KR960700213A - 항-안드로겐성 일고리-및 이고리-알켄(Anti-androgenic cyclo and bicyclo alkenes) - Google Patents
항-안드로겐성 일고리-및 이고리-알켄(Anti-androgenic cyclo and bicyclo alkenes)Info
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- KR960700213A KR960700213A KR1019950702903A KR19950702903A KR960700213A KR 960700213 A KR960700213 A KR 960700213A KR 1019950702903 A KR1019950702903 A KR 1019950702903A KR 19950702903 A KR19950702903 A KR 19950702903A KR 960700213 A KR960700213 A KR 960700213A
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- 230000002280 anti-androgenic effect Effects 0.000 title abstract 3
- 150000001336 alkenes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 34
- 125000000217 alkyl group Chemical group 0.000 claims abstract 8
- 241000124008 Mammalia Species 0.000 claims abstract 6
- 102000001307 androgen receptors Human genes 0.000 claims abstract 4
- 108010080146 androgen receptors Proteins 0.000 claims abstract 4
- 241000233866 Fungi Species 0.000 claims abstract 3
- 210000000481 breast Anatomy 0.000 claims abstract 3
- 244000005700 microbiome Species 0.000 claims abstract 3
- 208000002874 Acne Vulgaris Diseases 0.000 claims abstract 2
- 201000004384 Alopecia Diseases 0.000 claims abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract 2
- 208000002260 Keloid Diseases 0.000 claims abstract 2
- 206010000496 acne Diseases 0.000 claims abstract 2
- 230000015572 biosynthetic process Effects 0.000 claims abstract 2
- 239000002775 capsule Substances 0.000 claims abstract 2
- 210000001117 keloid Anatomy 0.000 claims abstract 2
- 201000008482 osteoarthritis Diseases 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 102000016942 Elastin Human genes 0.000 claims 1
- 108010014258 Elastin Proteins 0.000 claims 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 229920002549 elastin Polymers 0.000 claims 1
- 210000002950 fibroblast Anatomy 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 239000000051 antiandrogen Substances 0.000 abstract 2
- 230000004060 metabolic process Effects 0.000 abstract 2
- 206010068168 androgenetic alopecia Diseases 0.000 abstract 1
- 230000003416 augmentation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000001356 surgical procedure Methods 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
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- C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
- C07C403/06—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
- C07C403/10—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by etherified hydroxy groups
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- 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
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- A61P25/00—Drugs for disorders of the nervous system
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- 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
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07C29/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
- C07C29/128—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by alcoholysis
- C07C29/1285—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by alcoholysis of esters of organic acids
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
- C07C403/06—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
- C07C403/08—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by hydroxy groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
- C07C49/703—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
- C07C49/723—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups polycyclic
- C07C49/727—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system
- C07C49/733—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system having two rings
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
- C07C49/703—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
- C07C49/743—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups having unsaturation outside the rings, e.g. humulones, lupulones
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- C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
- C07C49/753—Unsaturated compounds containing a keto groups being part of a ring containing ether groups, groups, groups, or groups
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- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/185—Saturated compounds having only one carboxyl group and containing keto groups
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- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
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- C07C2601/14—The ring being saturated
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Abstract
본 발명은 제2안드로겐 수용체 부위에 대해 항-안드로겐 활성을 갖는 하기 일반식(ⅰ), (ⅱ) 및 (ⅲ)의 화합물에 관한 것으로서, 상기 화합물은 좌창, 남성 탈모증, 유착증 및 켈로이드를 앓고 있는 사람을 비롯한 포유동물을 치료하는데 유용하고, 여성의 유방 확대 수술후 비바람직한 유방 캡슐의 형성, 골관절염 및 알쯔하이머질병 증후군과 같은, 안드로겐 수용체와 관련이 있는 기타 질병 또는 질환을 치료하는데 효과적이며, 또한 항-안드로겐 화합물에 의해 조절되는 것으로 공지된, 특정 유기물과 군류의 물질 대사에 대해 억제 효과를 나타낸다:
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (38)
- 하기 일반식 (ⅰ), (ⅱ) 및 (ⅲ)의 화합물로 구성되는 군에서 선택되는 화합물:(ⅰ) (ⅱ) (ⅲ)상기 식중에서, R은 H, C1-6알킬 또는 CO-R2(식중, R2는 C1-6알킬임)이고; R1은 H, CH3또는 (CH2)m-CH3이며; n은 2 내지 10의 정수이고; m은 1 내지 6의 정수이다.
- 제1항에 있어서, 일반식(ⅰ)을 갖는 화합물.
- 제2항에 있어서, n이 3이고, R1이 H인 화합물.
- 제3항에 있어서, R이 H인 화합물.
- 제3항에 있어서, R이 OCH3인 화합물.
- 제2항에 있어서, n이 3이고, R1이 CH2CH3인 화합물.
- 제6항에 있어서, R이 H인 화합물.
- 제6항에 있어서, R이 OCH3인 화합물.
- 제2항에 있어서, R이 CO-R2인 화합물.
- 제1항에 있어서, 일반식(ⅱ)을 갖는 화합물.
- 제10항에 있어서, n이 3이고, R1이 H인 화합물.
- 제11항에 있어서, R이 H인 화합물.
- 제11항에 있어서, R이 OCH3인 화합물.
- 제10항에 있어서, n이 3이고, R1이 CH2CH3인 화합물.
- 제14항에 있어서, R이 H인 화합물.
- 제14항에 있어서, R이 OCH3인 화합물.
- 제10항에 있어서, R이 CO-R2인 화합물.
- 제1항에 있어서, 일반식(ⅲ)을 갖는 화합물.
- 제18항에 있어서, n이 3이고, R1이 H인 화합물.
- 제19항에 있어서, R이 H인 화합물.
- 제19항에 있어서, R이 OCH3인 화합물.
- 제18항에 있어서, n이 3이고, R1이 CH2CH3인 화합물.
- 제22항에 있어서, R이 H인 화합물.
- 제22항에 있어서, R이 OCH3인 화합물.
- 제18항에 있어서, R이 CO-R2인 화합물.
- 하기 일반식 (ⅰ),(ⅱ) 및(ⅲ)의 화합물로 구성되는 군에서 선택되는 화합물을 효과적인 투여량으로 함유하는 약학적 조성물을 포유 동물에 투여하는 것을 포함하여, 상기 포유 동물의 안드로겐 수용체 부위를 차단시키는 방법:(ⅰ) (ⅱ) (ⅲ)상기 식중에서, R은 H, C1-6알킬 또는 CO-R2(식중, R2는 C1-6알킬임)이고; R1은 H, CH3또는 (CH2)m-CH3이며; n은 2 내지 10의 정수이고; m은 1 내지 6의 정수이다.
- 제26항에 있어서, 상기 약학적 조성물은 국소 투여에 적합하도록 조제하여 국소 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 체내 투여에 적합하도록 조제하여 체내 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 좌창을 앓고 있는 포유 동물에 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 남성 탈모증을 앓고 있는 사람에게 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 켈로이드를 앓고 있는 포유 동물에 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 엘라스틴의 합성을 촉진시킬 목적으로 포유 동물에 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 삽입물 주위에 형성된 섬유 아세포 캡슐을 감소시킬 목적으로, 이질제 유방 삽입물을 지닌 여성에게 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 사람의 주름진 피부를 치료할 목적으로, 국소 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 알쯔하이머 질병을 앓고 있는 사람에게 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 이스트균 감염된 사람에게 투여하는 방법.
- 제26항에 있어서, 상기 약학적 조성물은 골관절염을 앓고 있는 사람에게 투여하는 방법.
- 안드로겐 수용체 부위를 차단시킴으로써, 상기 부위를 지닌 미생물 또는 균류의 성장을 조절하는 방법으로서, 상기 방법은 하기 일반식 (ⅰ), (ⅱ) 및 (ⅲ)의 화합물을 효과적인 투여량으로 함유하는 약학적 조성물을 상기 미생물 또는 균류에 투여하는 단계를 포함하는 것을 특징으로 하는 방법:(ⅰ) (ⅱ) (ⅲ)상기 식중에서, R은 H, C1-6알킬 또는 CO-R2(식중, R2는 C1-6알킬임)이고; R1은 H, CH3또는 (CH2)m-CH3이며; n은 2 내지 10의 정수이고; m은 1 내지 6의 정수이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08004972 US5264619B1 (en) | 1993-01-15 | 1993-01-15 | Anti-androgenic cyclo and bicyclo alkenes |
US08/004,972 | 1993-01-15 | ||
PCT/US1993/009844 WO1994015900A1 (en) | 1993-01-15 | 1993-10-14 | Anti-androgenic cyclo and bicyclo alkenes |
Publications (1)
Publication Number | Publication Date |
---|---|
KR960700213A true KR960700213A (ko) | 1996-01-19 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019950702903A KR960700213A (ko) | 1993-01-15 | 1993-10-14 | 항-안드로겐성 일고리-및 이고리-알켄(Anti-androgenic cyclo and bicyclo alkenes) |
Country Status (21)
Country | Link |
---|---|
US (1) | US5264619B1 (ko) |
EP (1) | EP0679152B1 (ko) |
JP (1) | JPH08505851A (ko) |
KR (1) | KR960700213A (ko) |
CN (1) | CN1051758C (ko) |
AT (1) | ATE157342T1 (ko) |
AU (1) | AU672265B2 (ko) |
BR (1) | BR9307758A (ko) |
CA (1) | CA2152588C (ko) |
DE (1) | DE69313466T2 (ko) |
DK (1) | DK0679152T3 (ko) |
ES (1) | ES2107793T3 (ko) |
GR (1) | GR3025092T3 (ko) |
IL (1) | IL107699A0 (ko) |
MX (1) | MX9307235A (ko) |
MY (1) | MY109679A (ko) |
NO (1) | NO952787L (ko) |
PH (1) | PH30285A (ko) |
TW (1) | TW294656B (ko) |
WO (1) | WO1994015900A1 (ko) |
ZA (1) | ZA938767B (ko) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4311870C2 (de) * | 1993-04-10 | 1998-07-30 | Altramed Holdings Ltd | Verwendung eines Anti-Östrigens zur Therapie und Prophylaxe von Demenz-Erkrankungen |
DE4320896A1 (de) * | 1993-06-24 | 1995-01-05 | Denecke Rainer Dr Med Vet | Präparat zur Therapie und Prophylaxe von Demenz-Erkrankungen |
WO1997002041A1 (en) | 1995-07-03 | 1997-01-23 | Crandall Wilson T | Transdermal and oral treatment of androgenic alopecia |
EA200001246A1 (ru) * | 1998-06-03 | 2001-08-27 | Джи Пи Ай Нил Холдингс, Инк. | Карбамиды и карбаматы n-гетероциклических карбоновых кислот и изостер карбоновых кислот |
US6417189B1 (en) | 1999-11-12 | 2002-07-09 | Gpi Nil Holdings, Inc. | AZA compounds, pharmaceutical compositions and methods of use |
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KR20040086262A (ko) * | 2002-01-09 | 2004-10-08 | 트라이던트 사이언스 엘엘씨 | 안드로겐 수용체 차단 화합물 |
US20070048246A1 (en) * | 2005-09-01 | 2007-03-01 | Biophysica Research, Inc. | Novel skin care compositions |
US20110021869A1 (en) * | 2009-07-24 | 2011-01-27 | Hilary John Cholhan | Single-incision minimally-invasive surgical repair of pelvic organ/vaginal prolapse conditions |
US8410314B1 (en) | 2010-06-21 | 2013-04-02 | Bcs Business Consulting Services Pte Ltd. | Method of synthesis |
MX2015012020A (es) | 2013-03-11 | 2016-04-06 | Bcs Business Consulting Services Pte Ltd | Procedimiento de sintesis. |
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Publication number | Priority date | Publication date | Assignee | Title |
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BE816441A (fr) * | 1973-06-20 | 1974-12-17 | Nouvelles amidines substituees et leurs procedes de preparation | |
US4689345A (en) * | 1982-05-06 | 1987-08-25 | Cbd Corporation | Oxygenated alkyl substituted bicyclo alkanes |
US4535182A (en) * | 1982-08-26 | 1985-08-13 | Sumitomo Chemical Company, Limited | Process for preparing 2-cyclopentenone esters |
GB8406000D0 (en) * | 1984-03-07 | 1984-04-11 | Ici Plc | Olefine derivatives |
JPH0637388B2 (ja) * | 1986-02-17 | 1994-05-18 | 千寿製薬株式会社 | 水性液剤 |
US4963583A (en) * | 1987-10-05 | 1990-10-16 | Ciba-Geigy Corporation | Beta-ionone derivatives as antifungal agents |
JP2608089B2 (ja) * | 1988-03-09 | 1997-05-07 | 帝人株式会社 | 4−ヒドロキシ−2−シクロペンテノン類およびそれを含有する薬剤組成物 |
US5010105A (en) * | 1989-06-09 | 1991-04-23 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
-
1993
- 1993-01-15 US US08004972 patent/US5264619B1/en not_active Expired - Fee Related
- 1993-10-14 AT AT94901162T patent/ATE157342T1/de not_active IP Right Cessation
- 1993-10-14 KR KR1019950702903A patent/KR960700213A/ko not_active Application Discontinuation
- 1993-10-14 DE DE69313466T patent/DE69313466T2/de not_active Expired - Fee Related
- 1993-10-14 WO PCT/US1993/009844 patent/WO1994015900A1/en active IP Right Grant
- 1993-10-14 JP JP6515960A patent/JPH08505851A/ja not_active Ceased
- 1993-10-14 ES ES94901162T patent/ES2107793T3/es not_active Expired - Lifetime
- 1993-10-14 CA CA002152588A patent/CA2152588C/en not_active Expired - Fee Related
- 1993-10-14 BR BR9307758A patent/BR9307758A/pt not_active Application Discontinuation
- 1993-10-14 EP EP94901162A patent/EP0679152B1/en not_active Expired - Lifetime
- 1993-10-14 DK DK94901162.1T patent/DK0679152T3/da active
- 1993-10-14 AU AU55847/94A patent/AU672265B2/en not_active Ceased
- 1993-11-19 MX MX9307235A patent/MX9307235A/es unknown
- 1993-11-22 PH PH47301A patent/PH30285A/en unknown
- 1993-11-22 IL IL10769993A patent/IL107699A0/xx unknown
- 1993-11-22 CN CN93114713A patent/CN1051758C/zh not_active Expired - Fee Related
- 1993-11-22 MY MYPI93002449A patent/MY109679A/en unknown
- 1993-11-23 ZA ZA938767A patent/ZA938767B/xx unknown
- 1993-11-23 TW TW082109864A patent/TW294656B/zh active
-
1995
- 1995-07-13 NO NO952787A patent/NO952787L/no unknown
-
1997
- 1997-10-20 GR GR970402733T patent/GR3025092T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
US5264619A (en) | 1993-11-23 |
DK0679152T3 (da) | 1998-02-23 |
GR3025092T3 (en) | 1998-01-30 |
ZA938767B (en) | 1994-06-30 |
JPH08505851A (ja) | 1996-06-25 |
AU5584794A (en) | 1994-08-15 |
EP0679152B1 (en) | 1997-08-27 |
TW294656B (ko) | 1997-01-01 |
AU672265B2 (en) | 1996-09-26 |
CN1091733A (zh) | 1994-09-07 |
NO952787D0 (no) | 1995-07-13 |
MX9307235A (es) | 1994-07-29 |
BR9307758A (pt) | 1995-10-24 |
US5264619B1 (en) | 1996-05-14 |
EP0679152A1 (en) | 1995-11-02 |
PH30285A (en) | 1997-02-20 |
ATE157342T1 (de) | 1997-09-15 |
NO952787L (no) | 1995-09-01 |
CA2152588A1 (en) | 1994-07-21 |
CA2152588C (en) | 1998-05-05 |
IL107699A0 (en) | 1994-02-27 |
DE69313466D1 (en) | 1997-10-02 |
WO1994015900A1 (en) | 1994-07-21 |
MY109679A (en) | 1997-04-30 |
CN1051758C (zh) | 2000-04-26 |
ES2107793T3 (es) | 1997-12-01 |
DE69313466T2 (de) | 1998-04-02 |
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