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AR053235A1 - Derivados de tienopirimidinas para el tratamiento de enfermedades inflamatorias - Google Patents

Derivados de tienopirimidinas para el tratamiento de enfermedades inflamatorias

Info

Publication number
AR053235A1
AR053235A1 ARP060101573A ARP060101573A AR053235A1 AR 053235 A1 AR053235 A1 AR 053235A1 AR P060101573 A ARP060101573 A AR P060101573A AR P060101573 A ARP060101573 A AR P060101573A AR 053235 A1 AR053235 A1 AR 053235A1
Authority
AR
Argentina
Prior art keywords
alkynyl
alkenyl
alkyl
aryl
ring
Prior art date
Application number
ARP060101573A
Other languages
English (en)
Inventor
Christoph Hoenke
Birgit Jung
Domnic Martyres
Peter Mickolaus
Pascale Pouzet
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR053235A1 publication Critical patent/AR053235A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D521/00Heterocyclic compounds containing unspecified hetero rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Epidemiology (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)

Abstract

Compuesto de la formula (1) en los que: X es O, S, SO o SO2; R1 es H, alquilo C1-6-, alquenilo C2-6, alquinilo C2-6, arilo C6-10 o aril C6-10-alquileno C1-6, heteroarilo C5-10-alquileno C1-6; R2 es H o un radical eventualmente mono- polisustituido seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, mono- o bicíclico eventualmente puenteado una o varias veces, arilo C6-10, un anillo C3-10 heterocíclico aromático o no aromático, un anillo bicíclico y un arilo C6-10 condensado con un heterociclo C3-10; o NR1R2 significan juntos un anillo heterocíclico que está eventualmente sustituido con uno o varios radicales seleccionados de alquilo C1-4, alquenilo C2-6, alquinilo C2-6, alcanol C1- 6 lineal o ramificado y oxo; R3 un radical mono- o polisustituido seleccionado del grupo compuesto por un anillo C6-10 heterocíclico, cicloalquilo C3-7, aril C6-10-alquileno C1-6, heteroaril C5-10-alquileno C1-6, un anillo bicíclico condensado que eventualmente puede contener 1-4 heteroátomos seleccionados, de modo independiente entre sí, de N, O, S; o R3 significa fenilo eventualmente sustituido; o R3 significa un grupo COR3.7, COCH2R3.8, CONHR3.8 o SO2R3.8; en donde R3.7 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7 o un radical seleccionado del grupo compuesto por arilo C6-10, un anillo C3-10 heterocíclico y un anillo bicíclico que eventualmente está sustituido con uno o varios radicales seleccionados del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, halogeno, NR3.8.1R3.8.1, arilo C6-10 y un anillo C3-10 heterocíclico; en donde R3.8.1 es H, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; R3.8.2 es H, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; R4 es H, alquilo C1-4, alquenilo C2-4,alquinilo C2-4 u oxo; R5 es H, alquilo C1-4, alquenilo C2-4, o alquinilo C2-4; R6 es H, alquilo C1-4, alquenilo C2-4, o alquinilo C2-4; R7 es H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, arilo C6-10 u OH; R8 es H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, arilo C6-10 u OH; o R7 y R8 forman juntos oxo, así como sus sales, diastereomeros, enantiomeros, racematos, hidratos o solvatos farmacologicamente tolerables.
ARP060101573A 2006-04-19 2006-04-21 Derivados de tienopirimidinas para el tratamiento de enfermedades inflamatorias AR053235A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005019201A DE102005019201A1 (de) 2006-04-19 2006-04-19 Neue Verbindungen zur Behandlung von entzündlichen Erkrankungen

Publications (1)

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US (3) US7511045B2 (es)
EP (2) EP1874781B9 (es)
JP (1) JP5021624B2 (es)
KR (1) KR101335964B1 (es)
CN (1) CN101163706A (es)
AR (1) AR053235A1 (es)
AT (1) ATE434620T1 (es)
AU (1) AU2006237354B2 (es)
BR (1) BRPI0608387A2 (es)
CA (1) CA2605161A1 (es)
CY (1) CY1109348T1 (es)
DE (2) DE502006004066D1 (es)
DK (1) DK1874781T3 (es)
EA (1) EA013108B1 (es)
ES (1) ES2328400T3 (es)
HR (1) HRP20090395T1 (es)
IL (1) IL186749A (es)
MX (1) MX2007012313A (es)
NO (1) NO20074615L (es)
NZ (1) NZ563488A (es)
PL (1) PL1874781T3 (es)
PT (1) PT1874781E (es)
RS (1) RS51163B (es)
SI (1) SI1874781T1 (es)
TW (1) TWI380984B (es)
UA (1) UA93872C2 (es)
WO (1) WO2006111549A1 (es)
ZA (1) ZA200707591B (es)

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US8637519B2 (en) 2007-10-19 2014-01-28 Boehringer Ingelheim International Gmbh Heterocycle-substituted piperazino-dihydrothienopyrimidines
US8754073B2 (en) 2007-10-19 2014-06-17 Boehringer Ingelheim International Gmbh Substituted piperazino-dihydrothienopyrimidines
US9090626B2 (en) 2007-10-19 2015-07-28 Boehringer Ingelheim International Gmbh Piperazino-dihydrothienopyrimidine derivatives
US9150586B2 (en) 2011-08-24 2015-10-06 Boehringer Ingelheim International Gmbh Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma
US10745411B2 (en) 2011-08-24 2020-08-18 Boehringer Ingelheim International Gmbh Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma

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KR20250046278A (ko) * 2022-08-09 2025-04-02 시젱 하이스코 파마수티칼 씨오., 엘티디. Pde4b 억제제 및 이의 용도
CN119947728A (zh) 2022-09-28 2025-05-06 勃林格殷格翰国际有限公司 生物标志物在用pde4b抑制剂治疗纤维化病症中的用途
WO2024067660A1 (zh) 2022-09-29 2024-04-04 苏州爱科百发生物医药技术有限公司 氮杂稠环类化合物、其制备方法及其在医药上的应用
CN115887463A (zh) * 2022-12-27 2023-04-04 瑞石生物医药有限公司 一种含环酰胺化合物的药物组合物
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WO2025067168A1 (zh) * 2023-09-25 2025-04-03 苏州爱科百发生物医药技术有限公司 氮杂稠环类化合物及其制备方法和用途
CN120398908A (zh) * 2024-02-01 2025-08-01 艾派克斯生物科技有限公司 Pde4b抑制剂及其药物组合物和用途
WO2025162289A2 (zh) * 2024-02-04 2025-08-07 西藏海思科制药有限公司 一种pde4b抑制剂的晶型及其在医药上的用途
WO2025162431A1 (zh) * 2024-02-04 2025-08-07 西藏海思科制药有限公司 一种pde4b抑制剂化合物的口服药物组合物及其制备方法

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US8114878B2 (en) * 2006-04-19 2012-02-14 Boehringer Ingelheim International Gmbh 6,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases
US8604039B2 (en) 2006-04-19 2013-12-10 Boehringer Ingelheim International Gmbh Dihydrothienopyrimidines for the treatment of inflammatory diseases
US8822474B2 (en) 2006-04-19 2014-09-02 Boehringer Ingelheim International Gmbh 6,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases
US8637519B2 (en) 2007-10-19 2014-01-28 Boehringer Ingelheim International Gmbh Heterocycle-substituted piperazino-dihydrothienopyrimidines
US8754073B2 (en) 2007-10-19 2014-06-17 Boehringer Ingelheim International Gmbh Substituted piperazino-dihydrothienopyrimidines
US9090626B2 (en) 2007-10-19 2015-07-28 Boehringer Ingelheim International Gmbh Piperazino-dihydrothienopyrimidine derivatives
US9115142B2 (en) 2007-10-19 2015-08-25 Boehringer Ingelheim International Gmbh Heterocycle-substituted piperazino-dihydrothienopyrimidines
US9150586B2 (en) 2011-08-24 2015-10-06 Boehringer Ingelheim International Gmbh Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma
US10745411B2 (en) 2011-08-24 2020-08-18 Boehringer Ingelheim International Gmbh Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma

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US20070259846A1 (en) 2007-11-08
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US8354531B2 (en) 2013-01-15
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