ECSP13012703A - Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak - Google Patents

Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak

Info

Publication number
ECSP13012703A
ECSP13012703A ECSP13012703A ECSP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A EC SP13012703 A ECSP13012703 A EC SP13012703A
Authority
EC
Ecuador
Prior art keywords
cyclobutyl
pyrrolopyridine
derivatives substituted
jak inhibitors
pyrrolopyrimidine derivatives
Prior art date
Application number
Other languages
English (en)
Inventor
Joseph Glenn
James D Rodgers
Wenyu Zhu
Lixin Shao
Stacey Shepard
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 ECSP13012703A publication Critical patent/ECSP13012703A/es

Links

Classifications

    • 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
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/90Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • 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
    • 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
    • A61P5/10Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Wood Science & Technology (AREA)
  • Plant Pathology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Dentistry (AREA)
  • Pest Control & Pesticides (AREA)
  • Agronomy & Crop Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

La presente invención provee pirrolopirimidinas y pirrolopiridinas sustituidas con ciclobutilo de la fórmula I:en donde X, Y, Z, L, A, R5, n y m se definen con anterioridad, así como sus composiciones y métodos de uso que modulan la actividad de Janus quinasas (JAKs) y son de utilidad en el tratamiento de enfermedades relacionadas con la actividad de JAKs que incluyen, por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer y otras enfermedades.
ECSP13012703 2010-11-19 2013-06-19 Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak ECSP13012703A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41570510P 2010-11-19 2010-11-19

Publications (1)

Publication Number Publication Date
ECSP13012703A true ECSP13012703A (es) 2013-08-30

Family

ID=45094278

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012703 ECSP13012703A (es) 2010-11-19 2013-06-19 Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak

Country Status (22)

Country Link
US (3) US8933085B2 (es)
EP (1) EP2640723A1 (es)
JP (1) JP5917545B2 (es)
KR (1) KR20140019300A (es)
CN (1) CN103415515B (es)
AR (1) AR083933A1 (es)
AU (1) AU2011329734B2 (es)
BR (1) BR112013012502A2 (es)
CA (1) CA2818542A1 (es)
CL (1) CL2013001412A1 (es)
CO (1) CO6761386A2 (es)
CR (1) CR20130280A (es)
EA (1) EA026201B1 (es)
EC (1) ECSP13012703A (es)
IL (1) IL226407A (es)
MX (1) MX344478B (es)
NZ (1) NZ611151A (es)
PE (1) PE20140146A1 (es)
SG (1) SG190839A1 (es)
TW (1) TW201249845A (es)
UA (1) UA113156C2 (es)
WO (1) WO2012068450A1 (es)

Families Citing this family (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
LT2432472T (lt) * 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
SI2448938T1 (sl) 2009-06-29 2014-08-29 Incyte Corporation Experimental Station Pirimidinoni kot zaviralci pi3k
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
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
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
ES2764848T3 (es) 2010-12-20 2020-06-04 Incyte Holdings Corp N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
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
PL2753606T3 (pl) * 2011-09-02 2018-02-28 Purdue Pharma L.P. Pirymidyny jako blokery kanałów sodowych
HUE030869T2 (en) 2011-09-02 2017-06-28 Incyte Holdings Corp Heterocyclic amines as inhibitors of PI3K
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2013173720A1 (en) * 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
WO2014076127A1 (en) 2012-11-16 2014-05-22 F. Hoffmann-La Roche Ag Process for the preparation of 2-trifluoromethyl isonicotinic acid and esters
WO2014110574A1 (en) 2013-01-14 2014-07-17 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
US20160123982A1 (en) 2013-02-04 2016-05-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
TWI719401B (zh) 2013-05-17 2021-02-21 美商英塞特公司 作為jak抑制劑之聯吡唑衍生物
PT3030227T (pt) 2013-08-07 2020-06-25 Incyte Corp Formas de dosagem de libertação prolongada para um inibidor de jak1
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
PE20160532A1 (es) 2013-08-23 2016-05-21 Incyte Corp Compuesto de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim
CN104804001B9 (zh) * 2014-01-24 2022-02-08 江苏柯菲平医药股份有限公司 4-取代吡咯并[2,3-d]嘧啶化合物及其用途
EA201691745A1 (ru) 2014-02-28 2016-12-30 Инсайт Корпорейшн Ингибиторы jak1 для лечения миелодиспластических синдромов
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
WO2015168246A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
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
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
MA40240B1 (fr) 2014-06-19 2019-03-29 Ariad Pharma Inc Composés hétéroaryle d'inhibition de la kinase
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
HUE053595T2 (hu) * 2014-09-08 2021-07-28 Janssen Sciences Ireland Unlimited Co Pirrolopirimidinek influenzavírus-fertõzésnél történõ alkalmazásra
WO2016130501A1 (en) 2015-02-09 2016-08-18 Incyte Corporation Aza-heteroaryl compounds as pi3k-gamma inhibitors
TWI748941B (zh) 2015-02-27 2021-12-11 美商英塞特公司 Pi3k抑制劑之鹽及製備方法
ES2872553T3 (es) 2015-03-06 2021-11-02 Pharmakea Inc Inhibidores de lisil oxidasa tipo-2 y usos de los mismos
CA2977947A1 (en) 2015-03-06 2016-09-15 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
CA2995430C (en) * 2015-09-25 2023-07-11 Dizal (Jiangsu) Pharmaceutical Co., Limited Compounds and methods for inhibiting jak
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
MA43169B1 (fr) 2015-11-06 2022-05-31 Incyte Corp Composés héterocycliques en tant qu' inhibiteurs pi3k-gamma
EP3400221B1 (en) 2016-01-05 2020-08-26 Incyte Corporation Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors
RS65129B1 (sr) 2016-03-28 2024-02-29 Incyte Corp Jedinjenja pirolotriazina kao inhibitori tam
TW201803871A (zh) 2016-06-24 2018-02-01 英塞特公司 作為PI3K-γ抑制劑之雜環化合物
SI3484875T1 (sl) * 2016-07-14 2021-08-31 Eli Lilly And Company Derivati pirazolilaminobenzimidazola kot zaviralci JAK
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
BR112019004517A2 (pt) 2016-09-07 2019-08-13 Pharmakea Inc formas cristalinas de um inibidor lisil-oxidase-semelhante 2 e métodos de preparação
EP4052707A1 (en) * 2016-09-07 2022-09-07 Pharmakea, Inc. Uses of a lysyl oxidase-like 2 inhibitor
CA3031585A1 (en) 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
WO2018189335A1 (en) 2017-04-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
EP3988552A1 (en) 2017-09-27 2022-04-27 Incyte Corporation Salts of pyrrolotriazine derivatives useful as tam inhibitors
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
AU2018360577A1 (en) 2017-11-01 2020-06-18 Bristol-Myers Squibb Company Bridged bicyclic compounds as farnesoid X receptor modulators
CN111566095B (zh) 2017-11-03 2024-09-27 阿克拉瑞斯治疗股份有限公司 被取代的吡咯并吡啶jak抑制剂及其制造方法和使用方法
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR20200129099A (ko) * 2018-01-30 2020-11-17 인사이트 코포레이션 (1-(3-플루오로-2-(트리플루오로메틸)이소니코티닐)피페리딘-4-온)의 제조 방법
IL276725B2 (en) 2018-02-16 2024-09-01 Incyte Corp JAK1 pathway inhibitors for the treatment of cytokine-related disorders
CN112423759A (zh) * 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
JP7565798B2 (ja) 2018-03-30 2024-10-11 インサイト・コーポレイション 炎症性皮膚疾患のバイオマーカー
SG11202010092XA (en) 2018-04-13 2020-11-27 Incyte Corp Biomarkers for graft-versus-host disease
AU2019269372A1 (en) 2018-05-14 2020-11-26 Takeda Pharmaceutical Company Limited Pharmaceutical salts of pyrimidine derivatives and method of treating disorders
MA52761A (fr) 2018-06-01 2021-04-14 Incyte Corp Schéma posologique destiné au traitement de troubles liés à la pi3k
AU2019293618A1 (en) 2018-06-29 2021-02-18 Incyte Corporation Formulations of an AXL/MER inhibitor
AU2019317625A1 (en) 2018-08-10 2021-02-18 Aclaris Therapeutics, Inc. Pyrrolopyrimidine ITK inhibitors
JP2021535182A (ja) 2018-09-05 2021-12-16 インサイト・コーポレイションIncyte Corporation ホスホイノシチド3−キナーゼ(pi3k)阻害剤の結晶形態
TW202023386A (zh) 2018-09-13 2020-07-01 瑞士商先正達合夥公司 殺有害生物活性唑-醯胺化合物
JP7431845B2 (ja) 2018-10-31 2024-02-15 インサイト・コーポレイション 血液疾患の治療のための併用療法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
CN113692278A (zh) 2018-12-19 2021-11-23 因赛特公司 用于治疗胃肠道疾病的jak1途径抑制剂
MA55201A (fr) 2019-03-05 2022-01-12 Incyte Corp Inhibiteurs de la voie jak1 pour le traitement d'un dysfonctionnement chronique de l'allogreffe pulmonaire
JP2022526301A (ja) 2019-03-19 2022-05-24 インサイト・コーポレイション 尋常性白斑のバイオマーカー
EP3962897A4 (en) 2019-05-02 2022-12-14 Aclaris Therapeutics, Inc. SUBSTITUTED PYRROLOPYRIDINES AS JAK INHIBITORS
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
WO2021102258A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
US11685731B2 (en) 2020-06-02 2023-06-27 Incyte Corporation Processes of preparing a JAK1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN116057045A (zh) 2020-06-05 2023-05-02 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
TW202212341A (zh) 2020-08-18 2022-04-01 美商英塞特公司 製備jak1抑制劑之方法及中間體
KR20230128472A (ko) 2020-12-04 2023-09-05 인사이트 코포레이션 피부 질환의 치료를 위한 비타민 d 유사체를 함유하는jak 억제제
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
US11918581B2 (en) 2021-01-11 2024-03-05 Incyte Corporation Combination therapy comprising JAK pathway inhibitor and rock inhibitor
CA3219092A1 (en) 2021-05-03 2022-11-10 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
EP4174077A1 (en) * 2021-10-27 2023-05-03 Merck Patent GmbH Electronic switching device
TW202419088A (zh) 2022-08-05 2024-05-16 美商英塞特公司 使用jak抑制劑之蕁麻疹治療
US20240307353A1 (en) 2023-03-16 2024-09-19 Incyte Corporation Jak1 pathway inhibitors for the treatment of asthma

Family Cites Families (291)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
US3832460A (en) 1971-03-19 1974-08-27 C Kosti Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue
US4140755A (en) 1976-02-13 1979-02-20 Hoffmann-La Roche Inc. Sustained release tablet formulations
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
DE3220113A1 (de) 1982-05-28 1983-12-01 Basf Ag, 6700 Ludwigshafen Difluormethoxiphenylthiophosphorsaeureester
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4548990A (en) 1983-08-15 1985-10-22 Ciba-Geigy Corporation Crosslinked, porous polymers for controlled drug delivery
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
US4921947A (en) 1986-03-31 1990-05-01 Eli Lilly And Company Process for preparing macrolide derivatives
US5378700A (en) 1989-10-11 1995-01-03 Teijin Limited Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
IT1258781B (it) 1992-01-16 1996-02-29 Zambon Spa Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (fr) 1992-08-27 1994-11-10 Sanofi Elf Dérivés d'acide thiényl ou pyrrolyl carboxyliques, leur préparation et médicaments les contenant.
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
JPH0710876A (ja) 1993-06-24 1995-01-13 Teijin Ltd 4位に環状アミノ基を有するピロロ[2,3―d]ピリミジン
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
MX9800136A (es) 1995-07-05 1998-03-29 Du Pont Pirimidinonas fungicidas.
CA2224435C (en) 1995-07-06 2008-08-05 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
CA2250232A1 (en) 1996-04-03 1997-10-09 Allen I. Oliff A method of treating cancer
AU2802297A (en) 1996-04-18 1997-11-07 Merck & Co., Inc. A method of treating cancer
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
EP0934270A1 (en) 1996-05-30 1999-08-11 Merck & Co., Inc. A method of treating cancer
US6624138B1 (en) 2001-09-27 2003-09-23 Gp Medical Drug-loaded biological material chemically treated with genipin
WO1998044797A1 (en) 1997-04-07 1998-10-15 Merck & Co., Inc. A method of treating cancer
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
JP2001513502A (ja) 1997-08-11 2001-09-04 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 5,6−ヘテロアリールジピリド[2,3−b:3’,2’−f]アゼピン類及びHIV感染の予防及び治療におけるそれらの使用
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
US6025366A (en) 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
BR9910864A (pt) 1998-06-04 2002-02-05 Abbott Lab Compostos anti-inflamatórios para inibição de aderência celular
JP4666762B2 (ja) 1998-06-19 2011-04-06 ファイザー・プロダクツ・インク ピロロ[2.3−d]ピリミジン化合物
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
JP2000119271A (ja) 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h―イミダゾピリジン誘導体
JP5026635B2 (ja) 1998-09-10 2012-09-12 ニュコメデ ダンマルク アンパーツセルスカブ 医薬物質の迅速放出医薬組成物
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
EP1165084A4 (en) 1999-03-03 2002-05-15 Merck & Co Inc PRENYL PROTEIN TRANSFERASES INHIBITORS
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6217895B1 (en) 1999-03-22 2001-04-17 Control Delivery Systems Method for treating and/or preventing retinal diseases with sustained release corticosteroids
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
WO2000063168A1 (en) 1999-04-16 2000-10-26 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
ATE275141T1 (de) 1999-10-13 2004-09-15 Banyu Pharma Co Ltd Substituierte imidazolin-derivate
KR100477818B1 (ko) 1999-12-10 2005-03-22 화이자 프로덕츠 인코포레이티드 피롤로[2,3-d] 피리미딘 화합물
OA12514A (en) 1999-12-24 2006-05-29 Aventis Pharma Ltd 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
ES2206363T3 (es) 2000-04-07 2004-05-16 Laboratoire Medidom S.A. Formulaciones oftalmicas a base de ciclosporina, de acido hialuronico y de polisorbato.
AU4878601A (en) 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
SI2223922T1 (sl) 2000-04-25 2016-04-29 Icos Corporation Inhibitorji humane fosfatidil-inositol 3-kinazne delta izoforme
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
JP4954426B2 (ja) 2000-06-16 2012-06-13 キュリス,インコーポレイテッド 血管形成調節組成物及び利用
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
AU2001274598A1 (en) 2000-06-23 2002-01-02 Mitsubishi Pharma Corporation Antitumor effect potentiators
PT1294724E (pt) 2000-06-26 2006-07-31 Pfizer Prod Inc Compostos pirrolo (2,3-d ) pirimidina como agentes imunosupressivos
CZ303572B6 (cs) 2000-06-28 2012-12-12 Smithkline Beecham P. L. C. Jemne rozmelnený prostredek a zpusob jeho prípravy
AU2001278790A1 (en) 2000-08-22 2002-03-04 Hokuriku Seiyaku Co. Ltd 1h-imidazopyridine derivatives
AU2002228783A1 (en) 2000-12-05 2002-06-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
WO2002055496A1 (en) 2001-01-15 2002-07-18 Glaxo Group Limited Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression
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
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003011285A1 (en) 2001-08-01 2003-02-13 Merck & Co., Inc. BENZIMIDAZO[4,5-f]ISOQUINOLINONE DERIVATIVES
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
US6429231B1 (en) 2001-09-24 2002-08-06 Bradley Pharmaceuticals, Inc. Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
CA2462657C (en) 2001-10-30 2011-04-26 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
WO2003048111A1 (en) 2001-11-30 2003-06-12 Teijin Limited Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of ERK2 and uses thereof
US7125888B2 (en) 2002-05-02 2006-10-24 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2484632C (en) 2002-05-07 2012-12-11 Control Delivery Systems, Inc. Processes for forming a drug delivery device
CA2486183C (en) 2002-05-23 2012-01-10 Cytopia Pty Ltd. Protein kinase inhibitors
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
WO2004003026A1 (ja) 2002-06-26 2004-01-08 Idemitsu Kosan Co., Ltd. 共重合体水素添加物、その製造方法及びそれを用いたホットメルト接着剤組成物
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
US20060004010A1 (en) 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
AU2003278727A1 (en) 2002-09-20 2004-04-08 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
JP4688498B2 (ja) 2002-11-04 2011-05-25 バーテックス ファーマシューティカルズ インコーポレイテッド Jakインヒビターとしてのヘテロアリール−ピリミジン誘導体
US8034831B2 (en) 2002-11-06 2011-10-11 Celgene Corporation Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies
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
US20040099204A1 (en) 2002-11-25 2004-05-27 Nestor John J. Sheet, page, line, position marker
JP2006509000A (ja) 2002-11-26 2006-03-16 ファイザー・プロダクツ・インク 移植片拒絶反応の処置の方法
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
TWI335819B (en) 2002-12-24 2011-01-11 Alcon Inc Use of oculosurface selective glucocorticoid in the treatment of dry eye
TW200418806A (en) 2003-01-13 2004-10-01 Fujisawa Pharmaceutical Co HDAC inhibitor
US7167750B2 (en) 2003-02-03 2007-01-23 Enteromedics, Inc. Obesity treatment with electrically induced vagal down regulation
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
CA2522595A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
FR2857454B1 (fr) 2003-07-08 2006-08-11 Aventis Pasteur Dosage des acides techoiques des bacteries gram+
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
WO2005020921A2 (en) 2003-08-29 2005-03-10 Exelixis, Inc. C-kit modulators and methods of use
US8084457B2 (en) 2003-09-15 2011-12-27 Lead Discovery Center Gmbh Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CA2543452C (en) 2003-10-24 2012-03-13 Santen Pharmaceutical Co., Ltd. Therapeutic agent for keratoconjunctival disorder
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005051393A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
EP1734967A2 (en) 2003-12-17 2006-12-27 Pfizer Products Incorporated Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
EP1696920B8 (en) 2003-12-19 2015-05-06 Plexxikon Inc. Compounds and methods for development of ret modulators
MXPA06007076A (es) 2003-12-19 2006-08-31 Pharmacopeia Drug Discovery Tiadiazoles como ligandos del receptor cxc y cc-quimiocina.
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
WO2005069865A2 (en) 2004-01-13 2005-08-04 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
EP1744751A4 (en) 2004-03-18 2010-03-10 Brigham & Womens Hospital TREATMENT OF SYNUCLEINOPATHIES
EP2332940B1 (en) 2004-03-30 2012-10-31 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
EP1740559B1 (en) 2004-04-20 2014-10-15 Merck Sharp & Dohme Corp. 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
JP2007536310A (ja) 2004-05-03 2007-12-13 ノバルティス アクチエンゲゼルシャフト S1p受容体アゴニストおよびjak3キナーゼ阻害剤を含む、組合せ剤
JP2007537296A (ja) 2004-05-14 2007-12-20 アボット・ラボラトリーズ 治療薬としてのキナーゼ阻害薬
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
RU2401265C2 (ru) 2004-06-10 2010-10-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
WO2006001463A1 (ja) 2004-06-23 2006-01-05 Ono Pharmaceutical Co., Ltd. S1p受容体結合能を有する化合物およびその用途
AU2005260689B2 (en) 2004-06-30 2012-05-10 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7138423B2 (en) 2004-07-20 2006-11-21 Bristol-Myers Squibb Company Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
FR2873691B1 (fr) 2004-07-29 2006-10-06 Sanofi Synthelabo Derives d'amino-piperidine, leur preparation et leur application en therapeutique
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
CN101006186A (zh) 2004-08-23 2007-07-25 财团法人牧岩生命工学研究所 用于检测sars冠状病毒的引物和探针,包括该引物和/或探针的试剂盒及其检测方法
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
ES2308551T3 (es) 2004-10-13 2008-12-01 F. Hoffmann-La Roche Ag Pirazolobenzodiazepinas disustituidas utiles como inhibidores para cdk2 y angiogenesis, y para el tratamiento de cancer de mama, colon, pulmon y prostata.
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
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
CA2586375A1 (en) 2004-11-04 2006-05-18 Juan-Miguel Jimenez Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
US20090156602A1 (en) 2004-11-24 2009-06-18 Nigel Graham Cooke Organic Compounds
US7517870B2 (en) 2004-12-03 2009-04-14 Fondazione Telethon Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
US20060128803A1 (en) 2004-12-14 2006-06-15 Alcon, Inc. Method of treating dry eye disorders using 13(S)-HODE and its analogs
WO2006067445A2 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Csf-1r kinase inhibitors
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.
JP2008528477A (ja) 2005-01-20 2008-07-31 ファイザー・リミテッド 化合物
MX2007009429A (es) 2005-02-03 2008-03-18 Vertex Pharma Pirrolopirimidinas utiles como inhibidores de proteinas cinasas.
US7683171B2 (en) 2005-02-04 2010-03-23 Bristol-Myers Squibb Company 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
MX2007011316A (es) 2005-03-15 2007-11-12 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
WO2006108103A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
EP2354140A1 (en) * 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
FR2889662B1 (fr) 2005-08-11 2011-01-14 Galderma Res & Dev Emulsion de type huile-dans-eau pour application topique en dermatologie
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
SG151327A1 (en) 2005-09-30 2009-04-30 Vertex Pharmaceuticals Incopor Deazapurines useful as inhibitors of janus kinases
WO2007044894A2 (en) 2005-10-11 2007-04-19 Chembridge Research Laboratories, Inc. Cell-free protein expression systems and methods of use thereof
DK1937664T3 (da) 2005-10-14 2011-07-18 Sumitomo Chemical Co Hydrazidforbindelse og pesticid anvendelse af den samme
EP2388259A1 (en) 2005-10-28 2011-11-23 AstraZeneca AB 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007062459A1 (en) 2005-11-29 2007-06-07 Cytopia Research Pty Ltd Selective kinase inhibitors based on pyridine scaffold
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
UA98449C2 (en) 2005-12-13 2012-05-25 Инсайт Корпорейшин Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
KR20080083680A (ko) 2005-12-23 2008-09-18 스미스클라인 비참 코포레이션 오로라 키나제의 아자인돌 억제제
JP4643455B2 (ja) 2006-01-12 2011-03-02 株式会社ユニバーサルエンターテインメント 遊技システム
RU2453548C2 (ru) 2006-01-17 2012-06-20 Вертекс Фармасьютикалз Инкорпорейтед Азаиндолы, полезные в качестве ингибиторов янус-киназ
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
JP2009525350A (ja) 2006-02-01 2009-07-09 スミスクライン ビーチャム コーポレーション Rafキナーゼ阻害薬として有用なピロロ[2,3,b]ピリジン誘導体
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
BRPI0708731A2 (pt) 2006-03-10 2011-06-07 Ono Pharmaceutical Co derivado heterocìclico nitrogenado, e agente farmacêutico compreendendo o derivado como ingrediente ativo
PL2003132T3 (pl) 2006-04-03 2014-10-31 Astellas Pharma Inc Pochodne oksadiazolu jako agoniści S1P1
CA2648250A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
EP2059515A2 (en) 2006-04-12 2009-05-20 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
CA2652751A1 (en) 2006-05-18 2007-11-29 Bayer Healthcare Ag Pharmaceutical compositions and methods of using same
US7691811B2 (en) 2006-05-25 2010-04-06 Bodor Nicholas S Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
TWI398252B (zh) 2006-05-26 2013-06-11 Novartis Ag 吡咯并嘧啶化合物及其用途
EP2044061A2 (en) 2006-07-20 2009-04-08 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008022164A2 (en) 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
AR062677A1 (es) 2006-09-08 2008-11-26 Novartis Ag Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
WO2008035376A2 (en) 2006-09-19 2008-03-27 Council Of Scientific & Industrial Research A novel bio-erodible insert for ophthalmic applications and a process for the preparation thereof
CL2007002866A1 (es) 2006-10-04 2008-07-04 Pharmacopeia Inc Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m
AR063141A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2- ( benzimidazolil ) purina 8- sustituida para inmunosupresion
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
SG176461A1 (en) 2006-11-06 2011-12-29 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20080119496A1 (en) 2006-11-16 2008-05-22 Pharmacopeia Drug Discovery, Inc. 7-Substituted Purine Derivatives for Immunosuppression
AU2007323725B2 (en) 2006-11-22 2014-02-20 Incyte Holdings Corporation Imidazotriazines and imidazopyrimidines as kinase inhibitors
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
NZ577111A (en) 2006-12-15 2012-05-25 Abbott Lab Novel oxadiazole compounds
AU2007338793B2 (en) 2006-12-20 2012-05-03 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
BRPI0720434A2 (pt) 2006-12-22 2014-01-07 Sigma Tau Ind Farmaceuti Gel útil para liberação de fármacos oftálmicos
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008106692A1 (en) 2007-03-01 2008-09-04 Novartis Vaccines And Diagnostics, Inc. Pim kinase inhibitors and methods of their use
UA101611C2 (ru) 2007-04-03 2013-04-25 Аррей Байофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ
US8188178B2 (en) 2007-05-07 2012-05-29 3M Innovative Properties Company Cold shrinkable article including an epichlorohydrin composition
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
JP5603770B2 (ja) 2007-05-31 2014-10-08 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 Ccr2受容体拮抗薬およびその使用
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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.
CN101743009A (zh) 2007-07-11 2010-06-16 辉瑞大药厂 治疗干眼病的药物组合物和方法
CA2695114A1 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
CA2743756A1 (en) 2007-11-15 2009-05-22 Musc Foundation For Research Development Inhibitors of pim protein kinases, compositions, and methods for treating cancer
MY152948A (en) 2007-11-16 2014-12-15 Incyte Corp 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
PL3133080T3 (pl) 2008-01-18 2018-12-31 Inst Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Nowe cytostatyczne nukleozydy 7-deazapurynowe
KR20100115789A (ko) 2008-02-04 2010-10-28 머큐리 테라퓨틱스, 인코포레이티드 Ampk 조절자
UY31679A1 (es) 2008-03-03 2009-09-30 Inhibidores de cinasa pim y metodos para su uso
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
KR101408517B1 (ko) 2008-03-21 2014-06-17 노파르티스 아게 신규한 헤테로시클릭 화합물 및 그의 용도
AU2009260389A1 (en) 2008-06-18 2009-12-23 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
BRPI0914630A2 (pt) 2008-06-26 2019-09-24 Anterios Inc liberação dérmica
TWI461423B (zh) 2008-07-02 2014-11-21 Astrazeneca Ab 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物
FR2933409B1 (fr) 2008-07-03 2010-08-27 Centre Nat Rech Scient NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
TWI496779B (zh) 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
BRPI0917459B1 (pt) 2008-08-20 2017-09-12 Zoetis Services Llc N-methyl-1- [trans-4- [methyl (7h-pyrrol [2,3-d] pyridol [2,3-d] pyrimidine compounds, use of these in therapy and crystalline a form of n-methyl- pyrimidin-4-yl) amino] cyclohexyl} methanosulphonamide
EP2342190A1 (en) 2008-09-02 2011-07-13 Novartis AG Bicyclic kinase inhibitors
MX2011002362A (es) 2008-09-02 2011-04-04 Novartis Ag Inhibidores heterociclicos de cinasa pim.
EP2344474B1 (en) 2008-09-02 2015-09-23 Novartis AG Picolinamide derivatives as kinase inhibitors
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.
WO2010043052A1 (en) 2008-10-17 2010-04-22 Merck Frosst Canada Ltd. Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
US20100197924A1 (en) 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
EP2210890A1 (en) 2009-01-19 2010-07-28 Almirall, S.A. Oxadiazole derivatives as S1P1 receptor agonists
US8263601B2 (en) 2009-02-27 2012-09-11 Concert Pharmaceuticals, Inc. Deuterium substituted xanthine derivatives
LT2432472T (lt) 2009-05-22 2020-02-10 Incyte Holdings Corporation 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai
BRPI1012159B1 (pt) 2009-05-22 2022-01-25 Incyte Holdings Corporation Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077465A1 (es) 2009-07-08 2011-08-31 Leo Pharma As Derivados de pirrolopirimidina como inhibidores de receptores jak y protein tirosin quinasas y uso farmaceutico de los mismos
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme INHIBITION OF JAK BLOCKES TOXICITIES ASSOCIATED WITH INTERFERENCE RNA
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
CN102625807B (zh) 2009-09-08 2016-03-09 霍夫曼-拉罗奇有限公司 4-取代的吡啶-3-基-甲酰胺化合物和使用方法
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
JP5946768B2 (ja) 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation 3−(4−(7H−ピロロ[2,3−d]ピリミジン−4−イル)−1H−ピラゾール−1−イル)−3−シクロペンチルプロパンニトリルのヒドロキシル、ケト及びグルクロニド誘導体
BR112012009327A2 (pt) 2009-10-20 2017-06-06 Cellzome Ltd análogos de heterociclil pirazolopirimidina como inibidores de jak
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
WO2011066374A2 (en) 2009-11-24 2011-06-03 Alder Biopharmaceuticals, Inc. Antagonists of il-6 to prevent or treat cachexia, weakness, fatigue, and/or fever
WO2011069141A2 (en) 2009-12-04 2011-06-09 Board Of Regents, The University Of Texas System Interferon therapies in combination with blockade of stat3 activation
TW201129565A (en) 2010-01-12 2011-09-01 Hoffmann La Roche Tricyclic heterocyclic compounds, compositions and methods of use thereof
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
CA2790070C (en) 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
AU2011224484A1 (en) 2010-03-10 2012-09-27 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
AU2011240808B2 (en) 2010-04-14 2015-01-22 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of JAK kinases
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
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
WO2011156698A2 (en) 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
US20130252917A1 (en) 2010-09-30 2013-09-26 Portola Pharmaceuticals, Inc. Combination therapy of 4-(3-(2h-1,2,3-triazo-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide and fludarabine
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CN103370068A (zh) 2010-12-03 2013-10-23 Ym生物科学澳大利亚私人有限公司 Jak-2 介导的病症的治疗
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
AR086983A1 (es) 2011-06-20 2014-02-05 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
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
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
EA201590272A1 (ru) 2012-07-27 2015-05-29 Рациофарм Гмбх Пероральные дозированные формы для модифицированного высвобождения, содержащие руксолитиниб
JP2015526520A (ja) 2012-08-31 2015-09-10 プリンシピア バイオファーマ インコーポレイテッド Itk阻害剤としてのベンズイミダゾール誘導体
MX2015005428A (es) 2012-11-01 2015-07-21 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak).
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
UA120162C2 (uk) 2013-03-06 2019-10-25 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки при отриманні інгібітора jak
TWI719401B (zh) 2013-05-17 2021-02-21 美商英塞特公司 作為jak抑制劑之聯吡唑衍生物
PT3030227T (pt) 2013-08-07 2020-06-25 Incyte Corp Formas de dosagem de libertação prolongada para um inibidor de jak1
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
EA201691745A1 (ru) 2014-02-28 2016-12-30 Инсайт Корпорейшн Ингибиторы jak1 для лечения миелодиспластических синдромов
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
WO2015168246A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
EP4233870A3 (en) 2014-05-28 2024-01-24 Onco Tracker, Inc. Anti-cancer effects of jak2 inhibitors in combination with thalidomide derivatives and glucocorticoids
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

Also Published As

Publication number Publication date
WO2012068450A1 (en) 2012-05-24
EA201390736A1 (ru) 2013-11-29
TW201249845A (en) 2012-12-16
MX2013005603A (es) 2013-06-13
US8933085B2 (en) 2015-01-13
JP5917545B2 (ja) 2016-05-18
CO6761386A2 (es) 2013-09-30
CN103415515B (zh) 2015-08-26
EP2640723A1 (en) 2013-09-25
JP2014500260A (ja) 2014-01-09
US20120149681A1 (en) 2012-06-14
AU2011329734A1 (en) 2013-05-02
KR20140019300A (ko) 2014-02-14
AU2011329734B2 (en) 2015-05-28
US10640506B2 (en) 2020-05-05
PE20140146A1 (es) 2014-02-06
IL226407A (en) 2017-04-30
SG190839A1 (en) 2013-07-31
MX344478B (es) 2016-12-16
CA2818542A1 (en) 2012-05-24
CN103415515A (zh) 2013-11-27
US20150087632A1 (en) 2015-03-26
IL226407A0 (en) 2013-07-31
UA113156C2 (xx) 2016-12-26
EA026201B1 (ru) 2017-03-31
CR20130280A (es) 2013-08-09
NZ611151A (en) 2015-06-26
US20190135813A1 (en) 2019-05-09
AR083933A1 (es) 2013-04-10
CL2013001412A1 (es) 2013-12-20
BR112013012502A2 (pt) 2019-03-06

Similar Documents

Publication Publication Date Title
ECSP13012703A (es) Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
ECSP12012218A (es) Derivados de piperidin-4-il azetidina como inhibidores de jak1
CL2012001073A1 (es) Compuestos derivados de pirido[4,3-d]pirimidin-5-ona, sus composiciones farmaceuticas y su uso como inhibidores de quinasa para tratar asma, epoc, colitis ulcerante, bronquitis, lupus, cancer de mamas, enfermedad de alzheimer, enfermedad de parkinson, osteoporosis, esclerosis multiple, diabetes, trastornos oculares, restenosis, enfermedades inflamatorias.
CR20150633A (es) Derivados del bipirazol como inhibidores jak
SV2016005209A (es) Acrilamidas de pirrolo(2,3-d)pirimidinilo, pirrolo(2,3-b)pirazinilo y pirrolo(2,3-d)piridinilo
BR112012020693A2 (pt) derivados de ciclobutano e metilciclobutano como inibidores de janus quinase
CR20150255A (es) Derivados triciclicos fusionados de tiofeno como inhibidores de jak
ECSP14013148A (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
CO6440524A2 (es) 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.
ECSP11011534A (es) 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octano- o heptano-nitrilo como inhibidores de jak
UY33503A (es) Imidazo [1,2-a]pirimidinas y piridinas sustituidas
ECSP12011855A (es) COMPUESTOS DE pIrrolo[2,3-d]pIrimidinA
NZ597050A (en) Pyrimidinones as pi3k inhibitors
CL2012002937A1 (es) Compuestos derivados de 1h-pirrolo[2,3-b]piridina o 7h-pirrolo[2,3-d]pirimidina sustituidos, moduladores de quinasa; composición farmacéutica; kit farmacéutico; método de preparación;y su uso para tratar artritis reumatoide, osteoporosis, alzheimer, cancer pancreatico, cancer de protata y mieloma multiple.
AU2014270524A8 (en) 2-phenylimidazo [1,2-a]pyrimidines as imaging agents
ECSP14013274A (es) Heterociclaminas como inhibidores de pi3k
DOP2010000270A (es) Derivados de azetidina y ciclobutano como inhibidores de jak
MX2014002442A (es) Inhibidores de pirrolopirazina cinasa.
PH12014502057A1 (en) Diacylglycerol acyltransferase 2 inhibitors
NZ596571A (en) Pyrazolopyrimidines and related heterocycles as kinase inhibitors
CR20110427A (es) Derivados de triazolo [4,3-b] piridazina y sus usos para el cáncer de próstata
MX2012002327A (es) Inhibidores de cinasa, formas de profarmaco de los mismos y su uso en terapia.
EA201101604A1 (ru) [1,2,4]триазоло[4,3-b]пиридазины в качестве лигандов андрогенового рецептора
PE20151940A1 (es) Derivados de triazina
ECSP15021681A (es) Derivados tricíclicos fusionados de tiofeno como inhibidores de jak