AR058071A1 - Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas. - Google Patents

Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas.

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Publication number
AR058071A1
AR058071A1 ARP060104273A ARP060104273A AR058071A1 AR 058071 A1 AR058071 A1 AR 058071A1 AR P060104273 A ARP060104273 A AR P060104273A AR P060104273 A ARP060104273 A AR P060104273A AR 058071 A1 AR058071 A1 AR 058071A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
halogen
heteroaryl
Prior art date
Application number
ARP060104273A
Other languages
English (en)
Inventor
Peter Sjoe
Peter Storm
Annea Lisius
Krister Henriksson
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR058071A1 publication Critical patent/AR058071A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Procesos para preparar dichos compuestos, el uso de dichos compuestos en el tratamiento de un estado de enfermedad mediado por PDE 4, y composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) donde R1 es un anillo carbocíclico o heterocíclico e 5 o 6 miembros, saturado o no saturado; cuando R1 es arilo o heteroarilo entonces dicho arilo o heteroarilo se sustituye opcionalmente como se muestra a continuacion; cuando R1 es un carbociclo no aromático o heterociclilo no aromático entonces dicho anillo esta opcionalmente sustituido con alquilo C1-6; R2 es alquilo C1-4, alcoxi C1-4 o alquiltio C1-4; R3 es H o alquilo C1-4; R4 es alquilo C1-6 (opcionalmente sustituido con CO2R26 o C(O)NR27R28), arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R25 es H o fenilo opcionalmente sustituido; los anillos arilo, heteroarilo y fenilo mencionados se sustituyen opcionalmente en forma independiente con: halogeno, ciano, nitro, hidroxi, S(O)qR5, OC(O)NR6R7, NR8R9, NR10C(O)R11, NR12C(O)NR13R14, S(O)2NR15R16, NR17S(O)2R18, C(O)NR19R20, C(O)R21, CO2R22, NR23CO2R24, alquilo C1-6, haloalquilo C1-6 alcoxi C1-6-alquilo C1-6, alcoxi C1-6, haloalcoxi C1-6, alcoxi C1-6-alcoxi C1-6, alquiltio C1-6, O(CH2)nO, fenilalquilo C1-6, fenoxialquilo C1-6 o fenilalcoxi C1-6; los anillos fenilo de los ultimos tres sustituyentes se sustituyen opcionalmente con halogeno, alquilo C1-4, alcoxi C1-4, CF3 o OCF3; n es 1, 2 o 3; q es 0, 1 o 2; R6 y R7, R13 y R14, R15 y R16, o R19 y R20 se pueden unir para formar, con e N al cual están unidos, un anillo de 5 o 6 miembros; R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24 y R26 son, en forma independiente, alquilo C1-6, (opcionalmente sustituido con halogeno, hidroxi o alcoxi C1-6) o fenilo (él mismo opcionalmente sustituido con halogeno, alquilo C1-4, alcoxi C1-4, CF3 o OCF3); R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R19, R20, R21, R22, R23 y R26 pueden también ser H; R27 es H o alquilo C1-6; R28 es H o alquilo C1-6 (opcionalmente sustituido con NH2, NH(alquilo C1-6) o N(alquil C1-6)2); o un N-oxido de los mismos; o una sal aceptable para uso farmacéutico de los mismos.
ARP060104273A 2005-10-03 2006-09-28 Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas. AR058071A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0502176 2005-10-03

Publications (1)

Publication Number Publication Date
AR058071A1 true AR058071A1 (es) 2008-01-23

Family

ID=37906399

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060104273A AR058071A1 (es) 2005-10-03 2006-09-28 Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas.

Country Status (7)

Country Link
US (1) US20090054413A1 (es)
EP (1) EP1931672A1 (es)
JP (1) JP2009510159A (es)
AR (1) AR058071A1 (es)
TW (1) TW200745106A (es)
UY (1) UY29821A1 (es)
WO (1) WO2007040435A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2694506T3 (es) * 2009-03-12 2018-12-21 Cumberland Pharmaceuticals Inc. Administración de ibuprofeno por vía intravenosa
BRPI1012980A2 (pt) * 2009-05-19 2016-03-29 Vivia Biotech Sl dispositivo e métodos para analisar a capacidade de resposta celular e a resposta de células neoplásticas a drogas
US8871810B2 (en) 2009-07-15 2014-10-28 Cumberland Pharmaceuticals Inc. Treating critically ill patients with intravenous ibuprofen
US9072710B2 (en) 2012-03-16 2015-07-07 Cumberland Pharmaceuticals Inc. Injectable ibuprofen formulation
US9072661B2 (en) 2012-03-16 2015-07-07 Cumberland Pharmaceuticals Inc. Injectable ibuprofen formulation
US11065257B2 (en) 2016-12-12 2021-07-20 Leo Pharma A/S Substituted pyrazoloazepin-4-ones and their use as phosphodiesterase inhibitors
ES2875128T3 (es) * 2016-12-12 2021-11-08 Union Therapeutics As Pirazoloazepin-8-onas sustituidas y su uso como inhibidores de la fosfodiesterasa
US10793580B2 (en) 2016-12-12 2020-10-06 Leo Pharma A/S Substituted pyrazoloazepin-8-ones and their use as phosphodiesterase inhibitors
TWI812739B (zh) * 2018-06-21 2023-08-21 景凱生物科技股份有限公司 Nadph氧化酶抑制劑、含其的醫藥組合物、及其應用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ20021151A3 (cs) * 1999-10-11 2003-03-12 Pfizer Inc. 5-(2-substituovaný-5-heterocyklylsulfonylpyrid-3-yl)-dihydropyrazolo[4,3-d]-pyrimidin-7-ony jako inhibitory fosfodiesterasy
FR2803299B1 (fr) * 2000-01-05 2004-09-17 Warner Lambert Co NOUVELLES PYRAZOLO [4,3-e] DIAZEPINES SUBSTITUEES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
KR100358083B1 (ko) * 2000-02-17 2002-10-25 에스케이케미칼주식회사 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도
GB0113344D0 (en) * 2001-06-01 2001-07-25 Bayer Ag Novel heterocycles 3
DE60222931T2 (de) * 2001-12-13 2008-07-10 Asubio Pharma Co., Ltd. Pyrazolopyrimidinonderivate mit pde7-hemmender wirkung

Also Published As

Publication number Publication date
UY29821A1 (es) 2007-05-31
TW200745106A (en) 2007-12-16
JP2009510159A (ja) 2009-03-12
US20090054413A1 (en) 2009-02-26
WO2007040435A1 (en) 2007-04-12
EP1931672A1 (en) 2008-06-18

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