DK161197C - 1alfa-hydroxy-2-substituerede vitamin d3 derivater samt fremgangsmaade til fremstilling af disse - Google Patents

1alfa-hydroxy-2-substituerede vitamin d3 derivater samt fremgangsmaade til fremstilling af disse

Info

Publication number
DK161197C
DK161197C DK561485A DK561485A DK161197C DK 161197 C DK161197 C DK 161197C DK 561485 A DK561485 A DK 561485A DK 561485 A DK561485 A DK 561485A DK 161197 C DK161197 C DK 161197C
Authority
DK
Denmark
Prior art keywords
group
hydroxy
1alfa
procedures
derivatives
Prior art date
Application number
DK561485A
Other languages
English (en)
Other versions
DK561485A (da
DK561485D0 (da
DK161197B (da
Inventor
Katsuhito Miyamoto
Noboru Kubodera
Kiyoshige Ochi
Isao Matsunaga
Eigoro Murayama
Original Assignee
Chugai Pharmaceutical Co Ltd
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.)
Filing date
Publication date
Application filed by Chugai Pharmaceutical Co Ltd filed Critical Chugai Pharmaceutical Co Ltd
Publication of DK561485D0 publication Critical patent/DK561485D0/da
Publication of DK561485A publication Critical patent/DK561485A/da
Publication of DK161197B publication Critical patent/DK161197B/da
Application granted granted Critical
Publication of DK161197C publication Critical patent/DK161197C/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C401/00—Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0011—Unsubstituted amino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0027—Azides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
DK561485A 1984-12-05 1985-12-04 1alfa-hydroxy-2-substituerede vitamin d3 derivater samt fremgangsmaade til fremstilling af disse DK161197C (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP25571384 1984-12-05
JP25571384 1984-12-05

Publications (4)

Publication Number Publication Date
DK561485D0 DK561485D0 (da) 1985-12-04
DK561485A DK561485A (da) 1986-06-06
DK161197B DK161197B (da) 1991-06-10
DK161197C true DK161197C (da) 1991-11-25

Family

ID=17282605

Family Applications (1)

Application Number Title Priority Date Filing Date
DK561485A DK161197C (da) 1984-12-05 1985-12-04 1alfa-hydroxy-2-substituerede vitamin d3 derivater samt fremgangsmaade til fremstilling af disse

Country Status (10)

Country Link
US (1) US4666634A (da)
EP (1) EP0184206B1 (da)
JP (1) JPH0623185B2 (da)
KR (1) KR940002981B1 (da)
CN (1) CN1008368B (da)
AT (1) ATE41924T1 (da)
CA (1) CA1330806C (da)
DE (1) DE3569238D1 (da)
DK (1) DK161197C (da)
IL (1) IL77122A (da)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
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JP3030157B2 (ja) * 1991-03-13 2000-04-10 株式会社クラレ シクロヘキサントリオール誘導体
US5403832A (en) * 1992-03-12 1995-04-04 The Johns Hopkins University Vitamin D3 analogues
IL107748A (en) * 1992-11-27 1998-08-16 Chugai Pharmaceutical Co Ltd A method for producing a history of vitamin D.
JP2898882B2 (ja) * 1993-04-05 1999-06-02 ウイスコンシン アラムナイ リサーチ フオンデーシヨン ２−位に置換基を有する１９−ノル−ビタミンｄ３ 化合物
AU4459296A (en) * 1995-01-23 1996-08-14 Chugai Seiyaku Kabushiki Kaisha 2-substituted vitamin d3 derivatives
KR100554560B1 (ko) * 1996-07-01 2006-05-25 쥬가이 세이야쿠 가부시키가이샤 비타민d유도체결정및그의제조방법
TWI247001B (en) 1996-07-01 2006-01-11 Chugai Pharmaceutical Co Ltd The method for purifying vitamin d derivatives and its crystalline products
US6392071B1 (en) * 1997-03-17 2002-05-21 Wisconsin Alumni: Research Foundation 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds
US6306844B1 (en) 1997-03-17 2001-10-23 Wisconsin Alumni Research Foundation Use of 2α-methyl-19-nor-20(S)-1α, 25-dihydroxyvitamin D3 to increase bone strength
US5843928A (en) * 1997-03-17 1998-12-01 Wisconsin Alumni Research Foundation 2-alkylidene-19-nor-vitamin D compounds
US5945410A (en) * 1997-03-17 1999-08-31 Wisconsin Alumni Research Foundation 2-alkyl-19-nor-vitamin D compounds
US6316642B1 (en) 1997-03-17 2001-11-13 Wisconsin Alumni Research Foundation 26,27-Homologated-20-EPI-2alkyl-19-nor-vitamin D compounds
DE69939106D1 (de) * 1998-02-24 2008-08-28 Chugai Pharmaceutical Co Ltd Verfahren zur Herstellung von ED-71
US6410523B1 (en) 1998-04-10 2002-06-25 Chugai Seiyaku Kabushiki Kaisha Vitamin D derivatives substituted at the 2beta-position
US6114317A (en) 1998-05-21 2000-09-05 Wisconsin Alumni Research Foundation Method of locking 1α-OH of vitamin D compounds in axial orientation
CN1341213A (zh) * 1999-02-18 2002-03-20 中外制药株式会社 筛选具有维生素d受体亲和性的化合物的方法
EP1284259A4 (en) * 2000-05-23 2009-11-11 Hiroaki Takayama 5,6-TRANS-2-alkyl-vitamin D derivatives
NZ522909A (en) * 2000-05-31 2004-09-24 Wisconsin Alumni Res Found 2-ethyl and 2-ethylidene-19-nor-vitamin D compounds
AU6428001A (en) * 2000-06-15 2001-12-24 Chugai Pharmaceutical Co Ltd Vitamin d derivatives
NZ537036A (en) * 2000-07-14 2006-07-28 Wisconsin Alumni Res Found Use of 2-methylene-19-nor-20(S)-1alpha,25-dihydroxyvitamin D3 to increase bone strength
WO2002012182A1 (fr) * 2000-08-08 2002-02-14 Chugai Seiyaku Kabushiki Kaisha Derives de 3-methyl-20-epi-vitamine d
KR100672886B1 (ko) 2000-09-08 2007-01-24 위스콘신 얼럼나이 리서어치 화운데이션 1α-히드록시-2-메틸렌-19-노르-호모프레그나칼시페롤 및그의 치료적 용도
JPWO2002066424A1 (ja) * 2001-02-23 2004-06-17 中外製薬株式会社 ２位に置換基を有するビタミンｄ誘導体
US6627622B2 (en) 2002-02-18 2003-09-30 Wisconsin Alumni Research Foundation (20S)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol and its uses
US6566352B1 (en) 2002-02-18 2003-05-20 Wisconsin Alumni Research Foudation 1 α-hydroxy-2-methylene-19-nor-pregnacalciferol and its uses
US20030195175A1 (en) * 2002-03-25 2003-10-16 Deluca Hector F. Use of carbon-2-modified-vitamin D analogs to induce the formation of new bone
US6774251B2 (en) * 2002-03-29 2004-08-10 Wisconsin Alumni Research Foundation Method of synthesizing 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol
US20050256092A1 (en) * 2002-08-01 2005-11-17 Shin Shimaoka Antipsoriatic agent
NZ541158A (en) * 2003-01-30 2008-03-28 Teijin Pharma Ltd Vitamin D3 lactone derivative
CN101293894B (zh) * 2003-04-10 2011-04-06 威斯康星校友研究基金会 制备2-亚丙基-19-去甲维生素d化合物的中间体
US6894037B2 (en) * 2003-07-03 2005-05-17 Wisconsin Alumni Research Foundation 2-methylene-19-nor-20(S)-25-methyl-1α-hydroxycalciferol and its uses
US20050009792A1 (en) * 2003-07-08 2005-01-13 Deluca Hector F. (20S)-1alpha-hydroxy-2-methylene-19-nor-vitamin D3 and its uses
US7232810B2 (en) * 2003-08-20 2007-06-19 Wisconsin Alumni Research Foundation 2-methylene-19-nor-vitamin D2 compounds
CN1938034B (zh) * 2004-02-06 2010-12-08 中外制药株式会社 Ed-71制剂
US7713951B2 (en) * 2004-04-09 2010-05-11 Wisconsin Alumni Research Foundation 2-alkylidene-18,19-dinor-vitamin D compounds
CA2588038A1 (en) * 2004-11-22 2006-06-01 Wisconsin Alumni Research Foundation 2-methylene-19-nor-(20r)-1-.alpha.-hydroxy-bishomopregnacalciferol
ATE465144T1 (de) * 2004-11-22 2010-05-15 Wisconsin Alumni Res Found 17,20(e)-dehydro-vitamin-d-analoga und deren verwendungen
CA2588060A1 (en) * 2004-11-22 2006-06-01 Wisconsin Alumni Research Foundation 2-methylene-19-nor-(20s)-1alpha-hydroxy-trishomopregnacalciferol
MX2007006545A (es) * 2004-11-22 2007-09-21 Wisconsin Alumni Res Found 2a-metil-19-nor-1a-hidroxi-homopregnacalciferol y sus usos.
AU2005309820B2 (en) * 2004-11-22 2011-06-23 Wisconsin Alumni Research Foundation 2-methylene-19,21-dinor-1alpha-hydroxy-bishomopregnacalciferol
DE602005021245D1 (de) * 2004-11-22 2010-06-24 Wisconsin Alumni Res Found 2-methylen-19,26,27-trinor-(20s)-1-alpha-hydroxyvitamin d3 and dessen verwendungen
DK1848442T3 (da) * 2005-02-11 2012-05-29 Wisconsin Alumni Res Found 2-methylene-19-nor-(20s-24epi)-1alfa,25-dihydroxyvitamine-d2
JP5036566B2 (ja) * 2005-02-11 2012-09-26 ウイスコンシン アラムニ リサーチ ファンデーション ２−メチレン−１９−ノル−（２０Ｓ−２４Ｓ）−１α，２５−ジヒドロキシビタミン−Ｄ２
JP2008538214A (ja) * 2005-03-29 2008-10-16 ウイスコンシン アラムニ リサーチ ファンデーション ２−メチレン−１９−ノル−（２３Ｓ）−２５−デヒドロ−１α−ヒドロキシビタミンＤ３−２６，２３−ラクトンおよび２−メチレン−１９−ノル−（２３Ｒ）−２５−デヒドロ−１α−ヒドロキシビタミンＤ３−２６，２３−ラクトン
EP1877063A4 (en) * 2005-05-03 2009-11-04 Wisconsin Alumni Res Found COMPOUNDS OF 19,26,27-TRINOR-1ALPHA, 25-DIHYDROXYVITAMIN D3
US7534777B2 (en) * 2005-08-30 2009-05-19 Wisconsin Alumni Research Foundation Des-C,D analogs of 1α,25-dihydroxy-19-norvitamin D3
JP2009511433A (ja) * 2005-09-22 2009-03-19 ウイスコンシン アラムニ リサーチ ファンデーション １９，２３，２４，２５，２６，２７−ヘキサノール−１α−ヒドロキシビタミンＤ３
US7803789B2 (en) 2006-02-02 2010-09-28 Wisconsin Alumni Research Foundation Vitamin D analog—RAK, methods and uses thereof
US7528122B2 (en) * 2006-02-02 2009-05-05 Wisconsin Alumni Research Foundation Vitamin D analog—NEL, methods and uses thereof
NZ571896A (en) * 2006-04-05 2011-09-30 Wisconsin Alumni Res Found 1-Alpha.-hydroxy-2-(3'-hydroxypropylidene)-19-nor-vitamin D compounds and methods of making and use thereof
US20090281340A1 (en) * 2006-04-05 2009-11-12 Deluca Hector F 1alpha-hydroxy-2-(3'-hydroxypropylidene)-19-nor-vitamin d compounds and methods of making and treatment thereof
US7648972B2 (en) * 2006-04-06 2010-01-19 Wisconsin Alumni Research Foundation 2-methylene-1α-hydroxy-19,21-dinorvitamin D3 analogs and uses thereof
AU2007298673A1 (en) 2006-04-06 2008-03-27 Wisconsin Alumni Research Foundation 2- substituted-1alpha, 25-dihydroxy-19,26,27-trinor vitamin D analogs and uses thereof
WO2008125901A2 (en) * 2006-04-06 2008-10-23 Wisconsin Alumni Research Foundation 2-methylene-1alpha,25-dihydroxy-18,19,21-trinorvitamin d3 and uses thereof
MX2008012672A (es) * 2006-04-06 2008-10-15 Wisconsin Alumni Res Found Analogos de 2-metilen-1a-hidroxi-18,19,21-trinor vitamina d3 y sus usos.
AU2007291005A1 (en) * 2006-04-06 2008-03-06 Wisconsin Alumni Research Foundation 19-nor-vitamin D analogs with 1,2,or 3,2 heterocyclic ring
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CA2662992A1 (en) * 2006-09-28 2008-04-03 Wisconsin Alumni Research Foundation 2-methylene-(20r,25s)-19,27-dinor-(22e)-vitamin d analogs
ATE552238T1 (de) * 2006-09-28 2012-04-15 Wisconsin Alumni Res Found 2-methylen-(20s,25s)-19,27-dinor-(22e)-vitamin- - analoga
US20090075953A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched ed-71
MX2010007264A (es) * 2007-12-28 2011-03-15 Wisconsin Alumni Res Foundation Star Análogos de vitamina d 2-metilen-(20s, 25r)-19, 26-dinor.
EP2240438B1 (en) * 2007-12-28 2012-04-04 Wisconsin Alumni Research Foundation 2-methylene-20-methyl-19,24,25,26,27-pentanor-vitamin d analogs
AU2008345083B2 (en) * 2007-12-28 2014-05-08 Wisconsin Alumni Research Foundation (20R)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs
WO2009086439A2 (en) * 2007-12-28 2009-07-09 Wisconsin Alumni Research Foundation 2-methylene-(20s,25s)-19,26-dinor-vitamin d analogs
AU2008345082B2 (en) * 2007-12-28 2014-03-06 Wisconsin Alumni Research Foundation (20S)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs
US7893043B2 (en) * 2008-07-10 2011-02-22 Wisconsin Alumni Research Foundation 2-methylene-(17Z)-17(20)-dehydro-19,21-dinor-vitamin D analogs
US8399439B2 (en) * 2008-07-10 2013-03-19 Wisconsin Alumni Research Foundation 2-methylene-19,26-dinor-(20S,22E,25R)-vitamin D analogs
US7888339B2 (en) * 2008-07-10 2011-02-15 Wisconsin Alumni Research Foundation 2-methylene-20(21)-dehydro-19-nor-vitamin D analogs
US7713953B2 (en) * 2008-07-10 2010-05-11 Wisconsin Alumni Research Foundation 2-methylene-(22E)-25-(1-methylene-hexyl)-26,27-cyclo-22-dehydro-19-nor-vitamin D analogs
US8222236B2 (en) * 2008-07-10 2012-07-17 Wisconsin Alumni Research Foundation 2-methylene-(20E)-20(22)-dehydro-19-nor-vitamin D analogs
US8642579B2 (en) 2009-10-02 2014-02-04 Wisconsin Alumni Research Foundation 1-desoxy-2-methylene-19-nor-vitamin D analogs and their uses
EP2525799B1 (en) 2009-10-02 2014-09-03 Wisconsin Alumni Research Foundation (20s,22e)-2-methylene-19-nor-22-ene-1alpha,25-dihydroxyvitamin d3 analogs
US8349818B2 (en) * 2009-10-21 2013-01-08 Wisconsin Alumni Research Foundation Method of preventing Type 1 diabetes
JP2011241170A (ja) * 2010-05-18 2011-12-01 Mercian Corp ビタミンｄ誘導体およびその製造方法
WO2012065050A1 (en) 2010-11-12 2012-05-18 Wisconsin Alumni Research Foundation 22-haloacetoxy-homopregnacalciferol analogs and their uses
WO2012151058A1 (en) 2011-05-03 2012-11-08 Wisconsin Alumni Research Foundation (20s)-24-(p-toluenesulfonyloxy)-25,26,27-trinorvitamin d3 analogs and their uses
WO2012158794A1 (en) 2011-05-17 2012-11-22 Wisconsin Alumni Research Foundation N-cyclopropyl-(20r)-2-methylene-19,26,27-trinor-25-aza-vitamin d analogs and their uses
JP6059716B2 (ja) 2011-06-03 2017-01-11 ウイスコンシン アラムニ リサーチ ファンデーション （２２Ｅ）−２−メチレン−２６，２７−シクロ−２２−デヒドロ−１α−ヒドロキシ−１９−ノルビタミンＤ３誘導体
CA2824870C (en) 2011-06-14 2018-08-14 Wisconsin Alumni Research Foundation 3-desoxy-2-methylene-19-nor-vitamin d analogs and their uses
WO2013003307A1 (en) 2011-06-28 2013-01-03 Wisconsin Alumni Research Foundation 2-methylene-(22e)-25-hexanoyl-24-oxo-26,27-cyclo-22-dehydro-19-nor-vitamin d analogs
WO2013012644A1 (en) 2011-07-18 2013-01-24 Wisconsin Alumni I Research Foundation 2-methylene-20(21)-dehydro-19,24,25,26,27,-pentanor-vitamin d analogs
US8410080B1 (en) 2011-10-21 2013-04-02 Wisconsin Alumni Research Foundation 2-methylene-vitamin D analogs and their uses
US8729054B2 (en) 2011-10-21 2014-05-20 Wisconsin Alumni Research Foundation 3-desoxy-2-methylene-vitamin D analogs and their uses
AU2012326538B2 (en) * 2011-10-21 2016-12-08 Wisconsin Alumni Research Foundation 2-methylene-vitamin D analogs and their uses
US8785422B2 (en) * 2012-06-06 2014-07-22 Wisconsin Alumni Research Foundation A-ring modified 19-nor-vitamin D analogs and their uses
JP2018030839A (ja) * 2016-08-23 2018-03-01 日産化学工業株式会社 ビタミンｄ３誘導体の新規な結晶形及びその製造方法
CN107540589B (zh) * 2017-09-14 2022-05-03 上海彩迩文生化科技有限公司 一种艾尔骨化醇晶型、药物组合物及制备方法和应用
CN109456244A (zh) * 2018-12-12 2019-03-12 无锡福祈制药有限公司 一种维生素d3类化合物及其制备方法

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US4307025A (en) * 1981-02-17 1981-12-22 Wisconsin Alumni Research Foundation 1α, 25-dihydroxy-2β-fluorovitamin D3

Also Published As

Publication number Publication date
CN1008368B (zh) 1990-06-13
EP0184206A2 (en) 1986-06-11
EP0184206B1 (en) 1989-04-05
CN85108857A (zh) 1986-07-09
ATE41924T1 (de) 1989-04-15
KR860004850A (ko) 1986-07-14
DK561485A (da) 1986-06-06
DE3569238D1 (en) 1989-05-11
JPH0623185B2 (ja) 1994-03-30
DK561485D0 (da) 1985-12-04
IL77122A (en) 1990-11-29
US4666634A (en) 1987-05-19
IL77122A0 (en) 1986-04-29
KR940002981B1 (ko) 1994-04-09
EP0184206A3 (en) 1987-01-14
DK161197B (da) 1991-06-10
JPS61267549A (ja) 1986-11-27
CA1330806C (en) 1994-07-19

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