JP2003503387A5 - - Google Patents
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- Publication number
- JP2003503387A5 JP2003503387A5 JP2001506989A JP2001506989A JP2003503387A5 JP 2003503387 A5 JP2003503387 A5 JP 2003503387A5 JP 2001506989 A JP2001506989 A JP 2001506989A JP 2001506989 A JP2001506989 A JP 2001506989A JP 2003503387 A5 JP2003503387 A5 JP 2003503387A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- group
- aryl
- compound according
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 description 44
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 43
- 229910052736 halogen Inorganic materials 0.000 description 34
- 150000002367 halogens Chemical class 0.000 description 34
- 0 C*c1cc(*)c(**)cc1* Chemical compound C*c1cc(*)c(**)cc1* 0.000 description 28
- 125000004404 heteroalkyl group Chemical group 0.000 description 21
- 125000003118 aryl group Chemical group 0.000 description 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 15
- 125000003545 alkoxy group Chemical group 0.000 description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 14
- 125000001424 substituent group Chemical group 0.000 description 10
- 125000004093 cyano group Chemical group *C#N 0.000 description 8
- 125000000217 alkyl group Chemical group 0.000 description 7
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- -1 -CF 3 Chemical group 0.000 description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- 239000001257 hydrogen Substances 0.000 description 5
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 description 4
- 201000010099 disease Diseases 0.000 description 3
- 208000016097 disease of metabolism Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 208000027866 inflammatory disease Diseases 0.000 description 3
- 230000001404 mediated effect Effects 0.000 description 3
- 208000030159 metabolic disease Diseases 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 2
- OHDLZTDSTWANIC-UHFFFAOYSA-N C[I]1CCCC1 Chemical compound C[I]1CCCC1 OHDLZTDSTWANIC-UHFFFAOYSA-N 0.000 description 2
- CHOJVEYZTDHFDD-UHFFFAOYSA-N Cc(cc(c(Cl)c1)S(Nc(cc2Cl)cc(Cl)c2Oc2cnc(cccc3)c3c2)(=O)=O)c1Cl Chemical compound Cc(cc(c(Cl)c1)S(Nc(cc2Cl)cc(Cl)c2Oc2cnc(cccc3)c3c2)(=O)=O)c1Cl CHOJVEYZTDHFDD-UHFFFAOYSA-N 0.000 description 2
- YZCKVEUIGOORGS-UHFFFAOYSA-N Hydrogen atom Chemical compound [H] YZCKVEUIGOORGS-UHFFFAOYSA-N 0.000 description 2
- NMRWDFUZLLQSBN-UHFFFAOYSA-N O=S(c(c(Cl)c1)ccc1Cl)(Nc(cc1Cl)cc(Cl)c1Oc1cnc(cccc2)c2c1)=O Chemical compound O=S(c(c(Cl)c1)ccc1Cl)(Nc(cc1Cl)cc(Cl)c1Oc1cnc(cccc2)c2c1)=O NMRWDFUZLLQSBN-UHFFFAOYSA-N 0.000 description 2
- 102000000536 PPAR gamma Human genes 0.000 description 2
- 108010016731 PPAR gamma Proteins 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 2
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- URNHKABEDJIWRH-UHFFFAOYSA-N Nc(cc1Cl)cc(Cl)c1Sc1cc(cccc2)c2nc1 Chemical compound Nc(cc1Cl)cc(Cl)c1Sc1cc(cccc2)c2nc1 URNHKABEDJIWRH-UHFFFAOYSA-N 0.000 description 1
- QWRAHLJXUPOZRK-UHFFFAOYSA-N O=S(c1ccccc1Cl)(Nc(cc1Cl)cc(Cl)c1Sc1cc(cccc2)c2nc1)=O Chemical compound O=S(c1ccccc1Cl)(Nc(cc1Cl)cc(Cl)c1Sc1cc(cccc2)c2nc1)=O QWRAHLJXUPOZRK-UHFFFAOYSA-N 0.000 description 1
- XSPOHQBAMUMLLS-UHFFFAOYSA-N O=Sc(ccc(C(F)(F)F)c1)c1Cl Chemical compound O=Sc(ccc(C(F)(F)F)c1)c1Cl XSPOHQBAMUMLLS-UHFFFAOYSA-N 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 125000005237 alkyleneamino group Chemical group 0.000 description 1
- 125000005529 alkyleneoxy group Chemical group 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14167299P | 1999-06-30 | 1999-06-30 | |
| US60/141,672 | 1999-06-30 | ||
| PCT/US2000/018178 WO2001000579A1 (en) | 1999-06-30 | 2000-06-28 | COMPOUNDS FOR THE MODULATION OF PPARη ACTIVITY |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003503387A JP2003503387A (ja) | 2003-01-28 |
| JP2003503387A5 true JP2003503387A5 (https=) | 2006-01-05 |
| JP4295458B2 JP4295458B2 (ja) | 2009-07-15 |
Family
ID=22496697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001506989A Expired - Lifetime JP4295458B2 (ja) | 1999-06-30 | 2000-06-28 | Ｐｐａｒ−ガンマ活性調節用化合物 |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1192137B1 (https=) |
| JP (1) | JP4295458B2 (https=) |
| CN (1) | CN1171872C (https=) |
| CA (1) | CA2377309C (https=) |
| DK (1) | DK1192137T3 (https=) |
| EA (1) | EA004887B1 (https=) |
| ES (1) | ES2437103T3 (https=) |
| HK (1) | HK1043369B (https=) |
| IL (2) | IL147308A0 (https=) |
| MX (2) | MXPA01013199A (https=) |
| NZ (2) | NZ516455A (https=) |
| SG (1) | SG148834A1 (https=) |
| WO (1) | WO2001000579A1 (https=) |
| ZA (1) | ZA200200057B (https=) |
Families Citing this family (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6583157B2 (en) | 1998-01-29 | 2003-06-24 | Tularik Inc. | Quinolinyl and benzothiazolyl modulators |
| US7041691B1 (en) | 1999-06-30 | 2006-05-09 | Amgen Inc. | Compounds for the modulation of PPARγ activity |
| WO2001082916A2 (en) * | 2000-05-03 | 2001-11-08 | Tularik Inc. | Combination therapeutic compositions and methods of use |
| KR100771286B1 (ko) * | 2000-06-28 | 2007-10-29 | 암젠 인크 | 퀴놀리닐 및 벤조티아졸릴 ｐｐａｒ-감마 조절물질 |
| US20030171399A1 (en) | 2000-06-28 | 2003-09-11 | Tularik Inc. | Quinolinyl and benzothiazolyl modulators |
| US6982251B2 (en) | 2000-12-20 | 2006-01-03 | Schering Corporation | Substituted 2-azetidinones useful as hypocholesterolemic agents |
| IL156445A0 (en) | 2001-01-26 | 2004-01-04 | Schering Corp | Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications |
| US7071181B2 (en) | 2001-01-26 | 2006-07-04 | Schering Corporation | Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors |
| AR035533A1 (es) | 2001-01-26 | 2004-06-02 | Schering Corp | Uso de por lo menos un inhibidor de la absorcion de los esteroles o sus sales, solvatos, prodrogas farmaceuticamente aceptables o mezclas de los mismos para la preparacion de un medicamento para el tratamiento de la sitosterolemia, composiciones farmaceuticas, el uso de dichas composiciones para la |
| EP1911462A3 (en) | 2001-01-26 | 2011-11-30 | Schering Corporation | Compositions comprising a sterol absorption inhibitor |
| WO2003005025A1 (en) * | 2001-07-03 | 2003-01-16 | Biovitrum Ab | Methods for identifying compounds modulating the activity of ppar-gamma |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| EP1435946B8 (en) | 2001-09-14 | 2013-12-18 | Amgen Inc. | Linked biaryl compounds |
| US7053080B2 (en) | 2001-09-21 | 2006-05-30 | Schering Corporation | Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors |
| MXPA04002573A (es) | 2001-09-21 | 2004-06-18 | Schering Corp | Tratamiento de xantoma con derivados de azetidinona como inhibidores de la absorcion de esterol. |
| US7056906B2 (en) | 2001-09-21 | 2006-06-06 | Schering Corporation | Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women |
| EP2399903A1 (en) | 2002-05-24 | 2011-12-28 | Millennium Pharmaceuticals, Inc. | Ccr9 inhibitors and methods of use thereof |
| WO2004043457A1 (en) | 2002-11-06 | 2004-05-27 | Schering Corporation | Cholesterol absorptions inhibitors for the treatment of autoimmune disorders |
| US7227035B2 (en) | 2002-11-18 | 2007-06-05 | Chemocentryx | Bis-aryl sulfonamides |
| US7420055B2 (en) | 2002-11-18 | 2008-09-02 | Chemocentryx, Inc. | Aryl sulfonamides |
| US7741519B2 (en) | 2007-04-23 | 2010-06-22 | Chemocentryx, Inc. | Bis-aryl sulfonamides |
| US6939885B2 (en) | 2002-11-18 | 2005-09-06 | Chemocentryx | Aryl sulfonamides |
| EP1601668B1 (en) | 2003-03-07 | 2008-08-27 | Schering Corporation | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| CA2517572C (en) | 2003-03-07 | 2011-12-13 | Schering Corporation | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| JP2006519869A (ja) | 2003-03-07 | 2006-08-31 | シェーリング コーポレイション | 置換アゼチジノン化合物、置換アゼチジノン化合物を調製するためのプロセス、それらの処方物および使用 |
| US7459442B2 (en) | 2003-03-07 | 2008-12-02 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| JP2009513523A (ja) * | 2003-07-08 | 2009-04-02 | ノバルティス アクチエンゲゼルシャフト | ベンゼンスルホニルアミノ化合物およびそれらを含む医薬組成物 |
| DE10344223A1 (de) * | 2003-09-24 | 2005-04-21 | Merck Patent Gmbh | 1,3-Benzoxazolylderivate als Kinase-Inhibitoren |
| US7223761B2 (en) * | 2003-10-03 | 2007-05-29 | Amgen Inc. | Salts and polymorphs of a potent antidiabetic compound |
| GB0401334D0 (en) | 2004-01-21 | 2004-02-25 | Novartis Ag | Organic compounds |
| US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
| WO2006020830A2 (en) | 2004-08-12 | 2006-02-23 | Amgen Inc. | Bisaryl-sulfonamides |
| CA2614746C (en) | 2005-07-09 | 2011-05-10 | Astrazeneca Ab | Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes |
| CN101528734B (zh) * | 2006-09-21 | 2013-02-13 | 皮拉玛生命科学有限公司 | 治疗代谢障碍的3-氨基吡啶衍生物 |
| TW200820970A (en) * | 2006-09-21 | 2008-05-16 | Nicholas Piramal India Ltd | Compounds for the treatment of metabolic disorders |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| EP2527360B1 (en) | 2007-06-04 | 2015-10-28 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| US8304441B2 (en) | 2007-09-14 | 2012-11-06 | Metabolic Solutions Development Company, Llc | Thiazolidinedione analogues for the treatment of metabolic diseases |
| KR101537830B1 (ko) | 2007-09-14 | 2015-07-17 | 메타볼릭 솔루션스 디벨롭먼트 컴퍼니, 엘엘씨 | 고혈압 치료용 티아졸리딘디온 유사체 |
| EP2810951B1 (en) | 2008-06-04 | 2017-03-15 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| EP3241839B1 (en) | 2008-07-16 | 2019-09-04 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| CN102361857B (zh) * | 2008-09-26 | 2015-09-16 | 默沙东公司 | 可用作抗糖尿病剂的环状苯并咪唑衍生物 |
| WO2010047982A1 (en) | 2008-10-22 | 2010-04-29 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| JP5557845B2 (ja) | 2008-10-31 | 2014-07-23 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体 |
| EA020017B1 (ru) | 2009-04-30 | 2014-08-29 | Новартис Аг | Производные имидазола и их применение в качестве модуляторов циклинзависимых киназ |
| RU2564661C2 (ru) | 2009-12-15 | 2015-10-10 | МЕТАБОЛИК СОЛЮШНЗ ДЕВЕЛОПМЕНТ КОМПАНИ, ЭлЭлСи | Соли тиазолидиндиона со сниженным сродством к ppar для лечения нарушений обмена веществ |
| WO2011084459A1 (en) * | 2009-12-15 | 2011-07-14 | Metabolic Solutions Development Company | Ppar-sparing thiazolidinediones and combinations for the treatment of obesity and other metabolic diseases |
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US20130156720A1 (en) | 2010-08-27 | 2013-06-20 | Ironwood Pharmaceuticals, Inc. | Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| WO2012040082A2 (en) | 2010-09-21 | 2012-03-29 | Intekrin Therapeutics, Inc. | Antidiabetic solid pharmaceutical compositions |
| BR112013021236B1 (pt) | 2011-02-25 | 2021-05-25 | Merck Sharp & Dohme Corp | composto derivado de benzimidazol, e, composição |
| WO2013082106A1 (en) | 2011-12-02 | 2013-06-06 | The General Hospital Corporation | Differentiation into brown adipocytes |
| US20130158077A1 (en) | 2011-12-19 | 2013-06-20 | Ares Trading S.A. | Pharmaceutical compositions |
| ES2656292T3 (es) | 2012-05-01 | 2018-02-26 | Translatum Medicus Inc. | Métodos de tratamiento y diagnóstico de enfermedades oculares que causan ceguera |
| US9527875B2 (en) | 2012-08-02 | 2016-12-27 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| RU2015140066A (ru) | 2013-02-22 | 2017-03-30 | Мерк Шарп И Доум Корп. | Противодиабетические бициклические соединения |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
| CA2905438A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| SI3004138T1 (sl) | 2013-06-05 | 2024-07-31 | Bausch Health Ireland Limited | Ultra čisti agonisti gvanilat ciklaze C, postopek za njihovo pripravo in uporabo |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| EA201791982A1 (ru) | 2015-03-09 | 2020-02-17 | Интекрин Терапьютикс, Инк. | Способы лечения неалкогольной жировой болезни печени и/или липодистрофии |
| JP6902748B2 (ja) * | 2016-09-29 | 2021-07-14 | 雪印種苗株式会社 | 植物成長調整剤 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| WO2018118670A1 (en) | 2016-12-20 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| AU2018249822A1 (en) | 2017-04-03 | 2019-10-31 | Coherus Biosciences Inc. | PPArgamma agonist for treatment of progressive supranuclear palsy |
| CN116693433B (zh) * | 2023-06-02 | 2024-04-16 | 济南悟通生物科技有限公司 | 一种烷基取代苯硫酚的合成方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3264551D1 (en) * | 1981-07-06 | 1985-08-08 | Eastman Kodak Co | Color-forming sulfonamidodiphenylamines, photographic elements containing them and corresponding sulfonimide dyes |
| DE3632329A1 (de) * | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| JP3894949B2 (ja) * | 1993-06-30 | 2007-03-22 | ザ、ウェルカム、ファンデーション、リミテッド | 抗アテローム性動脈硬化症ジアリール化合物 |
| TW321649B (https=) * | 1994-11-12 | 1997-12-01 | Zeneca Ltd | |
| TWI238064B (en) * | 1995-06-20 | 2005-08-21 | Takeda Chemical Industries Ltd | A pharmaceutical composition for prophylaxis and treatment of diabetes |
| GB9604242D0 (en) * | 1996-02-28 | 1996-05-01 | Glaxo Wellcome Inc | Chemical compounds |
| JP3243733B2 (ja) * | 1996-08-07 | 2002-01-07 | 雪印乳業株式会社 | 新規イソキノリン誘導体 |
| ZA986732B (en) * | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
| US6284923B1 (en) * | 1997-08-22 | 2001-09-04 | Tularik Inc | Substituted benzene compounds as antiproliferative and cholesterol lowering action |
| CA2318731C (en) * | 1998-01-29 | 2012-05-29 | Tularik Inc. | Ppar-gamma modulators |
-
2000
- 2000-06-28 IL IL14730800A patent/IL147308A0/xx unknown
- 2000-06-28 CN CNB008113076A patent/CN1171872C/zh not_active Expired - Lifetime
- 2000-06-28 HK HK02105143.3A patent/HK1043369B/en unknown
- 2000-06-28 JP JP2001506989A patent/JP4295458B2/ja not_active Expired - Lifetime
- 2000-06-28 NZ NZ516455A patent/NZ516455A/xx not_active IP Right Cessation
- 2000-06-28 MX MXPA01013199A patent/MXPA01013199A/es active IP Right Grant
- 2000-06-28 EA EA200200105A patent/EA004887B1/ru not_active IP Right Cessation
- 2000-06-28 EP EP00946961.0A patent/EP1192137B1/en not_active Expired - Lifetime
- 2000-06-28 NZ NZ530833A patent/NZ530833A/en not_active IP Right Cessation
- 2000-06-28 DK DK00946961.0T patent/DK1192137T3/da active
- 2000-06-28 WO PCT/US2000/018178 patent/WO2001000579A1/en not_active Ceased
- 2000-06-28 SG SG200403480-7A patent/SG148834A1/en unknown
- 2000-06-28 CA CA2377309A patent/CA2377309C/en not_active Expired - Lifetime
- 2000-06-28 ES ES00946961.0T patent/ES2437103T3/es not_active Expired - Lifetime
-
2001
- 2001-12-18 MX MX2011005852A patent/MX339420B/es unknown
- 2001-12-25 IL IL147308A patent/IL147308A/en active IP Right Grant
-
2002
- 2002-01-03 ZA ZA200200057A patent/ZA200200057B/en unknown
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