PE20001002A1 - SINGLE CYCLIC COMPOUNDS WITH ANTAGONIST NK2 ACTION AND THE COMPOSITION THAT CONTAINS THEM - Google Patents

SINGLE CYCLIC COMPOUNDS WITH ANTAGONIST NK2 ACTION AND THE COMPOSITION THAT CONTAINS THEM

Info

Publication number
PE20001002A1
PE20001002A1 PE1999000784A PE00078499A PE20001002A1 PE 20001002 A1 PE20001002 A1 PE 20001002A1 PE 1999000784 A PE1999000784 A PE 1999000784A PE 00078499 A PE00078499 A PE 00078499A PE 20001002 A1 PE20001002 A1 PE 20001002A1
Authority
PE
Peru
Prior art keywords
alkyl
antagonist
tetrahydropyranil
ch2nh
colic
Prior art date
Application number
PE1999000784A
Other languages
Spanish (es)
Inventor
Antonio Guidi
Maria Altamura
Marco Criscuoli
Enzo Perrotta
Carlo Alberto Maggi
Original Assignee
Menarini Ricerche 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 Menarini Ricerche Spa filed Critical Menarini Ricerche Spa
Publication of PE20001002A1 publication Critical patent/PE20001002A1/en

Links

Classifications

    • 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
    • C07K7/22—Tachykinins, e.g. Eledoisins, Substance P; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A PEPTIDOS MONOCICLICOS DE FORMULA I, DONDE X1, X2, X3 Y X4 SON -CONR-, -CH2NR-, -NRCH2-; R ES H, ALQUILO C1-C3, BENCILO; f Y m SON 0-2; R1 Y R2 SON -(CH2)r-Ar; r ES 0-2; Ar ES BENCENO, NAFTALINA, TIOFENO, BENZOTIOFENO, PIRIDINA, QUINOLINA, INDOL, FURANO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C3, OH, NH2, NR6R7, ENTRE OTROS; R6 Y R7 SON H, ALQUILO C1-C3; R3 ES (CH2)r-Ar1; r ES 0-2; Ar1 ES BENCENO, NAFTALINA, TIOFENO, BENZOTIOFENO, PIRIDINA, QUINOLINA, ENTRE OTROS; R5 ES H; R4 ES NR8R9, N(R11)CO(CH2)h-R12, COR13; R8 ES H, ALQUILO C1-C3, R9 ES METANOSULFONILO, TOSILO, TETRAHIDROPIRANILO, TETRAHIDROTIOPIRANILO OPCIONALMENTE SUSTITUIDO POR O EN S, EN N DE PIPERIDILO POR ALQUILO C1-C3, ACILO; O R8 Y R9 FORMAN PIPERACINA; R11 ES H, ALQUILO C1-C3; h ES 0-3; R12 ES MORFOLINO, PIRROLIDINO; R13 ES MORFOLINO, PIPERACINA. SON COMPUESTOS PREFERIDOS CICLO{SUC[1-(R)-(4-TETRAHIDROPIRANIL)AMINO)-TRP-PHE-[(R)-NH-CH(CH2-C6H5)-CH2NH]}, CICLO{SUC[1-(4-MORFOLIN)CARBONIL]-TRP-PHE-[(R)-NH-CH(CH2-C6H5)-CH2NH]}, ENTRE OTROS. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE TAQUININA (NK2) POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DE BRONCOESPASMO, TOS, IRRITACION PULMONAR, ESPASMO INTESTINAL, ESPASMO LOCAL DE VEJIGA, INFECCIONES, COLICOS DE RINONREFERS TO MONOCYCLE PEPTIDES OF FORMULA I, WHERE X1, X2, X3 AND X4 ARE -CONR-, -CH2NR-, -NRCH2-; R IS H, C1-C3 ALKYL, BENZYL; f and m ARE 0-2; R1 AND R2 ARE - (CH2) r-Ar; r IS 0-2; Ar IS BENZENE, NAPTHALINE, THIOPHENE, BENZOTHYOPHENE, PYRIDINE, QUINOLINE, INDOL, FURANE OPTIONALLY SUBSTITUTED WITH C1-C3 ALKYL, OH, NH2, NR6R7, AMONG OTHERS; R6 AND R7 ARE H, C1-C3 ALKYL; R3 IS (CH2) r-Ar1; r IS 0-2; Ar1 IS BENZENE, NAPHTHALINE, THIOPHENE, BENZOTHIOPHENE, PYRIDINE, QUINOLINE, AMONG OTHERS; R5 IS H; R4 IS NR8R9, N (R11) CO (CH2) h-R12, COR13; R8 IS H, C1-C3 ALKYL, R9 IS METHANOSULFONYL, TOSYL, TETRAHYDROPYRANIL, TETRAHYDROTHYRANIL OPTIONALLY SUBSTITUTED BY O IN S, IN N OF PIPERIDYL BY C1-C3 ALKYL, ACILO; OR R8 AND R9 FORM PIPERACINE; R11 IS H, C1-C3 ALKYL; h ES 0-3; R12 IS MORPHOLINE, PYRROLIDINE; R13 IS MORPHOLINE, PIPERACIN. THE PREFERRED COMPOUNDS ARE CYCLE {SUC [1- (R) - (4-TETRAHYDROPYRANIL) AMINO) -TRP-PHE - [(R) -NH-CH (CH2-C6H5) -CH2NH]}, CYCLE {SUC [1- ( 4-MORPHOLIN) CARBONYL] -TRP-PHE - [(R) -NH-CH (CH2-C6H5) -CH2NH]}, AMONG OTHERS. COMPOUND I IS AN ANTAGONIST OF THE TACHININE RECEPTOR (NK2) SO IT MAY BE USEFUL FOR THE TREATMENT OF BRONCHOSPASM, COUGH, PULMONARY IRRITATION, INTESTINAL SPASM, LOCAL BLADDER SPASM, INFECTIONS, COLIC COLIC OF RINON

PE1999000784A 1998-08-05 1999-08-04 SINGLE CYCLIC COMPOUNDS WITH ANTAGONIST NK2 ACTION AND THE COMPOSITION THAT CONTAINS THEM PE20001002A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT1998FI000186A IT1304888B1 (en) 1998-08-05 1998-08-05 MONOCYCLIC ACTION COMPOUNDS NK-2 ANTAGONIST AND FORMULATIONS THAT CONTAIN

Publications (1)

Publication Number Publication Date
PE20001002A1 true PE20001002A1 (en) 2000-10-16

Family

ID=11352646

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999000784A PE20001002A1 (en) 1998-08-05 1999-08-04 SINGLE CYCLIC COMPOUNDS WITH ANTAGONIST NK2 ACTION AND THE COMPOSITION THAT CONTAINS THEM

Country Status (11)

Country Link
EP (1) EP1102789A1 (en)
JP (1) JP2002522450A (en)
AR (1) AR021751A1 (en)
AU (1) AU5507999A (en)
CA (1) CA2339638A1 (en)
CO (1) CO5080789A1 (en)
IT (1) IT1304888B1 (en)
PE (1) PE20001002A1 (en)
TR (1) TR200100354T2 (en)
TW (1) TW491857B (en)
WO (1) WO2000008046A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1307809B1 (en) * 1999-10-21 2001-11-19 Menarini Ricerche Spa BASIC MONOCYCLIC COMPOUNDS WITH NK-2 ANTAGONIST ACTION, MANUFACTURING PROCESSES AND FORMULATIONS CONTAINING THEM.
US7723349B2 (en) 2003-04-24 2010-05-25 Incyte Corporation Aza spiro alkane derivatives as inhibitors of metalloproteases
UY38485A (en) 2018-11-27 2020-06-30 Novartis Ag CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN / KEXIN TYPE 9 (PCSK9) INHIBITORS, METHOD OF TREATMENT, USE AND PREPARATION

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4703034A (en) * 1986-04-28 1987-10-27 Merck & Co., Inc. Novel cyclic tetrapeptide
EP0606222A1 (en) * 1991-08-08 1994-07-20 A. Menarini Industrie Farmaceutiche Riunite S.R.L. Cyclic hexapeptides as tachyquinin antagonists, their preparation and pharmaceutical compositions thereof
DE69220861T2 (en) * 1991-08-13 1997-11-20 Takeda Chemical Industries Ltd Cyclic peptides and their use
IT1277835B1 (en) * 1995-03-13 1997-11-12 Menarini Farma Ind BICYCLE COMPOUNDS, THEIR PREPARATION AND USE IN PHARMACEUTICAL COMPOSITIONS
IT1291776B1 (en) * 1997-02-07 1999-01-21 Menarini Ricerche Spa MONOCYCLIC COMPOUNDS WITH FOUR BIFUNCTIONAL RESIDUES, HAVING NK-2 ANTAGONIST ACTION

Also Published As

Publication number Publication date
AU5507999A (en) 2000-02-28
IT1304888B1 (en) 2001-04-05
CO5080789A1 (en) 2001-09-25
TW491857B (en) 2002-06-21
TR200100354T2 (en) 2001-05-21
ITFI980186A1 (en) 2000-02-05
WO2000008046A1 (en) 2000-02-17
EP1102789A1 (en) 2001-05-30
AR021751A1 (en) 2002-08-07
CA2339638A1 (en) 2000-02-17
JP2002522450A (en) 2002-07-23

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