AR021161A1 - DERIVATIVES OF IMIDAZOL, CYCLICAL ANALOGS OF THE SOMATOSTATINE, PHARMACEUTICAL COMPOSITION THAT INCLUDE THEM, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINE - Google Patents

DERIVATIVES OF IMIDAZOL, CYCLICAL ANALOGS OF THE SOMATOSTATINE, PHARMACEUTICAL COMPOSITION THAT INCLUDE THEM, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINE

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Publication number
AR021161A1
AR021161A1 ARP990102857A ARP990102857A AR021161A1 AR 021161 A1 AR021161 A1 AR 021161A1 AR P990102857 A ARP990102857 A AR P990102857A AR P990102857 A ARP990102857 A AR P990102857A AR 021161 A1 AR021161 A1 AR 021161A1
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AR
Argentina
Prior art keywords
optionally substituted
alkyl
group
independently
substituents
Prior art date
Application number
ARP990102857A
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Spanish (es)
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Scient S A S Soc De Conseils De Rech S Et D Applic S
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Publication date
Application filed by Scient S A S Soc De Conseils De Rech S Et D Applic S filed Critical Scient S A S Soc De Conseils De Rech S Et D Applic S
Publication of AR021161A1 publication Critical patent/AR021161A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/655—Somatostatins
    • C07K14/6555—Somatostatins at least 1 amino acid in D-form
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Zoology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Derivados del imidazol, análogos cíclicos de somatostina, que comprenden un compuesto de la formula (1) o una sal farmacéuticamente aceptable del mismo,donde Y y Z, en cada caso, son independientemente un D- o L-alfa-aminoácido natural o no natural;n es, en cada caso, independientemente 0 a 50, siempre queambas n no sean 0 al mismo tiempo; m es 0 o un numero entero de 1 a 10; a es H o R1; b es OH, -OR1 o-NR9R9; o a se une con b para formar un enlace amídico; R1es independientemente H, alquilo (C1-4) o arilalquilo (C1-4); R2 es H o una porcion optativamente sustituida seleccionada entre el grupo que consiste enalquilo (C1-4), fenilo, fenilalquilo (C1-4) y heterociclil-alquilo (C1-4), donde la porcion optativamente sustituida está optativamente sustituida con uno omás sustituyentes, cada uno de los cuales es independientemente seleccionado entre el grupo que consiste en alquilo (C1-4), cicloalquilo (C3-8), -O-R6,S(O)q-R7, -N(R9R9), -NHCO-R6, NHSO2R9, -CO2-R9, -CONR9R9 y SO2NR9R9 donde qes 0, 1, 2 o 3; cada uno de R3 y R4 es independientemente H, halo o una porcionoptativamente sustituida seleccionada entre el grupo que consiste en alquilo (C1-4), cicloalquilo (C3-8), arilo y arilalquilo (C1-4); donde la porcionoptativamente sustituida está optativamente sustituida con uno o más sustituyentes seleccionados entre el grupo que consiste en OH, alquilo (C1-4), alcoxi(C1-4), ariloxi, arilalcoxi (C1-4).-NR9R9, COOH, -CONR9R9, y halo; o R3 y R4 junto con los carbonos a los cuales están unidos forman arilo optativamentesustituido, donde el arilo está optativamente sustituido con uno o más sustituyentes, cada uno de los cuales es independientemente seleccionado entre el grupoque consiste en OH, alquilo (C1-4), alcoxi (C1-4), ariloxi, arilalcoxi (C1-4), -NR9R9, -COOR5, -CONR9R9, y halo; R5 es, en cada caso, independientemente H, ouna porcion optativamente sustituida seleccionada entre el grupo que consiste en alquilo (C1-4) y arilalquilo (C1-4), donde la porcion optativamentesustituidaestá optativamente sustituida con uno o más sustituyentes, cada uno de los cuales es independientemente seleccionado entre el grupo que consiste en alquiloImidazole derivatives, cyclic somatostine analogues, which comprise a compound of the formula (1) or a pharmaceutically acceptable salt thereof, where Y and Z, in each case, are independently a natural or non-natural D- or L-alpha-amino acid natural, n is, in each case, independently 0 to 50, provided that n is not 0 at the same time; m is 0 or an integer from 1 to 10; a is H or R1; b is OH, -OR1 or-NR9R9; or a binds with b to form an amide bond; R1 is independently H, (C1-4) alkyl or (C1-4) arylalkyl; R2 is H or an optionally substituted portion selected from the group consisting of alkyl (C1-4), phenyl, phenylalkyl (C1-4) and heterocyclyl-alkyl (C1-4), where the optionally substituted portion is optionally substituted with one or more substituents, each of which is independently selected from the group consisting of (C1-4) alkyl, cycloalkyl (C3-8), -O-R6, S (O) q-R7, -N (R9R9), - NHCO-R6, NHSO2R9, -CO2-R9, -CONR9R9 and SO2NR9R9 where 0, 1, 2 or 3; each of R3 and R4 is independently H, halo or an optionally substituted portion selected from the group consisting of (C1-4) alkyl, cycloalkyl (C3-8), aryl and arylalkyl (C1-4); where the optionally substituted portion is optionally substituted with one or more substituents selected from the group consisting of OH, (C1-4) alkyl, (C1-4) alkoxy, aryloxy, arylalkoxy (C1-4) .- NR9R9, COOH, - CONR9R9, and halo; or R3 and R4 together with the carbons to which they are attached form optionally substituted aryl, where the aryl is optionally substituted with one or more substituents, each of which is independently selected from the group consisting of OH, (C1-4) alkyl , (C1-4) alkoxy, aryloxy, (C1-4) aryloxy, -NR9R9, -COOR5, -CONR9R9, and halo; R5 is, in each case, independently H, an optionally substituted portion selected from the group consisting of alkyl (C1-4) and arylalkyl (C1-4), where the optionally substituted portion is optionally substituted with one or more substituents, each of which is independently selected from the group consisting of alkyl

ARP990102857A 1998-06-16 1999-06-15 DERIVATIVES OF IMIDAZOL, CYCLICAL ANALOGS OF THE SOMATOSTATINE, PHARMACEUTICAL COMPOSITION THAT INCLUDE THEM, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINE AR021161A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8950398P 1998-06-16 1998-06-16
US9818198A 1998-06-16 1998-06-16

Publications (1)

Publication Number Publication Date
AR021161A1 true AR021161A1 (en) 2002-07-03

Family

ID=26780645

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990102857A AR021161A1 (en) 1998-06-16 1999-06-15 DERIVATIVES OF IMIDAZOL, CYCLICAL ANALOGS OF THE SOMATOSTATINE, PHARMACEUTICAL COMPOSITION THAT INCLUDE THEM, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINE

Country Status (12)

Country Link
EP (1) EP1086131A1 (en)
JP (1) JP2002518409A (en)
CN (1) CN1200000C (en)
AR (1) AR021161A1 (en)
AU (1) AU745493B2 (en)
CA (1) CA2335184A1 (en)
HU (1) HUP0102902A3 (en)
NO (1) NO20006320L (en)
PL (1) PL345037A1 (en)
RU (1) RU2242481C2 (en)
TW (3) TWI242442B (en)
WO (1) WO1999065942A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20004568A3 (en) 1998-06-12 2001-11-14 Societe De Conseils De Recherches Et D'application Imidazolyl compound, pharmaceutical preparation and preparation process thereof
FR2796945B1 (en) * 1999-07-30 2002-06-28 Sod Conseils Rech Applic NOVEL DERIVATIVES OF HYDANTOINS, THIOHYDANTOINS, PYRIMIDINEDIONES AND THIOXOPYRIMIDINONES, PROCESSES FOR THEIR PREPARATION AND THEIR APPLICATION AS MEDICAMENTS
WO2002010140A2 (en) 2000-08-01 2002-02-07 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Imidazolyl derivatives
US20040186151A1 (en) * 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
WO2006063465A1 (en) * 2004-12-15 2006-06-22 Diamedica Inc. Treatment of insulin resistance by modulating somatostatin using somatostatin receptor antagonists
ES2365815T3 (en) * 2005-12-14 2011-10-11 Bristol-Myers Squibb Company ANALOGS OF ARILPROPIONAMIDA, ARILACRILAMIDA, ARILPROPINAMIDA OR ARILMETILUREA AS INHIBITORS OF THE XIA FACTOR.
CA2633252A1 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
KR101732054B1 (en) 2008-09-26 2017-05-02 암브룩스, 인코포레이티드 Non-natural amino acid replication-dependent microorganisms and vaccines
EP2168983A1 (en) 2008-09-30 2010-03-31 Ipsen Pharma New octapeptide compounds and their therapeutic use
JP5535931B2 (en) * 2008-10-27 2014-07-02 武田薬品工業株式会社 Bicyclic compound
AU2017217271C1 (en) * 2016-02-09 2021-08-05 Cdrd Ventures Inc. Somatostatin receptor antagonist compounds and methods of using the same

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5770687A (en) * 1995-06-07 1998-06-23 Peptor Limited Comformationally constrained backbone cyclized somatostatin analogs
US6673927B2 (en) * 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors

Also Published As

Publication number Publication date
TW527361B (en) 2003-04-11
EP1086131A1 (en) 2001-03-28
JP2002518409A (en) 2002-06-25
TW200410986A (en) 2004-07-01
NO20006320L (en) 2001-02-12
PL345037A1 (en) 2001-11-19
RU2242481C2 (en) 2004-12-20
AU4822399A (en) 2000-01-05
CN1305496A (en) 2001-07-25
CN1200000C (en) 2005-05-04
TWI242442B (en) 2005-11-01
NO20006320D0 (en) 2000-12-12
WO1999065942A1 (en) 1999-12-23
CA2335184A1 (en) 1999-12-23
HUP0102902A3 (en) 2002-02-28
HUP0102902A2 (en) 2002-01-28
WO1999065942A8 (en) 2000-02-17
TWI242441B (en) 2005-11-01
AU745493B2 (en) 2002-03-21

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