BR9611760A - Novos antagonistas lh-rh com efeito aperfeiçoado - Google Patents

Novos antagonistas lh-rh com efeito aperfeiçoado

Info

Publication number
BR9611760A
BR9611760A BR9611760-5A BR9611760A BR9611760A BR 9611760 A BR9611760 A BR 9611760A BR 9611760 A BR9611760 A BR 9611760A BR 9611760 A BR9611760 A BR 9611760A
Authority
BR
Brazil
Prior art keywords
antagonists
new
improved effect
salts
free
Prior art date
Application number
BR9611760-5A
Other languages
English (en)
Inventor
Bernhard Kutscher
Michael Bernd
Thomas Beckers
Thomas Klenner
Peter Paul Emig
Patricia Marie Charpentier
Original Assignee
Asta Medica Ag
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 Asta Medica Ag filed Critical Asta Medica Ag
Publication of BR9611760A publication Critical patent/BR9611760A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2632-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/272-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/80Acids; Esters in position 3
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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
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    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30Oxygen or sulfur atoms
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    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
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    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
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Abstract

Patente de Invenção:<B>"NOVOS ANTAGONISTAS LH-RH COM EFEITO APERFEIçOADO"<D>. A invenção refere-se a novos antagonistas LH-RH, especialmente peptidomiméticos e peptídeos modificados em uma cadeia laterail, sais dos mesmos com ácidos aceitáveis farmaceuticamente, bem como processos para a preparação dos antagonistas LH-RH e seus sais. Os peptídeos de acordo com a invenção representam análogos do hormónio (LH-RH) que libera hormónio luteinizante. Os compostos de acordo com a invenção apresentam uma alta potência antagónica e estão isentos de efeitos colaterais indesejados, especialmente livres de efeitos edematogêneos.
BR9611760-5A 1995-11-28 1996-11-14 Novos antagonistas lh-rh com efeito aperfeiçoado BR9611760A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19544212A DE19544212A1 (de) 1995-11-28 1995-11-28 Neue LH-RH-Antagonisten mit verbesserter Wirkung
PCT/DE1996/002171 WO1997019953A2 (de) 1995-11-28 1996-11-14 Neue lh-rh-antagonisten mit verbesserter wirkung

Publications (1)

Publication Number Publication Date
BR9611760A true BR9611760A (pt) 1999-10-05

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Application Number Title Priority Date Filing Date
BR9611760-5A BR9611760A (pt) 1995-11-28 1996-11-14 Novos antagonistas lh-rh com efeito aperfeiçoado

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EP (1) EP0876337B1 (pt)
JP (1) JP2000501083A (pt)
KR (1) KR100460165B1 (pt)
CN (1) CN1087283C (pt)
AR (1) AR004354A1 (pt)
AT (1) ATE289588T1 (pt)
AU (1) AU706546B2 (pt)
BG (1) BG64386B1 (pt)
BR (1) BR9611760A (pt)
CA (1) CA2238570A1 (pt)
CZ (1) CZ290098B6 (pt)
DE (2) DE19544212A1 (pt)
DK (1) DK0876337T3 (pt)
EE (1) EE04318B1 (pt)
ES (1) ES2238704T3 (pt)
HK (1) HK1016999A1 (pt)
HU (1) HUP9901656A3 (pt)
IL (1) IL119703A (pt)
IS (1) IS1914B (pt)
MX (1) MX9804120A (pt)
NO (1) NO311023B1 (pt)
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PL (1) PL186872B1 (pt)
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RU (1) RU2163910C2 (pt)
SI (1) SI0876337T1 (pt)
SK (1) SK282760B6 (pt)
UA (1) UA65531C2 (pt)
WO (1) WO1997019953A2 (pt)
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Publication number Priority date Publication date Assignee Title
DE19911771B4 (de) * 1999-03-17 2006-03-30 Zentaris Gmbh LHRH-Antagonist, Verfahren zu seiner Herstellung und seiner Verwendung
US7005418B1 (en) 1999-09-23 2006-02-28 Zentaris Gmbh Method for the therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction
MXPA02008870A (es) 2000-03-14 2003-06-24 Zentaris Ag Novedosos antagonistas de lhrh, produccion de los mismos y sus uso como medicamentos.
SE0100567D0 (sv) * 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
CN104086632A (zh) * 2014-08-05 2014-10-08 杭州诺泰制药技术有限公司 一种制备西曲瑞克的方法

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IL101074A (en) * 1991-03-14 1997-09-30 Salk Inst For Biological Studi GnRH ANALOGS AND THEIR PREPARATION
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WO1994014841A1 (en) * 1992-12-18 1994-07-07 Abbott Laboratories Lhrh antagonists having modified aminoacyl residues at postions 5 and 6
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IL119703A (en) 2001-04-30
RU2163910C2 (ru) 2001-03-10
EE04318B1 (et) 2004-06-15
PL186872B1 (pl) 2004-03-31
IS1914B (is) 2004-02-03
NO982366L (no) 1998-05-25
NZ330521A (en) 1999-01-28
WO1997019953A2 (de) 1997-06-05
HUP9901656A2 (hu) 1999-08-30
ES2238704T3 (es) 2005-09-01
NO982366D0 (no) 1998-05-25
WO1997019953A3 (de) 1997-08-28
HK1016999A1 (en) 1999-11-22
ATE289588T1 (de) 2005-03-15
WO1997019953A8 (de) 2002-09-26
HUP9901656A3 (en) 2001-10-29
CZ290098B6 (cs) 2002-05-15
CN1202882A (zh) 1998-12-23
UA65531C2 (en) 2004-04-15
KR100460165B1 (ko) 2005-06-01
JP2000501083A (ja) 2000-02-02
SK62998A3 (en) 1999-07-12
AU706546B2 (en) 1999-06-17
SK282760B6 (sk) 2002-12-03
DE59611201D1 (de) 2005-03-31
KR19990071864A (ko) 1999-09-27
EP0876337A2 (de) 1998-11-11
SI0876337T1 (en) 2005-06-30
CZ135898A3 (cs) 1998-09-16
CA2238570A1 (en) 1997-06-05
AU1867097A (en) 1997-06-19
MX9804120A (es) 1998-09-30
BG64386B1 (bg) 2004-12-30
BG102514A (en) 1999-04-30
DK0876337T3 (da) 2005-05-09
CN1087283C (zh) 2002-07-10
EP0876337B1 (de) 2005-02-23
DE19544212A1 (de) 1997-06-05
IL119703A0 (en) 1997-02-18
IS4733A (is) 1998-05-05
NO311023B1 (no) 2001-10-01
ZA969987B (en) 1997-06-17
AR004354A1 (es) 1998-11-04
PL326977A1 (en) 1998-11-09
PT876337E (pt) 2005-06-30
EE9800165A (et) 1998-12-15

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