AR058067A1 - Azepinas inhibidoras de quinasas janus - Google Patents

Azepinas inhibidoras de quinasas janus

Info

Publication number
AR058067A1
AR058067A1 ARP060104186A ARP060104186A AR058067A1 AR 058067 A1 AR058067 A1 AR 058067A1 AR P060104186 A ARP060104186 A AR P060104186A AR P060104186 A ARP060104186 A AR P060104186A AR 058067 A1 AR058067 A1 AR 058067A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkynyl
alkenyl
nrcrd
cycloalkyl
Prior art date
Application number
ARP060104186A
Other languages
English (en)
Inventor
Richard B Sparks
Krishna Vaddi
Andrew P Combs
James D Rodgers
Jordan S Fridman
Argyrios G Arvanitis
Darius J Robinson
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of AR058067A1 publication Critical patent/AR058067A1/es

Links

Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic 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 four or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biotechnology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)

Abstract

Los compuestos de la presente son utiles en el tratamiento de enfermedades relacionadas con la actividad de las quinasa Janus, entre las que se incluyen, por ejemplo, enfermedades relacionadas con el sistema inmune, trastornos dermatologicos, trastornos proliferativos mieloides, cáncer y otras enfermedades. Reivindicacion 1: un compuesto caracterizado porque responde a la formula (1a), (1b), o (1c); o sus sales aceptables para uso farmacéutico o prodrogas de los mismos, en donde: D1, D2, D3, D4, D5, D6 y D7 son, en forma independiente, CR1 o N; E es O, S, SO, SO2, o NR2a; G es N o CR2b; Q1 y Q2 son cada uno, en forma independiente, N o CR2; W1 está ausente, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, O, S, NR3, CO, COO, CONR3, SO, SO2, SONR3, SO2NR, o NR3CONR4, en donde dicho alquilo C1-6, alquenilo C2-6 o alquinilo C2-6 está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, OH, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y dialquilamino C2-8; W2 está ausente, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, en donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, CN, NO2, OH, =NH, =NOH, =NO-(alquilo C1-4), -NR3C(O)O-(alquilo C1-4), -NR3C(O)-(alquilo C1-4), -C(O)O-(alquilo C1-4), haloalquilo C1-4, cianoalquilo C1-4, pentahalosulfanilo, hidroxialquilo C1-4, alquiltio C1-4,haloalquiltio C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y dialquilamino C2-8; W3 está ausente, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, O, S, NR3, =N-, =N-O-, =N-O-(alquil C1-4)-, -O-(alquilo C1-4), S-(alquilo C1-4), NR3-(alquilo C1-4), (alquil C1-4)-O-(alquilo C1-4), (alquil C1-4)-S-(alquilo C1-4), (alquil C1-4)-NR3-(alquilo C1-4), CO, COO, C(O)- (alquilo C1-4), C(O)O-(alquilo C1-4), C(O)- (alquil C1-4)-C(O), NR3C(O)O-(alquilo C1-4), -C(O)NR3-(alquilo C1-4),NR3C(O)O-(alquilo C1-4), NR3C(O)O, CONR3, SO, SO2, SONR3, SO2NR3, o NR3CONR4, en donde dicho alquilo C1-6, alquenilo C2-6 o alquinilo C2-6 está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados en forma independiente entre halo, OH, CN, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, y dialquilamino C2-8; W4 es H, NR3R4, CN, alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, en donde cada uno de dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados en forma independiente entre halo, OH, alcoxi C1-4, =NH, =NOH, =NO-(alquilo C1-4), haloalquilo C1-4, haloalcoxi C1-4, pentahalosulfanilo, COOH, CONH2, COO-(alquilo C1-4), amino, alquilamino C1-4, y dialquilamino C2-8; R1 es, en forma independiente, H, halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, NRc(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, S(O)Rb, S(O)NRcRd, NRcS(O)NRcRd, pentahalosulfanilo, S(O)2Rb, o S(O)2NRcRd; R2a es H, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, OH, alcoxi C1-4, C(O)Rb, C(O)NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, o S(O)2NRcRd; R2b y R2c son cada uno, en forma independiente, H, halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcC(O)NRcRd, NRcRd, NRcC(O)Rd, NRcC(O)ORa, S(O)Rb, S(O)NRcRd, NRcS(O)NRcRd, S(O)2Rb, o S(O)2NRcRd; R3 y R4 son cada uno, en forma independiente H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo, cicloalquilo COORa', CORb', SORb', o SO2Rb' en donde cada uno de dichos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo, o cicloalquilalquilo está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre halo, alquilo C1-4, haloalquilo C1-4, OH, alcoxi C1- 4, haloalcoxi C1-4, amino, alquilamino C1-4, dialquilamino C2-8, aminocarbonilo, alquilaminocarbonilo C1-4, dialquilaminocarbonilo C2-8, CN y NO2; o R3 y R4 junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre halo, alquilo C1-4, haloalquilo C1-4, OH, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4, dialquilamino C2-8, aminocarbonilo, alquilaminocarbonilo C1-4 y dialquilaminocarbonilo C2-8; Ra y Ra' son cada uno, en forma independiente H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo; Rb y Rb' son cada uno, en forma independiente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, y Rc y Rd son cada uno, en forma independiente H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, arilalquilo, o cicloalquilalquilo; o Rc y Rd junto con el átomo de N al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; con la salvedad de que cuando D7 es N, E es O o S, y G es N; entonces -W1-W2-W3-W4 es distinto de H.
ARP060104186A 2005-09-22 2006-09-25 Azepinas inhibidoras de quinasas janus AR058067A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US71946205P 2005-09-22 2005-09-22
US81049006P 2006-06-02 2006-06-02

Publications (1)

Publication Number Publication Date
AR058067A1 true AR058067A1 (es) 2008-01-23

Family

ID=37747347

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060104186A AR058067A1 (es) 2005-09-22 2006-09-25 Azepinas inhibidoras de quinasas janus

Country Status (7)

Country Link
US (4) US20070149506A1 (es)
EP (2) EP1926735A1 (es)
JP (1) JP5119154B2 (es)
AR (1) AR058067A1 (es)
CA (1) CA2621261C (es)
TW (1) TWI406865B (es)
WO (1) WO2007038215A1 (es)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
EP1926735A1 (en) 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
PT1951684T (pt) * 2005-11-01 2016-10-13 Targegen Inc Inibidores de cinases de tipo biaril-meta-pirimidina
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CN103214483B (zh) 2005-12-13 2014-12-17 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2，3-b]吡啶和吡咯并[2，3-b]嘧啶
US20070248961A1 (en) * 2006-04-20 2007-10-25 Maher Albitar Methods for detecting mutations in JAK2 nucleic acid
AU2007322033B2 (en) 2006-11-20 2013-07-11 President And Fellows Of Harvard College Methods, compositions, and kits for treating pain and pruritis
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
KR101549876B1 (ko) 2007-06-13 2015-09-03 인사이트 코포레이션 야누스 키나제 억제제（Ｒ）―３―（４―（７Ｈ―피롤로［２，３－ｄ］피리미딘―4―일）―1Ｈ―피라졸―1―일）―３―사이클로펜틸프로판니트릴의 염
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
US20090123920A1 (en) * 2007-11-08 2009-05-14 Maher Albitar Jak2 mutations
KR101580482B1 (ko) * 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 ４－피라졸릴－ｎ－아릴피리미딘－２－아민 및 ４－피라졸릴－ｎ－헤테로아릴피리미딘－２－아민
JP5275371B2 (ja) 2008-03-11 2013-08-28 インサイト・コーポレイション Ｊａｋ阻害剤としてのアゼチジン誘導体およびシクロブタン誘導体
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
US8512948B2 (en) 2008-10-31 2013-08-20 Quest Diagnostics Investments Incorporated Compositions and methods for detecting mutations in JAK2 nucleic acid
US20100112571A1 (en) * 2008-10-31 2010-05-06 Quest Diagnostics Investments Incorporated Compositions and methods for detecting mutations in jak2 nucleic acid
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2414360A1 (en) 2009-03-31 2012-02-08 ArQule, Inc. Substituted dipyrido-pyrimido-diazepine and benzo-pyrido-pyrimido compounds
TW201103939A (en) 2009-03-31 2011-02-01 Arqule Inc Substituted tetrahydropyrazolo-pyrido-azepine compounds
AR076794A1 (es) * 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
RS59632B1 (sr) * 2009-05-22 2020-01-31 Incyte Holdings Corp 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori
AU2010271269B2 (en) 2009-07-10 2016-09-08 Childrens' Medical Center Corporation Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
US9249145B2 (en) * 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
BR112012008267B1 (pt) 2009-10-09 2022-10-04 Incyte Holdings Corporation Derivados hidroxila, ceto e glucuronida de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1- il)-3-ciclopentilpropanonitrila
AU2011217961B2 (en) * 2010-02-18 2016-05-05 Incyte Holdings Corporation Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors
TWI766281B (zh) 2010-03-10 2022-06-01 美商英塞特控股公司 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
US20120196899A1 (en) * 2010-09-17 2012-08-02 Rock Creek Pharmaceuticals, Inc. Methods and products for treating inflammation
US20120245202A1 (en) * 2010-09-17 2012-09-27 Rock Creek Pharmaceuticals, Inc. Methods and products for treating inflammation
US8569331B2 (en) 2010-11-01 2013-10-29 Arqule, Inc. Substituted benzo[f]lmidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
WO2012099968A1 (en) * 2011-01-19 2012-07-26 The Trustees Of The University Of Pennsylvania Compositions and methods for treating skin cancer associated diseases
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
RU2466132C1 (ru) * 2011-03-09 2012-11-10 Автономная некоммерческая организация "Научно-исследовательский центр биотехнологии антибиотиков и других биологических активных веществ "БИОАН" ИНГИБИТОР PIM1-КИНАЗЫ 6-[(4-МЕТИЛ-1-1-ПИПЕРАЗИНИЛ)МЕТИЛ]-ИНДОЛО[1',7':1,2,3]ПИРРОЛО[3',4':6,7]АЗЕПИНО[4,5-b]ИНДОЛ-1,3(2Н, 10Н)-ДИОН, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ
WO2012144661A1 (en) 2011-04-20 2012-10-26 Shionogi & Co., Ltd. Aromatic heterocyclic derivative having trpv4-inhibiting activity
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
JP2014521725A (ja) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013082476A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
TWI638802B (zh) * 2012-05-24 2018-10-21 芬蘭商奧利安公司 兒茶酚ｏ－甲基轉移酶活性抑制化合物
UA117572C2 (uk) 2012-11-01 2018-08-27 Інсайт Холдинґс Корпорейшн Трициклічні конденсовані похідні тіофену як інгібітори jak
SG10202111768XA (en) 2012-11-15 2021-11-29 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
WO2014085154A1 (en) 2012-11-27 2014-06-05 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
LT2964650T (lt) 2013-03-06 2019-04-25 Incyte Holdings Corporation Būdai ir tarpiniai junginiai, skirti jak inhibitoriaus gamybai
SI3030227T1 (sl) 2013-08-07 2020-08-31 Incyte Corporation Dozirne oblike s podaljšanim sproščanjem za inhibitor JAK1
TW201601632A (zh) 2013-11-20 2016-01-16 杜邦股份有限公司 １－芳基－３－烷基吡唑殺蟲劑
JP2017514832A (ja) 2014-04-30 2017-06-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ１抑制剤を調製する方法及びその新しい形態
CA2974960A1 (en) * 2014-05-09 2015-11-12 Pimera, Inc. Novel quinoline compounds and uses thereof
US9758518B2 (en) 2015-03-04 2017-09-12 Pimera, Inc. Compositions, uses and methods for making them
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
GB2535427A (en) 2014-11-07 2016-08-24 Nicoventures Holdings Ltd Solution
WO2017024037A1 (en) 2015-08-03 2017-02-09 President And Fellows Of Harvard College Charged ion channel blockers and methods for use
WO2018183540A1 (en) 2017-03-28 2018-10-04 Pimera, Inc. Novel crystal forms of a pol1 inhibitor
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MX2020007973A (es) 2018-01-30 2020-12-07 Incyte Corp Procesos para preparar (1-(3-fluoro-2-(trifluorometil)isonicotinil )piperidin-4-ona).
PE20212186A1 (es) 2018-02-16 2021-11-11 Incyte Corp Inhibidores de la via de jak1 para el tratamiento de trastornos relacionados con citoquinas
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
UA127925C2 (uk) 2018-03-30 2024-02-14 Інсайт Корпорейшн Лікування гнійного гідраденіту з використанням інгібіторів jak
KR20210018218A (ko) 2018-04-13 2021-02-17 인사이트 코포레이션 이식편대숙주질환용 바이오마커
WO2020092726A1 (en) 2018-10-31 2020-05-07 Incyte Corporation Combination therapy for treatment of hematological diseases
MX2021010869A (es) 2019-03-11 2022-01-19 Nocion Therapeutics Inc Bloqueadores de canales iónicos sustituidos por éster y métodos para su uso.
CA3129117A1 (en) 2019-03-11 2020-09-17 Bridget Mccarthy Cole Charged ion channel blockers and methods for use
US10934263B2 (en) 2019-03-11 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10780083B1 (en) 2019-03-11 2020-09-22 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US10828287B2 (en) 2019-03-11 2020-11-10 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
CA3155586A1 (en) 2019-11-06 2021-05-14 Bridget M. Cole Charged ion channel blockers and methods for use
US10933055B1 (en) 2019-11-06 2021-03-02 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
EP4061367A1 (en) 2019-11-22 2022-09-28 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
EP4118070A4 (en) 2020-03-11 2024-04-10 Nocion Therapeutics, Inc. CHARGED ION CHANNEL BLOCKERS AND METHODS OF USE
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11957661B2 (en) 2020-12-08 2024-04-16 Incyte Corporation JAK1 pathway inhibitors for the treatment of vitiligo

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4105128A (en) * 1976-08-16 1978-08-08 Buckeye International, Inc. Wear surface arrangement for coupler carrier assembly
US4344541A (en) * 1977-08-26 1982-08-17 Holland Company Coupler carrier arrangement for railroad cars
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US4445618A (en) * 1981-12-30 1984-05-01 Midland-Ross Corporation Spring biased rotary railway car coupler carrier
US4706826A (en) * 1985-04-22 1987-11-17 Mcconway & Torley Corporation Striker carrier having an adjustable wear plate for a railway coupler
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
DE69618959T2 (de) 1995-07-05 2002-08-29 E.I. Du Pont De Nemours And Co., Wilmington Pyrimidone und ihre verwendug als fungizide
CA2295620A1 (en) * 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-heteroaryl-dipyrido¬2,3-b:3',2'-f|azepines and their use in the prevention or treatment of hiv infection
TR200100189T2 (tr) 1998-06-04 2001-05-21 Abbott Laboratories Hücre yapışması engelleyici iltihaplanmaya karşı bileşikler
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
TW505646B (en) 1998-06-19 2002-10-11 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
PL354998A1 (en) 1999-07-28 2004-03-22 Aventis Pharmaceuticals Products Inc. Substituted oxoazaheterocyclyl compounds
PL218519B1 (pl) 1999-12-10 2014-12-31 Pfizer Prod Inc Związki pirolo [2,3-d] pirymidynowe, środek farmaceutyczny zawierający te związki oraz ich zastosowanie
EP1263759B1 (en) * 1999-12-24 2010-09-08 Aventis Pharma Limited Azaindoles
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7235551B2 (en) * 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
EP1295607B9 (en) * 2000-06-23 2011-10-05 Mitsubishi Tanabe Pharma Corporation Antitumor effect potentiators
SK17342002A3 (sk) 2000-06-26 2004-06-08 Pfizer Products Inc. Derivát pyrolo[2,3-d]pyrimidínu ako činidlo potlačujúce imunitu
DE60105023T2 (de) 2000-06-28 2005-08-18 Smithkline Beecham P.L.C., Brentford Nassvermahlungsverfahren
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
JP2004528295A (ja) 2001-01-30 2004-09-16 サイトピア ピーティワイ リミテッド キナーゼ阻害方法
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
JP4286134B2 (ja) * 2001-08-01 2009-06-24 メルク エンド カムパニー インコーポレーテッド ベンズイミダゾ［４，５−ｆ］イソキノリノン誘導体
ATE420879T1 (de) 2001-09-19 2009-01-15 Aventis Pharma Sa Indolizine als kinaseproteinhemmer
ATE335490T1 (de) 2001-10-30 2006-09-15 Novartis Pharma Gmbh Staurosporin-derivate als hemmer der flt3- rezeptor-tyrosinkinase-wirkung
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
EP1572213A1 (en) 2002-11-26 2005-09-14 Pfizer Products Inc. Method of treatment of transplant rejection
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
AU2004212421B2 (en) 2003-02-07 2009-08-20 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
PL1678166T3 (pl) 2003-10-14 2009-12-31 Univ Arizona Inhibitory kinaz białkowych
CA2545192A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
CN1893952A (zh) 2003-12-17 2007-01-10 辉瑞产品公司 用于治疗移植排斥的吡咯并[2,3－d]嘧啶化合物
US20050239806A1 (en) * 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
US7507826B2 (en) 2004-03-30 2009-03-24 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
CA2563569A1 (en) 2004-05-03 2005-11-10 Novartis Ag Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
BRPI0518152A (pt) * 2004-10-13 2008-11-04 Hoffmann La Roche pirazolbenzodiazepinas dissubstituìdas úteis como inibidores para cdk2 e angiogênese e para o tratamento de cánceres de mama, cólon, pulmão e próstata
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
CA2586605A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
MX2007009429A (es) 2005-02-03 2008-03-18 Vertex Pharma Pirrolopirimidinas utiles como inhibidores de proteinas cinasas.
AU2006239236A1 (en) 2005-04-28 2006-11-02 Supergen, Inc. Protein kinase inhibitors
CN101228161B (zh) 2005-05-20 2012-10-10 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的吡咯并吡啶类
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP1926735A1 (en) * 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
SG151327A1 (en) 2005-09-30 2009-04-30 Vertex Pharmaceuticals Incopor Deazapurines useful as inhibitors of janus kinases
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
CN103214483B (zh) * 2005-12-13 2014-12-17 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2，3-b]吡啶和吡咯并[2，3-b]嘧啶
JP2009521504A (ja) 2005-12-22 2009-06-04 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性阻害剤
AU2007207533B8 (en) 2006-01-17 2012-06-28 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of Janus kinases
CA2648250A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases

Also Published As

Publication number Publication date
WO2007038215A1 (en) 2007-04-05
US20090197869A1 (en) 2009-08-06
EP2270014A1 (en) 2011-01-05
JP2009508968A (ja) 2009-03-05
US8563541B2 (en) 2013-10-22
US8835423B2 (en) 2014-09-16
TWI406865B (zh) 2013-09-01
US20070149506A1 (en) 2007-06-28
EP1926735A1 (en) 2008-06-04
US20140031344A1 (en) 2014-01-30
TW200804391A (en) 2008-01-16
CA2621261A1 (en) 2007-04-05
CA2621261C (en) 2014-05-20
JP5119154B2 (ja) 2013-01-16
US20120329782A1 (en) 2012-12-27

Similar Documents

Publication Publication Date Title
AR058067A1 (es) Azepinas inhibidoras de quinasas janus
AR057712A1 (es) Dihidropteridinonas en el tratamiento de enfermedades respiratorias
AR057965A1 (es) Compuestos de lactama y metodos de uso de los mismos
AR034119A1 (es) Compuestos de 5-alquilpirido pirimidinas, composicion farmaceutica, uso para prepararla y metodo para inhibir cinasas con dichos compuestos
AR051735A1 (es) Inhibidores pirrolicos de la proteina quinasa erk, sintesis e intermediarios de los mismos.
AR039341A1 (es) Derivados de 2,6-quinolinilo y 2,6-naftilo, procesos para su preparacion y sus usos
ES2561507T3 (es) Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus
AR041066A1 (es) 2,5-dioxoimidazolidin-4-il-acetamidas y analogos como inhibidores de la metaloproteinasa mmp12
AR056470A1 (es) Sulfonamidos n- ciclicos puenteados inhibidores de gamma secretasa
EA200700441A1 (ru) НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB
AR078012A1 (es) Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
AR085903A1 (es) Compuestos de pirazol sustituidos con halogeno
AR039649A1 (es) Compuestos de pirrolo-triazina anilina utiles como inhibidores de cinasa y las composiciones farmaceuticas que las contienen
DE602006015963D1 (de) Immunstimulatorisches verfahren
DK1805192T3 (da) Salte af isophosphoramidsennep og analoger deraf som antitumor-midler
AR060438A1 (es) 2-(piridin-2-il) - pirimidinas como fungicidas.
AR073043A1 (es) Compuestos de azetidinas polisustituidos, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos en el tratamiento de enfermedades respiratorias, metabolicas y del sistema nervioso central, entre otras.
CO5080791A1 (es) Derivados de la piperidina que tienen efectos sobre sistemas con serotonina
AR027296A1 (es) Derivados de 4-heteroaril-1,4-diazabiciclo[3.2.2]nonano, su preparacion y su aplicacion terapeutica
DK1970372T3 (da) Salte af 9-oxoacridin-10-eddikesyre med 1-alkylamino-1-deoxy-polyoler
ZA200803206B (en) Crystalline forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid
AR057823A1 (es) Compuestos quimicos derivados de quinazolina, un metodo para su preparacion y composicion farmaceutica
RU2018115718A (ru) Терапевтические соединения и способы их применения
AR043179A1 (es) Derivados sustituidos de 3-(benzoilureido)-tiofeno, procedimientos para su preparacion y su uso
ITMI20042231A1 (it) Cefdinir sale d'ammonio in forma cristallina

Legal Events

Date Code Title Description
FA Abandonment or withdrawal