ES2524910T3 - Piperidino-dihidrotienopirimidinas sustituidas - Google Patents

Piperidino-dihidrotienopirimidinas sustituidas Download PDF

Info

Publication number
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
Authority
ES
Spain
Prior art keywords
alkyl
aryl
alkylene
group
hetaryl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES13154790.3T
Other languages
English (en)
Inventor
Pascale Pouzet
Klaus Klinder
Ralf Anderskewitz
Horst Dollinger
Dennis Fiegen
Thomas Fox
Rolf Goeggel
Christoph Hoenke
Domnic Martyres
Peter Nickolaus
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39154006&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2524910(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Application granted granted Critical
Publication of ES2524910T3 publication Critical patent/ES2524910T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • 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
    • A61P1/16—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
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P11/10—Expectorants
    • 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
    • A61P11/12—Mucolytics
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

Landscapes

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

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07118901 2007-10-19

Publications (1)

Publication Number Publication Date
ES2524910T3 true ES2524910T3 (es) 2014-12-15

Family

ID=39154006

Family Applications (2)

Application Number Title Priority Date Filing Date
ES08839793T Active ES2381452T3 (es) 2007-10-19 2008-10-16 PIPERIDINO-DIHIDROTIENOPIRIMIDINAS sustituidas
ES13154790.3T Active ES2524910T3 (es) 2007-10-19 2008-10-16 Piperidino-dihidrotienopirimidinas sustituidas

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES08839793T Active ES2381452T3 (es) 2007-10-19 2008-10-16 PIPERIDINO-DIHIDROTIENOPIRIMIDINAS sustituidas

Country Status (33)

Country Link
US (1) US8754073B2 (es)
EP (3) EP2380891B1 (es)
JP (2) JP5150728B2 (es)
KR (1) KR101548975B1 (es)
CN (2) CN101827852B (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) DK2610258T3 (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) PE20091386A1 (es)
PL (2) PL2215092T3 (es)
PT (2) PT2215092E (es)
RS (1) RS52271B (es)
SI (2) SI2610258T1 (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)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1847543A1 (de) 2006-04-19 2007-10-24 Boehringer Ingelheim Pharma GmbH & Co. KG Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen
JP5538231B2 (ja) * 2007-10-18 2014-07-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロチエノ［３，２−ｄ］ピリミジンおよびその中で使用される中間体の調製
RU2500681C2 (ru) 2007-10-19 2013-12-10 Берингер Ингельхайм Интернациональ Гмбх Замещенные гетероциклом пиперазинодигидротиенопиримидины
SI2610258T1 (sl) * 2007-10-19 2014-12-31 Boehringer Ingelheim International Gmbh Substituirani piperidino-dihidrotienopirimidini
EP2215093B1 (de) 2007-10-19 2011-12-14 Boehringer Ingelheim International GmbH Neue piperazino-dihydrothienopyrimidin-derivate
JP2012519160A (ja) * 2009-02-27 2012-08-23 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｄｅ４阻害剤及びｎｓａｉｄを含有する組み合わせ薬
EP2555773A1 (de) 2010-04-08 2013-02-13 Boehringer Ingelheim International GmbH Arzneimittelkombinationen enthaltend pde4-inhibitoren und ep4-rezeptor-antagonisten
WO2011124525A1 (de) 2010-04-08 2011-10-13 Boehringer Ingelheim International Gmbh Arnzeimittelkombinationen enthaltend pde4-inhibitoren und ep4-rezeptor-antagonisten
WO2011143057A1 (en) 2010-05-11 2011-11-17 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
US9802954B2 (en) 2011-08-24 2017-10-31 Boehringer Ingelheim International Gmbh Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma
US20130059866A1 (en) * 2011-08-24 2013-03-07 Boehringer Ingelheim International Gmbh Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma
US9013997B2 (en) * 2012-06-01 2015-04-21 Broadcom Corporation System for performing distributed data cut-through
US9422267B2 (en) 2012-12-26 2016-08-23 Medivation Technologies, Inc. Fused pyrimidine compounds and use thereof
JP6307525B2 (ja) * 2013-02-04 2018-04-04 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング 新規の置換縮合ピリミジン化合物
WO2014124860A1 (en) 2013-02-14 2014-08-21 Boehringer Ingelheim International Gmbh Specific pde4b-inhibitors for the treatment of diabetes mellitus
HUP1300139A2 (en) * 2013-03-06 2014-09-29 Richter Gedeon Nyrt Phenoxypiperidine h3 antagonists
CN104892720B (zh) * 2014-03-07 2016-10-26 华东师范大学 4,4-二甲基石胆酸-2,3-骈n-芳基吡唑衍生物及其制备方法和应用
EP3480198B1 (en) * 2016-06-30 2021-05-05 Riken Novel compound or pharmaceutically acceptable salt thereof
US11365204B2 (en) 2017-09-20 2022-06-21 UNION therapeutics A/S Substituted dihydrothienopyrimidines and their use as phosphodiesterase inhibitors
LT3700529T (lt) 2017-10-23 2025-10-10 Naujas veikliųjų medžiagų derinys, skirtas progresuojančių fibrozinių intersticinių plaučių ligų (pf-ild) gydymui
WO2019115775A1 (en) 2017-12-15 2019-06-20 Leo Pharma A/S Substituted tetrahydropyran dihydrothienopyrimidines and their use as phosphodiesterase inhibitors
WO2019115774A1 (en) 2017-12-15 2019-06-20 Leo Pharma A/S Substituted azetidine dihydrothienopyrimidines and their use as phosphodiesterase inhibitors
WO2019115776A1 (en) 2017-12-15 2019-06-20 Leo Pharma A/S Substituted azetidine dihydrothienopyridines and their use as phosphodiesterase inhibitors
WO2020048827A1 (en) * 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 1, 3, 9-triazaspiro[5.5] undecan-2-one compounds
CA3234847A1 (en) 2021-12-09 2023-06-15 Boehringer Ingelheim International Gmbh New oral pharmaceutical composition and dose regimen for the therapy of progressive fibrosing interstitial lung diseases
PL4426298T3 (pl) 2021-12-09 2026-07-20 Boehringer Ingelheim International Gmbh Nowe kombinacje terapeutyczne zawierające pirfenidon i inhibitor pde4 do leczenia postępujących włókniejących śródmiąższowych chorób płuc
CN119343352A (zh) * 2022-06-02 2025-01-21 西藏海思科制药有限公司 Pde4b抑制剂及其用途
TW202408518A (zh) * 2022-06-16 2024-03-01 大陸商武漢人福創新藥物研發中心有限公司 Pde4b抑制劑
CN115040503B (zh) * 2022-07-26 2023-10-10 云南民族大学 螺环二烯酮型木脂素类化合物在制药中的应用
JP2025528779A (ja) * 2022-08-09 2025-09-02 シーザン ハイスーク ファーマシューティカル カンパニー リミテッド Ｐｄｅ４ｂ阻害剤及びその用途
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
EP4596554A4 (en) 2022-09-29 2025-12-10 Suzhou Arkbiopharmaceutical Co Ltd Fused AZA Cyclic Compound, its Preparation Process and its Use in Medicine
CN118871444A (zh) * 2023-02-28 2024-10-29 上海翊石医药科技有限公司 二氢噻吩并嘧啶衍生物的制备方法和用途
CN121127461A (zh) * 2023-04-03 2025-12-12 上海壹迪生物技术有限公司 二氢噻吩并嘧啶类化合物、其制备方法和应用
EP4678644A1 (en) 2023-04-13 2026-01-14 Shanghai Yidi Biotechnology Co., Ltd. Substituted dihydrothienopyrimidine compound, preparation method therefor, and use thereof
CN116925099B (zh) * 2023-07-21 2025-06-03 厦门大学 手性二氢噻吩并嘧啶亚砜的制备方法及其应用与其2、4位取代化合物
EP4761728A2 (en) * 2023-08-17 2026-06-24 Katalytic Therapeutics, Inc. Pde4 protein degraders, pharmaceutical compositions, and therapeutic applications
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
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

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1470336A1 (de) 1962-07-04 1969-03-20 Thomae Gmbh Dr K Neue Dihydrothieno-[3,4-d]-pyrimidine und Verfahren zu ihrer Herstellung
NL124131C (es) 1963-06-17
DE1470356A1 (de) 1964-01-15 1970-04-30 Thomae Gmbh Dr K Neue Thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
BE663693A (es) 1965-03-31
DE1940572A1 (de) 1969-08-08 1971-02-11 Thomae Gmbh Dr K Neue 2-Aminoalkylamino-thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
DE2032687A1 (en) 1970-07-02 1972-01-05 Dr. Karl Thomae Gmbh, 7950 Biberach Cardiovascular 2-aminoalkylamino-thienopyrimidines - and 4-morpholino derivatives from 4-diethanolamino-compounds by intramolecular cyclisa
BE754606A (fr) * 1969-08-08 1971-02-08 Thomae Gmbh Dr K Nouvelles 2-aminoalcoylamino-thieno(3,2-d)pyrimidines et leurs procedesde fabrication
US3763156A (en) * 1970-01-28 1973-10-02 Boehringer Sohn Ingelheim 2-heterocyclic amino-4-morpholinothieno(3,2-d)pyrimidines
FR2082496A5 (es) 1970-03-18 1971-12-10 Westinghouse Freins & Signaux
DE2121950A1 (en) 1971-05-04 1972-11-23 Dr. Karl Thomae Gmbh, 7950 Biberach Thieno(3,2-d)pyrimidine derivs - with thrombocyte aggregation inhibiting activity
DE2750288A1 (de) * 1977-11-10 1979-05-17 Thomae Gmbh Dr K Neue 9-(omega-heteroarylamino- alkylamino)-erythromycine, ihre salze, verfahren zu ihrer herstellung und diese enthaltende arzneimittel
US4256737A (en) * 1979-06-11 1981-03-17 Syntex (U.S.A.) Inc. Long acting depot injectable formulations for LH-RH analogues
US5187168A (en) * 1991-10-24 1993-02-16 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
US5491201A (en) 1992-02-06 1996-02-13 The Dow Chemical Company Mesogenic cyclic imino ether-containing compositions and polymerization products thereof
JPH07330777A (ja) 1994-06-08 1995-12-19 Taisho Pharmaceut Co Ltd チエノ［３，２−ｄ］ピリミジン−４−オン誘導体
JPH09301958A (ja) 1996-05-09 1997-11-25 Nippon Shoji Kk 新規ピリミジン化合物及び抗ロタウイルス剤
US6339089B2 (en) 1997-08-13 2002-01-15 Fujirebio Inc. Pyrimidine nucleus-containing compound and a medicament containing the same for a blood oxygen partial pressure amelioration, and a method for preparing the same
JP2003520042A (ja) 2000-01-24 2003-07-02 アイシス・ファーマシューティカルス・インコーポレーテッド 誘導性一酸化窒素シンターゼ発現のアンチセンスモジュレーション
GB0004153D0 (en) 2000-02-23 2000-04-12 Astrazeneca Uk Ltd Novel use
AU2002214996B2 (en) 2000-10-12 2007-03-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Crystalline monohydrate, method for producing the same and the use thereof in the production of a medicament
DE10064994A1 (de) * 2000-12-23 2002-07-04 Merck Patent Gmbh Sulfamidothienopyrimidine
CN101100472A (zh) 2001-04-30 2008-01-09 美国拜尔公司 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用
AR035700A1 (es) 2001-05-08 2004-06-23 Astrazeneca Ab Derivados de arilheteroalquilamina, composicion farmaceutica, usos de estos derivados para la fabricacion de medicamentos, metodos de tratamiento, y proceso para la preparacion de estos derivados
CA2450961C (en) 2001-06-22 2010-03-30 Boehringer Ingelheim Pharma Gmbh & Co. Kg Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
US6587548B2 (en) * 2001-07-17 2003-07-01 Hewlett-Packard Development Co., L.P. Method and system of using a single telephone number for multiple services
WO2003055890A1 (en) 2001-12-21 2003-07-10 Bayer Pharmaceuticals Corporation Thienopyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
EP1465900B1 (en) 2002-01-10 2008-05-14 Bayer HealthCare AG Rho-kinase inhibitors
SE0203304D0 (sv) 2002-11-07 2002-11-07 Astrazeneca Ab Novel Coumpounds
KR100824193B1 (ko) 2003-04-29 2008-04-21 화이자 인코포레이티드 고혈압 치료에 유용한5,7-디아미노피라졸로[4,3-ｄ]피리미딘
EP1654385A4 (en) 2003-05-16 2006-11-08 Wisconsin Alumni Res Found PROCESS FOR THE INSULATION AND CLONING OF HIGH-MOLECULAR POLYNUCLEOTIDE MOLECULES FROM THE ENVIRONMENT
JP2005003345A (ja) 2003-05-21 2005-01-06 Showa Denko Kk 換気兼熱交換装置および空調システム
MX338455B (es) * 2003-10-02 2016-04-18 Dsm Ip Assets Bv Produccion de altos niveles de dha en microalgas usando cantidades modificadas de cloruro y potasio.
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
US20050137186A1 (en) 2003-12-18 2005-06-23 Abbott Gmbh & Co. Kg. Tetrahydrobenzazepines and their use
WO2005061483A2 (en) 2003-12-23 2005-07-07 Bio-Medisinsk Innovasjon As Modulators of peripheral 5-ht receptors
WO2005082865A1 (ja) 2004-02-27 2005-09-09 Astellas Pharma Inc. 縮合二環性ピリミジン誘導体
GB0427403D0 (en) 2004-12-15 2005-01-19 Astrazeneca Ab Novel compounds I
JP2008540486A (ja) 2005-05-11 2008-11-20 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｄｅ４インヒビター及びテトラヒドロビオプテリン誘導体との組合せ物
EP1847543A1 (de) * 2006-04-19 2007-10-24 Boehringer Ingelheim Pharma GmbH & Co. KG Dihydrothienopyrimidine zur Behandlung von entzündlichen Erkrankungen
HRP20090395T1 (hr) 2006-04-19 2009-08-31 Boehringer Ingelheim International Gmbh Dihidrotienpirimidini za liječenje upalnih bolesti
PT2137196E (pt) 2007-04-20 2010-12-16 Glaxo Group Ltd Compostos tricíclicos contendo azoto como agentes antibacterianos
JP5538231B2 (ja) * 2007-10-18 2014-07-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジヒドロチエノ［３，２−ｄ］ピリミジンおよびその中で使用される中間体の調製
WO2009052288A1 (en) * 2007-10-19 2009-04-23 Schering Corporation Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity
CA2702447A1 (en) * 2007-10-19 2009-04-30 Boehringer Ingelheim International Gmbh New phenyl-substituted piperazino-dihydrothienopyrimidines
SI2610258T1 (sl) * 2007-10-19 2014-12-31 Boehringer Ingelheim International Gmbh Substituirani piperidino-dihidrotienopirimidini
BRPI0818448A2 (pt) 2007-10-19 2015-05-12 Astrazeneca Ab Composto, composição farmacêutica, uso de um composto, e, métodos para o tratamento ou prevenção de um distúrbio madiano pelo receptor mglur5.
RU2500681C2 (ru) 2007-10-19 2013-12-10 Берингер Ингельхайм Интернациональ Гмбх Замещенные гетероциклом пиперазинодигидротиенопиримидины
EP2215093B1 (de) 2007-10-19 2011-12-14 Boehringer Ingelheim International GmbH Neue piperazino-dihydrothienopyrimidin-derivate
FR2922550B1 (fr) * 2007-10-19 2009-11-27 Sanofi Aventis Nouveaux derives de 6-aryl/heteroalkyloxy benzothiazole et benzimidazole, application comme medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de cmet
WO2010097332A1 (de) 2009-02-27 2010-09-02 Boehringer Ingelheim International Gmbh Arzneimittelkombinationen enthaltend pde4-inhibitoren und nsaids
JP2012519160A (ja) 2009-02-27 2012-08-23 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｄｅ４阻害剤及びｎｓａｉｄを含有する組み合わせ薬
US20130059866A1 (en) * 2011-08-24 2013-03-07 Boehringer Ingelheim International Gmbh Novel piperidino-dihydrothienopyrimidine sulfoxides and their use for treating copd and asthma

Also Published As

Publication number Publication date
CY1112703T1 (el) 2016-02-10
AR069075A1 (es) 2009-12-30
EA201000609A1 (ru) 2010-10-29
MX2010004026A (es) 2010-04-30
RS52271B (sr) 2012-10-31
EP2610258B1 (de) 2014-08-27
MA31845B1 (fr) 2010-11-01
JP5150728B2 (ja) 2013-02-27
PL2215092T3 (pl) 2012-07-31
EP2380891B1 (de) 2013-12-11
ME01330B (me) 2013-12-20
PL2610258T3 (pl) 2015-02-27
CA2705414A1 (en) 2009-04-23
BRPI0818006B1 (pt) 2019-10-22
SI2610258T1 (sl) 2014-12-31
BRPI0818006B8 (pt) 2021-05-25
CN101827852A (zh) 2010-09-08
CY1115858T1 (el) 2017-01-25
DK2215092T3 (da) 2012-05-07
EP2610258A1 (de) 2013-07-03
CN104069112A (zh) 2014-10-01
EP2215092B1 (de) 2012-01-25
US20110021501A1 (en) 2011-01-27
UA99309C2 (ru) 2012-08-10
NZ585346A (en) 2011-09-30
PE20131463A1 (es) 2013-12-23
UY31405A1 (es) 2009-05-29
CL2008003096A1 (es) 2010-02-12
TN2010000175A1 (fr) 2011-11-11
JP2013064001A (ja) 2013-04-11
JP2011500640A (ja) 2011-01-06
EP2215092A1 (de) 2010-08-11
ES2381452T3 (es) 2012-05-28
WO2009050248A1 (de) 2009-04-23
BRPI0818006A2 (pt) 2015-12-22
TW200918074A (en) 2009-05-01
HRP20141153T1 (hr) 2015-02-13
DK2610258T3 (da) 2014-11-10
TWI421077B (zh) 2014-01-01
SI2215092T1 (sl) 2012-04-30
ECSP10010156A (es) 2010-06-29
ZA201001683B (en) 2010-10-27
KR20100100807A (ko) 2010-09-15
HK1145677A1 (en) 2011-04-29
PE20091386A1 (es) 2009-10-17
PT2215092E (pt) 2012-04-10
CA2705414C (en) 2016-05-24
US8754073B2 (en) 2014-06-17
PT2610258E (pt) 2014-10-24
AU2008313660A1 (en) 2009-04-23
JP5615889B2 (ja) 2014-10-29
HRP20120334T1 (hr) 2012-05-31
AU2008313660B2 (en) 2013-11-07
CN101827852B (zh) 2014-07-30
MY153979A (en) 2015-04-30
EP2380891A1 (de) 2011-10-26
ATE542825T1 (de) 2012-02-15
EA019480B1 (ru) 2014-04-30
KR101548975B1 (ko) 2015-09-01

Similar Documents

Publication Publication Date Title
ES2632934T3 (es) Composición que comprende un plaguicida, un alcoxilato de 2- propilheptilamina y un tensioactivo adicional
AR076360A1 (es) Derivados de 3,3'-espiroindolinona y su uso en el tratamiento del cancer
ES2530522T3 (es) Composición de tratamiento para el lavado de ropa, que comprende colorantes de matizado bis-azoicos
ES2381452T3 (es) PIPERIDINO-DIHIDROTIENOPIRIMIDINAS sustituidas
AR087184A1 (es) Derivados de azaindol utiles para tratar infecciones por hiv y composiciones farmaceuticas que los contienen
AR091933A1 (es) Composiciones detergentes liquidas concentradas
MX2012008140A (es) Intermedios y surfactantes utiles en composiciones para la limpieza del hogar y el cuidado personal, y metodos para elaborarlos.
AR061034A1 (es) Alaninas sustituidas con benzoilo
AR084058A1 (es) Composicion y metodo para fabricar una composicion para el cuidado de telas
PE20120322A1 (es) Composicion farmaceutica que comprende faldaprevir o una sal del mismo en un vehiculo auto-emulsionante
AR073286A1 (es) Compuestos de imidazol y de triazol, su uso, asi como productos que los contienen
PE20141940A1 (es) Compuestos triciclicos, composiciones que los comprenden y usos de los mismos
AR082696A1 (es) Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras
AR046103A1 (es) Compuesto de 8-azoniabiciclo [3.2.1] octano,composicion farmaceutica para el tratamiento de enfermedades mediadas por receptores de acetilcolina muscarinicos y uso del compuesto para preparar dicha composicion
AR066492A1 (es) Derivados de imidazoquinolina, proceso para su preparacion, composiciones farmaceuticas que los contienen y usos para el tratamiento de enfermedades virales, bacterianas, alergicas y distintos tipos de canceres.
AR083879A1 (es) Analogos de aminoglicosidos antibacterianos, metodos de preparacion y uso como agentes terapeuticos
AR080074A1 (es) Naftiridinas sustituidas y su uso como medicamentos
AR082633A1 (es) Analogos de tetraciclina
AR068466A1 (es) Cianoisoquinolina
ES2421630T3 (es) Compuestos en calidad de antagonistas de bradiquinina B1
AR077525A1 (es) 4-aril-butan-1,3-diamidas y composiciones farmaceuticas
EA201891261A1 (ru) Фармацевтическая композиция, содержащая производные глутаримидов, их применение для лечения эозинофильных заболеваний
HRP20201905T1 (hr) Inhibitori aldoza reduktaze i postupci njihove upotrebe
AR084251A1 (es) Inhibidores dimericos de las iap
BR112014002594A2 (pt) uso de diésteres de isossorbida como espessantes