HRP20170090T1 - Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze - Google Patents

Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze Download PDF

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Publication number
HRP20170090T1
HRP20170090T1 HRP20170090TT HRP20170090T HRP20170090T1 HR P20170090 T1 HRP20170090 T1 HR P20170090T1 HR P20170090T T HRP20170090T T HR P20170090TT HR P20170090 T HRP20170090 T HR P20170090T HR P20170090 T1 HRP20170090 T1 HR P20170090T1
Authority
HR
Croatia
Prior art keywords
pyrrolo
pyridines
pyrimidines
kinase inhibitors
heteroaryl substituted
Prior art date
Application number
HRP20170090TT
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English (en)
Inventor
James D. Rodgers
Stacey Shepard
Thomas P. Maduskuie
Haisheng Wang
Nikoo Falahatpisheh
Maria Rafalski
Argyrios G. Arvanitis
Louis Storace
Ravi Kumar Jalluri
Jordan S. Fridman
Krishna Vaddi
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Incyte Holdings Corporation
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37903501&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20170090(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corporation filed Critical Incyte Holdings Corporation
Publication of HRP20170090T1 publication Critical patent/HRP20170090T1/hr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • C07D487/02—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 two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (1)

1. Upotreba spoja, koji je 3-ciklopentil-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]propionitril, ili njegove farmaceutski prihvatljive soli, naznačena time da je za pripremu lijeka za liječenje policitemije vera (PV).
HRP20170090TT 2005-12-13 2017-01-19 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze HRP20170090T1 (hr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US74990505P 2005-12-13 2005-12-13
US81023106P 2006-06-02 2006-06-02
US85062506P 2006-10-10 2006-10-10
US85687206P 2006-11-03 2006-11-03
US85940406P 2006-11-16 2006-11-16
EP11152730.5A EP2455382B1 (en) 2005-12-13 2006-12-12 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors

Publications (1)

Publication Number Publication Date
HRP20170090T1 true HRP20170090T1 (hr) 2017-03-24

Family

ID=37903501

Family Applications (7)

Application Number Title Priority Date Filing Date
HR20110903T HRP20110903T1 (hr) 2005-12-13 2011-12-01 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
HRP20150837TT HRP20150837T2 (hr) 2005-12-13 2015-08-06 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
HRP20160112TT HRP20160112T1 (hr) 2005-12-13 2016-02-02 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE
HRP20170090TT HRP20170090T1 (hr) 2005-12-13 2017-01-19 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
HRP20170162TT HRP20170162T1 (hr) 2005-12-13 2017-02-01 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE
HRP20170200TT HRP20170200T1 (hr) 2005-12-13 2017-02-07 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE
HRP20181912TT HRP20181912T1 (hr) 2005-12-13 2018-11-16 Derivati pirolo[2,3-d]pirimidina kao inhibitori janus kinaze

Family Applications Before (3)

Application Number Title Priority Date Filing Date
HR20110903T HRP20110903T1 (hr) 2005-12-13 2011-12-01 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
HRP20150837TT HRP20150837T2 (hr) 2005-12-13 2015-08-06 Heteroaril supstituirani pirolo[2,3-b]piridini i pirolo[2,3-b]pirimidini kao inhibitori janus kinaze
HRP20160112TT HRP20160112T1 (hr) 2005-12-13 2016-02-02 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE

Family Applications After (3)

Application Number Title Priority Date Filing Date
HRP20170162TT HRP20170162T1 (hr) 2005-12-13 2017-02-01 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE
HRP20170200TT HRP20170200T1 (hr) 2005-12-13 2017-02-07 HETEROARIL SUPSTITUIRANI PIROLO[2,3-b]PIRIDINI I PIROLO[2,3-b]PIRIMIDINI KAO INHIBITORI JANUS KINAZE
HRP20181912TT HRP20181912T1 (hr) 2005-12-13 2018-11-16 Derivati pirolo[2,3-d]pirimidina kao inhibitori janus kinaze

Country Status (36)

Country Link
US (16) US7598257B2 (hr)
EP (10) EP3466953B1 (hr)
JP (4) JP5017278B2 (hr)
KR (4) KR101324737B1 (hr)
CN (4) CN103214483B (hr)
AR (1) AR057995A1 (hr)
AT (1) ATE525374T1 (hr)
AU (1) AU2006326548B2 (hr)
BR (1) BRPI0619817B8 (hr)
CA (1) CA2632466C (hr)
CR (2) CR10065A (hr)
CY (8) CY1112762T1 (hr)
DK (7) DK1966202T3 (hr)
EA (3) EA035795B1 (hr)
EC (2) ECSP088540A (hr)
ES (10) ES2373688T3 (hr)
FR (2) FR13C0007I2 (hr)
HK (5) HK1124840A1 (hr)
HR (7) HRP20110903T1 (hr)
HU (7) HUE030418T2 (hr)
IL (3) IL192019A (hr)
LT (5) LT2426129T (hr)
LU (1) LU92137I2 (hr)
ME (1) ME01312B (hr)
MX (1) MX346183B (hr)
MY (2) MY162590A (hr)
NZ (2) NZ778831A (hr)
PL (7) PL2455382T3 (hr)
PT (7) PT1966202E (hr)
RS (7) RS55576B1 (hr)
SG (3) SG179430A1 (hr)
SI (7) SI2348023T1 (hr)
TW (6) TWI630207B (hr)
UA (2) UA116187C2 (hr)
WO (1) WO2007070514A1 (hr)
ZA (1) ZA200805165B (hr)

Families Citing this family (390)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
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.
CN101263140A (zh) * 2005-09-16 2008-09-10 阿斯利康(瑞典)有限公司 作为葡萄糖激酶活化剂的杂双环化合物
CA2621261C (en) * 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
NZ567851A (en) * 2005-11-01 2011-09-30 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
SI2348023T1 (sl) 2005-12-13 2015-10-30 Incyte Corporation S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
PT1962830E (pt) * 2005-12-23 2013-05-29 Glaxosmithkline Llc Inibidores azaindólicos de cinases aurora
BRPI0709866B8 (pt) 2006-04-03 2021-05-25 Astellas Pharma Inc compostos héteros e composição farmacêutica compreendendo ditos compostos
EP2001884A1 (en) * 2006-04-05 2008-12-17 Vertex Pharmaceuticals, Inc. Deazapurines useful as inhibitors of janus kinases
DK2101819T3 (da) 2006-11-20 2013-04-29 Harvard College Fremgangsmåder, sammensætninger og kits til behandling af smerte og pruritis
JP5492565B2 (ja) * 2006-12-22 2014-05-14 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
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.
CU24179B1 (es) * 2007-06-13 2016-04-25 Incyte Corp SALES DE ÁCIDO MALEICO Y DE ÁCIDO SULFÚRICO DE (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANITRILO
US20100240657A1 (en) * 2007-07-02 2010-09-23 Boehringer Ingelheim International Gmbh Chemical compounds
WO2009032338A1 (en) * 2007-09-09 2009-03-12 University Of Florida Research Foundation Apratoxin therapeutic agents: mechanism and methods of treatment
WO2009049028A1 (en) * 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
EP2211620B1 (en) * 2007-10-25 2013-12-25 Merck Sharp & Dohme Corp. 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES
BRPI0820544A2 (pt) * 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
EP2247591A1 (en) * 2008-02-06 2010-11-10 Novartis AG Pyrrolo [2, 3-d]pyridines and use thereof as tyrosine kinase inhibitors
WO2009114552A1 (en) * 2008-03-10 2009-09-17 The Board Of Trustees Of The Leland Stanford Junior University Heteroaryl compounds, compositions, and methods of use in cancer treatment
BRPI0909040B8 (pt) 2008-03-11 2021-05-25 Incyte Holdings Corp derivados de azetidina e ciclobutano, seus usos, e composição
US8278335B2 (en) * 2008-04-21 2012-10-02 Merck Sharp & Dohme Corp. Inhibitors of Janus kinases
US8871753B2 (en) * 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
AR071717A1 (es) 2008-05-13 2010-07-07 Array Biopharma Inc Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer.
WO2009155156A1 (en) * 2008-06-18 2009-12-23 Merck & Co., Inc. Inhibitors of janus kinases
KR20110031475A (ko) * 2008-06-20 2011-03-28 제넨테크, 인크. 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법
MX2010014005A (es) * 2008-06-20 2011-02-15 Genentech Inc Compuestos de triazolopiridina inhibidores de jak y los metodos.
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.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
WO2010085597A1 (en) * 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
US8716303B2 (en) * 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
HUE046493T2 (hu) * 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
ES2540964T3 (es) 2009-06-08 2015-07-15 Takeda Pharmaceutical Company Limited Compuestos de dihidropirrolonaftiridinona como inhibidores de JAK
RS53494B9 (sr) 2009-06-29 2020-11-30 Incyte Holdings Corp Pirimidinoni kao inhibitori pi3k
CA3027255C (en) 2009-07-10 2022-06-21 The General Hospital Corporation Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
TWI466885B (zh) 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2485589A4 (en) * 2009-09-04 2013-02-06 Biogen Idec Inc HETEROARYARY INHIBITORS OF BTK
CA2773182A1 (en) 2009-09-10 2011-03-17 F. Hoffmann-La Roche Ag Inhibitors of jak
NO2482815T3 (hr) 2009-10-02 2018-09-29
PT2486041E (pt) 2009-10-09 2013-11-14 Incyte Corp Derivados hidroxilo, ceto e glucuronido de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentil-propanonitrilo
US8389728B2 (en) * 2009-11-06 2013-03-05 The Arizona Board Of Regents Pollen tube stimulants from Arabidopsis pistils
JP5858434B2 (ja) * 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
WO2011109217A2 (en) * 2010-03-02 2011-09-09 Immunodiagnostics, Inc. Methods of treating or preventing rna polymerase dependent viral disorders by administration of jak2 kinase inhibitors
DK3050882T3 (en) * 2010-03-10 2018-03-19 Incyte Holdings Corp PIPERIDIN-4-YL-AZETIDINE DERIVATIVES AS JAK1 INHIBITORS
AU2015205858B2 (en) * 2010-03-10 2017-04-13 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
UA109131C2 (ru) * 2010-04-14 2015-07-27 Еррей Біофарма Інк. 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
WO2011133920A1 (en) 2010-04-23 2011-10-27 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
ME02445B (me) 2010-05-21 2016-09-20 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
NZ606751A (en) * 2010-08-20 2015-04-24 Hutchison Medipharma Ltd Pyrrolopyrimidine compounds and uses thereof
US8809377B2 (en) * 2010-09-24 2014-08-19 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
CA2816088A1 (en) 2010-10-28 2012-05-03 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
AU2010363329A1 (en) 2010-11-07 2013-05-09 Targegen, Inc. Compositions and methods for treating myelofibrosis
UA113156C2 (xx) 2010-11-19 2016-12-26 Циклобутилзаміщені похідні піролопіридину й піролопіримідину як інгібітори jak
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
EA036970B1 (ru) * 2010-11-19 2021-01-21 Инсайт Холдингс Корпорейшн Применение {1-{1-[3-фтор-2-(трифтометил)изоникотиноил] пиперидин-4-ил}-3-[4-(7h-пирроло[2,3-d]пиримидин-4-ил)-1н-пиразол-1-ил]азетидин-3-ил}ацетонитрила для лечения заболеваний, связанных с активностью jak1
JP6097998B2 (ja) * 2010-12-16 2017-03-22 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 ロイコトリエン生成のビアリールアミドインヒビター
AR084366A1 (es) 2010-12-20 2013-05-08 Incyte Corp N-(1-(fenil sustituido)etil)-9h-purin-6-aminas como inhibidores de pi3k
JP5681819B2 (ja) 2011-02-11 2015-03-11 バットマーク・リミテッド 吸入器コンポーネント
JP5936628B2 (ja) * 2011-02-18 2016-06-22 ノバルティス・ファルマ・アクチェンゲゼルシャフトＮｏｖａｒｔｉｓ Ｐｈａｒｍａ ＡＧ ｍＴＯＲ／ＪＡＫ阻害剤併用療法
AU2012220601B2 (en) 2011-02-24 2017-03-09 Cephalon, Inc. Vinyl -aryl - sulfones for use in peritoneal carcinomatosis
US9115133B2 (en) 2011-03-22 2015-08-25 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
US8759380B2 (en) 2011-04-22 2014-06-24 Cytokinetics, Inc. Certain heterocycles, compositions thereof, and methods for their use
MX2013013331A (es) * 2011-05-17 2014-10-17 Principia Biopharma Inc Derivados de azaindol como inhibidores de tirosina-cinasas.
EA027654B1 (ru) 2011-06-14 2017-08-31 Новартис Аг Комбинация панобиностата и руксолитиниба при лечении рака, такого как миелопролиферативное новообразование
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
ES2548414T3 (es) 2011-07-08 2015-10-16 Novartis Ag Novedosos derivados de pirrolo pirimidina
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
HUE043703T2 (hu) 2011-09-02 2019-09-30 Incyte Holdings Corp Heterociklusos aminok PI3K inhibitorokként
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
ES2640911T3 (es) * 2011-09-22 2017-11-07 Merck Sharp & Dohme Corp. Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus
JP2014528475A (ja) * 2011-10-12 2014-10-27 アレイ バイオファーマ、インコーポレイテッド ５，７置換イミダゾ［１，２−ｃ］ピリミジン
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
MX2014006479A (es) 2011-11-30 2015-01-22 Univ Emory Inhibidores antivirales de la janus cinasa utiles en el tratamiento o prevencion de infecciones retrovirales y otras infecciones virales.
EP2788000B1 (en) * 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
US20150197525A1 (en) 2012-06-15 2015-07-16 Concert Pharmaceuticals, Inc. Deuterated derivatives of ruxolitinib
CA2876306C (en) * 2012-06-15 2024-02-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of ruxolitinib
KR20150034209A (ko) 2012-06-26 2015-04-02 델 마 파마슈티컬스 인코포레이티드 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
US20150246043A1 (en) 2012-07-27 2015-09-03 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
RU2666538C2 (ru) * 2012-08-02 2018-09-11 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пирролы, активные в качестве ингибиторов киназ
IN2015DN02008A (hr) 2012-09-21 2015-08-14 Advinus Therapeutics Ltd
WO2014064131A2 (en) * 2012-10-26 2014-05-01 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
SG10201703533VA (en) 2012-11-01 2017-06-29 Incyte Corp Tricyclic fused thiophene derivatives as jak inhibitors
PE20151157A1 (es) * 2012-11-15 2015-08-19 Incyte Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
US9310374B2 (en) * 2012-11-16 2016-04-12 Redwood Bioscience, Inc. Hydrazinyl-indole compounds and methods for producing a conjugate
WO2014085154A1 (en) 2012-11-27 2014-06-05 Beth Israel Deaconess Medical Center, Inc. Methods for treating renal disease
EP2928459A4 (en) * 2012-12-06 2016-10-26 Baruch S Blumberg Inst FUNCTIONALIZED BENZAMIDE DERIVATIVES AS ANTIVIRAL AGENTS AGAINST HBV INFECTION
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
WO2014118195A1 (en) 2013-01-29 2014-08-07 Avexxin As Antiinflammatory and antitumor 2-oxothiazoles and 2-oxothiophenes compounds
US20150380681A1 (en) * 2013-02-12 2015-12-31 Konica Minolta, Inc. Organic electroluminescent element and lighting device
PE20151902A1 (es) 2013-03-06 2015-12-26 Incyte Corp Proceso e intermedios para hacer un inhibidor de jak
US20140343034A1 (en) 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
EP4275756A3 (en) 2013-05-17 2024-02-07 Incyte Holdings Corporation Bipyrazole derivatives as jak inhibitors
RS60469B1 (sr) 2013-08-07 2020-07-31 Incyte Corp Dozni oblici sa produženim oslobađanjem za jak1 inhibitor
MX2016002165A (es) * 2013-08-20 2017-01-05 Incyte Corp Beneficio de supervivencia en pacientes con tumores solidos con niveles elevados de proteina c reactiva.
EP3049442A4 (en) 2013-09-26 2017-06-28 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
WO2015054283A1 (en) * 2013-10-08 2015-04-16 Calcimedica, Inc. Compounds that modulate intracellular calcium
EP3057972A4 (en) * 2013-10-15 2017-03-22 V Jin Novel compositions, uses and methods for their preparation
CN105764528A (zh) 2013-11-27 2016-07-13 诺华股份有限公司 包含jak、cdk和pim抑制剂的联合疗法
CU24396B1 (es) 2013-12-05 2019-04-04 Pfizer Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinilo
JP6367545B2 (ja) * 2013-12-17 2018-08-01 コンサート ファーマシューティカルズ インコーポレイテッド ルキソリチニブの重水素化誘導体
CN104725380B (zh) * 2013-12-18 2019-06-28 康塞特医药品有限公司 卢索替尼的氘代衍生物
KR102261733B1 (ko) * 2013-12-18 2021-06-04 콘서트 파마슈티컬즈, 인크. 룩소리티닙의 중수소화된 유도체
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
JP6526065B2 (ja) 2014-02-28 2019-06-05 ニンバス ラクシュミ， インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
SI3110409T1 (sl) * 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
TWI697500B (zh) 2014-03-14 2020-07-01 瑞士商諾華公司 針對ｌａｇ-３之抗體分子及其用途
MA54622A (fr) 2014-04-08 2021-11-03 Incyte Corp Traitement d'affections malignes par lymphocytes b par un inhibiteur jak et pi3k combiné
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
RU2564891C1 (ru) * 2014-05-27 2015-10-10 Александр Александрович Кролевец Способ получения нанокапсул цитокининов
ES2946179T3 (es) * 2014-05-28 2023-07-13 Onco Tracker Inc Efectos antineoplásicos de inhibidores de JAK2 en combinación con derivados de talidomida y glucocorticoides
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
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
US9623028B2 (en) * 2014-07-14 2017-04-18 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
NZ629796A (en) * 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
GB201413695D0 (en) 2014-08-01 2014-09-17 Avexxin As Compound
SI3179992T1 (sl) 2014-08-11 2022-09-30 Acerta Pharma B.V. Terapevtske kombinacije zaviralca BTK, zaviralca PD-1 in/ali zaviralca PD-L1
TW201618772A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑及／或ｂｃｌ－２抑制劑之治療組合物
US20170224819A1 (en) 2014-08-11 2017-08-10 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK 4/6 Inhibitor
CN106715456B (zh) 2014-08-12 2023-08-29 莫纳什大学 定向淋巴的前药
ES2874537T3 (es) * 2014-08-21 2021-11-05 Ratiopharm Gmbh Sal oxalato de ruxolitinib
AU2015314756A1 (en) 2014-09-13 2017-03-16 Novartis Ag Combination therapies of alk inhibitors
CN105524067A (zh) * 2014-09-28 2016-04-27 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
JP2017535528A (ja) 2014-10-03 2017-11-30 ノバルティス アーゲー 組み合わせ治療
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
US9988452B2 (en) 2014-10-14 2018-06-05 Novartis Ag Antibody molecules to PD-L1 and uses thereof
WO2016063294A2 (en) * 2014-10-20 2016-04-28 Msn Laboratories Private Limited Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof
GB2535427A (en) 2014-11-07 2016-08-24 Nicoventures Holdings Ltd Solution
CZ2014773A3 (cs) 2014-11-10 2016-05-18 Zentiva, K.S. Soli (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu
CN105777754B (zh) * 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
PL3262046T3 (pl) 2015-02-27 2021-05-04 Incyte Corporation Sole inhibitora pi3k i sposoby ich wytwarzania
US20160251376A1 (en) 2015-02-27 2016-09-01 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CR20170410A (es) 2015-03-10 2017-11-08 Aduro Biotech Inc Composiciones y métodos para activar la señalización dependiente del "estimulador del gen interferon"
KR101859170B1 (ko) * 2015-04-17 2018-05-17 광주과학기술원 트리아졸 화합물 및 이의 용도
ES2734048T3 (es) * 2015-04-29 2019-12-04 Wuxi Fortune Pharmaceutical Co Ltd Inhibidores de Janus cinasas (JAK)
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CZ2015496A3 (cs) 2015-07-14 2017-01-25 Zentiva, K.S. Krystalické formy solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a jejich příprava
WO2017011720A1 (en) * 2015-07-16 2017-01-19 Signal Pharmaceuticals, Llc Solod forms 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d] oxazol-6-yl)17h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
EP4378957A3 (en) 2015-07-29 2024-08-07 Novartis AG Combination therapies comprising antibody molecules to pd-1
EP3964528A1 (en) 2015-07-29 2022-03-09 Novartis AG Combination therapies comprising antibody molecules to lag-3
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
AU2016301282B2 (en) 2015-08-03 2022-03-17 Children's Medical Center Corporation Charged ion channel blockers and methods for use
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
TWI707852B (zh) 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
CN114031658A (zh) 2015-09-08 2022-02-11 莫纳什大学 定向淋巴的前药
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
SI3364958T1 (sl) 2015-10-23 2023-05-31 Navitor Pharmaceuticals, Inc. Modulatorji interakcije sestrina in gator2 ter njihova uporaba
CA3004138A1 (en) 2015-11-03 2017-05-11 Janssen Biotech, Inc. Antibodies specifically binding pd-1 and tim-3 and their uses
HUE059324T2 (hu) 2015-11-06 2022-11-28 Incyte Corp Heterociklusos vegyületek, mint PI3K-gamma inhibitorok
DK3373937T3 (da) 2015-11-09 2022-03-14 Scherer Technologies Llc R P Anti-cd22-antistof-maytansin-konjugater og fremgangsmåder til anvendelse deraf
RU2601410C1 (ru) * 2015-11-13 2016-11-10 ЗАО "Р-Фарм" {3-[(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АЗОЛИЛ]АЗЕТИДИН-3-ИЛ}АЦЕТОНИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС КИНАЗ
EP3389664A4 (en) 2015-12-14 2020-01-08 Raze Therapeutics Inc. MTHFD2 CAFFEIN INHIBITORS AND USES THEREOF
WO2017101777A1 (zh) * 2015-12-15 2017-06-22 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物的盐
US20200261573A1 (en) 2015-12-17 2020-08-20 Novartis Ag Combination of c-met inhibitor with antibody molecule to pd-1 and uses thereof
JP2019503349A (ja) 2015-12-17 2019-02-07 ノバルティス アーゲー Ｐｄ−１に対する抗体分子およびその使用
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
ES2882118T3 (es) * 2015-12-31 2021-12-01 Chia Tai Tianqing Pharmaceutical Group Co Ltd Procedimiento de síntesis de ruxolitinib
WO2017123741A1 (en) 2016-01-12 2017-07-20 Institute For Myeloma & Bone Cancer Research Improved methods for monitoring immune status of a subject
CZ201629A3 (cs) 2016-01-22 2017-08-02 Zentiva, K.S. Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy
ES2877200T3 (es) * 2016-01-26 2021-11-16 Hangzhou Bangshun Pharmaceutical Co Ltd Derivado azacíclico de cinco miembros de pirrolopirimidina y aplicación del mismo
CN105541891B (zh) * 2016-02-04 2017-11-28 东南大学 巴瑞替尼的中间体及其制备方法及由该中间体制备巴瑞替尼的方法
EP3426243B1 (en) 2016-03-09 2021-05-19 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
WO2017156179A1 (en) 2016-03-09 2017-09-14 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
GB201604318D0 (en) 2016-03-14 2016-04-27 Avexxin As Combination therapy
PE20190175A1 (es) 2016-03-28 2019-02-01 Incyte Corp Compuestos de pirrolotriazina como inhibidores de tam
CA3019394A1 (en) 2016-04-08 2017-10-12 X4 Pharmaceuticals, Inc. Methods for treating cancer
WO2017192905A1 (en) 2016-05-04 2017-11-09 Concert Pharmaceuticals, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
CN107513067A (zh) 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
CN107513069A (zh) * 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
CN107759600A (zh) * 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
EP3808748A1 (en) 2016-06-21 2021-04-21 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
EP3472129A4 (en) 2016-06-21 2019-12-04 X4 Pharmaceuticals, Inc. CXCR4 INHIBITORS AND USES THEREOF
JP7084624B2 (ja) 2016-06-21 2022-06-15 エックス４ ファーマシューティカルズ， インコーポレイテッド Ｃｘｃｒ４阻害剤およびその使用
US10961247B2 (en) 2016-06-30 2021-03-30 Daewoong Pharmaceutical Co., Ltd. Pyrazolopyrimidine derivatives as kinase inhibitor
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
JP6978097B2 (ja) * 2016-07-26 2021-12-08 スーヂョウ ロングバイオテック ファーマシューティカルズ カンパニー リミテッドSuzhou Longbiotech Pharmaceuticals Co., Ltd. Ｊａｋ阻害剤としての複素環化合物、該化合物の塩類および治療への使用
CN109890821A (zh) 2016-08-24 2019-06-14 艾科尔公司 氨基-吡咯并嘧啶酮化合物及其使用方法
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
IT201600092051A1 (it) * 2016-09-13 2018-03-13 Alessandro Antonelli Composto medicale per il trattamento di tumori della tiroide
CN109952303B (zh) 2016-10-14 2022-10-21 林伯士拉克许米公司 Tyk2抑制剂及其用途
CA3040286A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2018089499A1 (en) 2016-11-08 2018-05-17 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
CA3043768A1 (en) 2016-11-29 2018-06-07 PureTech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
RU2644155C1 (ru) * 2016-12-12 2018-02-08 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ
US11730819B2 (en) 2016-12-23 2023-08-22 Bicycletx Limited Peptide derivatives having novel linkage structures
US10624968B2 (en) 2017-01-06 2020-04-21 Bicyclerd Limited Compounds for treating cancer
EA039352B1 (ru) * 2017-01-19 2022-01-17 Сучжоу Лонгбайотек Фармасьютикалз Ко., Лтд. Соединение в качестве селективного ингибитора jak и его соли и терапевтическое применение
TW202321243A (zh) 2017-03-08 2023-06-01 美商林伯士拉克許米公司 Ｔｙｋ２抑制劑之生產方法
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
US11339144B2 (en) 2017-04-10 2022-05-24 Navitor Pharmaceuticals, Inc. Heteroaryl Rheb inhibitors and uses thereof
JOP20180036A1 (ar) 2017-04-18 2019-01-30 Vifor Int Ag أملاح لمثبطات فروبورتين جديدة
CA3061611A1 (en) 2017-04-26 2018-11-01 Navitor Pharmaceuticals, Inc. Modulators of sestrin-gator2 interaction and uses thereof
WO2018197893A1 (en) 2017-04-27 2018-11-01 Bicycletx Limited Bicyclic peptide ligands and uses thereof
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
CN110662747A (zh) 2017-05-23 2020-01-07 施万生物制药研发Ip有限责任公司 Janus激酶抑制剂的葡糖苷酸前药
US11635435B2 (en) 2017-06-13 2023-04-25 Oncotracker, Inc. Diagnostic, prognostic, and monitoring methods for solid tumor cancers
US20200172628A1 (en) 2017-06-22 2020-06-04 Novartis Ag Antibody molecules to cd73 and uses thereof
US11312783B2 (en) 2017-06-22 2022-04-26 Novartis Ag Antibody molecules to CD73 and uses thereof
CN111032678A (zh) 2017-06-26 2020-04-17 拜西克尔德有限公司 具有可检测部分的双环肽配体和其用途
CN107298680A (zh) * 2017-07-12 2017-10-27 海门华祥医药科技有限公司 一种4‑氯‑7‑氮杂吲哚的生产工艺
PT3658557T (pt) 2017-07-28 2024-09-11 Nimbus Lakshmi Inc Inibidores de tyk2 e usos dos mesmos
EP3661948B1 (en) 2017-08-04 2022-06-01 BicycleTx Limited Bicyclic peptide ligands specific for cd137
EP3668887A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand sting conjugates and uses thereof
EP3668550A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
EP3675838A4 (en) 2017-08-29 2021-04-21 PureTech LYT, Inc. LIPID PRODUCTS DIRECTED TO THE LYMPHATIC SYSTEM
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
AU2018338314A1 (en) 2017-09-22 2020-04-09 Kymera Therapeutics, Inc Protein degraders and uses thereof
US10633387B2 (en) 2017-09-27 2020-04-28 Incyte Corporation Salts of TAM inhibitors
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
BR112020008850A2 (pt) 2017-11-03 2020-10-20 Aclaris Therapeutics, Inc. composto, composição farmacêutica e método para tratar uma doença mediada por jak1 e jak3
US10800775B2 (en) 2017-11-03 2020-10-13 Aclaris Therapeutics, Inc. Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same
KR102034538B1 (ko) 2017-11-28 2019-10-21 주식회사한국파마 Jak 저해제 화합물, 및 이의 제조방법
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc IRAK joints and used in them
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
CN111918651B (zh) 2018-01-29 2024-01-30 默克专利股份有限公司 Gcn2抑制剂及其用途
US10793563B2 (en) 2018-01-29 2020-10-06 Merck Patent Gmbh GCN2 inhibitors and uses thereof
MA51771B1 (fr) 2018-01-30 2022-03-31 Incyte Corp Procédés de préparation de (1-(3-fluoro-2-(trifluorométhyl)isonicotinyl)pipéridine-4-one)
BR112020016628A2 (pt) 2018-02-16 2020-12-15 Incyte Corporation Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
CA3091142C (en) 2018-02-26 2023-04-11 Gilead Sciences, Inc. Substituted pyrrolizine compounds and uses thereof
EP3759086A1 (en) 2018-02-27 2021-01-06 Artax Biopharma Inc. Chromene derivatives as inhibitors of tcr-nck interaction
US20210002374A1 (en) 2018-03-08 2021-01-07 Novartis Ag USE OF an anti-P-selectin antibody
CN110357887B (zh) * 2018-03-26 2022-09-16 武汉誉祥医药科技有限公司 取代的7H-吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
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
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
WO2019200030A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
PL3784666T3 (pl) 2018-04-24 2022-07-18 Merck Patent Gmbh Związki przeciwproliferacyjne i ich zastosowania
CA3097774A1 (en) 2018-04-24 2019-10-31 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
TW202015726A (zh) 2018-05-30 2020-05-01 瑞士商諾華公司 Ｅｎｔｐｄ２抗體、組合療法、及使用該等抗體和組合療法之方法
US20210214459A1 (en) 2018-05-31 2021-07-15 Novartis Ag Antibody molecules to cd73 and uses thereof
US12065441B2 (en) 2018-06-06 2024-08-20 Gengle Therapeutics, Inc. Pyrazolopyrimidine derivative, use thereof and pharmaceutical composition
DK3813946T3 (da) 2018-06-15 2024-08-19 Janssen Pharmaceutica Nv Rapamycin-analoger og anvendelser deraf
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
JP7520732B2 (ja) 2018-06-29 2024-07-23 インサイト・コーポレイション Ａｘｌ／ｍｅｒ阻害剤の製剤
JP6830460B2 (ja) * 2018-07-05 2021-02-17 コンサート ファーマシューティカルズ インコーポレイテッド ルキソリチニブの重水素化誘導体
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
KR102612513B1 (ko) 2018-07-31 2023-12-12 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
MX2021001558A (es) 2018-08-10 2021-04-28 Aclaris Therapeutics Inc Inhibidores de itk de pirrolopirimidina.
WO2020039401A1 (en) 2018-08-24 2020-02-27 Novartis Ag Treatment comprising il-1βeta binding antibodies and combinations thereof
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
US12030875B2 (en) 2018-09-07 2024-07-09 PIC Therapeutics, Inc. EIF4E inhibitors and uses thereof
AU2019360941A1 (en) 2018-10-15 2021-04-29 Takeda Pharmaceutical Company Limited TYK2 inhibitors and uses thereof
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
US11345654B2 (en) 2018-10-24 2022-05-31 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
US11324749B2 (en) 2018-10-31 2022-05-10 Incyte Corporation Combination therapy for treatment of hematological diseases
CN113271938A (zh) 2018-11-30 2021-08-17 林伯士拉克许米公司 Tyk2抑制剂和其用途
MX2021006154A (es) 2018-11-30 2021-08-24 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina 1 (irak) y usos de los mismos.
CN109394768B (zh) * 2018-12-10 2019-08-23 牡丹江医学院 一种治疗湿疹的药物及其制备方法
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
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
CN113195000A (zh) 2018-12-21 2021-07-30 第一三共株式会社 抗体-药物缀合物和激酶抑制剂的组合
CA3126034A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
CN111620873B (zh) * 2019-02-28 2021-12-28 沈阳药科大学 一类含哌啶的吡咯并[2,3-d]嘧啶衍生物及其制备和用途
CN114007621A (zh) 2019-03-05 2022-02-01 因赛特公司 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂
SG11202109720WA (en) 2019-03-11 2021-10-28 Nocion Therapeutics Inc Charged ion channel blockers and methods for use
JP2022527731A (ja) 2019-03-11 2022-06-06 ノシオン セラピューティクス，インコーポレイテッド エステル置換イオンチャンネル遮断薬および使用方法
KR20210143791A (ko) 2019-03-11 2021-11-29 녹시온 테라퓨틱스 인코포레이티드 하전된 이온 채널 차단제 및 사용 방법
US10786485B1 (en) 2019-03-11 2020-09-29 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
WO2020191041A2 (en) 2019-03-19 2020-09-24 Incyte Corporation Biomarkers for vitiligo
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
EP3946462A1 (en) 2019-04-02 2022-02-09 BicycleTX Limited Bicycle toxin conjugates and uses thereof
US11485750B1 (en) 2019-04-05 2022-11-01 Kymera Therapeutics, Inc. STAT degraders and uses thereof
KR20210141634A (ko) 2019-04-24 2021-11-23 엘랑코 유에스 인코포레이티드 7h-피롤로[2,3-d]피리미딘 jak-억제제
MX2021013224A (es) 2019-05-02 2022-01-06 Aclaris Therapeutics Inc Pirrolopiridinas sustituidas como inhibidores de jak.
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
KR102286372B1 (ko) 2019-05-27 2021-08-05 주식회사한국파마 Jak 저해제 화합물, 및 이를 포함하는 의약 조성물
AU2020282759A1 (en) 2019-05-31 2021-12-23 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
AU2020290995A1 (en) * 2019-06-10 2022-04-07 Incyte Corporation Topical treatment of vitiligo by a JAK inhibitor
AU2020307667A1 (en) 2019-06-27 2022-01-20 Crispr Therapeutics Ag Use of chimeric antigen receptor T cells and NK cell inhibitors for treating cancer
TW202118770A (zh) 2019-07-30 2021-05-16 英商拜西可泰克斯有限公司 異質雙環肽複合物
CN110305140B (zh) 2019-07-30 2020-08-04 上海勋和医药科技有限公司 二氢吡咯并嘧啶类选择性jak2抑制剂
US20220235043A1 (en) * 2019-07-31 2022-07-28 Aclaris Therapeutics, Inc. Substituted sulfonamide pyrrolopyridines as jak inhibitors
US20220251097A1 (en) * 2019-08-01 2022-08-11 St. Jude Childrens's Research Hospital Molecules and methods related to treatment of uncontrolled cellular proliferation
US11845724B2 (en) 2019-09-11 2023-12-19 Vincere Biosciences, Inc. USP30 inhibitors and uses thereof
MX2022002877A (es) 2019-09-13 2022-08-08 Nimbus Saturn Inc Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos.
JP2022548627A (ja) 2019-09-16 2022-11-21 ノバルティス アーゲー 骨髄線維症の治療のための、高親和性のリガンドを遮断するヒト化抗ｔ細胞免疫グロブリンドメイン及びムチンドメイン３（ｔｉｍ－３）ｉｇｇ４抗体の使用
MX2022003129A (es) 2019-09-16 2022-04-06 Novartis Ag Uso de un inhibidor de mdm2 para el tratamiento de la mielofibrosis.
EP4031578A1 (en) 2019-09-18 2022-07-27 Novartis AG Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
JP2022551649A (ja) 2019-10-10 2022-12-12 インサイト・コーポレイション 移植片対宿主病のバイオマーカー
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)
MX2022005215A (es) 2019-11-01 2022-06-08 Navitor Pharm Inc Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1).
CN114828845A (zh) 2019-11-06 2022-07-29 诺西恩医疗公司 带电的离子通道阻滞剂及其使用方法
WO2021091586A1 (en) 2019-11-06 2021-05-14 Nocion Therapeutics, Inc. Charged ion channel blockers and methods for use
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021102258A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
CN115209897A (zh) 2019-12-05 2022-10-18 安纳库利亚治疗公司 雷帕霉素类似物及其用途
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
IL294150A (en) 2019-12-23 2022-08-01 Kymera Therapeutics Inc Smarca joints and their uses
EP4085056A1 (en) 2020-01-03 2022-11-09 Berg LLC Polycyclic amides as ube2k modulators for treating cancer
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115348864A (zh) 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
CN111728975A (zh) * 2020-02-25 2020-10-02 广东省检迅检测科技有限公司 用于减少运动损伤和促进运动损伤修复的组合物
BR112022017727A2 (pt) 2020-03-03 2022-11-16 Pic Therapeutics Inc Inibidores de eif4e e usos dos mesmos
JP2023517604A (ja) 2020-03-11 2023-04-26 ノシオン セラピューティクス，インコーポレイテッド 荷電したイオンチャンネル遮断薬および使用方法
IL296451A (en) 2020-03-19 2022-11-01 Kymera Therapeutics Inc mdm2 joints and their uses
US11324750B2 (en) 2020-04-09 2022-05-10 Children's Hospital Medical Center Compositions and methods for the treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection
EP3892280A3 (en) 2020-04-09 2022-01-12 Children's Hospital Medical Center Sars-cov-2 infection biomarkers and uses thereof
WO2021206766A1 (en) 2020-04-09 2021-10-14 Children's Hospital Medical Center Sars-cov-2 infection biomarkers and uses thereof
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
WO2021236139A1 (en) 2020-05-21 2021-11-25 Concert Pharmaceuticals, Inc. Novel deuterated jak inhibitor and uses thereof
CA3184275A1 (en) 2020-06-02 2021-12-09 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
CA3184633A1 (en) 2020-06-03 2021-12-09 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
CA3181162A1 (en) 2020-06-05 2021-12-09 Stephen W. Kaldor Inhibitors of fibroblast growth factor receptor kinases
WO2021260657A1 (en) 2020-06-26 2021-12-30 Crispr Therapeutics Ag Allogeneic cell therapy of b cell malignancies using genetically engineered t cells targeting cd19
EP3944859A1 (en) 2020-07-30 2022-02-02 Assistance Publique Hôpitaux de Paris Method for treating immune toxicities induced by immune checkpoint inhibitors
US11751108B2 (en) * 2020-08-05 2023-09-05 Qualcomm Incorporated Execution of reduced signaling handover
EP4196481A1 (en) * 2020-08-12 2023-06-21 Concert Pharmaceuticals Inc. Process for preparing enantiomerically enriched jak inhibitors
KR20230074721A (ko) 2020-08-17 2023-05-31 바이사이클티엑스 리미티드 Nectin-4에 특이적인 이환 콘쥬게이트 및 이의 용도
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
CA3192055A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
US20230348474A1 (en) * 2020-09-16 2023-11-02 Axceso Biopharma Co., Ltd. Pyrimido pyrimidinone compound and pharmaceutical composition comprising the same
EP4213800A1 (en) 2020-09-16 2023-07-26 Incyte Corporation Topical treatment of vitiligo
WO2022072814A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Topical ruxolitinib for treating lichen planus
TW202227076A (zh) 2020-10-08 2022-07-16 瑞士商諾華公司 Ｅｒｋ抑制劑用於治療骨髓纖維化之用途
WO2022074600A1 (en) 2020-10-08 2022-04-14 Novartis Ag Use of an erk inhibitor for the treatment of myelofibrosis
CN114437079A (zh) * 2020-10-30 2022-05-06 杭州邦顺制药有限公司 吡咯嘧啶五元氮杂环化合物的晶型
KR102551758B1 (ko) 2020-11-30 2023-07-05 주식회사한국파마 신규한 jak 특이 저해제 화합물, 및 이의 제조방법
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
AU2021392040A1 (en) 2020-12-02 2023-06-29 Ikena Oncology, Inc. Tead inhibitors and uses thereof
KR20230128472A (ko) 2020-12-04 2023-09-05 인사이트 코포레이션 피부 질환의 치료를 위한 비타민 d 유사체를 함유하는jak 억제제
TW202237089A (zh) 2020-12-08 2022-10-01 美商英塞特公司 用於治療白斑病之ｊａｋ１途徑抑制劑
CA3201608A1 (en) 2020-12-18 2022-06-23 Boehringer Ingelheim Animal Health USA Inc. Boron containing pyrazole compounds, compositions comprising them, methods and uses thereof
MX2023008141A (es) 2021-01-11 2023-10-20 Incyte Corp Terapia combinada que comprende el inhibidor de la vía de proteínas tirosina cinasas de janus cinasas (jak) y el inhibidor de la proteína cinasa asociada a rho (rock).
US20240174662A1 (en) * 2021-02-01 2024-05-30 Janssen Biotech, Inc. Small molecule inhibitors of salt inducible kinases
US20230091528A1 (en) 2021-02-02 2023-03-23 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
BR112023015590A2 (pt) 2021-02-02 2023-10-17 Liminal Biosciences Ltd Antagonistas de gpr84 e usos dos mesmos
TW202245774A (zh) * 2021-02-05 2022-12-01 大陸商上海齊魯製藥研究中心有限公司 嘧啶或吡啶並雜環類腺苷受體抑制劑及其製備方法和用途
MX2023009178A (es) 2021-02-15 2023-08-21 Kymera Therapeutics Inc Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos.
KR20230148208A (ko) 2021-02-25 2023-10-24 임팩트 바이오메디신스, 인코포레이티드 골수섬유증과 같은 혈액 악성종양을 치료하기 위한 bet 억제제 단독 또는 페드라티닙 또는 룩솔리티닙과의 조합물의 용도
JP2024509192A (ja) 2021-03-05 2024-02-29 ニンバス サターン， インコーポレイテッド Ｈｐｋ１アンタゴニスト及びその使用
US12071442B2 (en) 2021-03-29 2024-08-27 Nimbus Saturn, Inc. Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists
JP2024514879A (ja) 2021-04-16 2024-04-03 イケナ オンコロジー， インコーポレイテッド Ｍｅｋ阻害剤及びその使用
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
EP4370504A1 (en) 2021-07-12 2024-05-22 Incyte Corporation Process and intermediates for preparing baricitinib
EP4392421A1 (en) 2021-08-25 2024-07-03 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
IL310924A (en) 2021-08-25 2024-04-01 Pic Therapeutics Inc EIF4E inhibitors and their uses
WO2023042224A1 (en) * 2021-09-18 2023-03-23 Natco Pharma Limited An improved process for the preparation of ruxolitinib phosphate
EP4423086A1 (en) 2021-10-25 2024-09-04 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
WO2023102559A1 (en) 2021-12-03 2023-06-08 Incyte Corporation Topical formulations of ruxolitinib with an organic amine ph adjusting agent for treatment of skin diseases
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CN114044777B (zh) * 2022-01-10 2022-04-19 南京佰麦生物技术有限公司 一种磷酸芦可替尼的制备方法
IL314437A (en) 2022-01-31 2024-09-01 Kymera Therapeutics Inc IRAK joints and their uses
CN114456181A (zh) * 2022-02-21 2022-05-10 浙江乐普药业股份有限公司 一种芦可替尼的制备方法
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
TW202415650A (zh) 2022-08-02 2024-04-16 英商利米那生物科技有限公司 芳基-三唑基及相關gpr84拮抗劑及其用途
TW202416950A (zh) 2022-08-02 2024-05-01 英商利米那生物科技有限公司 雜芳基甲醯胺及相關gpr84拮抗劑及其用途
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
WO2024028193A1 (en) 2022-08-03 2024-02-08 Medichem, S.A. Stable oral pharmaceutical formulation containing ruxolitinib hemifumarate
WO2024099396A1 (zh) * 2022-11-11 2024-05-16 浙江奥翔药业股份有限公司 芦可替尼晶体及其药物组合物
US20240208961A1 (en) 2022-11-22 2024-06-27 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2024184926A1 (en) * 2023-03-08 2024-09-12 Aarti Pharmalabs Limited Process for preparation of chiral ruxolitinib and salts thereof
WO2024187415A1 (en) * 2023-03-15 2024-09-19 Zhejiang Qizheng Pharmaceutical Co., Ltd. Pharmaceutical composition comprising ruxolitinib
WO2024187416A1 (en) * 2023-03-15 2024-09-19 Zhejiang Qizheng Pharmaceutical Co., Ltd. Pharmaceutical composition comprising ruxolitinib

Family Cites Families (311)

* 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
US3632836A (en) 1968-10-25 1972-01-04 Dow Chemical Co Solid curable polyepoxides modified with hydrolyzed liquid polyepoxides
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
US4404335A (en) 1982-08-16 1983-09-13 The Dow Chemical Company Hydrolyzing epoxy resins in absence of solvent and in presence of oxalic acid and a phosphonium compound
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
JPH0710876Y2 (ja) 1989-08-31 1995-03-15 石垣機工株式会社 スクリュープレスにおける脱水筒の洗浄装置
CA2067221C (en) 1989-10-11 1997-04-15 Yasuji Sakuma Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
US5403593A (en) 1991-03-04 1995-04-04 Sandoz Ltd. Melt granulated compositions for preparing sustained release dosage forms
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
USH1439H (en) 1993-10-18 1995-05-02 The Dow Chemical Company Method to increase the level of α-glycol in liquid epoxy resin
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
BR9609613A (pt) 1995-07-05 1999-05-25 Du Pont Composto composição fungicida e método de controle de doenças de plantas
DE69619114T2 (de) 1995-07-06 2002-10-02 Novartis Ag, Basel Pyrolopyrimidine und verfahren zu ihrer herstellung
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
JP2000508335A (ja) 1996-05-30 2000-07-04 メルク エンド カンパニー インコーポレーテッド 癌の治療方法
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
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
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
US7153845B2 (en) 1998-08-25 2006-12-26 Columbia Laboratories, Inc. Bioadhesive progressive hydration tablets
US6075056A (en) 1997-10-03 2000-06-13 Penederm, Inc. Antifungal/steroid topical compositions
SE9800729L (sv) 1998-03-06 1999-09-07 Scotia Lipidteknik Ab Ny topikal formulering I
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
CN1332743A (zh) 1998-06-04 2002-01-23 艾博特公司 抑制细胞粘附抗炎化合物
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
ID26698A (id) 1998-06-19 2001-02-01 Pfizer Prod Inc SENYAWA-SENYAWA PIROLO [2,3-d] PIRIMIDINA
JP4516690B2 (ja) 1998-08-11 2010-08-04 ノバルティス アーゲー 血管形成阻害活性を有するイソキノリン誘導体
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
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
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
AU3565999A (en) 1999-04-16 2000-11-02 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
US7235258B1 (en) 1999-10-19 2007-06-26 Nps Pharmaceuticals, Inc. Sustained-release formulations for treating CNS-mediated disorders
DE60007552T2 (de) * 1999-12-10 2004-09-23 Pfizer Products Inc., Groton PYRROLO[2,3-d]PYRIMIDIN-VERBINDUNGEN ALS PROTEIN KINASEN HEMMER
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
DE60100866T2 (de) 2000-04-07 2004-07-29 Laboratoire Medidom S.A. Cyklosporin, Hyaluronsäure und Polysorbate enthaltenes Augenarzneimittel
AU4878601A (en) 2000-04-20 2001-11-07 Mitsubishi Corporation Aromatic amide compounds
ES2527754T3 (es) * 2000-04-25 2015-01-29 Icos Corporation Inhibidores de la isoforma delta de la fosfatidilinositol 3-quinasa humana
US20030022819A1 (en) 2000-06-16 2003-01-30 Ling Leona E. Angiogenesis-modulating compositions and uses
US7498304B2 (en) 2000-06-16 2009-03-03 Curis, Inc. Angiogenesis-modulating compositions and uses
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
DE60137734D1 (de) * 2000-06-26 2009-04-02 Pfizer Prod Inc PyrroloÄ2,3-DÜpyrimidin Verbindungen als Immunosuppressive Wirkstoffe
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
WO2002016370A1 (fr) 2000-08-22 2002-02-28 Hokuriku Seiyaku Co., Ltd. Derives de 1h-imidazopyridine
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
US20040077654A1 (en) 2001-01-15 2004-04-22 Bouillot Anne Marie Jeanne 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
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
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
DK1441737T3 (da) 2001-10-30 2006-11-13 Novartis Ag Staurosporin-derivater som inhibitorer af FLT3-receptor-tyrosinkinase-aktivitet
JP2003155285A (ja) 2001-11-19 2003-05-27 Toray Ind Inc 環状含窒素誘導体
US6949668B2 (en) 2001-11-30 2005-09-27 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
AU2003237807B2 (en) 2002-04-15 2008-10-23 Rb Health (Us) Llc Sustained release of guaifenesin combination drugs
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
ATE381332T1 (de) 2002-05-02 2008-01-15 Merck & Co Inc Tyrosinkinase-hemmer
EP1503731A1 (en) 2002-05-07 2005-02-09 Control Delivery Systems, Inc. Processes for forming a drug delivery device
CN100558715C (zh) 2002-05-23 2009-11-11 西托匹亚有限公司 蛋白激酶抑制剂
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
US7385018B2 (en) * 2002-06-26 2008-06-10 Idemitsu Kosan Co., Ltd. Hydrogenated copolymer, process for producing the same, and hot-melt adhesive composition containing the same
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
BR0314603A (pt) 2002-09-20 2005-07-26 Alcon Inc Uso de inibidores da sìntese de citoquina para o tratamento de distúrbios de olhos secos
US20040204404A1 (en) 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
ES2289349T3 (es) 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
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
AU2003276591A1 (en) 2002-11-26 2004-06-18 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
UY28126A1 (es) 2002-12-24 2004-06-30 Alcon Inc Uso de glucocorticoides selectivos para la superficie ocular en el tratamiento de la sequedad ocular
US7135493B2 (en) 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
US7444183B2 (en) 2003-02-03 2008-10-28 Enteromedics, Inc. Intraluminal electrode apparatus and method
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
US7547794B2 (en) 2003-04-03 2009-06-16 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
SE0301372D0 (sv) * 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301373D0 (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
EP1678147B1 (en) 2003-09-15 2012-08-08 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
DK1679074T3 (da) 2003-10-24 2011-03-21 Santen Pharmaceutical Co Ltd Terapeutisk middel til keratoconjunktive forstyrrelser
US7387793B2 (en) 2003-11-14 2008-06-17 Eurand, Inc. Modified release dosage forms of skeletal muscle relaxants
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
BRPI0416909A (pt) 2003-11-25 2007-01-16 Pfizer Prod Inc método de tratamento de aterosclerose
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
CA2550189A1 (en) 2003-12-19 2005-07-21 Schering Corporation Thiadiazoles as cxc- and cc- chemokine receptor ligands
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
CA2548374C (en) 2003-12-23 2014-05-27 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
US20050187389A1 (en) * 2004-01-13 2005-08-25 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2005089502A2 (en) 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
DK2332940T3 (da) 2004-03-30 2013-02-11 Vertex Pharma Azaindoler, der kan anvendes som inhibitorer af JAK og andre proteinkinaser
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
US7558717B2 (en) 2004-04-28 2009-07-07 Vertex Pharmaceuticals Incorporated Crystal structure of human JAK3 kinase domain complex and binding pockets thereof
MXPA06012663A (es) 2004-05-03 2007-01-16 Novartis Ag Combinaciones que comprenden un agonista del receptor s1p y un inhibidor de quinasa jak3.
US20060074102A1 (en) 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
MXPA06014247A (es) 2004-06-10 2007-03-12 Irm Llc Compuestos y composiciones como inhibidores de la proteina quinasa.
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
CA2572058A1 (en) 2004-06-30 2006-01-12 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
WO2006022459A1 (en) 2004-08-23 2006-03-02 Mogam Biotechnology Institute Primer and probe for detection of sars coronavirus, kit comprising the primer and/or the probe, and detection method thereof
GB0421525D0 (en) 2004-09-28 2004-10-27 Novartis Ag Inhibitors of protein kineses
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
SI1802625T1 (sl) 2004-10-13 2008-10-31 Hoffmann La Roche Disubstituirani pirazolobenzodiazepini, koristni kot inhibitorji za cdk2 in angiogenezo ter za zdravljenje prsnega raka, raka kolona, pljuäśnega rakain raka prostate
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
AU2005304784B2 (en) 2004-11-04 2011-03-24 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
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
WO2006065916A1 (en) 2004-12-14 2006-06-22 Alcon, Inc. Method of treating dry eye disorders using 13(s)-hode and its analogs
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.
WO2006067445A2 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Csf-1r kinase inhibitors
CA2595574A1 (en) 2005-01-20 2006-07-27 Pfizer Limited. Chemical compounds
ES2320487T3 (es) 2005-02-03 2009-05-22 Vertex Pharmaceuticals, Inc. Pirrolopirimidinas utiles como inhibidores de proteina quinasas.
WO2007044050A2 (en) 2005-02-04 2007-04-19 Bristol-Myers Squibb Company 1h-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
BRPI0608513A2 (pt) 2005-03-15 2010-01-05 Irm Llc compostos e composições como inibidores da proteìna quinase
MX2007012393A (es) 2005-04-05 2008-02-22 Pharmacopeia Inc Derivados de purina e imidazopiridina para la inmunosupresion.
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2609126A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
CN105348203B (zh) 2005-06-08 2018-09-18 里格尔药品股份有限公司 抑制jak途径的组合物和方法
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
EP1893612B1 (en) 2005-06-22 2011-08-03 Plexxikon, Inc. Pyrrolo [2, 3-b]pyridine derivatives as protein kinase inhibitors
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
FR2889662B1 (fr) 2005-08-11 2011-01-14 Galderma Res & Dev Emulsion de type huile-dans-eau pour application topique en dermatologie
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
AU2006297351A1 (en) 2005-09-30 2007-04-12 Vertex Pharmaceuticals Incorporated 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
CA2623202C (en) 2005-10-14 2014-09-16 Sumitomo Chemical Company, Limited Hydrazide compound and pesticidal use of the same
BRPI0618011A2 (pt) 2005-10-28 2011-08-16 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, métodos para produzir um efeito anti-proliferativo e um efeito pró-apoptósico em um animal de sangue quente, para tratar doença e para produzir um efeito inibidor de jak em um animal de sangue quente
NZ567851A (en) 2005-11-01 2011-09-30 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
SI2348023T1 (sl) 2005-12-13 2015-10-30 Incyte Corporation S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
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
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
PT1962830E (pt) 2005-12-23 2013-05-29 Glaxosmithkline Llc Inibidores azaindólicos de cinases aurora
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
TW201412738A (zh) 2006-01-17 2014-04-01 Vertex Pharma 適合作為傑納斯激酶（ｊａｎｕｓ ｋｉｎａｓｅ）抑制劑之氮雜吲哚
US20070208053A1 (en) 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
EP1981887A2 (en) 2006-02-01 2008-10-22 SmithKline Beecham Corporation Pyrrolo[2,3,b]pyridine derivatives useful as raf kinase inhibitors
US7745477B2 (en) 2006-02-07 2010-06-29 Hoffman-La Roche Inc. Heteroaryl and benzyl amide compounds
PL1842534T3 (pl) 2006-02-24 2012-05-31 Teva Pharma Tabletki bursztynianu metoprololu o przedłużonym uwalnianiu oraz sposoby ich wytwarzania
CA2644368A1 (en) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient
BRPI0709866B8 (pt) 2006-04-03 2021-05-25 Astellas Pharma Inc compostos héteros e composição farmacêutica compreendendo ditos compostos
EP2001884A1 (en) 2006-04-05 2008-12-17 Vertex Pharmaceuticals, Inc. Deazapurines useful as inhibitors of janus kinases
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
US20080051427A1 (en) 2006-05-18 2008-02-28 Fritz Schuckler 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
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
NZ573174A (en) 2006-06-01 2012-01-12 Msd Consumer Care Inc Sustained release pharmaceutical dosage form containing phenylephrine
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
CA2660560A1 (en) 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
JP2010502675A (ja) 2006-09-08 2010-01-28 ノバルティス アクチエンゲゼルシャフト リンパ球相互作用が介在する疾患または障害を処置するために有用なｎ−ビアリール（ヘテロ）アリールスルホンアミド誘導体
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
CL2007002867A1 (es) 2006-10-04 2008-06-27 Pharmacopeia Inc Compuestos derivados de 2-(bencimidazolil)purina, inhibidores de janus quinasa 3; composicion farmaceutica que los contiene; y su uso para tratar enfermedades autoinmune, inflamatorias, cardiovasculares, rechazo de implante, entre otras.
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
WO2008058126A2 (en) 2006-11-06 2008-05-15 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
ME01507B (me) 2006-11-22 2014-04-20 Incyte Holdings Corp Imidazotriazini i imidazopirimidini kao inhibitori kinaze
WO2008067119A2 (en) 2006-11-27 2008-06-05 Smithkline Beecham Corporation Novel compounds
CA2672616A1 (en) 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
WO2008079291A2 (en) 2006-12-20 2008-07-03 Amgen Inc. Substituted heterocycles and methods of use
ES2387471T3 (es) 2006-12-20 2012-09-24 Amgen Inc. Compuestos heterocíclicos y su uso en el tratamiento de la inflamación, la angiogénesis y el cáncer
MX2009005644A (es) 2006-12-22 2009-06-08 Sigma Tau Ind Farmaceuti Gel util para el suministro de farmacos oftalmicos.
JP5492565B2 (ja) 2006-12-22 2014-05-14 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
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
US8822497B2 (en) 2007-03-01 2014-09-02 Novartis Ag PIM kinase inhibitors and methods of their use
ES2420113T3 (es) 2007-04-03 2013-08-22 Array Biopharma, Inc. Compuestos de imidazo[1,2-a]piridina como inhibidores de receptores tirosina quinasa
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
WO2008145681A2 (en) 2007-05-31 2008-12-04 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
CU24179B1 (es) 2007-06-13 2016-04-25 Incyte Corp SALES DE ÁCIDO MALEICO Y DE ÁCIDO SULFÚRICO DE (R)-3-(4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL)-3-CICLOPENTILPROPANITRILO
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.
CA2691914C (en) 2007-07-11 2012-06-26 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
WO2009016460A2 (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
EP2217235A4 (en) 2007-11-15 2011-01-12 Musc Found For Res Dev PROTEIN INHIBITORS PIM KINASES, COMPOSITIONS AND METHODS FOR TREATING CANCER
BRPI0820544A2 (pt) 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
GB0723815D0 (en) 2007-12-05 2008-01-16 Glaxo Group Ltd Compounds
CN101977923B (zh) 2008-01-18 2014-10-08 捷克有机化学和生物化学研究院 抑制细胞生长的7-脱氮嘌呤核苷
CA2714181C (en) 2008-02-04 2013-12-24 Mercury Therapeutics, Inc. Ampk modulators
AR070531A1 (es) 2008-03-03 2010-04-14 Novartis Ag Inhibidores de cinasa pim y metodos para su uso
BRPI0909040B8 (pt) 2008-03-11 2021-05-25 Incyte Holdings Corp derivados de azetidina e ciclobutano, seus usos, e composição
AU2009227013B2 (en) 2008-03-21 2013-01-10 Novartis Ag Novel heterocyclic compounds and uses therof
WO2009155156A1 (en) 2008-06-18 2009-12-23 Merck & Co., Inc. Inhibitors of janus kinases
CA2726836C (en) 2008-06-26 2019-06-18 Anterios, Inc. Use of nanoemulsions in the manufacture of a medicament for treating skin disorders
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
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
WO2010022081A1 (en) 2008-08-19 2010-02-25 Array Biopharma Inc. Triazolopyridine compounds as pim kinase inhibitors
SI2384326T1 (sl) 2008-08-20 2014-06-30 Zoetis Llc Pirolo(2,3-d)pirimidinske spojine
KR20110058866A (ko) 2008-09-02 2011-06-01 노파르티스 아게 비시클릭 키나제 억제제
US8329732B2 (en) 2008-09-02 2012-12-11 Novartis Ag Kinase inhibitors and methods of their use
BRPI0918846A2 (pt) 2008-09-02 2019-09-24 Novartis Ag inibidores de cinase heterocíclica
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.
EP2350054A4 (en) 2008-10-17 2012-03-28 Merck Canada Inc AZETIDINE DERIVATIVES AS INHIBITORS OF THE STEAROYL COENZYME A DELTA 9 DESATURASE
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
HUE046493T2 (hu) 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
EP2451813B1 (en) 2009-07-08 2014-10-01 Leo Pharma A/S Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors
US20120157500A1 (en) 2009-08-24 2012-06-21 Weikang Tao Jak inhibition blocks rna interference associated toxicities
TW201111385A (en) 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
SG10201405568UA (en) 2009-09-08 2014-11-27 Hoffmann La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
EP2305660A1 (en) 2009-09-25 2011-04-06 Almirall, S.A. New thiadiazole derivatives
PT2486041E (pt) 2009-10-09 2013-11-14 Incyte Corp Derivados hidroxilo, ceto e glucuronido de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciclopentil-propanonitrilo
EP2491039A1 (en) 2009-10-20 2012-08-29 Cellzome Limited Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors
US8671402B2 (en) 2009-11-09 2014-03-11 Bank Of America Corporation Network-enhanced control of software updates received via removable computer-readable medium
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
WO2011066378A2 (en) 2009-11-24 2011-06-03 Alder Biopharmaceuticals, Inc. Antagonists of il-6 to prevent or treat thrombosis
US20130129675A1 (en) 2009-12-04 2013-05-23 Board Of Regents, The University Of Texas System Interferon therapies in combination with blockade of stat3 activation
ES2461967T3 (es) 2009-12-18 2014-05-21 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
US8461328B2 (en) 2010-01-12 2013-06-11 Genentech, Inc. Tricyclic heterocyclic compounds, compositions and methods of use thereof
EP2531508A1 (en) 2010-02-05 2012-12-12 Pfizer Inc. Pyrrolo [ 2, 3 - d]pyrimidine urea compounds as jak inhibitors
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
JP5858434B2 (ja) 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
DK3050882T3 (en) 2010-03-10 2018-03-19 Incyte Holdings Corp PIPERIDIN-4-YL-AZETIDINE DERIVATIVES AS JAK1 INHIBITORS
UA109131C2 (ru) 2010-04-14 2015-07-27 Еррей Біофарма Інк. 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ
EP2390252A1 (en) 2010-05-19 2011-11-30 Almirall, S.A. New pyrazole derivatives
ME02445B (me) 2010-05-21 2016-09-20 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
US9351943B2 (en) 2010-07-01 2016-05-31 Matthew T. McLeay Anti-fibroblastic fluorochemical emulsion therapies
WO2012045010A1 (en) 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combinations of 4-(3-(2h-1,2,3-triazo-2-yl) phenylamino)-2-((1r,2s)-2-aminocyclohexylamino) pyrimidine-5-carboxamide and fludarabine
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
UA113156C2 (xx) 2010-11-19 2016-12-26 Циклобутилзаміщені похідні піролопіридину й піролопіримідину як інгібітори jak
CN104473933A (zh) 2010-12-03 2015-04-01 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
JP5936628B2 (ja) 2011-02-18 2016-06-22 ノバルティス・ファルマ・アクチェンゲゼルシャフトＮｏｖａｒｔｉｓ Ｐｈａｒｍａ ＡＧ ｍＴＯＲ／ＪＡＫ阻害剤併用療法
CN102247368B (zh) 2011-05-19 2013-05-29 安徽永生堂药业有限责任公司 一种复方阿伐斯汀缓释片及其制备方法
CN102218042A (zh) 2011-05-26 2011-10-19 青岛黄海制药有限责任公司 富马酸喹硫平组合物的缓释片剂及其制备方法
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives 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
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
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
US10155987B2 (en) 2012-06-12 2018-12-18 Dana-Farber Cancer Institute, Inc. Methods of predicting resistance to JAK inhibitor therapy
CA2876306C (en) 2012-06-15 2024-02-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of ruxolitinib
US20150246043A1 (en) 2012-07-27 2015-09-03 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
CN102772384A (zh) 2012-08-07 2012-11-14 四川百利药业有限责任公司 一种盐酸米诺环素缓释片及其制备方法
WO2014036016A1 (en) 2012-08-31 2014-03-06 Principia Biopharma Inc. Benzimidazole derivatives as itk inhibitors
SG10201703533VA (en) 2012-11-01 2017-06-29 Incyte Corp Tricyclic fused thiophene derivatives as jak inhibitors
PE20151157A1 (es) 2012-11-15 2015-08-19 Incyte Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
PE20151902A1 (es) 2013-03-06 2015-12-26 Incyte Corp Proceso e intermedios para hacer un inhibidor de jak
EP4275756A3 (en) 2013-05-17 2024-02-07 Incyte Holdings Corporation Bipyrazole derivatives as jak inhibitors
RS60469B1 (sr) 2013-08-07 2020-07-31 Incyte Corp Dozni oblici sa produženim oslobađanjem za jak1 inhibitor
MX2016002165A (es) 2013-08-20 2017-01-05 Incyte Corp Beneficio de supervivencia en pacientes con tumores solidos con niveles elevados de proteina c reactiva.
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
MA54622A (fr) 2014-04-08 2021-11-03 Incyte Corp Traitement d'affections malignes par lymphocytes b par un inhibiteur jak et pi3k combiné
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
ES2946179T3 (es) 2014-05-28 2023-07-13 Onco Tracker Inc Efectos antineoplásicos de inhibidores de JAK2 en combinación con derivados de talidomida y glucocorticoides
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
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
KR20210124345A (ko) 2019-02-06 2021-10-14 콘서트 파마슈티컬즈, 인크. 거울상 이성질체 풍부한 jak 억제제를 제조하는 방법

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