ATE240736T1 - Verfahren zur herstellung von 1-alpha-24- dihydroxy-vitamin d2 - Google Patents

Verfahren zur herstellung von 1-alpha-24- dihydroxy-vitamin d2

Info

Publication number: ATE240736T1
Authority: AT; Austria
Prior art keywords: vitamin; dihydroxy; proportional; converted; alpha
Prior art date: 1991-01-08

Application number

AT98110802T

Other languages

English (en)

Inventor

Charles W Bishop

Glenville Jones

Joyce C Knutson

Robert M Moriarty

Raju Penmasta

Stephen Strugnell

Original Assignee

Bone Care Int Inc

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.)

1991-01-08

Filing date

1992-01-07

Publication date

2003-06-15

1992-01-07 Application filed by Bone Care Int Inc filed Critical Bone Care Int Inc

2003-06-15 Application granted granted Critical

2003-06-15 Publication of ATE240736T1 publication Critical patent/ATE240736T1/de

Links

238000004519 manufacturing process Methods 0.000 title 1
MECHNRXZTMCUDQ-UHFFFAOYSA-N Vitamin D2 Natural products C1CCC2(C)C(C(C)C=CC(C)C(C)C)CCC2C1=CC=C1CC(O)CCC1=C MECHNRXZTMCUDQ-UHFFFAOYSA-N 0.000 abstract 3
229960002061 ergocalciferol Drugs 0.000 abstract 3
MECHNRXZTMCUDQ-RKHKHRCZSA-N vitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/[C@H](C)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C MECHNRXZTMCUDQ-RKHKHRCZSA-N 0.000 abstract 3
235000001892 vitamin D2 Nutrition 0.000 abstract 3
239000011653 vitamin D2 Substances 0.000 abstract 3
LHXJPXPNCMSHPV-KAOCCWGPSA-N (3s,9s,10r,13r,14r,17r)-17-[(e,2r,5s)-5-hydroxy-5,6-dimethylhept-3-en-2-yl]-10,13-dimethyl-2,3,4,9,11,12,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthren-3-ol Chemical compound C1[C@@H](O)CC[C@]2(C)[C@@H](CC[C@@]3([C@@H]([C@H](C)/C=C/[C@@](C)(O)C(C)C)CC[C@H]33)C)C3=CC=C21 LHXJPXPNCMSHPV-KAOCCWGPSA-N 0.000 abstract 2
OILXMJHPFNGGTO-UHFFFAOYSA-N (22E)-(24xi)-24-methylcholesta-5,22-dien-3beta-ol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(C)C(C)C)C1(C)CC2 OILXMJHPFNGGTO-UHFFFAOYSA-N 0.000 abstract 1
RQOCXCFLRBRBCS-UHFFFAOYSA-N (22E)-cholesta-5,7,22-trien-3beta-ol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CCC(C)C)CCC33)C)C3=CC=C21 RQOCXCFLRBRBCS-UHFFFAOYSA-N 0.000 abstract 1
HVAVRRBYXYEBNC-RKULPTJNSA-N 24-hydroxyvitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/C(C)(O)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C HVAVRRBYXYEBNC-RKULPTJNSA-N 0.000 abstract 1
OQMZNAMGEHIHNN-UHFFFAOYSA-N 7-Dehydrostigmasterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CC(CC)C(C)C)CCC33)C)C3=CC=C21 OQMZNAMGEHIHNN-UHFFFAOYSA-N 0.000 abstract 1
DNVPQKQSNYMLRS-NXVQYWJNSA-N Ergosterol Natural products CC(C)[C@@H](C)C=C[C@H](C)[C@H]1CC[C@H]2C3=CC=C4C[C@@H](O)CC[C@]4(C)[C@@H]3CC[C@]12C DNVPQKQSNYMLRS-NXVQYWJNSA-N 0.000 abstract 1
208000022458 calcium metabolism disease Diseases 0.000 abstract 1
150000001875 compounds Chemical class 0.000 abstract 1
DNVPQKQSNYMLRS-SOWFXMKYSA-N ergosterol Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H](CC[C@]3([C@H]([C@H](C)/C=C/[C@@H](C)C(C)C)CC[C@H]33)C)C3=CC=C21 DNVPQKQSNYMLRS-SOWFXMKYSA-N 0.000 abstract 1
239000000543 intermediate Substances 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
238000002360 preparation method Methods 0.000 abstract 1
208000017520 skin disease Diseases 0.000 abstract 1
238000003786 synthesis reaction Methods 0.000 abstract 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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- 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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/592—9,10-Secoergostane derivatives, e.g. ergocalciferol, i.e. vitamin D2
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- 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
- 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
- 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

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Medicinal Chemistry (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Physical Education & Sports Medicine (AREA)
Orthopedic Medicine & Surgery (AREA)
Rheumatology (AREA)
Nutrition Science (AREA)
Oncology (AREA)
Obesity (AREA)
Communicable Diseases (AREA)
Diabetes (AREA)
Hematology (AREA)
Dermatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Saccharide Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

AT98110802T 1991-01-08 1992-01-07 Verfahren zur herstellung von 1-alpha-24- dihydroxy-vitamin d2 ATE240736T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US63786791A	1991-01-08	1991-01-08

Publications (1)

Publication Number	Publication Date
ATE240736T1 true ATE240736T1 (de)	2003-06-15

Family

ID=24557692

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
AT92904947T ATE179604T1 (de)	1991-01-08	1992-01-07	Verfahren zur herstellung und verwendung von 1alpha,24-dihydroxy vitamin-d2
AT98110802T ATE240736T1 (de)	1991-01-08	1992-01-07	Verfahren zur herstellung von 1-alpha-24- dihydroxy-vitamin d2

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
AT92904947T ATE179604T1 (de)	1991-01-08	1992-01-07	Verfahren zur herstellung und verwendung von 1alpha,24-dihydroxy vitamin-d2

Country Status (14)

Country	Link
US (1)	US6211168B1 (de)
EP (2)	EP0914825B1 (de)
CN (3)	CN1032256C (de)
AT (2)	ATE179604T1 (de)
AU (1)	AU1247592A (de)
DE (2)	DE69229103T2 (de)
DK (1)	DK0550702T3 (de)
ES (2)	ES2200238T3 (de)
GR (1)	GR3030466T3 (de)
MX (1)	MX9200070A (de)
NZ (1)	NZ241255A (de)
PT (1)	PT99998B (de)
WO (1)	WO1992012165A1 (de)
ZA (1)	ZA92108B (de)

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US5602116A (en) *	1988-08-02	1997-02-11	Bone Care International, Inc.	Method for treating and preventing secondary hyperparathyroidism
US6538037B2 (en)	1991-01-08	2003-03-25	Bone Care International, Inc.	Methods for preparation and use of 1α,24(S)-dihydroxyvitamin D2
US20040009958A1 (en) *	1991-01-08	2004-01-15	Bone Care International, Inc.	Methods for preparation and use of 1alpha,24(S)-dihydroxyvitamin D2
EP0614456B1 (de) *	1992-08-28	1999-06-09	Bone Care International, Inc.	1alpha,24(s)-dihydroxy vitamin d2, seine synthese und verwendung
US5763429A (en) *	1993-09-10	1998-06-09	Bone Care International, Inc.	Method of treating prostatic diseases using active vitamin D analogues
US6376479B1 (en)	1995-04-03	2002-04-23	Bone Care International, Inc.	Method for treating and preventing hyperparathyroidism
US6242434B1 (en) *	1997-08-08	2001-06-05	Bone Care International, Inc.	24-hydroxyvitamin D, analogs and uses thereof
US6566353B2 (en) *	1996-12-30	2003-05-20	Bone Care International, Inc.	Method of treating malignancy associated hypercalcemia using active vitamin D analogues
US20020128240A1 (en) *	1996-12-30	2002-09-12	Bone Care International, Inc.	Treatment of hyperproliferative diseases using active vitamin D analogues
US6573256B2 (en)	1996-12-30	2003-06-03	Bone Care International, Inc.	Method of inhibiting angiogenesis using active vitamin D analogues
US6503893B2 (en)	1996-12-30	2003-01-07	Bone Care International, Inc.	Method of treating hyperproliferative diseases using active vitamin D analogues
JP2001511811A (ja)	1997-02-13	2001-08-14	ボーンケアインターナショナルインコーポレイテッド	ビタミンｄ化合物の標的治療放出
US20030129194A1 (en) *	1997-02-13	2003-07-10	Bone Care International, Inc.	Targeted therapeutic delivery of vitamin D compounds
US6087350A (en) *	1997-08-29	2000-07-11	University Of Pittsburgh Of The Commonwealth System Of Higher Education	Use of pretreatment chemicals to enhance efficacy of cytotoxic agents
ES2368824T3 (es) *	1998-03-27	2011-11-22	Oregon Health & Science University	Vitamina d y sus análogos en el tratamiento de tumores y otros desórdenes hiperproliferativos.
EP1091936B1 (de)	1998-05-29	2003-07-30	Bone Care International, Inc.	Verfahren zur herstellung von hydroxy-25-ene vitamin d verbindungen
AU7895601A (en) *	2000-07-18	2002-01-30	Bone Care Int Inc	Stabilized 1alpha-hydroxy vitamin d
ATE527372T1 (de)	2002-01-10	2011-10-15	Teva Pharma	Selektive enzymatische veresterung und solvolyse eines epimeren vitamin-d-analogs sowie trennung der epimere
US7148211B2 (en)	2002-09-18	2006-12-12	Genzyme Corporation	Formulation for lipophilic agents
US7094775B2 (en)	2004-06-30	2006-08-22	Bone Care International, Llc	Method of treating breast cancer using a combination of vitamin D analogues and other agents
US20060003950A1 (en) *	2004-06-30	2006-01-05	Bone Care International, Inc.	Method of treating prostatic diseases using a combination of vitamin D analogues and other agents
CA2576307A1 (en) *	2004-07-01	2006-03-09	Teva Pharmaceutical Industries Ltd.	Crystalline forms of 1,24(s)-dihydroxy vitamin d2
CN101607931B (zh) *	2009-07-23	2012-01-11	青岛正大海尔制药有限公司	一种骨化三醇的制备方法
CN103122009B (zh) *	2013-01-09	2015-11-25	江苏吉贝尔药业股份有限公司	两种用于合成他卡西醇支链的重要中间体化合物
CN103012463B (zh) *	2013-01-17	2016-02-10	南京理工大学	(s)-3-甲基-2-(叔丁基二甲基硅氧基)-1-溴丁烷的合成方法
CN104496871B (zh) *	2014-12-22	2016-03-09	上海皓元生物医药科技有限公司	一种他卡西醇的制备方法
CN109627279A (zh) *	2019-02-01	2019-04-16	浙江花园营养科技有限公司	一种活性维生素d3中间体的制备方法

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US4022891A (en) *	1974-06-18	1977-05-10	Teijin Limited	Novel 1α,24-dihydroxycholecalciferol compositions, novel precursors thereof, and processes for preparing them
US3970676A (en) *	1974-10-29	1976-07-20	The Upjohn Company	Novel process and intermediate compounds used is preparation of -Δ5,7- steroid dienes
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US4448721A (en) *	1982-09-20	1984-05-15	Wisconsin Alumni Research Foundation	Hydroxyvitamin D2 compounds and process for preparing same
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US4588528A (en) *	1984-05-31	1986-05-13	Wisconsin Alumni Research Foundation	1,24-dihydroxy-Δ22 -vitamin D3 and process for preparing same
US4728643A (en) *	1984-11-02	1988-03-01	The General Hospital Corporation	Method of treating psoriasis
JPH07100685B2 (ja) *	1985-08-02	1995-11-01	レオ・ファ−マシュ−ティカル・プロダクツ・リミテッド・エイ／エス（レ−ベンス・ケミスケ・ファブリック・プロデュクチオンスアクチ−セルスカブ）	新規ビタミンｄ類似体
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US5104864A (en) *	1988-08-02	1992-04-14	Bone Care International, Inc.	Method for treating and preventing loss of bone mass
US5242824A (en) *	1988-12-22	1993-09-07	Oncogen	Monoclonal antibody to human carcinomas
US5098899A (en) *	1989-03-06	1992-03-24	Trustees Of Boston University	Method for therapeutically treating psoriatic arthritis using vitamin D analogues and metabolites

1992
- 1992-01-07 AU AU12475/92A patent/AU1247592A/en not_active Abandoned
- 1992-01-07 EP EP98110802A patent/EP0914825B1/de not_active Expired - Lifetime
- 1992-01-07 AT AT92904947T patent/ATE179604T1/de not_active IP Right Cessation
- 1992-01-07 EP EP92904947A patent/EP0550702B1/de not_active Expired - Lifetime
- 1992-01-07 ES ES98110802T patent/ES2200238T3/es not_active Expired - Lifetime
- 1992-01-07 AT AT98110802T patent/ATE240736T1/de not_active IP Right Cessation
- 1992-01-07 DK DK92904947T patent/DK0550702T3/da active
- 1992-01-07 DE DE69229103T patent/DE69229103T2/de not_active Expired - Lifetime
- 1992-01-07 DE DE69233074T patent/DE69233074T2/de not_active Expired - Lifetime
- 1992-01-07 WO PCT/US1992/000313 patent/WO1992012165A1/en not_active Ceased
- 1992-01-07 ES ES92904947T patent/ES2134207T3/es not_active Expired - Lifetime
- 1992-01-08 ZA ZA92108A patent/ZA92108B/xx unknown
- 1992-01-08 MX MX9200070A patent/MX9200070A/es unknown
- 1992-01-08 CN CN92100866A patent/CN1032256C/zh not_active Expired - Lifetime
- 1992-01-08 PT PT99998A patent/PT99998B/pt not_active IP Right Cessation
- 1992-01-08 NZ NZ241255A patent/NZ241255A/xx not_active IP Right Cessation
1995
- 1995-06-07 US US08/483,371 patent/US6211168B1/en not_active Expired - Lifetime
- 1995-11-10 CN CN95118188A patent/CN1071574C/zh not_active Expired - Lifetime
- 1995-11-10 CN CN95118187A patent/CN1078072C/zh not_active Expired - Lifetime
1999
- 1999-06-09 GR GR990401539T patent/GR3030466T3/el unknown

Also Published As

Publication number	Publication date
EP0550702B1 (de)	1999-05-06
CN1067243A (zh)	1992-12-23
US6211168B1 (en)	2001-04-03
ATE179604T1 (de)	1999-05-15
EP0914825B1 (de)	2003-05-21
EP0914825A2 (de)	1999-05-12
EP0914825A3 (de)	1999-05-19
MX9200070A (es)	1992-07-01
CN1071574C (zh)	2001-09-26
CN1032256C (zh)	1996-07-10
DK0550702T3 (da)	1999-11-01
ES2200238T3 (es)	2004-03-01
DE69229103T2 (de)	1999-10-14
ZA92108B (en)	1992-10-28
DE69233074D1 (de)	2003-06-26
CN1133712A (zh)	1996-10-23
EP0550702A1 (de)	1993-07-14
DE69233074T2 (de)	2004-03-18
EP0550702A4 (en)	1994-06-08
WO1992012165A1 (en)	1992-07-23
AU1247592A (en)	1992-08-17
DE69229103D1 (de)	1999-06-10
ES2134207T3 (es)	1999-10-01
CN1143500A (zh)	1997-02-26
CN1078072C (zh)	2002-01-23
GR3030466T3 (en)	1999-10-29
PT99998A (pt)	1993-01-29
PT99998B (pt)	1999-06-30
NZ241255A (en)	1999-05-28

Legal Events

Date	Code	Title	Description
2003-11-15	RER	Ceased as to paragraph 5 lit. 3 law introducing patent treaties

Publication	Publication Date	Title
ATE240736T1 (de)	2003-06-15	Verfahren zur herstellung von 1-alpha-24- dihydroxy-vitamin d2
DE69415535D1 (de)	1999-02-04	Verfahren zur regulierung der sexuellen reaktion beim menschen
DE3684190D1 (de)	1992-04-16	Verwendung von tetrahydrobiopterinen zur herstellung eines medikaments zur behandlung von kinderautismus.
DE69317306D1 (de)	1998-04-09	Verfahren zur herstellung von pharmazeutische zusammensetzungen mittels ultraschall
DE68923819D1 (de)	1995-09-21	Verwendung von gamma-Hydroxy-Buttersäuresalzen zur Herstellung von pharmazeutischen Zusammensetzungen zur Verwendung bei der Behandlung von Alkoholismus und die hergestellten Zusammensetzungen.
HUT59313A (en)	1992-05-28	Process for producing pharmaceutical composition comprising flupirtin as active ingredient and suitable for combatting muscular tensions
ES2134267T3 (es)	1999-10-01	1alfa,24(s)-dihidroxi vitamina d2, su preparacion y utilizacion.
DE69325393D1 (de)	1999-07-22	Pharmazeutische zusammensetzungen und verfahren unter verwendung von isobutyramid zur behandlung von betaglobinerkrankungen
ATA278988A (de)	1990-05-15	Verfahren zur herstellung von 3-5-dimethyl-4methoxypyridinderivaten sowie neues zwischenprodukt hierfuer
WO1994005630B1 (en)	1994-04-14	1α,24(S)-DIHYDROXY VITAMIN D2, ITS FORMATION AND USE
ATE160561T1 (de)	1997-12-15	L-carnitin-salz, dieses enthaltende kosmetische und pharmazeutische zusammensetzungen zur behandlung von dermatosen
AT383123B (de)	1987-05-25	Verfahren zur herstellung von neuen (+)-catechin- alpha- monohydrat
DE69209166D1 (de)	1996-04-25	Diclofenac-Cholinsalz, Verfahren zur Herstellung und pharmazeutische Zusammensetzungen, die es enthalten
ATE130845T1 (de)	1995-12-15	Verfahren zur herstellung von 3-amino-2- (het)aroyl-acrylsäurederivaten.
ATE116636T1 (de)	1995-01-15	Verfahren zur herstellung von 2,6- dichlordiphenylaminessigsäurederivaten.
DK0505129T3 (da)	1995-08-07	Fremgangsmåde til fremstilling af et syntetisk detergentsæbegrundlag af N-acyl-sarcosin
ATE131155T1 (de)	1995-12-15	Verfahren zur herstellung von zwischenprodukten und zur synthese von n-(2-hydroxyethyl)-2- hydroxymethyl-3,4,5-trihydroxypiperidine.
ATE220915T1 (de)	2002-08-15	Einen basischen fibroblastwachstumsfaktor enthaltende mittel zur behandlung von knochenkrankheiten
ATE177748T1 (de)	1999-04-15	Enantiomerenreine cis-2-oxa-5,8-diazabicyclo (4.3.0)nonane sowie verfahren zu ihrer herstellung
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