Hoffmann La Roche | Verfahren zur Darstellung des p-Dimethylaminomethylbenzoesäurebenzylesters. |
US2406627A (en) * | 1942-04-16 | 1946-08-27 | American Cyanamid Co | Alkamine derivatives of para aminomethyl benzoic acid |
US3591584A (en) * | 1968-08-27 | 1971-07-06 | Pfizer | Benzothiazine dioxides |
US3787324A (en) | 1971-03-01 | 1974-01-22 | Warner Lambert Co | 4-hydroxy-3-(3-isoxazolocarbamyl)-2h-1,2-benzothiazine 1,dioxides and process for their production |
JPS4810078U (ko) * | 1971-06-17 | 1973-02-03 | ||
US3788324A (en) * | 1972-05-05 | 1974-01-29 | P Lim | External catheter device |
JPS5070888A (ko) * | 1973-10-27 | 1975-06-12 | ||
US3900470A (en) * | 1974-09-23 | 1975-08-19 | Mcneilab Inc | Esters of benzothiazine-1,1-dioxides derivatives |
US3925371A (en) * | 1974-09-23 | 1975-12-09 | Mcneilab Inc | Benzothiazine-1,1-dioxides |
AU518216B2 (en) * | 1977-09-06 | 1981-09-17 | Hafslund Nycomed Pharma Aktiengesellschaft | Thienothiazine derivatives |
IT1126509B (it) * | 1979-12-07 | 1986-05-21 | Medea Res Srl | Benzimidi ad attivita' anestetica locale e antiaritmica,processo per la loro preparazione e composizioni farmaceutiche che le contengono |
JPS5714589A (en) * | 1980-06-27 | 1982-01-25 | Mitsui Toatsu Chem Inc | Benzothiazine derivative, its preparation and drug composition |
JPS5770888A (en) * | 1980-10-18 | 1982-05-01 | Shinichi Ito | Benzothiazine derivative, its preparation and medicinal composition |
US4309427A (en) * | 1981-01-15 | 1982-01-05 | Pfizer Inc. | Benzothiazine dioxide derivatives |
US4434164A (en) * | 1981-06-01 | 1984-02-28 | Pfizer Inc. | Crystalline benzothiazine dioxide salts |
IT1168064B (it) * | 1981-11-12 | 1987-05-20 | Prodotti Antibiotici Spa | Composto ad azione antinfiammatoria |
IT8219486A0 (it) * | 1982-02-05 | 1982-02-05 | Chiesi Farma Spa | Nuovi composti ad attivita'antiinfiammatoria, procedimento per la loro preparazione e relative composizioni farmaceutiche. |
JPS59193879A (ja) * | 1983-03-31 | 1984-11-02 | Fujisawa Pharmaceut Co Ltd | トロポン誘導体 |
US4551452A (en) * | 1983-12-21 | 1985-11-05 | Pfizer Inc. | Anti-inflammatory 2-methyl-2H-1,2-benzo-(or -thieno-)thiazine-3-carboxamide 1,1-dioxide derivatives, compositions, and method of use therefor |
JPS60184077A (ja) * | 1984-02-23 | 1985-09-19 | フアイザー・インコーポレーテツド | 抗炎症性オキシム前駆薬 |
-
1985
- 1985-05-29 US US06/738,805 patent/US4623486A/en not_active Expired - Lifetime
-
1986
- 1986-05-26 IL IL78912A patent/IL78912A/xx unknown
- 1986-05-27 EP EP86304017A patent/EP0208404B1/en not_active Expired - Lifetime
- 1986-05-27 NZ NZ216310A patent/NZ216310A/xx unknown
- 1986-05-27 CA CA000510033A patent/CA1270485A/en not_active Expired - Fee Related
- 1986-05-27 PL PL1986259740A patent/PL147843B1/pl unknown
- 1986-05-27 AT AT86304017T patent/ATE56010T1/de not_active IP Right Cessation
- 1986-05-27 DE DE8686304017T patent/DE3673710D1/de not_active Expired - Fee Related
- 1986-05-27 PT PT82649A patent/PT82649B/pt not_active IP Right Cessation
- 1986-05-27 ES ES555374A patent/ES8707211A1/es not_active Expired
- 1986-05-28 KR KR1019860004181A patent/KR870000913B1/ko not_active IP Right Cessation
- 1986-05-28 DD DD86290676A patent/DD247451A5/de not_active IP Right Cessation
- 1986-05-28 JP JP61123215A patent/JPS61277683A/ja active Granted
- 1986-05-28 HU HU862250A patent/HU200178B/hu not_active IP Right Cessation
- 1986-05-28 PH PH33823A patent/PH23146A/en unknown
- 1986-05-28 YU YU906/86A patent/YU44576B/xx unknown
- 1986-05-28 FI FI862252A patent/FI86065C/fi not_active IP Right Cessation
- 1986-05-28 DK DK249086A patent/DK249086A/da not_active Application Discontinuation
- 1986-05-28 HU HU872418A patent/HU199839B/hu unknown
- 1986-05-28 CN CN86103603.4A patent/CN1004628B/zh not_active Expired
- 1986-05-28 NO NO862124A patent/NO165240C/no not_active IP Right Cessation
- 1986-05-28 ZA ZA863986A patent/ZA863986B/xx unknown
- 1986-05-28 SU SU864027578A patent/SU1538896A3/ru active
- 1986-05-28 EG EG318/86A patent/EG17811A/xx active
- 1986-05-28 AU AU58013/86A patent/AU557396B1/en not_active Ceased
- 1986-05-28 GR GR861389A patent/GR861389B/el unknown
-
1987
- 1987-04-24 SU SU874202427A patent/SU1531855A3/ru active
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