[go: up one dir, main page]

PE20090547A1 - DERIVADOS DE PIRAZINONA COMO INHIBIDORES DE p38 QUINASA - Google Patents

DERIVADOS DE PIRAZINONA COMO INHIBIDORES DE p38 QUINASA

Info

Publication number
PE20090547A1
PE20090547A1 PE2008001103A PE2008001103A PE20090547A1 PE 20090547 A1 PE20090547 A1 PE 20090547A1 PE 2008001103 A PE2008001103 A PE 2008001103A PE 2008001103 A PE2008001103 A PE 2008001103A PE 20090547 A1 PE20090547 A1 PE 20090547A1
Authority
PE
Peru
Prior art keywords
cyclopropyl
amino
alkyl
methyl
pirazinone
Prior art date
Application number
PE2008001103A
Other languages
English (en)
Inventor
Stephen Brough
Richard Evans
Timothy Jon Luker
Piotr Raubo
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 PE20090547A1 publication Critical patent/PE20090547A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

Landscapes

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

Abstract

REFERIDA A UN DERIVADO A UN DERIVADO DE PIRAZINONA DE FORMULA (I), DONDE R1, R1a Y R2 SON H, ALQUILO C1-C6, ALCOXI C1-C6, CF3, HALO Y CN; R3 Y R4 SON H, ALQUILO C1-C6, OH, CF3, CN, ENTRE OTROS; R5 ES H, CICLOALQUILO C3-C7, ARILO, ENTRE OTROS; R6 ES H, ALQUILO C1-C6, ALCOXI C1-C6, CICLOALQUILO C3-C7, ENTRE OTROS; R7 ES H, ALQUILO C1-C6, ALCOXI C1-C6, CICLOALQUILO C3-C7, ARILO. SON COMPUESTOS PREFERIDOS: N-CICLOPROPIL-4-METIL-3-[3-[[1-METIL-1-[2-[2-(METILAMINO)ETOXI]FENIL]ETIL]AMINO]-2-OXO-1(2H)-PIRAZINIL]-BENZAMIDA, N-CICLOPROPIL-4-METIL-3-[3-[[1-[2-[2-(METILAMINO)ETOXI]FENIL]CICLOPROPIL]AMINO]-2-OXO-1(2H)-PIRAZINIL]-BENZAMIDA, N-CICLOPROPIL-3-FLUORO-5-[3-[[1-[2-[2-[(2-HIDROXIETIL)AMINO]ETOXI]FENIL]-1-METILETIL]AMINO]-2-OXO-1(2H)-PIRAZINIL]-4-METIL-BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBIDORA DE LA p38 QUINASA Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES DEL TRACTO RESPIRATORIO, HUESOS Y ARTICULACIONES, DOLOR, DE LA PIEL, ENTRE OTROS
PE2008001103A 2007-06-27 2008-06-27 DERIVADOS DE PIRAZINONA COMO INHIBIDORES DE p38 QUINASA PE20090547A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US94641507P 2007-06-27 2007-06-27
US97816707P 2007-10-08 2007-10-08
US2944408P 2008-02-18 2008-02-18

Publications (1)

Publication Number Publication Date
PE20090547A1 true PE20090547A1 (es) 2009-06-04

Family

ID=39745171

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001103A PE20090547A1 (es) 2007-06-27 2008-06-27 DERIVADOS DE PIRAZINONA COMO INHIBIDORES DE p38 QUINASA

Country Status (30)

Country Link
US (4) US8163905B2 (es)
EP (1) EP2170848B1 (es)
JP (2) JP5140154B2 (es)
KR (1) KR101541203B1 (es)
CN (1) CN101842361B (es)
AR (1) AR067444A1 (es)
AU (1) AU2008269516B2 (es)
BR (1) BRPI0813244B8 (es)
CA (1) CA2691215C (es)
CL (1) CL2008001898A1 (es)
CO (1) CO6251251A2 (es)
CY (1) CY1115836T1 (es)
DK (1) DK2170848T3 (es)
EC (1) ECSP109903A (es)
ES (1) ES2525716T3 (es)
HR (1) HRP20141174T1 (es)
IL (1) IL202826A (es)
MY (1) MY153258A (es)
NZ (1) NZ581942A (es)
PE (1) PE20090547A1 (es)
PL (1) PL2170848T3 (es)
PT (1) PT2170848E (es)
RS (1) RS53682B1 (es)
RU (1) RU2479580C2 (es)
SG (1) SG182958A1 (es)
SI (1) SI2170848T1 (es)
TW (1) TWI448288B (es)
UA (1) UA98961C2 (es)
UY (1) UY31183A1 (es)
WO (1) WO2009001132A1 (es)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2170848T3 (en) 2007-06-27 2015-01-05 Astrazeneca Ab Pyrazinonderivater and their use to treat lung diseases
US20090011994A1 (en) 2007-07-06 2009-01-08 Bristol-Myers Squibb Company Non-basic melanin concentrating hormone receptor-1 antagonists and methods
AR073711A1 (es) 2008-10-01 2010-11-24 Astrazeneca Ab Derivados de isoquinolina
WO2010043721A1 (en) 2008-10-17 2010-04-22 Oryzon Genomics, S.A. Oxidase inhibitors and their use
EP2379174A4 (en) * 2008-12-18 2012-11-14 Astrazeneca Ab PHARMACEUTICAL PRODUCT USING A P38 KINASE INHIBITOR AND A SECOND ACTIVE SUBSTANCE
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
TW201036957A (en) 2009-02-20 2010-10-16 Astrazeneca Ab Novel salt 628
GB0913345D0 (en) 2009-07-31 2009-09-16 Astrazeneca Ab New combination 802
EP2480528B1 (en) 2009-09-25 2018-08-29 Oryzon Genomics, S.A. Lysine specific demethylase-1 inhibitors and their use
WO2011042217A1 (en) 2009-10-09 2011-04-14 Oryzon Genomics S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2011061527A1 (en) 2009-11-17 2011-05-26 Astrazeneca Ab Combinations comprising a glucocorticoid receptor modulator for the treatment of respiratory diseases
CA2785658C (en) 2009-12-31 2017-10-24 Ira Milton Trachtman Compositions and method for treatment and prophylaxis of inflammatory bowel disease
WO2011106573A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011131697A1 (en) 2010-04-19 2011-10-27 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
CN104892525A (zh) 2010-07-29 2015-09-09 奥瑞泽恩基因组学股份有限公司 Lsd1的基于芳基环丙胺的脱甲基酶抑制剂及其医疗用途
TWI535712B (zh) * 2010-08-06 2016-06-01 阿斯特捷利康公司 化合物
GB201016912D0 (en) 2010-10-07 2010-11-24 Astrazeneca Ab Novel combination
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
GB201021979D0 (en) 2010-12-23 2011-02-02 Astrazeneca Ab New compound
GB201021992D0 (en) 2010-12-23 2011-02-02 Astrazeneca Ab Compound
WO2012107498A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative disorders
WO2012156531A2 (en) * 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
IN2014CN03337A (es) 2011-10-20 2015-07-03 Oryzon Genomics Sa
EP2768805B1 (en) 2011-10-20 2020-03-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
JP6088491B2 (ja) 2012-04-10 2017-03-01 大日本住友製薬株式会社 新規１位置換インダゾール誘導体
KR102057877B1 (ko) 2012-07-18 2019-12-20 노스 앤드 사우스 브라더 파마시 인베스트먼트 컴파니 리미티드 질소함유 헤테로고리 유도체 및 그의 약물에서의 용도
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
US9444925B2 (en) * 2013-04-05 2016-09-13 Microsoft Technology Licensing, Llc Smartphone proximity card emulation
DK3030323T3 (da) 2013-08-06 2019-07-15 Imago Biosciences Inc Kdm1a-inhibitorer til behandlingen af sygdom
US10011583B2 (en) 2014-06-27 2018-07-03 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
MX387224B (es) 2015-02-12 2025-03-18 Imago Biosciences Inc Inhibidores de kdm1a para el tratamiento de enfermedades.
CN108884057A (zh) * 2016-03-24 2018-11-23 阿斯利康(瑞典)有限公司 结晶形式
US10934272B2 (en) 2016-04-07 2021-03-02 Glaxosmithkline Intellectual Property (No. 2) Limited Pyridyl derivatives as bromodomain inhibitors
US11390590B2 (en) 2016-08-16 2022-07-19 Imago Biosciences, Inc. Methods and processes for the preparation of KDM1A inhibitors
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
EP3529242A1 (en) * 2016-10-19 2019-08-28 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
CN106674029B (zh) * 2016-12-23 2018-08-21 四川久凌制药科技有限公司 一种他喷他多中间体的制备方法
KR20240032157A (ko) 2017-05-02 2024-03-08 노파르티스 아게 병용 요법
US11578059B2 (en) * 2018-05-11 2023-02-14 Imago Biosciences. Inc. KDM1A inhibitors for the treatment of disease
WO2020193419A1 (en) * 2019-03-22 2020-10-01 Saniona A/S Novel potassium channel inhibitors
CN113795490A (zh) 2019-05-13 2021-12-14 诺华股份有限公司 N-(3-(2-(2-羟基乙氧基)-6-吗啉代吡啶-4-基)-4-甲基苯基)-2(三氟甲基)异烟酰胺的新结晶形式作为Raf抑制剂治疗癌症
AU2022204775B2 (en) * 2021-04-14 2023-03-30 National University Corporation Hokkaido University Triazine derivative having virus propagation inhibitory effect, and pharmaceutical composition containing same
CN113999129B (zh) * 2021-11-23 2023-09-01 长沙普济生物科技股份有限公司 一种含酚羟基氨基酸表面活性剂的合成方法
WO2025122555A1 (en) * 2023-12-05 2025-06-12 Valo Health, Inc. S1p 1 receptor agonists and uses thereof
CN119350255A (zh) * 2024-10-21 2025-01-24 海南大学 一种酮衍生物及其合成方法和用途

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU723234B2 (en) * 1996-09-06 2000-08-24 Nippon Kayaku Kabushiki Kaisha Novel acetamide derivatives and protease inhibitors
TWI328007B (en) 2002-01-16 2010-08-01 Astrazeneca Ab Novel compounds
BR0308429A (pt) 2002-03-14 2005-01-11 Bayer Healthcare Ag Aroilpiridinonas monocìclicas como agentes antiinflamatórios
CN1305871C (zh) 2002-07-19 2007-03-21 比奥维特罗姆股份公司 用于治疗与5－ht2a受体有关疾病的新哌嗪基－吡嗪酮衍生物
EP1670794A2 (en) 2003-09-30 2006-06-21 Amgen Inc. Vanilloid receptor ligands and their use in treatments
MXPA06003746A (es) * 2003-10-14 2006-06-14 Pharmacia Corp Compuestos de pirazinona sustituida para el tratamiento de inflamacion.
BRPI0417345A (pt) * 2003-12-03 2007-03-13 Cytopia Res Pty Ltd compostos inibidores de quìnase baseados em azola, composições e seus usos
GB0402812D0 (en) * 2004-02-09 2004-03-10 Tanabe Seiyaku Co Novel compounds
EP1763353A1 (en) 2004-06-29 2007-03-21 Warner-Lambert Company LLC COMBINATION THERAPIES UTILIZING BENZAMIDE INHIBITORS OF THE P2X<sb>7</sb> RECEPTOR
JP4496092B2 (ja) 2005-01-12 2010-07-07 信越化学工業株式会社 光ファイバ母材の製造方法及び装置
EP1966164B1 (en) 2005-12-21 2013-03-06 Janssen Pharmaceutica N.V. Novel substituted pyrazinone derivatives for use in mch-1 mediated diseases
CA2650970C (en) 2006-05-04 2014-09-16 Chroma Therapeutics Ltd. P38 map kinase inhibitors
GB0608837D0 (en) 2006-05-04 2006-06-14 Chroma Therapeutics Ltd Inhibitors of MAP kinase
TW200808771A (en) * 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds II
US20090281099A1 (en) * 2006-05-22 2009-11-12 Andres-Gil Jose Ignacio Substituted pyrazinone derivatives for use as a medicine
TW200924754A (en) * 2006-06-21 2009-06-16 Du Pont Pyrazinones as cellular proliferation inhibitors
US20090186907A1 (en) * 2006-06-21 2009-07-23 E.I. Dupont De Nemours And Company Pyrazinones As Cellular Proliferation Inhibitors
DK2170848T3 (en) 2007-06-27 2015-01-05 Astrazeneca Ab Pyrazinonderivater and their use to treat lung diseases

Also Published As

Publication number Publication date
BRPI0813244B1 (pt) 2019-03-26
JP5539473B2 (ja) 2014-07-02
JP2013018781A (ja) 2013-01-31
EP2170848A1 (en) 2010-04-07
CY1115836T1 (el) 2017-01-25
US20130012523A1 (en) 2013-01-10
US8299246B2 (en) 2012-10-30
US20120065214A1 (en) 2012-03-15
CA2691215A1 (en) 2008-12-31
RS53682B1 (sr) 2015-04-30
EP2170848B1 (en) 2014-10-22
AR067444A1 (es) 2009-10-14
BRPI0813244B8 (pt) 2021-05-25
MY153258A (en) 2015-01-29
HRP20141174T1 (hr) 2015-02-13
CN101842361B (zh) 2013-06-05
TW200908978A (en) 2009-03-01
WO2009001132A1 (en) 2008-12-31
HK1142908A1 (en) 2010-12-17
PT2170848E (pt) 2014-12-23
IL202826A (en) 2014-11-30
SI2170848T1 (sl) 2015-01-30
US8889692B2 (en) 2014-11-18
NZ581942A (en) 2012-01-12
KR101541203B1 (ko) 2015-07-31
CL2008001898A1 (es) 2009-07-17
KR20100038398A (ko) 2010-04-14
BRPI0813244A2 (pt) 2014-12-23
RU2009148673A (ru) 2011-08-10
ES2525716T3 (es) 2014-12-29
UA98961C2 (uk) 2012-07-10
JP5140154B2 (ja) 2013-02-06
CA2691215C (en) 2016-03-29
CN101842361A (zh) 2010-09-22
JP2010531345A (ja) 2010-09-24
AU2008269516B2 (en) 2011-11-17
US20150073136A1 (en) 2015-03-12
AU2008269516A1 (en) 2008-12-31
PL2170848T3 (pl) 2015-02-27
TWI448288B (zh) 2014-08-11
US20120214822A1 (en) 2012-08-23
IL202826A0 (en) 2010-06-30
US8163905B2 (en) 2012-04-24
UY31183A1 (es) 2009-01-30
DK2170848T3 (en) 2015-01-05
ECSP109903A (es) 2010-02-26
SG182958A1 (en) 2012-08-30
RU2479580C2 (ru) 2013-04-20
CO6251251A2 (es) 2011-02-21

Similar Documents

Publication Publication Date Title
PE20090547A1 (es) DERIVADOS DE PIRAZINONA COMO INHIBIDORES DE p38 QUINASA
PE20130385A1 (es) Derivados del acido naft-2-ilacetico para tratar el sida
PE20091201A1 (es) AMIDAS SUSTITUIDAS COMO INHIBIDORES DE LA TIROSINA QUINASA DE BRUTON (Btk)
PE20090210A1 (es) Compuestos derivados de pirazolo pirimidina como inhibidores de jak quinasa
PE20081263A1 (es) DERIVADOS DE 4-(2-AMINO-1-HIDROXIETIL)FENOL COMO AGONISTAS DEL RECEPTOR ß2 ADRENERGICO
NZ593030A (en) Pyridyloxyindoles inhibitors of vegf-r2 and use thereof for treatment of disease
NZ593295A (en) Preparation method of dihydroindene amide compounds, their pharmaceutical compositions containing compounds thereof and use as protein kinase inhibitor
NZ610312A (en) 6-amino-2-phenylamino-1h-benzimidazole-5-carboxamide- derivatives and their use as microsomal prostaglandin e2 synthase-1 inhibitors
SG170101A1 (en) 2-pyrazinone derivatives for the treatment of disease or condition in which inhibition of neutrophil elastase activity is beneficial.
PE20140836A1 (es) Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide
PE20120355A1 (es) DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1
PE20110398A1 (es) BENZAMIDAS CON ACTIVIDAD SOBRE LA ENZIMA p38 MAP-QUINASA
PE20110285A1 (es) Derivados de sulfonamidofenil propionamida como ligandos del receptor vaniloide del subtipo 1
UY29766A1 (es) Formas cristalinas delta y épsilon de mesilato de imatinib
MX2008013836A (es) Derivados de 2-piridona para el tratamiento de enfermedades o condiciones en las cuales es benefica la inhibicion de la actividad de elastasa de neutrofilos.
MY146662A (en) Novel n-(8-heteroaryltetrahydronaphtalene-2yl) or n-(5-heteroarylchromane-3-yl) carboxamide derivatives for the treatment of pain
PE20110063A1 (es) DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
PE20081704A1 (es) Derivados de azacicloalcanos como inhibidores de estearoil-coenzima a delta-9 desaturasa
PE20110062A1 (es) N-(3-(3,5-dimetoxifenetil)-1h-pirazol-5-il)-4-(3,4-dimetilpiperazin-1-il)benzamida y sales del mismo
PE20091065A1 (es) Derivados bis-(sulfonilamino) en terapia 066
CY1110014T1 (el) Παραγωγα τετραϋδροκαρβαζολιου χρησιμα ως τροποποιητες υποδοχεα ανδρογονων (sarm)
PE20091092A1 (es) Compuestos heterociclicos como inhibidores de la via hedgehog
RU2011138962A (ru) Производные 4-изопропилфенилглюцита в качестве ингибиторов sglt1
EA201071038A1 (ru) Производные 1-бензил-3-гидроксиметилиндазола и их применение для лечения заболеваний, основанных на экспрессии mcp-1, cx3cr1 и p40
ATE540037T1 (de) Triazolopyridine als phosphodiesterasehemmer zur behandlung von hautkrankheiten

Legal Events

Date Code Title Description
FG Grant, registration