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WO1988009789A3 - Derives d'acide 3-indolepyruvique et utilisation pharmaceutique desdits derives - Google Patents

Derives d'acide 3-indolepyruvique et utilisation pharmaceutique desdits derives Download PDF

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Publication number
WO1988009789A3
WO1988009789A3 PCT/IT1988/000041 IT8800041W WO8809789A3 WO 1988009789 A3 WO1988009789 A3 WO 1988009789A3 IT 8800041 W IT8800041 W IT 8800041W WO 8809789 A3 WO8809789 A3 WO 8809789A3
Authority
WO
WIPO (PCT)
Prior art keywords
acid derivatives
pharmaceutical use
indolepyruvic acid
indolepyruvic
acid
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IT1988/000041
Other languages
English (en)
Other versions
WO1988009789A2 (fr
Inventor
Luca Giovanna De
Stazio Giovanni Di
Andrea Margonelli
Mario Materazzi
Vincenzo Politi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Polifarma SpA
Original Assignee
Polifarma SpA
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 Polifarma SpA filed Critical Polifarma SpA
Priority to KR1019890700193A priority Critical patent/KR960016522B1/ko
Priority to DE8888904984T priority patent/DE3878866T2/de
Priority to AT88904984T priority patent/ATE86247T1/de
Publication of WO1988009789A2 publication Critical patent/WO1988009789A2/fr
Priority to NO89890408A priority patent/NO890408L/no
Priority to DK046789A priority patent/DK170438B1/da
Priority to FI890508A priority patent/FI92055C/fi
Publication of WO1988009789A3 publication Critical patent/WO1988009789A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Indole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'acide 3-indolepyruvique et ses dérivés sous forme de sels, d'esters et d'amides sont des composés pharmaceutiquement actifs en tant qu'agents ou antagonistes contre les troubles du système nerveux central, tels que l'épilepsie, les ischémies cérébrales, les ictus et la maladie d'Alzheimer, grâce à un mécanisme actif qui élève le niveau d'acide kynurénique dans le cerveau.
PCT/IT1988/000041 1987-06-03 1988-06-01 Derives d'acide 3-indolepyruvique et utilisation pharmaceutique desdits derives Ceased WO1988009789A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1019890700193A KR960016522B1 (ko) 1987-06-03 1988-06-01 3-인돌피루브산 유도체 및 이를 함유하는 중추 신경계 장애 치료용 제약 조성물
DE8888904984T DE3878866T2 (de) 1987-06-03 1988-06-01 3-indolpyruvsaeure-derivate und deren verwendung als arznemittel.
AT88904984T ATE86247T1 (de) 1987-06-03 1988-06-01 3-indolpyruvsaeure-derivate und deren verwendung als arznemittel.
NO89890408A NO890408L (no) 1987-06-03 1989-02-01 3-indolpyrodruesyre-derivater og deres farmasoeytiske anvendelse.
DK046789A DK170438B1 (da) 1987-06-03 1989-02-02 3-Indolpyrodruesyrederivater, lægemidler indeholdende sådanne, samt anvendelse af sådanne derivater til fremstilling af lægemidler
FI890508A FI92055C (fi) 1987-06-03 1989-02-02 Menetelmä farmaseuttisesti aktiivisten 3-indolipalorypälehappojohdannaisten valmistamiseksi

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT48014A/87 1987-06-03
IT8748014A IT1206078B (it) 1987-06-03 1987-06-03 Procedimento per la produzione di acido 3-indolpiruvico e suoi derivati loro uso farmaceutico

Publications (2)

Publication Number Publication Date
WO1988009789A2 WO1988009789A2 (fr) 1988-12-15
WO1988009789A3 true WO1988009789A3 (fr) 1989-02-09

Family

ID=11263959

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IT1988/000041 Ceased WO1988009789A2 (fr) 1987-06-03 1988-06-01 Derives d'acide 3-indolepyruvique et utilisation pharmaceutique desdits derives

Country Status (13)

Country Link
US (1) US5002963A (fr)
EP (1) EP0321516B1 (fr)
JP (1) JPH02500369A (fr)
KR (1) KR960016522B1 (fr)
AT (1) ATE86247T1 (fr)
AU (1) AU609500B2 (fr)
CA (1) CA1328658C (fr)
DE (1) DE3878866T2 (fr)
DK (1) DK170438B1 (fr)
FI (1) FI92055C (fr)
IT (1) IT1206078B (fr)
NO (1) NO890408L (fr)
WO (1) WO1988009789A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6943187B2 (en) 1997-06-04 2005-09-13 Gpi Nil Holdings, Inc. Pyrrolidine derivative hair growth compositions and uses
US7056935B2 (en) 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1224546B (it) * 1988-09-29 1990-10-04 Polifarma Spa Utilizzatore farmaceutica di acido 3 -indolpiruvico come agente inibitore di patologie degenerative
US4960786A (en) * 1989-04-24 1990-10-02 Merrell Dow Pharmaceuticals Inc. Excitatory amino acid antagonists
JPH0347123A (ja) * 1989-05-05 1991-02-28 G D Searle & Co インドール―２―カルボキシレート化合物類を含有するｃｎｓ疾患治療用組成物
DE3917880A1 (de) * 1989-06-01 1990-12-06 Kali Chemie Ag Neue acylaminosaeurederivate enthaltende arzneimittel und diaetetika
IT218019Z2 (it) * 1989-09-08 1992-03-05 Enea Dispositivo protettivo individuale, portatile ad isolamento totale conatmosfera controllata
IT1237472B (it) * 1989-10-04 1993-06-07 Polifarma Spa Derivati di acido 3-indolpiruvico, loro procedimento di produzione ed impiego terapeutico.
US5037846A (en) * 1990-01-02 1991-08-06 Pfizer Inc. Indolyl-3 polyamines and their use as antagonists of excitatory amino acid neurotransmitters
US5484814A (en) * 1991-02-28 1996-01-16 Merrell Dow Pharmaceuticals Inc. NMDA antagonists
ES2069921T3 (es) * 1991-02-28 1995-05-16 Merrell Dow Pharma Antagonistas del nmda.
US5360814A (en) * 1991-02-28 1994-11-01 Merrell Dow Pharmaceuticals Inc. NMDA antagonists
IT1261165B (it) * 1993-01-25 1996-05-09 Polifarma Spa Agente attivo per ridurre il livello ematico di glucocorticoidi e prevenire disturbi cerebrali da stress e senilita'.
FR2701948B1 (fr) * 1993-02-22 1996-07-26 Exsymol Sa Produit de couplage de l'histamine ou l'histamine méthyl-substituée et d'un acide aminé, procédé de préparation et applications thérapeutiques, cosmétologiques et agroalimentaires.
US5859031A (en) * 1995-06-07 1999-01-12 Gpi Nil Holdings, Inc. Small molecule inhibitors of rotamase enzyme activity
US5801197A (en) * 1995-10-31 1998-09-01 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US5786378A (en) * 1996-09-25 1998-07-28 Gpi Nil Holdings, Inc. Heterocyclic thioesters
US6218424B1 (en) 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses
US5801187A (en) 1996-09-25 1998-09-01 Gpi-Nil Holdings, Inc. Heterocyclic esters and amides
US6242468B1 (en) 1997-02-27 2001-06-05 Jia-He Li Carbamate and urea compositions and neurotrophic uses
US5846979A (en) 1997-02-28 1998-12-08 Gpi Nil Holdings, Inc. N-oxides of heterocyclic esters, amides, thioesters, and ketones
US6187784B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Pipecolic acid derivative hair growth compositions and uses
US6274602B1 (en) 1998-06-03 2001-08-14 Gpi Nil Holdings, Inc. Heterocyclic thioester and ketone hair growth compositions and uses
US6187796B1 (en) 1998-06-03 2001-02-13 Gpi Nil Holdings, Inc. Sulfone hair growth compositions and uses
US6271244B1 (en) 1998-06-03 2001-08-07 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses
US5945441A (en) 1997-06-04 1999-08-31 Gpi Nil Holdings, Inc. Pyrrolidine carboxylate hair revitalizing agents
US6075150A (en) * 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
EP1084106A1 (fr) 1998-06-03 2001-03-21 GPI NIL Holdings, Inc. Sulfonamides a liaison n d'acides carboxyliques n-heterocycliques ou d'isosteres d'acide carboxylique
US6331537B1 (en) 1998-06-03 2001-12-18 Gpi Nil Holdings, Inc. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
US6429215B1 (en) 1998-06-03 2002-08-06 Gpi Nil Holdings, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
EP1085853A1 (fr) 1998-06-03 2001-03-28 GPI NIL Holdings, Inc. Compositions pour la croissance des cheveux a base d'amides et d'esters heterocycliques et utilisation de ces compositions
US6172087B1 (en) 1998-06-03 2001-01-09 Gpi Nil Holding, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
US6395758B1 (en) 1998-08-14 2002-05-28 Gpi Nil Holdings, Inc. Small molecule carbamates or ureas for vision and memory disorders
US6339101B1 (en) 1998-08-14 2002-01-15 Gpi Nil Holdings, Inc. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders
US6506788B1 (en) 1998-08-14 2003-01-14 Gpi Nil Holdings, Inc. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders
US6384056B1 (en) 1998-08-14 2002-05-07 Gpi Nil Holdings, Inc. Heterocyclic thioesters or ketones for vision and memory disorders
US6335348B1 (en) 1998-08-14 2002-01-01 Gpi Nil Holdings, Inc. Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders
US6333340B1 (en) 1998-08-14 2001-12-25 Gpi Nil Holdings, Inc. Small molecule sulfonamides for vision and memory disorders
US6337340B1 (en) 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6399648B1 (en) 1998-08-14 2002-06-04 Gpi Nil Holdings, Inc. N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders
US6218423B1 (en) 1998-08-14 2001-04-17 Gpi Nil Holdings, Inc. Pyrrolidine derivatives for vision and memory disorders
US6376517B1 (en) 1998-08-14 2002-04-23 Gpi Nil Holdings, Inc. Pipecolic acid derivatives for vision and memory disorders
US7338976B1 (en) 1998-08-14 2008-03-04 Gpi Nil Holdings, Inc. Heterocyclic esters or amides for vision and memory disorders
US6462072B1 (en) 1998-09-21 2002-10-08 Gpi Nil Holdings, Inc. Cyclic ester or amide derivatives
US7253169B2 (en) 1999-11-12 2007-08-07 Gliamed, Inc. Aza compounds, pharmaceutical compositions and methods of use
US6417189B1 (en) 1999-11-12 2002-07-09 Gpi Nil Holdings, Inc. AZA compounds, pharmaceutical compositions and methods of use
MXPA02006134A (es) 1999-12-21 2002-12-13 Guilford Pharm Inc Compuestos derivados de hidantoina, composiciones farmaceuticas y metodos de uso de los mismos.
US6608196B2 (en) 2001-05-03 2003-08-19 Galileo Pharmaceuticals, Inc. Process for solid supported synthesis of pyruvate-derived compounds
US6916850B2 (en) 2001-05-03 2005-07-12 Galileo Pharmaceuticals, Inc. Pyruvate derivatives
CN101671707A (zh) 2001-12-27 2010-03-17 味之素株式会社 谷氨酸衍生物的制备方法
WO2009028338A1 (fr) * 2007-08-24 2009-03-05 Ajinomoto Co., Inc. Nouveau gène d'oxydase et procédé de production d'acide 3-indole-pyruvique à l'aide de ce gène
RU2505606C2 (ru) 2010-10-14 2014-01-27 Адзиномото Ко., Инк. Способ получения монатина
WO2020012373A1 (fr) * 2018-07-10 2020-01-16 Polindols S.R.L.S. Nouveaux médicaments pour des pathologies invalidantes chroniques et pour ralentir le vieillissement, sur la base d'une nouvelle route métabolique du tryptophane et leur procédé de production

Citations (4)

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Publication number Priority date Publication date Assignee Title
GB1550993A (en) * 1976-10-07 1979-08-22 Grace W R & Co Preparation of aliphatic and heteocyclic alphaketo carboxylic acids
EP0046291A2 (fr) * 1980-08-18 1982-02-24 Merck & Co. Inc. Dérivés de caprolactame substitués utilisables comme agents antihypertensifs, leur procédé de préparation, composition pharmaceutique les contenant et produits intermédiaires
EP0046953A2 (fr) * 1980-08-30 1982-03-10 Hoechst Aktiengesellschaft Dérivés des acides aminés, leurs procédés de préparation, compositions les contenant et leur application
EP0048159A2 (fr) * 1980-09-17 1982-03-24 University Of Miami Peptides carboxyalcoyliques, thioéthers et éthers de peptides comme agents antihypertensifs

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1148618B (it) * 1982-10-11 1986-12-03 Polifarma Spa Procedimento enzimatico per la produzione di acido 3-indolpiruvico e utilizzazione farmaceutica di questo
IT1184282B (it) * 1985-06-28 1987-10-22 Polifarma Spa Procedimento per la produzione di alfa-chetoacidi indolici a partire da un rispettivo alfa-ammino-acido,particolarmente per produrre acido indolpiruvico

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1550993A (en) * 1976-10-07 1979-08-22 Grace W R & Co Preparation of aliphatic and heteocyclic alphaketo carboxylic acids
EP0046291A2 (fr) * 1980-08-18 1982-02-24 Merck & Co. Inc. Dérivés de caprolactame substitués utilisables comme agents antihypertensifs, leur procédé de préparation, composition pharmaceutique les contenant et produits intermédiaires
EP0046953A2 (fr) * 1980-08-30 1982-03-10 Hoechst Aktiengesellschaft Dérivés des acides aminés, leurs procédés de préparation, compositions les contenant et leur application
EP0048159A2 (fr) * 1980-09-17 1982-03-24 University Of Miami Peptides carboxyalcoyliques, thioéthers et éthers de peptides comme agents antihypertensifs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Chemical Abstracts, volume 75, no. 13, 27 September 1971, (Columbus, Ohio, US), see page 150 *
Chemical Abstracts, volume 91, no. 3, 16 July 1979, (Columbus, Ohio, US), Yu.V. Erofeev et al.: "Synthesis of esters of 3-indolylpyruvic acid and tryptophan based on /3(3-indolyl)-D-nitroacrylic acid esters", see page 708 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7056935B2 (en) 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
US6943187B2 (en) 1997-06-04 2005-09-13 Gpi Nil Holdings, Inc. Pyrrolidine derivative hair growth compositions and uses

Also Published As

Publication number Publication date
AU609500B2 (en) 1991-05-02
FI92055C (fi) 1994-09-26
DK46789D0 (da) 1989-02-02
US5002963A (en) 1991-03-26
EP0321516A1 (fr) 1989-06-28
IT8748014A0 (it) 1987-06-03
EP0321516B1 (fr) 1993-03-03
DE3878866T2 (de) 1993-09-02
DK46789A (da) 1989-03-31
WO1988009789A2 (fr) 1988-12-15
DK170438B1 (da) 1995-09-04
FI890508L (fi) 1989-02-02
IT1206078B (it) 1989-04-14
KR960016522B1 (ko) 1996-12-14
NO890408D0 (no) 1989-02-01
NO890408L (no) 1989-03-30
ATE86247T1 (de) 1993-03-15
FI92055B (fi) 1994-06-15
AU1943388A (en) 1989-01-04
FI890508A0 (fi) 1989-02-02
JPH02500369A (ja) 1990-02-08
DE3878866D1 (de) 1993-04-08
CA1328658C (fr) 1994-04-19
KR890701559A (ko) 1989-12-20

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