SG10201703533VA - Tricyclic fused thiophene derivatives as jak inhibitors - Google Patents

Tricyclic fused thiophene derivatives as jak inhibitors

Info

Publication number
SG10201703533VA
SG10201703533VA SG10201703533VA SG10201703533VA SG10201703533VA SG 10201703533V A SG10201703533V A SG 10201703533VA SG 10201703533V A SG10201703533V A SG 10201703533VA SG 10201703533V A SG10201703533V A SG 10201703533VA SG 10201703533V A SG10201703533V A SG 10201703533VA
Authority
SG
Singapore
Prior art keywords
jak inhibitors
thiophene derivatives
tricyclic fused
fused thiophene
tricyclic
Prior art date
Application number
SG10201703533VA
Inventor
Yun-Long Li
Wenyu Zhu
Song Mei
Joseph Glenn
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=49578588&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG10201703533V(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of SG10201703533VA publication Critical patent/SG10201703533VA/en

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
SG10201703533VA 2012-11-01 2013-10-31 Tricyclic fused thiophene derivatives as jak inhibitors SG10201703533VA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261721308P 2012-11-01 2012-11-01
US201361783850P 2013-03-14 2013-03-14

Publications (1)

Publication Number Publication Date
SG10201703533VA true SG10201703533VA (en) 2017-06-29

Family

ID=49578588

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201503141TA SG11201503141TA (en) 2012-11-01 2013-10-31 Tricyclic fused thiophene derivatives as jak inhibitors
SG10201703533VA SG10201703533VA (en) 2012-11-01 2013-10-31 Tricyclic fused thiophene derivatives as jak inhibitors

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG11201503141TA SG11201503141TA (en) 2012-11-01 2013-10-31 Tricyclic fused thiophene derivatives as jak inhibitors

Country Status (22)

Country Link
US (6) US9181271B2 (en)
EP (1) EP2917221A1 (en)
JP (2) JP6359546B2 (en)
KR (1) KR20150074193A (en)
CN (2) CN104918945B (en)
AR (1) AR093308A1 (en)
AU (2) AU2013337824B2 (en)
BR (1) BR112015009942A2 (en)
CA (1) CA2888816A1 (en)
CL (1) CL2015001160A1 (en)
CR (1) CR20150255A (en)
EA (1) EA031882B1 (en)
HK (1) HK1214823A1 (en)
IL (2) IL238410B (en)
MX (1) MX2015005428A (en)
NZ (1) NZ707495A (en)
PE (1) PE20151141A1 (en)
PH (1) PH12015500963B1 (en)
SG (2) SG11201503141TA (en)
TW (1) TWI646099B (en)
UA (1) UA117572C2 (en)
WO (1) WO2014071031A1 (en)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2611588T3 (en) 2005-12-13 2017-05-09 Incyte Holdings Corporation Pyrrolo [2,3-b] pyridines and pyrrolo [2,3-b] pyrimidines substituted with heteroaryl as Janus kinase inhibitors
LT3070090T (en) 2007-06-13 2019-06-25 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
EA020494B1 (en) 2009-05-22 2014-11-28 Инсайт Корпорейшн 3-[4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANENITRILE AS JAK INHIBITORS
EA025520B1 (en) 2009-05-22 2017-01-30 Инсайт Холдингс Корпорейшн 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
CN104945420A (en) 2009-06-29 2015-09-30 因塞特公司 Pyrimidinones as PI3K 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
NZ602313A (en) 2010-03-10 2014-08-29 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
ME02445B (en) 2010-05-21 2016-09-20 Incyte Holdings Corp Topical formulation for a jak inhibitor
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
AR084366A1 (en) 2010-12-20 2013-05-08 Incyte Corp N- (1- (REPLACED PHENYL) ETIL) -9H-PURIN-6-AMINAS AS PI3K INHIBITORS
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
HUE043703T2 (en) 2011-09-02 2019-09-30 Incyte Holdings Corp Heterocyclylamines as pi3k inhibitors
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
AR090548A1 (en) 2012-04-02 2014-11-19 Incyte Corp BICYCLIC AZAHETEROCICLOBENCILAMINS AS PI3K INHIBITORS
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
CN104918945B (en) * 2012-11-01 2018-01-05 因赛特公司 Tricyclic condensed thiophene derivant as JAK inhibitor
LT2919766T (en) 2012-11-15 2021-09-27 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
JP6437452B2 (en) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
JP6554037B2 (en) 2013-01-15 2019-07-31 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Thiazole carboxamide and pyridine carboxamide compounds useful as PIM kinase inhibitors
SG10201707259PA (en) 2013-03-06 2017-10-30 Incyte Corp Processes and intermediates for making a jak inhibitor
US9096596B2 (en) 2013-03-14 2015-08-04 Janssen Pharmaceutica Nv P2X7 modulators
TWI644671B (en) 2013-03-14 2018-12-21 比利時商健生藥品公司 P2x7 modulators
US10053463B2 (en) 2013-03-14 2018-08-21 Janssen Pharmaceutica Nv Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
ES2845473T3 (en) 2013-03-14 2021-07-26 Boehringer Ingelheim Int (Benzyl-cyano-methyl) -substituted amides of 2-aza-bicyclo [2.2.1] heptane-3-carboxylic acid cathepsin-C inhibitors
JO3509B1 (en) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv P2x7 modulators
SI2997023T1 (en) 2013-05-17 2017-07-31 Incyte Corporation Bipyrazole derivatives as jak inhibitors
ES2792549T3 (en) 2013-08-07 2020-11-11 Incyte Corp Sustained-release dosage forms for a JAK1 inhibitor
AU2014308703A1 (en) 2013-08-23 2016-03-24 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as Pim kinase inhibitors
WO2015131031A1 (en) * 2014-02-28 2015-09-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
ES2829914T3 (en) 2014-04-08 2021-06-02 Incyte Corp Treatment of malignant B cell diseases using a combination of JAK and PI3K inhibitor
PE20170300A1 (en) 2014-04-30 2017-04-19 Incyte Corp PROCESSES TO PREPARE A JAK 1 INHIBITOR AND NEW FORMS OF IT
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
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
DK3191487T3 (en) 2014-09-12 2019-10-28 Boehringer Ingelheim Int SPIROCYCLIC CATHEPSIN-C INHIBITORS
EP3191492B1 (en) 2014-09-12 2019-01-09 Janssen Pharmaceutica NV P2x7 modulators
WO2016130501A1 (en) 2015-02-09 2016-08-18 Incyte Corporation Aza-heteroaryl compounds as pi3k-gamma inhibitors
TWI764392B (en) 2015-02-27 2022-05-11 美商英塞特公司 Salts and processes of preparing a pi3k inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
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
TWI734699B (en) 2015-09-09 2021-08-01 美商英塞特公司 Salts of a pim kinase inhibitor
TW201718546A (en) 2015-10-02 2017-06-01 英塞特公司 Heterocyclic compounds useful as PIM kinase inhibitors
WO2017079519A1 (en) 2015-11-06 2017-05-11 Incyte Corporation Heterocyclic compounds as pi3k-gamma inhibitors
AR107293A1 (en) 2016-01-05 2018-04-18 Incyte Corp PIRIDINE AND PYRIDIMINE COMPOUNDS AS PI3K-g INHIBITORS
CA3019145A1 (en) 2016-03-28 2017-10-05 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
US10738060B2 (en) * 2016-10-03 2020-08-11 TLL Pharmaceutical, LLC JAK1 selective inhibitors and uses thereof
AU2018208516B2 (en) * 2017-01-11 2021-07-08 Aqilion Ab Novel amino-imidazopyridine derivatives as Janus kinase inhibitors and pharmaceutical use thereof
LT3687996T (en) 2017-09-27 2022-01-10 Incyte Corporation Salts of pyrrolotriazine derivatives useful as tam inhibitors
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
AR114810A1 (en) 2018-01-30 2020-10-21 Incyte Corp PROCESSES AND INTERMEDIATES TO DEVELOP A JAK INHIBITOR
CN111936135A (en) 2018-02-16 2020-11-13 因赛特公司 JAK1 pathway inhibitors for the treatment of cytokine-related disorders
AU2019245420A1 (en) * 2018-03-30 2020-11-12 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
JP2021519772A (en) 2018-03-30 2021-08-12 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Biomarker for inflammatory skin diseases
EP3775923A1 (en) 2018-04-13 2021-02-17 Incyte Corporation Biomarkers for graft-versus-host disease
PE20211805A1 (en) 2018-06-29 2021-09-14 Incyte Corp FORMULATIONS OF AN AXL / MER INHIBITOR
CN112384514A (en) 2018-07-06 2021-02-19 利奥制药有限公司 Novel amino-imidazopyrimidine derivatives as JANUS kinase inhibitors and pharmaceutical use thereof
MX2021002551A (en) 2018-09-05 2021-07-15 Incyte Corp Crystalline forms of a phosphoinositide 3-kinase (pi3k) inhibitor.
WO2020065613A1 (en) 2018-09-28 2020-04-02 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
MX2021003661A (en) 2018-09-28 2021-08-19 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators.
MX2021004946A (en) 2018-10-31 2021-07-15 Incyte Corp Combination therapy for treatment of hematological diseases.
TW202038944A (en) 2018-12-19 2020-11-01 美商英塞特公司 Jak1 pathway inhibitors for the treatment of gastrointestinal disease
EA202192426A1 (en) 2019-03-05 2021-11-15 Инсайт Корпорейшн JAK1 PATH INHIBITORS FOR THE TREATMENT OF CHRONIC ALLOTRANSPLANT DYSFUNCTION
TW202102222A (en) 2019-03-19 2021-01-16 美商英塞特公司 Biomarkers for vitiligo
EP4248967A3 (en) * 2019-06-06 2023-10-11 Hangzhou Highlightll Pharmaceutical Co., Ltd. Synthesis method of furoimidazopyridine compound, crystal form of furoimidazopyridine compound, and crystal form of salt thereof
EP3981398A4 (en) * 2019-06-06 2023-03-15 Hangzhou Highlightll Pharmaceutical Co., Ltd. Method for synthesizing furoimidazopyridine compound, polymorphic substance and polymorphic substance of salt
US11839663B2 (en) 2019-09-30 2023-12-12 Janssen Pharmaceutica Nv Radiolabelled MGL pet ligands
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
JP2023506118A (en) * 2019-10-16 2023-02-15 インサイト・コーポレイション Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (LP)
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)
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
CN111297870B (en) * 2020-03-20 2021-03-26 中国医学科学院医药生物技术研究所 Application of nitrobenzoic acid compounds in preparation of drugs for treating tumors
WO2021191359A1 (en) 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
AU2021283271A1 (en) 2020-06-02 2022-12-15 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
CA3204186A1 (en) 2020-12-04 2022-06-09 Incyte Corporation Jak inhibitor with a vitamin d analog for treatment of skin diseases
EP4259131A1 (en) 2020-12-08 2023-10-18 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
WO2022150676A1 (en) 2021-01-11 2022-07-14 Incyte Corporation Combination therapy comprising jak pathway inhibitor and rock inhibitor
US20220378746A1 (en) 2021-05-03 2022-12-01 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
WO2023283345A1 (en) 2021-07-07 2023-01-12 Incyte Corporation Anti-b7-h4 antibodies and uses thereof
TW202330623A (en) 2021-12-08 2023-08-01 美商英塞特公司 Anti-mutant calreticulin (calr) antibodies and uses thereof
WO2024030600A1 (en) 2022-08-05 2024-02-08 Incyte Corporation Treatment of urticaria using jak inhibitors

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1306260C (en) 1985-10-18 1992-08-11 Shionogi & Co., Ltd. Condensed imidazopyridine derivatives
JP2513001B2 (en) 1988-11-01 1996-07-03 山川薬品工業株式会社 Method for racemization of optically active tetrahydrofuran-2-carboxylic acid
JPH02225463A (en) 1989-02-27 1990-09-07 Nissan Chem Ind Ltd Racemization of n-acetyl-indoline-2-carboxylic acid ester
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
FR2695126B1 (en) 1992-08-27 1994-11-10 Sanofi Elf Thienyl or pyrrolyl carboxylic acid derivatives, their preparation and medicaments containing them.
JP3178301B2 (en) 1994-08-08 2001-06-18 東レ株式会社 Process for producing racemic aliphatic heterocyclic carboxylate
EP0727217A3 (en) 1995-02-10 1997-01-15 Suntory Ltd Pharmaceutical composition containing god-type ellagitannin as active ingredient
US6025366A (en) * 1998-04-02 2000-02-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU5620299A (en) 1998-08-11 2000-03-06 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
JP2000119271A (en) * 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd 1h-imidazopyridine derivative
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
WO2002016370A1 (en) 2000-08-22 2002-02-28 Hokuriku Seiyaku Co., Ltd. 1h-imidazopyridine derivatives
JP2003002890A (en) 2000-08-22 2003-01-08 Hokuriku Seiyaku Co Ltd 1h-imidazopyridine derivative
IL160915A0 (en) 2001-09-19 2004-08-31 Aventis Pharma Sa Indolizines inhibiting kinase proteins
TWI302836B (en) 2001-10-30 2008-11-11 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
JP4374222B2 (en) 2003-09-01 2009-12-02 Ｈｏｙａ株式会社 Variable magnification optical system
AR045944A1 (en) 2003-09-24 2005-11-16 Novartis Ag ISOQUINOLINE DERIVATIVES 1.4-DISPOSED
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
MXPA06014247A (en) 2004-06-10 2007-03-12 Irm Llc Compounds and compositions as protein kinase inhibitors.
CN101106983A (en) 2004-11-24 2008-01-16 诺瓦提斯公司 Combinations comprising JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
AR054416A1 (en) 2004-12-22 2007-06-27 Incyte Corp PIRROLO [2,3-B] PIRIDIN-4-IL-AMINAS AND PIRROLO [2,3-B] PIRIMIDIN-4-IL-AMINAS AS INHIBITORS OF THE JANUS KINASES. PHARMACEUTICAL COMPOSITIONS.
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
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
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
ES2611588T3 (en) 2005-12-13 2017-05-09 Incyte Holdings Corporation Pyrrolo [2,3-b] pyridines and pyrrolo [2,3-b] pyrimidines substituted with heteroaryl as Janus kinase inhibitors
AU2007275577A1 (en) * 2006-07-21 2008-01-24 Vertex Pharmaceuticals Incorporated CGRP receptor antagonists
EP2118088B1 (en) * 2006-12-20 2012-05-30 Amgen Inc. Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
LT3070090T (en) 2007-06-13 2019-06-25 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
CL2008001709A1 (en) 2007-06-13 2008-11-03 Incyte Corp Compounds derived from pyrrolo [2,3-b] pyrimidine, jak kinase modulators; pharmaceutical composition; and use in the treatment of diseases such as cancer, psoriasis, rheumatoid arthritis, among others.
AU2008321046B2 (en) 2007-11-16 2013-10-24 Incyte Holdings Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
SG191660A1 (en) 2008-03-11 2013-07-31 Incyte Corp Azetidine and cyclobutane derivatives as jak inhibitors
WO2009155156A1 (en) * 2008-06-18 2009-12-23 Merck & Co., Inc. Inhibitors of janus kinases
CA2727036C (en) * 2008-06-20 2017-03-21 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
CL2009001884A1 (en) 2008-10-02 2010-05-14 Incyte Holdings Corp Use of 3-cyclopentyl-3- [4- (7h-pyrrolo [2,3-d] pyrimidin-4-yl) -1h-pyrazol-1-yl) propanonitrile, janus kinase inhibitor, and use of a composition that understands it for the treatment of dry eye.
JOP20190230A1 (en) 2009-01-15 2017-06-16 Incyte Corp Processes for preparing jak inhibitors and related intermediate compounds
EA020494B1 (en) 2009-05-22 2014-11-28 Инсайт Корпорейшн 3-[4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]OCTANE- OR HEPTANENITRILE AS JAK INHIBITORS
EA025520B1 (en) 2009-05-22 2017-01-30 Инсайт Холдингс Корпорейшн 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
US9346809B2 (en) * 2009-07-08 2016-05-24 Leo Pharma A/S Heterocyclic compounds as JAK receptor and protein tyrosine 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
US8486902B2 (en) 2009-10-09 2013-07-16 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d] pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
TW201129565A (en) * 2010-01-12 2011-09-01 Hoffmann La Roche Tricyclic heterocyclic compounds, compositions and methods of use thereof
CA2790070C (en) 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
NZ602313A (en) 2010-03-10 2014-08-29 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
ME02445B (en) 2010-05-21 2016-09-20 Incyte Holdings Corp Topical formulation for a jak inhibitor
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CN103732226B (en) 2011-02-18 2016-01-06 诺瓦提斯药物公司 MTOR/JAK inhibitor combination treatment
SI2684880T1 (en) 2011-03-10 2018-08-31 Daiichi Sankyo Company, Limited Dispiropyrrolidine derivative
WO2012177606A1 (en) 2011-06-20 2012-12-27 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
JP2014521725A (en) 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト JAKPI3K / mTOR combination therapy
TW201313721A (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
CN104918945B (en) 2012-11-01 2018-01-05 因赛特公司 Tricyclic condensed thiophene derivant as JAK inhibitor
LT2919766T (en) 2012-11-15 2021-09-27 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
SG10201707259PA (en) 2013-03-06 2017-10-30 Incyte Corp Processes and intermediates for making a jak inhibitor
SI2997023T1 (en) 2013-05-17 2017-07-31 Incyte Corporation Bipyrazole derivatives as jak inhibitors
ES2792549T3 (en) 2013-08-07 2020-11-11 Incyte Corp Sustained-release dosage forms for a JAK1 inhibitor
AU2014309017A1 (en) * 2013-08-20 2016-03-10 Incyte Corporation Survival benefit in patients with solid tumors with elevated C-reactive protein levels
WO2015131031A1 (en) 2014-02-28 2015-09-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
ES2829914T3 (en) * 2014-04-08 2021-06-02 Incyte Corp Treatment of malignant B cell diseases using a combination of JAK and PI3K inhibitor
PE20170300A1 (en) * 2014-04-30 2017-04-19 Incyte Corp PROCESSES TO PREPARE A JAK 1 INHIBITOR AND NEW FORMS OF IT
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
US10077277B2 (en) * 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
US10053465B2 (en) * 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
CN111936135A (en) * 2018-02-16 2020-11-13 因赛特公司 JAK1 pathway inhibitors for the treatment of cytokine-related disorders
JP2021519772A (en) * 2018-03-30 2021-08-12 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Biomarker for inflammatory skin diseases
AU2019245420A1 (en) * 2018-03-30 2020-11-12 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
EP3775923A1 (en) * 2018-04-13 2021-02-17 Incyte Corporation Biomarkers for graft-versus-host disease
MX2021004946A (en) * 2018-10-31 2021-07-15 Incyte Corp Combination therapy for treatment of hematological diseases.
TW202102222A (en) * 2019-03-19 2021-01-16 美商英塞特公司 Biomarkers for vitiligo

Also Published As

Publication number Publication date
US9908895B2 (en) 2018-03-06
IL257066A (en) 2018-03-29
IL238410B (en) 2018-02-28
US20140121198A1 (en) 2014-05-01
JP6359546B2 (en) 2018-07-18
SG11201503141TA (en) 2015-06-29
NZ707495A (en) 2019-01-25
TW201422624A (en) 2014-06-16
PH12015500963A1 (en) 2015-08-17
CR20150255A (en) 2015-09-09
TWI646099B (en) 2019-01-01
MX2015005428A (en) 2015-07-21
WO2014071031A1 (en) 2014-05-08
US20180148460A1 (en) 2018-05-31
US11851442B2 (en) 2023-12-26
US9777017B2 (en) 2017-10-03
PH12015500963B1 (en) 2015-08-17
CN104918945B (en) 2018-01-05
CN104918945A (en) 2015-09-16
CA2888816A1 (en) 2014-05-08
US9181271B2 (en) 2015-11-10
BR112015009942A2 (en) 2017-07-11
JP2015535288A (en) 2015-12-10
US20200040002A1 (en) 2020-02-06
CN107936039A (en) 2018-04-20
AU2013337824A1 (en) 2015-05-14
EA031882B1 (en) 2019-03-29
US10370387B2 (en) 2019-08-06
IL238410A0 (en) 2015-06-30
PE20151141A1 (en) 2015-08-06
UA117572C2 (en) 2018-08-27
HK1214823A1 (en) 2016-08-05
US20210387998A1 (en) 2021-12-16
AR093308A1 (en) 2015-05-27
US11161855B2 (en) 2021-11-02
CL2015001160A1 (en) 2015-08-28
AU2013337824B2 (en) 2018-03-08
US20160015695A1 (en) 2016-01-21
EP2917221A1 (en) 2015-09-16
US20160024109A1 (en) 2016-01-28
EA201590850A1 (en) 2015-09-30
AU2018204090A1 (en) 2018-06-28
JP2018141020A (en) 2018-09-13
KR20150074193A (en) 2015-07-01

Similar Documents

Publication Publication Date Title
IL257066A (en) Tricyclic fused thiophene derivatives as jak inhibitors
HUS2200040I1 (en) Benzimidazole-proline derivatives
IL245309B (en) Tricyclic heterocyclic compounds as jak inhibitors
HK1206722A1 (en) New bicyclic derivatives
IL227252A0 (en) Fused aminodihydrothiazine derivatives
HK1206723A1 (en) Thienopyrimidines
EP2862853A4 (en) Fused heterocyclic compound
EP2865671A4 (en) Fused heterocyclic compound
EP2857396A4 (en) Fused heterocyclic compound
EP2857397A4 (en) Fused heterocyclic compound
GB201101140D0 (en) Fused aminodihydrothiazine derivatives
HK1205740A1 (en) Pyrrolotriazinone derivatives
HK1205508A1 (en) New bicyclicpyridine derivatives
EP2865672A4 (en) Fused heterocyclic compound
EP2824106A4 (en) Tricyclic compound
AP2015008347A0 (en) Oxazolidin-2-one-pyrimidine derivatives
LT2838883T (en) New phenyl-tetrahydroisoquinoline derivatives
SG11201404325VA (en) Pyrimidooxazocine derivatives as mtor - inhibitors
HK1208997A1 (en) Novel cabergoline derivatives
GB201215033D0 (en) Diazepinone derivatives
GB201219689D0 (en) Novel Heteroaromatic derivatives I
GB201119592D0 (en) Novel heteroaromatic Derivatives I
GB201100183D0 (en) Fused aminodihydropyrimidone derivatives
AU2012177V (en) Daispanfunk Pandorea jasminoides