AR049773A1 - Derivados de tiadiazolurea. metodos de obtencion y composiciones farmaceuticas - Google Patents

Derivados de tiadiazolurea. metodos de obtencion y composiciones farmaceuticas

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Publication number
AR049773A1
AR049773A1 ARP050100704A ARP050100704A AR049773A1 AR 049773 A1 AR049773 A1 AR 049773A1 AR P050100704 A ARP050100704 A AR P050100704A AR P050100704 A ARP050100704 A AR P050100704A AR 049773 A1 AR049773 A1 AR 049773A1
Authority
AR
Argentina
Prior art keywords
mono
hal
unsubstituted
cha
atoms
Prior art date
Application number
ARP050100704A
Other languages
English (en)
Inventor
Lars Thore Burgdorf
Hans-Peter Buchstaller
Frank Stieber
Soheila Anzali
Christiane Amendt
Matthias Grell
Christian Sirrenberg
Frank Zenke
Hartmut Greiner
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR049773A1 publication Critical patent/AR049773A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Uso de compuestos de la formula (1), en donde: Ar1 es fenilo, naftilo, bifenilo, o Het insustituido o mono, di, tri, tetra o pentasustituido con R1; Ar2 es fenilo, naftilo, bifenilo, o Het insustituido o mono, di, tri, tetra o pentasustituido con R2; Y es O, S, CH-NO2, C(CN)2 o N-R4; Z es -O-, -S-, -CH2-(CH2)n-, -(CH2)n-CHA-, -CHA-(CH2)n-, -C(=O)-, ,-CH(OH)-, -(CHA)nO-, -(CH2)nO-, -O(CHA)n-, -O(CH2)n-, -(CH2)nS-, -S(CH2)n-, -(CH2)nNH-, -NH(CH2)n-, -(CH2)nNA-, -NA(CH2)n-, -CHHal- o -C(Hal)2-; Het es un heterociclo aromático mono o bicíclico con 1 a 4 átomos de N, O y/o S; R1, R2 son, de modo independiente entre sí, A, Ar', OR3, SR3, OAr', SAr', N(R3)2, NHAr', Hal, NO2, CN, (CH2)nCOOR3, (CH2)nCON(R3)n, COR3, S(O)mA, S(O)mAr', NHCOA, NHCOAr', NHSOmA, NHSOmAr', SOmN(R3)2, -O-(CH2)n-N(R3)2, O(CH2)nNHR3, O(CH2)nNA2,-O(CH2)nC(H3)2(CH2)nN(R3)2, NH(CH2)n(CH3)2(CH2)nN(R3)2, O(CH2)nN(R3)SOmA, O(CH2)nN(R3)SOmN(R3)A, O(CH2)nN(R3)SOmAr', (CH2)nN(R3)SOmA, (CH2)nN(R3)SOmN(R3)A, (CH2)nN(R3)SOmA, O(CH2)nSOmA, O(CH2)nSOmN(R3)A, O(CH2)nSOmAr', (CH2)nSOmA, (CH2)nN(R3)A, (CH2)nSOmAr', -NH-(CH2)n-NH2, -NH(CH2)n-NHA, -NH-(CH2)n-NA2, -NA-(CH2)n-NH2, -NA-(CH2)nNHA, -NA-(CH2)n-NA2, -O-(CH2)n-Het1 o Het1; R3 es H, A o -(CH2)nAr'; R4 es H, CN, OH, A, (CH2)mAr', COR3, COAr', S(O)mA o S(O)mAr'; Ar' es fenilo insustituido o mono, di, tri, tetra o pentasustituido con A, Ph, OH, OA, SH, SA, OPh, NH2, NHA, NA2, NHPh, Hal, NO2, CN, (CH2)nCOOH, (CH2)nCOOA, (CH2)nCONH2, (CH2)nCONHA, CHO, COA, S(O)mA, S(O)mPh, NHCOA, NHCOPh, NHSO2A, NHSO2Ph o SO2NH2; Ph es fenilo insustituido o mono, di o trisustituido con A, Hal, CN, COOR, COOH, NH2, NO2, OH u OA; Het1 es un heterociclo saturado monocíclico con 1 a 4 átomos de N, o y/o S, que puede estar insustituido, o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NH2, =NH, =N-OH, =N-OA y/o el oxígeno del carbonilo (=O); A es alquilo C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; Hal es F, Cl, Br o I; n es 0, 1, 2, 3, 4 o 5; m es 0, 1 o 2; así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones para preparar un medicamento para la prevencion en y/o el tratamiento de enfermedades en las cuales la inhibicion, la regulacion y/o la modulacion de la transduccion de senales de quinasas, en especial de las RAF-quinasas, desempena un papel importante. Método de obtencion de dichos compuestos y composiciones farmacéuticas que los contienen. Reivindicacion 11: Compuestos de acuerdo con la formula general (2), en donde: Ar1 es fenilo insustituido o mono, di, tri, tetra o pentasustituido con R1; Ar2 es fenilo o Het insustituido o mono, di, tri, tetra o pentasustituido con R2; Y es O; Z es -O-, -CH2-(CH2)n-, -(CH2)n-CHA-, -CHA-(CH2)n-, -C(=O)-, ,-CH(OH)-, --CH(OA)-, (CH2)nO-, -O(CH2)n-, -(CH2)nNH- o -NH(CH2)n-; Het es un heterociclo aromático mono o bicíclico con 1 a 4 átomos de N, O y/o S; R1, R2 son, de modo independiente entre sí, A, OR3, Hal, NO2, CN, S(O)mA, O(CH2)nNA2 o Het1; R3 es H o A; Het1 es un heterociclo saturado monocíclico con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NH2, =NH, =N-OH, =N-OA y/o el oxígeno del carbonilo (=O); A es alquilo C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; Hal es F, Cl, Br o I; n es 0, 1 o 2; m es 0, 1 o 2; así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
ARP050100704A 2004-02-26 2005-02-25 Derivados de tiadiazolurea. metodos de obtencion y composiciones farmaceuticas AR049773A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004009933A DE102004009933A1 (de) 2004-02-26 2004-02-26 Verwendung von Thiadiazolharnstoffderivaten

Publications (1)

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AR049773A1 true AR049773A1 (es) 2006-09-06

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Country Status (8)

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US (1) US20070191353A1 (es)
EP (1) EP1720846A1 (es)
JP (1) JP2007523922A (es)
AR (1) AR049773A1 (es)
AU (1) AU2005219499A1 (es)
CA (1) CA2557303A1 (es)
DE (1) DE102004009933A1 (es)
WO (1) WO2005085220A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007106391A1 (en) * 2006-03-10 2007-09-20 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
WO2010073011A2 (en) * 2008-12-23 2010-07-01 Betagenon Ab Compounds useful as medicaments
WO2022031736A1 (en) 2020-08-04 2022-02-10 Nura Bio, Inc. Substituted pyridine derivatives as sarm1 inhibitors
US11945796B2 (en) 2020-09-16 2024-04-02 Nura Bio, Inc. Substituted pyridine derivatives as SARM1 inhibitors
US11629136B1 (en) 2021-07-28 2023-04-18 Nura Bio, Inc. Substituted pyridine derivatives as SARM1 inhibitors
EP4282862A1 (en) * 2022-05-25 2023-11-29 Irbm S.P.A. Flavivirus inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD241740A1 (de) * 1985-10-15 1986-12-24 Univ Rostock Verfahren zur herstellung von substituierten 2-ureido-1,3,4-thiadiazolen
WO1999020617A1 (en) * 1997-10-21 1999-04-29 Active Biotech Ab Antiinflammatory thiadiazolyl ureas which act as lfa-1 and mac-1 inhibitors
US20030236287A1 (en) * 2002-05-03 2003-12-25 Piotrowski David W. Positive allosteric modulators of the nicotinic acetylcholine receptor
DE60335099D1 (de) * 2002-05-06 2011-01-05 Vertex Pharma Thiadiazole oder oxadiazole und ihre verwendung als jak proteinkinaseinhibitoren
GB0308511D0 (en) * 2003-04-14 2003-05-21 Astex Technology Ltd Pharmaceutical compounds

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AU2005219499A1 (en) 2005-09-15
JP2007523922A (ja) 2007-08-23
DE102004009933A1 (de) 2005-09-15
WO2005085220A1 (de) 2005-09-15
CA2557303A1 (en) 2005-09-15
US20070191353A1 (en) 2007-08-16
EP1720846A1 (de) 2006-11-15

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