HUP0002392A2 - Növekedési hormon kiválasztását fokozó diazol-, oxazolszármazékok, eljárás előállításukra, valamint ezeket tartalmazó gyógyászati készítmények - Google Patents

Növekedési hormon kiválasztását fokozó diazol-, oxazolszármazékok, eljárás előállításukra, valamint ezeket tartalmazó gyógyászati készítmények

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Publication number
HUP0002392A2
HUP0002392A2 HU0002392A HUP0002392A HUP0002392A2 HU P0002392 A2 HUP0002392 A2 HU P0002392A2 HU 0002392 A HU0002392 A HU 0002392A HU P0002392 A HUP0002392 A HU P0002392A HU P0002392 A2 HUP0002392 A2 HU P0002392A2
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Hungary
Prior art keywords
alkyl
aryl
alkylaryl
ylalkyl
naphthyl
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HU0002392A
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English (en)
Inventor
Charles Arthur Alt
Henry Uhlman Bryant
Jeffrey Daniel Cohen
James Densmore Copp
Jeffrey Alan Dodge
Kennan Joseph Fahey
William Harlan Gritton
Kenneth Lee Hauser
Mark Louis Heiman
Scott Alan Jones
Louis Nickolaus Jungheim
Joseph Henry Kennedy
Charles Willis Lugar III.
Brian Stephen Muehl
Alan David Palkowitz
Andrew Michael Ratz
Gary Anthony Rhodes
Robert Lewis Robey
David Edward Seyler
Timothy Alan Shepherd
Kenneth Jeff Thrasher
William George Trankle
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Eli Lilly And Co.
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Publication of HUP0002392A2 publication Critical patent/HUP0002392A2/hu
Publication of HUP0002392A3 publication Critical patent/HUP0002392A3/hu

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    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D207/30Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/402,5-Pyrrolidine-diones
    • C07D207/4162,5-Pyrrolidine-diones 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 other ring carbon atoms
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • 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
    • 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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    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D207/04Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic 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 no double bonds between ring members or between ring members and non-ring members 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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    • C07D207/30Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/42Nitro radicals
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • 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
    • C07D231/14Heterocyclic 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 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
    • C07D231/38Nitrogen atoms
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    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/66Heterocyclic 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 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
    • C07D233/88Nitrogen atoms, e.g. allantoin
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr

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Abstract

A találmány tárgyát az (I) általános képletű vegyületek, e vegyületekgyógyászatilag megfelelő sói vagy szolvátjai, valamint ezekettartalmazó gyógyászati készítmények képezik. A találmány tárgyáhoztartozik ezen kívül az (I) általános képletű vegyületek előállításáraszolgáló eljárás is. A találmány szerinti vegyületek kedvezőenbefolyásolják a növekedési hormonszintet. Az (I) általános képletben aszubsztituensek jelentése igen sokféle, többek között A jelentése alkil-, aril-, alkil-aril-, alkil-(O)-alkil-aril-, alkil-(S)-alkil-aril-, indolil-, indolinil-, tienil-, alkil-tienil-,benzotienil-, benzofuranil-, naftil-, ciklohexil-, alkil-indolil-,alkil-benzotienil-, alkil-naftil-, alkil-benzofuranil- vagy alkil-ciklohexil-csoport; B jelentése -NH2, -NHR1, alkil-NH2, alkil-NHR1, alkil-aril-NH2, alkil-aril-NHR1, alkil-ciklohexil-NH2, alkil-ciklohexil-NH-R1, R1-piperidin-3-il-alkil-, R1-piperidin-2-il-alkil-, R1-piperidin-4-il-alkil-, R1-kinolin-2-il-alkil-, R1-(2,4-dihidrokinolin-2-il-alkil-, R1-izokinolin-2-il-alkil- vagy R1-(2,4-dihidroizokinolin-2-il)-alkil-csoport; X jelentése alkilidenil-, O, S, NH- vagy N-alkil-csoport; V jelentése heterociklusos csoport, D jelentése hidrogénatom, alkil-, alkil-(O)(CO)-alkil-, alkil-(O)(CO)N-(alkil)2-, alkil-aril-, C(O)R6, alkil-(O)-R6, alkil-(OH)-,alkil-C(O)-R6, alkil-R6, aril-, alkil-NHSO2-alkil-, alkil)-NHSO2-arilcsoport; E jelentése hidrogénatom, alkil-, C(O)-alkil-, aril-, (aril)-C(O)NR6,aril-alkil-C(O)R6, alkil-aril-, C(O)-aril-, alkil-C(O)-aril-, naftil-,alkil-naftil, C(O)-naftil-, alkil-C(O)-naftil-, heteroaril-, alkil-heteroaril-, C(O)-heteroaril-, alkil-C(O)-heteroaril-, indanil-,alkil-indanil-, C(O)-indanil-, -C(O)-indanil- vagy cikloalkilcsoort; G jelentése hidrogénatom, alkil-, aril-, alkil-aril- vagyalkenilcsoport; J jelentése hidrogénatom, alkil-, aril- vagy alkil-aril-csoport; L jelentése hidrogénatom, alkil-, C(O)O-alkil-, aril-, alkil-aril-,C(O)O-alkil-aril-, alkenil-, -F vagy -CN, alkil-OH, alkil-O-alkil-,alkil-C(O)R6 képletű csoport. Ó
HU0002392A 1997-08-19 1998-08-19 Diazole and oxazole derivatives as growth hormone secretagogues, process for producing them and pharmaceutical compositions containing them HUP0002392A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5614297P 1997-08-19 1997-08-19
PCT/US1998/017229 WO1999008699A1 (en) 1997-08-19 1998-08-19 Growth hormone secretagogues

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HUP0002392A2 true HUP0002392A2 (hu) 2000-10-28
HUP0002392A3 HUP0002392A3 (en) 2000-11-28

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JP (1) JP2001515046A (hu)
KR (1) KR20010027947A (hu)
CN (1) CN1243567C (hu)
AR (1) AR018010A1 (hu)
AU (1) AU738204B2 (hu)
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CA (1) CA2302467A1 (hu)
CO (1) CO5121066A1 (hu)
EA (1) EA002746B1 (hu)
HR (1) HRP20000090A2 (hu)
HU (1) HUP0002392A3 (hu)
ID (1) ID25000A (hu)
IL (1) IL134596A0 (hu)
MY (1) MY138258A (hu)
NO (1) NO20000823L (hu)
NZ (1) NZ502947A (hu)
PE (1) PE115999A1 (hu)
PL (1) PL338883A1 (hu)
TR (1) TR200000930T2 (hu)
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UA (1) UA58472C2 (hu)
WO (1) WO1999008699A1 (hu)
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MY138258A (en) 2009-05-29
CO5121066A1 (es) 2002-01-30
CN1276727A (zh) 2000-12-13
KR20010027947A (ko) 2001-04-06
HRP20000090A2 (en) 2001-04-30
NO20000823D0 (no) 2000-02-18
TW577879B (en) 2004-03-01
AR018010A1 (es) 2001-10-31
NZ502947A (en) 2001-11-30
AU738204B2 (en) 2001-09-13
CA2302467A1 (en) 1999-02-25
AU9025698A (en) 1999-03-08
ZA987385B (en) 2000-04-18
NO20000823L (no) 2000-04-12
HUP0002392A3 (en) 2000-11-28
EP0933365A3 (en) 2003-03-19
JP2001515046A (ja) 2001-09-18
PE115999A1 (es) 1999-11-26
CN1243567C (zh) 2006-03-01
BR9811948A (pt) 2000-08-22
TR200000930T2 (tr) 2000-11-21
IL134596A0 (en) 2001-04-30
UA58472C2 (uk) 2003-08-15
PL338883A1 (en) 2000-11-20
EA002746B1 (ru) 2002-08-29
EP0933365A2 (en) 1999-08-04
EA200000239A1 (ru) 2000-10-30
ID25000A (id) 2000-09-07
WO1999008699A1 (en) 1999-02-25

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