AR057332A1 - Tienopiridinas, procedimientos de obtencion y composiciones farmaceuticas - Google Patents

Tienopiridinas, procedimientos de obtencion y composiciones farmaceuticas

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Publication number
AR057332A1
AR057332A1 ARP060102182A ARP060102182A AR057332A1 AR 057332 A1 AR057332 A1 AR 057332A1 AR P060102182 A ARP060102182 A AR P060102182A AR P060102182 A ARP060102182 A AR P060102182A AR 057332 A1 AR057332 A1 AR 057332A1
Authority
AR
Argentina
Prior art keywords
hal
nha
so2a
naa
mono
Prior art date
Application number
ARP060102182A
Other languages
English (en)
Inventor
Hans-Michael Eggenweiler
Michael Wolf
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 AR057332A1 publication Critical patent/AR057332A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biotechnology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)

Abstract

Son inhibidores de las HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempenan un papel importante. Reivindicacion 1: Compuestos de la formula (1), en donde, Y es OH, OA, SH, SA, NH2, NHA, NAA' o NHR5; R1 es Hal, OH, OA, SH, SA, H o A; R2, R3 son en cada caso, de modo independiente entre sí, -NHCO-(X)s-Q, -CONH-(X)s-Q, -CONA-(X)s-Q, -NH(CO)NH-(X)s-Q, -NH(CO)O-(X)s-Q, -NHSO2- (X)s-Q, -SO2NH-(X)s-Q, -SO2NA-(X)s-Q, -(X)s-Q o H, en donde, en caso de que R2 (distinto) H, entonces R3 = H o Cl, o en caso de que R3 (distinto) H, entonces R2 = H o Cl; R4 es H, Hal, CN, NO2, A, OH, OA, SH, SA, (CH2)nCOOH, (CH2)nCOOA, CONH2, CONHA, CONAA', NH2, NHA, NAA', NHCOOA, NHCONH2, NHCONHA, SOA, SO2A, SO2NH2, SO2NHA y/o SO2NAA', dos radicales adyacentes, seleccionados del grupo R1, R2, R3, R4 también son juntos metilendioxi o etilendioxi; R5 es -(CH2)o-Het1, -(CH2)o-NH2, -(CH2)o- NHA o -(CH2)o-NA2; A, A' son en cada caso, de modo independiente entre sí, alquilo C1-10 no ramificado o ramificado, en donde 1-5 átomos de H pueden estar reemplazados por F, Cl y/o Br; Alk o alquilo cíclico con C3-7; A y A' también son juntos una cadena alquileno con 2, 3, 4, 5 o 6 átomos de C, en donde uno o dos grupos CH2 pueden estar reemplazados por O, SO, SO2, NH, NA y/o N-COOA; Alk es alquileno C2-6; X es alquileno C1-10 o alquenileno C2-10 no ramificado o ramificado no sustituido o mono-, di-, tri- o tetrasustituido con A, OA, OH, SH, SA, Hal, NO2, CN, Ar, OAr, COOH, COOA, CHO, C(=O)A, C(=O)Ar, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA', NACONAA' y/u =O, en donde también uno, dos o tres grupos C pueden estar reemplazados por O, S, SO, SO2, NHCO, NACO, CONH, CONA, SO2NH, SO2NA, NHSO2, NASO2 y/o por grupos NH; Q es H, Carb, Ar o Het; Carb es cicloalquilo C3-7 o cicloalquenilo C3-7 no sustituido o mono-, di-, tri-, tetra- o pentasustituido con A, OA, OH, SH, SA, Hal, NO2, CN, (CH2)nAr', (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA' y/o NACONAA'; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di-, tri- tetra- o pentasustituido con A, OA, OH, SH, SA, Hal, NO2, CN, (CH2)nAr', (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA', NACONAA', NHCO(CH2)nNH2 y/u -O-(CH2)o-Het1; Ar' es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con A, OA, OH, SH, SA, Hal, NO2, CN, (CH2)nfenilo, (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA' y/o NACONAA'; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con A, OA, OH, SH, SA, Hal, NO2, CN, (CH2)nAr', (CH2)nCOOH, (CH2)nCOOA, CHO, COA, SO2A, CONH2, SO2NH2, CONHA, CONAA', SO2NHA, SO2NAA', NH2, NHA, NAA', OCONH2, OCONHA, OCONAA', NHCOA, NHCOOA, NACOOA, NHSO2OA, NASO2OA, NHCONH2, NACONH2, NHCONHA, NACONHA, NHCONAA', NACONAA', SO2A, =S, =NH, =NA y/u =O (oxígeno del carbonilo); Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, Hal y/o =O (oxígeno del carbonilo); Hal es F, Cl, Br o I; n es 0, 1, 2, 3 o 4; o es 1, 2, 3 o 4; s 0 o 1; así como sus derivados, sales, solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones.
ARP060102182A 2005-05-27 2006-05-26 Tienopiridinas, procedimientos de obtencion y composiciones farmaceuticas AR057332A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005024245A DE102005024245A1 (de) 2005-05-27 2005-05-27 Thienopyridine

Publications (1)

Publication Number Publication Date
AR057332A1 true AR057332A1 (es) 2007-11-28

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ARP060102182A AR057332A1 (es) 2005-05-27 2006-05-26 Tienopiridinas, procedimientos de obtencion y composiciones farmaceuticas

Country Status (14)

Country Link
US (1) US7989625B2 (es)
EP (1) EP1888593A2 (es)
JP (1) JP2008542213A (es)
KR (1) KR20080021054A (es)
CN (1) CN101163707A (es)
AR (1) AR057332A1 (es)
AU (1) AU2006251420A1 (es)
BR (1) BRPI0610204A2 (es)
CA (1) CA2609385A1 (es)
DE (1) DE102005024245A1 (es)
MX (1) MX2007014720A (es)
RU (1) RU2415859C2 (es)
WO (1) WO2006125531A2 (es)
ZA (1) ZA200711142B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007049451A1 (de) 2007-10-16 2009-04-23 Merck Patent Gmbh 5-Cyano-thienopyridine
US20090118276A1 (en) * 2007-11-02 2009-05-07 Wyeth Thienopyrimidines, thienopyridines, and pyrrolopyrimidines as b-raf inhibitors
GB0908394D0 (en) * 2009-05-15 2009-06-24 Univ Leuven Kath Novel viral replication inhibitors
AR077405A1 (es) 2009-07-10 2011-08-24 Sanofi Aventis Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer
FR2949467B1 (fr) 2009-09-03 2011-11-25 Sanofi Aventis Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation
CN102933390B (zh) 2010-09-13 2017-02-08 艾利丹尼森公司 用于热密封包装的可再密封的层压材料
TWI458732B (zh) * 2012-06-27 2014-11-01 Univ Nat Chiao Tung 具硼酸基團連接子及含有其之生物感測元件
ES2779748T3 (es) 2012-08-23 2020-08-19 Janssen Biopharma Inc Compuestos para el tratamiento de infecciones víricas por paramixovirus
MA41614A (fr) 2015-02-25 2018-01-02 Alios Biopharma Inc Composés antiviraux
WO2023213761A1 (en) * 2022-05-03 2023-11-09 Universite De Geneve Adenosine 2a receptor modulators for use in the treatment of cancer

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0323810D0 (en) * 2003-10-10 2003-11-12 Cancer Rec Tech Ltd Pyridothiophene compounds
WO2005058315A1 (en) * 2003-12-12 2005-06-30 Ribapharm, Inc. Novel heterocyclic compounds as ikk2 inhibitors with anti-hbv activity
DE102005009440A1 (de) * 2005-03-02 2006-09-07 Merck Patent Gmbh Thienopyridinderivate

Also Published As

Publication number Publication date
RU2415859C2 (ru) 2011-04-10
WO2006125531A3 (de) 2007-04-12
MX2007014720A (es) 2008-02-15
BRPI0610204A2 (pt) 2010-06-01
CA2609385A1 (en) 2006-11-30
RU2007147593A (ru) 2009-07-10
ZA200711142B (en) 2008-11-26
AU2006251420A1 (en) 2006-11-30
JP2008542213A (ja) 2008-11-27
DE102005024245A1 (de) 2006-11-30
US20100048558A1 (en) 2010-02-25
WO2006125531A2 (de) 2006-11-30
KR20080021054A (ko) 2008-03-06
EP1888593A2 (de) 2008-02-20
US7989625B2 (en) 2011-08-02
CN101163707A (zh) 2008-04-16

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