ES2524910T3 - Piperidino-dihidrotienopirimidinas sustituidas - Google Patents

Piperidino-dihidrotienopirimidinas sustituidas Download PDF

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ES2524910T3
ES2524910T3 ES13154790.3T ES13154790T ES2524910T3 ES 2524910 T3 ES2524910 T3 ES 2524910T3 ES 13154790 T ES13154790 T ES 13154790T ES 2524910 T3 ES2524910 T3 ES 2524910T3
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alkyl
aryl
alkylene
group
hetaryl
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Pascale Pouzet
Klaus Klinder
Ralf Anderskewitz
Horst Dollinger
Dennis Fiegen
Thomas Fox
Rolf Goeggel
Christoph Hoenke
Domnic Martyres
Peter Nickolaus
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Boehringer Ingelheim International GmbH
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A—HUMAN NECESSITIES
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/22—Anxiolytics
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    • 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
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    • 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
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    • 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]
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    • A61P35/00—Antineoplastic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • 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
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
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  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos de fórmula 1, así como sus sales farmacológicamente compatibles para uso en el tratamiento de una enfermedad elegida del grupo de fibrosis pulmonar idiopática, fibrosis quística, deficiencia en anti-tripsina alfa-1 y artritis reumatoide,**Fórmula** en la cual X es SO o SO2; R1 es H, alquilo C1-6, R2 es H o un radical seleccionado del grupo consistente en alquilo C1-10 y alquenilo C2-6, que eventualmente puede estar sustituido con uno o varios radicales seleccionados de halógeno y fluoroalquilo C1-3 o que eventualmente puede estar sustituido con uno o varios radicales seleccionados del grupo que consiste en OR2.1, COOR2.1, CONR2.2R2.3, SR2.1, SO-R2.1, SO2-R2.1, arilo C6-10, -Het, Hetarilo, un cicloalquilo C3-10 monocíclico o bicíclico, CH2-NR2.2R2.3 y NR2.2R2.3, que, de nuevo, puede estar eventualmente sustitudo con uno o varios radicales seleccionados del grupo consistente en OH, halógeno, OR2.1, oxo, CF3, CHF2, CH2F, alquilo C1-6, alcanol C1-6, arilo C6-10, COOR2.1, CH2-NR2.2R2.3 y NR2.2R2.3, en donde Het es un heterociclo de uno a once miembros, mono- o bi-cíclico, saturado o parcialmente saturado, eventualmente condensado o eventualmente puenteado, que contiene 1, 2, 3 ó 4 heteroátomos elegidos, independientemente uno de otro, del grupo consistente en N, S u O, y en donde Hetarilo es un heteroarilo de cinco a diez miembros, mono- o bi-cíclico, eventualmente condensado, que 25 contiene 1, 2, 3 ó 4 heteroátomos seleccionados, independientemente uno de otro, del grupo consistente en N, S u O, y en donde cicloalquilo puede estar saturado o parcialmente saturado, en donde R2.1 es H o un radical seleccionado del grupo consistente en alquilo 30 C1-6-, alcanol C1-6, haloalquilo C1-3, cicloalquilo C3-10 mono- o bi-cíclico, aril C6-10-alquileno C1-6, hetaril-alquileno C1-6, Het-alquileno C1-6, cicloalquil C3-10-alquileno C1-6, un arilo C6-10 mono- o bi-cíclico, heteroarilo y un -Het, que eventualmente puede estar sustituido con uno varios radicales seleccionados del grupo consistente en OH, O-(alquilo C1-3), halógeno, alquilo C1-6 y arilo C6-10, 35 en donde R2.2 y R2.3 son, de modo independiente entre sí, H o un radical que está seleccionado del grupo compuesto por alquilo C1-6, cicloalquilo C3-10 mono- o bicíclico, aril C6-10-alquileno C1-6, hetarilalquileno C1-6, arilo C6-10 mono- o bicíclico, Het, Hetarilo, CO-NH2, CO-NHCH3, CO-N(CH3)2, SO2- (alquilo C1-C2), CO-R2.1 y COOR2.1, que eventualmente puede estar sustituido con uno o más radicales seleccionados del grupo 40 consistente en OH, halógeno, alquilo C1-6, arilo C6-10 y COOR2.1, o R2 es un cicloalquilo C3-10 mono- o policíclico que eventualmente puede estar puenteado una o varias veces a través de grupos alquilo C1-3 y que eventualmente puede estar sustituido con un radical seleccionado del grupo compuesto por alcanol C1-6 ramificado o no ramificado, fluoroalquilo C1-3, alquilen C1-3-OR2.1, OR2.1, 45 COOR2.1, -SO2-NR2.2R2.3, Het, -NH-CO-O-(alquilo C1-6), -NH-CO-(alquilo C1-6), -NH-CO-O-(arilo C6-10), -NH-CO-(arilo C6-10), -NH-CO-O-Hetarilo, -NH-CO-Hetarilo, -NH-CO-O-(alquilen C1-3)-(arilo C6-10), -NH-CO-(alquilen C1-3)- (arilo C6-10), -N(alquil C1-3)-CO-(alquilo C1-6), -N(alquil C1-3)-CO-O-(arilo C6-10), -N(alquil C1-3)-CO-(arilo C6-10), -N(alquil C1-3)-CO-O-Hetarilo, -N(alquil C1-3)-CO-hetarilo, -N(alquil C1-3)-CO-O-(alquilen C1-3)-(arilo C6-10), - 50 N(alquil C1-3)-CO-(alquilen C1-3)-(arilo C6-10), arilo C6-10, alquilo C1-6, aril C6-10-alquileno C1-6, Hetaril-alquileno C1-6, cicloalquilo C3-10 mono- o bi-cíclcico y NR2.2R2.3,
ES13154790.3T 2007-10-19 2008-10-16 Piperidino-dihidrotienopirimidinas sustituidas Active ES2524910T3 (es)

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EP07118901 2007-10-19

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US (1) US8754073B2 (es)
EP (3) EP2215092B1 (es)
JP (2) JP5150728B2 (es)
KR (1) KR101548975B1 (es)
CN (2) CN104069112A (es)
AR (1) AR069075A1 (es)
AT (1) ATE542825T1 (es)
AU (1) AU2008313660B2 (es)
BR (1) BRPI0818006B8 (es)
CA (1) CA2705414C (es)
CL (1) CL2008003096A1 (es)
CY (2) CY1112703T1 (es)
DK (2) DK2215092T3 (es)
EA (1) EA019480B1 (es)
EC (1) ECSP10010156A (es)
ES (2) ES2381452T3 (es)
HR (2) HRP20120334T1 (es)
MA (1) MA31845B1 (es)
ME (1) ME01330B (es)
MX (1) MX2010004026A (es)
MY (1) MY153979A (es)
NZ (1) NZ585346A (es)
PE (2) PE20131463A1 (es)
PL (2) PL2610258T3 (es)
PT (2) PT2215092E (es)
RS (1) RS52271B (es)
SI (2) SI2215092T1 (es)
TN (1) TN2010000175A1 (es)
TW (1) TWI421077B (es)
UA (1) UA99309C2 (es)
UY (1) UY31405A1 (es)
WO (1) WO2009050248A1 (es)
ZA (1) ZA201001683B (es)

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