DK48690A - Effektive antagonister for det luteiniserende hormon-frigoerende hormon, der frigoer meget lidt histamin - Google Patents

Effektive antagonister for det luteiniserende hormon-frigoerende hormon, der frigoer meget lidt histamin Download PDF

Info

Publication number: DK48690A
Authority: DK; Denmark
Prior art keywords: antide; releasing; hormon; histamine; niclys
Prior art date: 1987-08-24

Application number

DK048690A

Other languages

English (en)

Other versions

DK48690D0 (da

DK173753B1 (da

Inventor

Karl Folkers

Cyril Y Bowers

Anders Ljungquist

Pui-Fun Louisa Tang

Minoru Kobota

Dong-Mei Feng

Original Assignee

Univ Texas

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.)

1987-08-24

Filing date

1990-02-23

Publication date

1990-04-19

1990-02-23 Application filed by Univ Texas filed Critical Univ Texas

1990-02-23 Publication of DK48690D0 publication Critical patent/DK48690D0/da

1990-04-19 Publication of DK48690A publication Critical patent/DK48690A/da

2001-09-10 Application granted granted Critical

2001-09-10 Publication of DK173753B1 publication Critical patent/DK173753B1/da

Links

NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 title abstract 4
239000005557 antagonist Substances 0.000 title abstract 2
229960001340 histamine Drugs 0.000 title abstract 2
QRYFGTULTGLGHU-NBERXCRTSA-N iturelix Chemical compound C([C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CCCCNC(=O)C=1C=NC=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)CCCNC(=O)C1=CC=CN=C1 QRYFGTULTGLGHU-NBERXCRTSA-N 0.000 abstract 6
108010083551 iturelix Proteins 0.000 abstract 6
230000002513 anti-ovulatory effect Effects 0.000 abstract 4
DFZVZEMNPGABKO-SSDOTTSWSA-N (2r)-2-amino-3-pyridin-3-ylpropanoic acid Chemical compound OC(=O)[C@H](N)CC1=CC=CN=C1 DFZVZEMNPGABKO-SSDOTTSWSA-N 0.000 abstract 2
108700012941 GNRH1 Proteins 0.000 abstract 2
239000000579 Gonadotropin-Releasing Hormone Substances 0.000 abstract 2
108090000765 processed proteins & peptides Proteins 0.000 abstract 2
102000004196 processed proteins & peptides Human genes 0.000 abstract 2
HQMLIDZJXVVKCW-UWTATZPHSA-N (2r)-2-aminopropanamide Chemical compound C[C@@H](N)C(N)=O HQMLIDZJXVVKCW-UWTATZPHSA-N 0.000 abstract 1
QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 abstract 1
241000288906 Primates Species 0.000 abstract 1
239000000556 agonist Substances 0.000 abstract 1
239000002285 corn oil Substances 0.000 abstract 1
235000005687 corn oil Nutrition 0.000 abstract 1
239000003814 drug Substances 0.000 abstract 1
238000011156 evaluation Methods 0.000 abstract 1
238000009472 formulation Methods 0.000 abstract 1
239000000203 mixture Substances 0.000 abstract 1
230000003389 potentiating effect Effects 0.000 abstract 1
238000009781 safety test method Methods 0.000 abstract 1
238000013341 scale-up Methods 0.000 abstract 1
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S930/00—Peptide or protein sequence
- Y10S930/01—Peptide or protein sequence
- Y10S930/13—Luteinizing hormone-releasing hormone; related peptides

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Molecular Biology (AREA)
Endocrinology (AREA)
Genetics & Genomics (AREA)
Biophysics (AREA)
Biochemistry (AREA)
Veterinary Medicine (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Public Health (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Gastroenterology & Hepatology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Epidemiology (AREA)
Reproductive Health (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Polyesters Or Polycarbonates (AREA)
Macromonomer-Based Addition Polymer (AREA)
Preparation Of Compounds By Using Micro-Organisms (AREA)

DK199000486A 1987-08-24 1990-02-23 LHRH-antagonist med negligerbar histaminfrigørelsesaktivitet, som er et decapeptid og anvendelse af decapeptidet DK173753B1 (da)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
US8843187		1987-08-24
US07/088,431 US4935491A (en)	1987-08-24	1987-08-24	Effective antagonists of the luteinizing hormone releasing hormone which release negligible histamine
PCT/US1988/002922 WO1989001944A1 (en)	1987-08-24	1988-08-24	Effective antagonists of the luteinizing hormone releasing hormone which release negligible histamine
US8802922		1988-08-24

Publications (3)

Publication Number	Publication Date
DK48690D0 DK48690D0 (da)	1990-02-23
DK48690A true DK48690A (da)	1990-04-19
DK173753B1 DK173753B1 (da)	2001-09-10

Family

ID=22211329

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK199000486A DK173753B1 (da)	1987-08-24	1990-02-23	LHRH-antagonist med negligerbar histaminfrigørelsesaktivitet, som er et decapeptid og anvendelse af decapeptidet

Country Status (14)

Country	Link
US (3)	US4935491A (da)
EP (1)	EP0377665B1 (da)
JP (1)	JP2621970B2 (da)
KR (1)	KR0135276B1 (da)
AT (1)	ATE124957T1 (da)
AU (1)	AU619221B2 (da)
DE (1)	DE3854159T2 (da)
DK (1)	DK173753B1 (da)
FI (1)	FI102074B1 (da)
HU (2)	HU213098B (da)
MX (1)	MX9203688A (da)
NO (1)	NO301015B1 (da)
OA (1)	OA09786A (da)
WO (1)	WO1989001944A1 (da)

Families Citing this family (38)

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US5110904A (en) *	1989-08-07	1992-05-05	Abbott Laboratories	Lhrh analogs
IL87055A (en) *	1988-07-08	1994-06-24	Illana Gozes	Conjugates of vasoactive intestinal peptide (vip) and of fragments thereof and pharmaceutical compositions comprising them
US5171835A (en) *	1988-10-21	1992-12-15	The Administrators Of The Tulane Educational Fund	LHRH antagonists
US5447912A (en) *	1989-09-18	1995-09-05	Senetek, Plc	Erection-inducing methods and compositions
US5169932A (en) *	1989-10-30	1992-12-08	The Salk Institute For Biological Studies	Gnrh analogs
US5296468A (en) *	1989-10-30	1994-03-22	The Salk Institute For Biological Studies	GnRH analogs
US5352796A (en) *	1989-10-30	1994-10-04	The Salk Institute For Biological Studies	Amino acids useful in making GnRH analogs
US5212288A (en) *	1990-02-20	1993-05-18	Syntex (U.S.A.) Inc.	Temporary minimal protection synthesis of serine-containing polypeptides
US5180711A (en) *	1990-06-14	1993-01-19	Applied Research Systems Ars Holding N.V.	Combined treatment with gnrh antagonist and gnrh to control gonadotropin levels in mammals
US5169935A (en) *	1990-06-20	1992-12-08	The Salk Institute For Biological Studies	Method of making peptides
US5744450A (en) *	1991-03-14	1998-04-28	The Salk Institute For Biological Studies	GnRH analogs
DE69214818T2 (de) *	1991-04-25	1997-02-27	Romano S.-Cergue Deghenghi	LHRH-Antagonisten
DE4117507A1 (de) *	1991-05-24	1992-11-26	Schering Ag	Verfahren zur herstellung von n(pfeil hoch)6(pfeil hoch)-substituierten lysin-derivaten
US5656727A (en) *	1992-09-15	1997-08-12	The Administrators Of The Tulane Educational Fund	Antagonists of LHRH
US5480969A (en) *	1992-09-15	1996-01-02	The Administrators Of The Tulane Educational Fund	Antagonists of LHRH
JPH08510260A (ja) *	1993-05-20	1996-10-29	バイオテック・オーストラリア・プロプライエタリー・リミテッド	Ｌｈｒｈ拮抗剤
US5843901A (en)	1995-06-07	1998-12-01	Advanced Research & Technology Institute	LHRH antagonist peptides
US6043218A (en)	1996-10-22	2000-03-28	Medical University Of South Carolina	Positively charged non-natural amino acids, methods of making thereof, and use thereof in peptides
US6566330B1 (en)	1996-10-22	2003-05-20	Medical University Of South Carolina Foundation Research Development	Positively charged non-natural amino acids, methods of making and using thereof in peptides
US5968895A (en)	1996-12-11	1999-10-19	Praecis Pharmaceuticals, Inc.	Pharmaceutical formulations for sustained drug delivery
US5821230A (en) *	1997-04-11	1998-10-13	Ferring Bv	GnRH antagonist decapeptides
US5925730A (en)	1997-04-11	1999-07-20	Ferring Bv	GnRH antagonists
EP0880969A1 (en) *	1997-05-28	1998-12-02	Applied Research Systems ARS Holdings N.V.	Pharmaceutical compositions of peptides having low solubility in physiological medium
EP0882736A1 (en) *	1997-06-02	1998-12-09	Laboratoire Theramex S.A.	LH-RH peptide analogues, their uses and pharmaceutical compositions containing them
US6217844B1 (en)	1998-04-27	2001-04-17	Praecis Pharmaceuticals, Inc.	Methods for detecting lesions in dense breast tissue using LHRH antagonists
US7953788B2 (en)	2001-09-29	2011-05-31	Siebel Systems, Inc.	System and method for queuing data for an application server
DE69939036D1 (de)	1998-04-28	2008-08-14	Serono Lab	PEG Konjugate von LHRH Analogen
US6455499B1 (en)	1999-02-23	2002-09-24	Indiana University Foundation	Methods for treating disorders associated with LHRH activity
US7109171B2 (en)	2000-02-28	2006-09-19	Praecis Pharmaceuticals Inc.	Methods for treating FSH related conditions with GnRH antagonists
US6598784B2 (en) *	2000-12-20	2003-07-29	Meadwestvaco Packaging Syatens, Llc	Beverage carton with strap type carrying handle
DK1345593T3 (da) *	2000-12-27	2007-12-10	Ares Trading Sa	Lipidmikropartikler ved kryogen mikronisering
JP2002201168A (ja) *	2000-12-28	2002-07-16	Kaken Pharmaceut Co Ltd	シクロヘキサン誘導体
WO2002056903A2 (en) *	2001-01-17	2002-07-25	Praecis Pharmaceuticals Inc.	Methods for treating hormone associated conditions using a combination of lhrh antagonists and specific estrogen receptor modulators
FR2840532B1 (fr) *	2002-06-11	2005-05-06	Ethypharm Sa	Nanocapsules lipidiques furtives, procede de preparation et utilisation comme vecteur de principes(s) actif(s)
GB0320806D0 (en)	2003-09-05	2003-10-08	Astrazeneca Ab	Therapeutic treatment
AU2004313245B2 (en)	2003-12-30	2011-04-14	Durect Corporation	Polymeric implants, preferably containing a mixture of PEG and PLG, for controlled release of active agents, preferably a GNRH
JP4927729B2 (ja) *	2004-07-16	2012-05-09	オークウッドラボラトリーズ，エル．エル．シー．	性腺刺激ホルモン放出ホルモンアンタゴニスト
WO2006080256A1 (ja) *	2005-01-26	2006-08-03	Sumitomo Seika Chemicals Co., Ltd.	１－（６－メチルピリジン－３－イル）－２－［４－（メチルスルホニル）フェニル］エタノンの製造方法および製造中間体

Family Cites Families (22)

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US4431635A (en) *	1979-06-13	1984-02-14	Coy David Howard	LH-RH Antagonists
AU9102582A (en) *	1981-12-10	1983-06-16	David Howard Coy	Lh-rh antagonists
FI832053L (fi) *	1982-06-10	1983-12-11	Syntex Inc	Nonapeptid- och dekapeptidanaloger av lhrh anvaendbara som lhrh-antagonister samt deras framstaellningsfoerfarande
US4444759A (en) *	1982-07-26	1984-04-24	The Salk Institute For Biological Studies	GnRH Antagonists II
US4504414A (en) *	1983-03-28	1985-03-12	Board Of Regents, The University Of Texas System	Synthetic pyridyl-alanyl decapeptides having antiovulatory activity
US4530920A (en) *	1983-11-07	1985-07-23	Syntex (U.S.A.) Inc.	Nonapeptide and decapeptide analogs of LHRH, useful as LHRH agonist
US4547370A (en) *	1983-11-29	1985-10-15	The Salk Institute For Biological Studies	GnRH Antagonists
US4845077A (en) *	1984-04-03	1989-07-04	Serono Laboratories, Inc.	Method of inducing ovulation
US4652550A (en) *	1984-05-21	1987-03-24	The Salk Institute For Biological Studies	GnRH antagonists VII
IL74827A (en) *	1984-05-21	1989-06-30	Salk Inst For Biological Studi	Peptides active as gnrh antagonists and pharmaceutical compositions containing them
US4647653A (en) *	1984-08-23	1987-03-03	Tulane Educational Fund	Therapeutic peptides
US4565804A (en) *	1984-09-07	1986-01-21	The Salk Institute For Biological Studies	GnRH Antagonists VI
ZA862570B (en) *	1985-04-09	1986-12-30	Univ Tulane	Therapeutic decapeptides
AU5638886A (en) *	1985-04-19	1986-10-23	Syntex (U.S.A.) Inc.	Contraceptive methods for dogs using the decapeptide lhrh
EP0225746A3 (en) *	1985-11-14	1989-12-20	The Administrators of The Tulane Educational Fund	Therapeutic decapeptides
US4801577A (en) *	1987-02-05	1989-01-31	Syntex (U.S.A.) Inc.	Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists
US4851385A (en) *	1987-07-15	1989-07-25	Indiana University Foundation	LHRH antagonist analogs having low histamine-release activity
DE68928278T2 (de) *	1988-02-10	1998-03-12	Tap Pharmaceuticals Inc	Lhrh-analog
US5300492A (en) *	1988-02-10	1994-04-05	Tap Pharmaceuticals	LHRH analogs
US5140009A (en) *	1988-02-10	1992-08-18	Tap Pharmaceuticals, Inc.	Octapeptide LHRH antagonists
US5180711A (en) *	1990-06-14	1993-01-19	Applied Research Systems Ars Holding N.V.	Combined treatment with gnrh antagonist and gnrh to control gonadotropin levels in mammals
US5413990A (en) *	1993-08-06	1995-05-09	Tap Pharmaceuticals Inc.	N-terminus modified analogs of LHRH

1987
- 1987-08-24 US US07/088,431 patent/US4935491A/en not_active Expired - Lifetime
1988
- 1988-08-24 AU AU25294/88A patent/AU619221B2/en not_active Expired
- 1988-08-24 AT AT88908786T patent/ATE124957T1/de not_active IP Right Cessation
- 1988-08-24 KR KR1019890700699A patent/KR0135276B1/ko not_active Expired - Fee Related
- 1988-08-24 MX MX9203688A patent/MX9203688A/es unknown
- 1988-08-24 WO PCT/US1988/002922 patent/WO1989001944A1/en not_active Ceased
- 1988-08-24 EP EP88908786A patent/EP0377665B1/en not_active Expired - Lifetime
- 1988-08-24 JP JP63507982A patent/JP2621970B2/ja not_active Expired - Lifetime
- 1988-08-24 DE DE3854159T patent/DE3854159T2/de not_active Expired - Lifetime
- 1988-08-24 HU HU885868A patent/HU213098B/hu unknown
1989
- 1989-06-26 US US07/371,552 patent/US5470947A/en not_active Expired - Lifetime
1990
- 1990-02-23 NO NO900888A patent/NO301015B1/no not_active IP Right Cessation
- 1990-02-23 FI FI900947A patent/FI102074B1/fi not_active IP Right Cessation
- 1990-02-23 DK DK199000486A patent/DK173753B1/da not_active IP Right Cessation
- 1990-02-26 OA OA59743A patent/OA09786A/en unknown
1995
- 1995-06-06 US US08/466,333 patent/US5763404A/en not_active Expired - Lifetime
- 1995-06-29 HU HU95P/P00574P patent/HU211882A9/hu unknown

Also Published As

Publication number	Publication date
FI102074B (fi)	1998-10-15
HU211882A9 (en)	1995-12-28
EP0377665B1 (en)	1995-07-12
AU2529488A (en)	1989-03-31
WO1989001944A1 (en)	1989-03-09
HUT59940A (en)	1992-07-28
HU885868D0 (en)	1991-12-30
US5763404A (en)	1998-06-09
EP0377665A1 (en)	1990-07-18
DE3854159D1 (de)	1995-08-17
FI900947A0 (fi)	1990-02-23
DK48690D0 (da)	1990-02-23
AU619221B2 (en)	1992-01-23
NO900888D0 (no)	1990-02-23
JP2621970B2 (ja)	1997-06-18
OA09786A (en)	1994-04-15
US5470947A (en)	1995-11-28
KR890701117A (ko)	1989-12-19
NO900888L (no)	1990-04-23
FI102074B1 (fi)	1998-10-15
JPH03501969A (ja)	1991-05-09
US4935491A (en)	1990-06-19
MX9203688A (es)	1992-09-01
KR0135276B1 (ko)	1998-04-23
NO301015B1 (no)	1997-09-01
HU213098B (en)	1997-02-28
DE3854159T2 (de)	1996-02-15
ATE124957T1 (de)	1995-07-15
DK173753B1 (da)	2001-09-10

Legal Events

Date	Code	Title	Description
2001-09-10	B1	Patent granted (law 1993)
2008-09-08	PUP	Patent expired

Publication	Publication Date	Title
DK48690A (da)	1990-04-19	Effektive antagonister for det luteiniserende hormon-frigoerende hormon, der frigoer meget lidt histamin
Vickery	1986	Comparison of the potential for therapeutic utilities with gonadotropin-releasing hormone agonists and antagonists
LU90425I2 (fr)	1999-10-04	Cetrorelix et ses seis et d-riv-s pharmaceutiquement acceptables sp-cialement l'ac-tate de c-trorelix
AU746132B2 (en)	2002-04-18	LH-RH peptide analogues, their uses and pharmaceutical compositions containing them
FI880509A7 (fi)	1988-08-06	LHRH:n nonapeptidi- ja dekapeptidianalogeja, jotka ovat käyttökelpoisia LHRH:n antagonisteina
Hahn et al.	1985	Reproductive/endocrine and anaphylactoid properties of an LHRH-antagonist, ORF 18260 [Ac-DNAL1 (2), 4FDPhe2, D-Trp3, D-Arg6]-GnRH
Sandow et al.	1978	Structure-activity relationships in the LH-RH molecule
PH18965A (en)	1985-11-26	Gnrh antagonists,pharmaceutical compositions containing the same and method of use thereof
EP0182627A3 (en)	1988-10-05	Basic v1-vasopressin antagonists
EP0122712A3 (en)	1986-05-14	Gnrh antagonists
ES8207510A1 (es)	1982-09-16	Un metodo de preparacion de un peptido inhibidor de la liberacion de gonadotropinas por la glandula pituitaria en mamiferos.
Nekola et al.	1984	LHRH antagonists in females
Kovacs et al.	1984	Long-term inhibition of ovulation by a GnRH-antagonist at low dose level
Pinski et al.	1993	Recovery of pituitary‐gonadal function in male rats after long‐term suppression induced by a single injection of microcapsules of LH‐RH antagonist Cetrorelix (SB‐75)
Pinski et al.	1992	Comparison of biological effects of a sustained delivery system and nonencapsulated LH-RH antagonist SB-75 in rats
ATE59393T1 (de)	1991-01-15	Peptide.
Crighton	1973	The effects of synthetic gonadotrophin releasing factor on the release of luteinizing hormone and follicle-stimulating hormone from ovine pituitary tissue in vitro
Pinski et al.	1993	Evaluation of biological activities of new LH‐RH antagonists (T‐series) in male and female rats
Hahn et al.	1988	Contraceptive Potential of GnRH Antagonists
FI933629L (fi)	1993-08-17	Antagonistpeptider till hormon som frigoer luteiniserande hormon (lhrh)