SMT202000244T1 - Composti di tiazolocarbossammide e piridincarbossammide utili come inibitori di chinasi pim - Google Patents

Composti di tiazolocarbossammide e piridincarbossammide utili come inibitori di chinasi pim

Info

Publication number
SMT202000244T1
SMT202000244T1 SM20200244T SMT202000244T SMT202000244T1 SM T202000244 T1 SMT202000244 T1 SM T202000244T1 SM 20200244 T SM20200244 T SM 20200244T SM T202000244 T SMT202000244 T SM T202000244T SM T202000244 T1 SMT202000244 T1 SM T202000244T1
Authority
SM
San Marino
Prior art keywords
thiazolecarboxamides
kinase inhibitors
compounds useful
pim kinase
pyridinecarboxamide compounds
Prior art date
Application number
SM20200244T
Other languages
English (en)
Italian (it)
Inventor
Chu-Biao Xue
Anlai Wang
Wenqing Yao
Yun-Long Li
Jincong Zhuo
Fenglei Zhang
Hao Feng
Jun Pan
Ke Zhang
Original Assignee
Incyte Holdings Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of SMT202000244T1 publication Critical patent/SMT202000244T1/it

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
    • A61K31/4355—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 oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D495/02—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 two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
SM20200244T 2013-01-15 2014-01-14 Composti di tiazolocarbossammide e piridincarbossammide utili come inibitori di chinasi pim SMT202000244T1 (it)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361752897P 2013-01-15 2013-01-15
US201361790952P 2013-03-15 2013-03-15
US201361859118P 2013-07-26 2013-07-26
PCT/US2014/011486 WO2014113388A1 (en) 2013-01-15 2014-01-14 Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
EP14702389.9A EP2945939B1 (en) 2013-01-15 2014-01-14 Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors

Publications (1)

Publication Number Publication Date
SMT202000244T1 true SMT202000244T1 (it) 2020-07-08

Family

ID=50031607

Family Applications (1)

Application Number Title Priority Date Filing Date
SM20200244T SMT202000244T1 (it) 2013-01-15 2014-01-14 Composti di tiazolocarbossammide e piridincarbossammide utili come inibitori di chinasi pim

Country Status (35)

Country Link
US (7) US9200004B2 (enExample)
EP (3) EP3670506B1 (enExample)
JP (3) JP6554037B2 (enExample)
KR (2) KR102311840B1 (enExample)
CN (2) CN105051029B (enExample)
AR (1) AR094664A1 (enExample)
AU (3) AU2014207691B2 (enExample)
BR (2) BR122019024759B1 (enExample)
CA (1) CA2897333C (enExample)
CL (1) CL2015001985A1 (enExample)
CR (1) CR20150412A (enExample)
CY (1) CY1122933T1 (enExample)
DK (1) DK2945939T3 (enExample)
EA (1) EA035929B1 (enExample)
EC (1) ECSP15035343A (enExample)
ES (2) ES2790419T3 (enExample)
HR (1) HRP20200770T1 (enExample)
HU (1) HUE050215T2 (enExample)
IL (1) IL239886B (enExample)
LT (1) LT2945939T (enExample)
ME (1) ME03780B (enExample)
MX (2) MX376306B (enExample)
NZ (2) NZ749911A (enExample)
PE (2) PE20191245A1 (enExample)
PH (2) PH12015501567A1 (enExample)
PL (1) PL2945939T3 (enExample)
PT (1) PT2945939T (enExample)
RS (1) RS60244B1 (enExample)
SG (3) SG10201705662WA (enExample)
SI (1) SI2945939T1 (enExample)
SM (1) SMT202000244T1 (enExample)
TW (2) TWI662030B (enExample)
UA (1) UA121098C2 (enExample)
WO (1) WO2014113388A1 (enExample)
ZA (1) ZA202108141B (enExample)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3409278T3 (pl) 2011-07-21 2021-02-22 Sumitomo Pharma Oncology, Inc. Heterocykliczne inhibitory kinazy białkowej
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
CA2897200C (en) 2013-01-14 2021-07-06 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
PE20191245A1 (es) * 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
LT3212629T (lt) * 2014-10-31 2019-01-10 Genoscience Pharma Sas Pakeistieji 2,4 diamino-chinolinai, kaip nauji priešvėžiniai agentai
CN104876929B (zh) * 2015-05-15 2016-10-05 华南理工大学 一种1,2,3,4-四氢萘啶类化合物的合成方法及应用
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) * 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2016358100B2 (en) 2015-11-19 2021-05-27 Incyte Corporation Heterocyclic compounds as immunomodulators
TW201726623A (zh) 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
TWI850624B (zh) 2015-12-22 2024-08-01 美商英塞特公司 作為免疫調節劑之雜環化合物
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
DK3472167T3 (da) 2016-06-20 2022-09-05 Incyte Corp Heterocykliske forbindelser som immunomodulatorer
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
CN106336371A (zh) * 2016-08-16 2017-01-18 成都百事兴科技实业有限公司 叔丁氧羰基‑l‑焦谷氨酸甲酯的合成方法
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3558963B1 (en) 2016-12-22 2022-03-23 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
EP3558973B1 (en) 2016-12-22 2021-09-15 Incyte Corporation Pyridine derivatives as immunomodulators
ES2929193T3 (es) 2016-12-22 2022-11-25 Incyte Corp Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de la internalización de PD-L1
IL295660A (en) 2016-12-22 2022-10-01 Incyte Corp Benzooxazole derivatives as immunomodulators
WO2018177993A1 (de) 2017-03-31 2018-10-04 Bayer Cropscience Aktiengesellschaft Pyrazole zur bekämpfung von arthropoden
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
TWI903299B (zh) 2018-03-08 2025-11-01 美商英塞特公司 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物
RS64055B1 (sr) 2018-03-30 2023-04-28 Incyte Corp Heterociklična jedinjenja kao imunomodulatori
CN117959303A (zh) 2018-04-13 2024-05-03 住友制药肿瘤公司 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂
EP4219492B1 (en) 2018-05-11 2024-11-27 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CA3118919A1 (en) * 2018-11-09 2020-05-14 Prelude Therapeutics, Incorporated Spiro-sulfonamide derivatives as inhibitors of myeloid cell leukemia-1 (mcl-1) protein
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
US12303515B2 (en) * 2019-04-30 2025-05-20 City University Of Hong Kong PIM1 inhibitors for use in treatment of viral infection and pharmaceutical compositions thereof
EP3997081A1 (en) 2019-07-11 2022-05-18 Escape Bio, Inc. Indazoles and azaindazoles as lrrk2 inhibitors
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
EP4037773A1 (en) 2019-09-30 2022-08-10 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
EP4240739A1 (en) 2020-11-06 2023-09-13 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
WO2023170024A1 (en) * 2022-03-11 2023-09-14 University Of Copenhagen Camk2 modulators and their use in medicine
EP4611753A1 (en) 2022-10-31 2025-09-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
US20250171435A1 (en) * 2023-11-27 2025-05-29 Rubedo Life Sciences, Inc. Carbon Linked BCL Inhibitors and Senolytic Compounds and Uses Thereof

Family Cites Families (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60105023T2 (de) 2000-06-28 2005-08-18 Smithkline Beecham P.L.C., Brentford Nassvermahlungsverfahren
WO2002055489A2 (en) 2000-12-27 2002-07-18 Univ Columbia Pim kinase-related methods
DE10123055A1 (de) 2001-05-11 2003-03-20 Gruenenthal Gmbh Screeningverfahren mit PIM1-Kinase oder PIM3-Kinase
DE10226702A1 (de) 2002-06-14 2004-09-09 Grünenthal GmbH Antisense Oligonukleotide gegen PIM1
CA2503905A1 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
WO2006078228A1 (en) 2002-09-16 2006-07-27 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
TW200413273A (en) * 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
CL2003002287A1 (es) 2002-11-25 2005-01-14 Wyeth Corp COMPUESTOS DERIVADOS DE TIENO[3,2-b]-PIRIDINA-6-CARBONITRILOS Y TIENEO[2,3-b]-PIRIDINA-5-CARBONITRILOS, COMPOSICION FARMACEUTICA, PROCEDIMIENTO DE PREPARACION Y COMPUESTOS INTERMEDIARIOS, Y SU USO EN EL TRATAMIENTO DEL CANCER, APOPLEJIA, OSTEOPOROSIS
WO2004090106A2 (en) 2003-04-04 2004-10-21 Vertex Pharmaceuticals Incorporated Crystal structures of human pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design
WO2005028624A2 (en) 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
WO2005033310A1 (de) 2003-10-01 2005-04-14 Grünenthal GmbH Pim-1-spezifische dsrna-verbindungen
WO2006006569A1 (ja) 2004-07-12 2006-01-19 Nihon Nohyaku Co., Ltd. フェニルピリジン類又はその塩類、これらを有効成分とする除草剤及びその使用方法
WO2006071960A2 (en) 2004-12-28 2006-07-06 Kinex Pharmaceuticals, Llc Compositions and methods of treating cell proliferation disorders
PL2395004T3 (pl) 2005-06-22 2016-08-31 Plexxikon Inc Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej
WO2007011760A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
WO2007044724A2 (en) 2005-10-06 2007-04-19 Exelixis, Inc. Aminopyrimidine, aminopyridine and aniline derivatives inhibitors of pim-i and/or pim-3
US7776865B2 (en) 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
JP5119157B2 (ja) 2005-10-21 2013-01-16 エクセリクシス， インク． カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピラゾロ−ピリミジン類
WO2007052843A1 (ja) 2005-11-04 2007-05-10 Takeda Pharmaceutical Company Limited 複素環アミド化合物およびその用途
WO2007084857A2 (en) 2006-01-13 2007-07-26 President And Fellows Of Harvard College Methods and compositions for treating cell proliferative disorders
WO2007131191A2 (en) 2006-05-05 2007-11-15 Perkinelmer Life And Analytical Sciences Mass spectrometry methods for multiplexed quantification of protein kinases and phosphatases
WO2008002676A2 (en) 2006-06-29 2008-01-03 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
AU2007265373B2 (en) 2006-06-29 2013-02-21 Atnx Spv, Llc Biaryl compositions and methods for modulating a kinase cascade
ATE517868T1 (de) 2006-08-16 2011-08-15 Boehringer Ingelheim Int Pyrazinverbindungen, ihre verwendung und herstellungsverfahren
WO2008045252A2 (en) 2006-10-04 2008-04-17 The Board Of Trustees Of The Leland Stanford Junior University Engineered integrin binding peptides
PE20080928A1 (es) * 2006-10-31 2008-08-15 Schering Corp Derivados de anilinopiperazina como inhibidores de proteina quinasa
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
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
EP2139888A2 (en) 2007-03-28 2010-01-06 Array Biopharma, Inc. Imidazoý1,2-a¨pyridine compounds as receptor tyrosine kinase inhibitors
WO2008124323A1 (en) 2007-04-03 2008-10-16 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
CN102317266A (zh) 2007-04-25 2012-01-11 埃克塞利希斯股份有限公司 作为pim调节剂的6-苯基嘧啶酮类
KR20100017359A (ko) 2007-04-25 2010-02-16 엑셀리시스, 인코포레이티드 카제인 키나제 ⅱ （ｃｋ２）조절제로서의 피리미디논
US8293747B2 (en) * 2007-07-19 2012-10-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
EP2182986A2 (en) * 2007-07-31 2010-05-12 Schering Corporation Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment
PA8792401A1 (es) 2007-08-06 2009-03-31 Janssen Pharmaceutica Nv Fenilendiaminas
EP2217235A4 (en) 2007-11-15 2011-01-12 Musc Found For Res Dev INHIBITORS OF PIM PROTEIN KINASES, COMPOSITIONS AND METHOD FOR THE TREATMENT OF CANCER
WO2009065080A1 (en) 2007-11-16 2009-05-22 San Diego State University Research Foundation Compositions and method for manipulating pim-1 activity in circulatory system cells
AU2009219154A1 (en) 2008-02-29 2009-09-03 Cylene Pharmaceuticals, Inc. Protein kinase modulators
US8168794B2 (en) 2008-03-03 2012-05-01 Novartis Ag Pim kinase inhibitors and methods of their use
UY31679A1 (es) * 2008-03-03 2009-09-30 Inhibidores de cinasa pim y metodos para su uso
WO2009151845A1 (en) 2008-05-12 2009-12-17 Amnestix, Inc. Compounds for rho kinase inhibition and for improving learning and memory
BRPI0914942A2 (pt) 2008-06-30 2015-08-11 Cylene Pharmaceuticals Inc Compostos de oxindol
UY31952A (es) 2008-07-02 2010-01-29 Astrazeneca Ab 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim
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
US8557809B2 (en) 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
CA2735782A1 (en) 2008-09-02 2010-03-11 Novartis Ag Heterocyclic pim-kinase inhibitors
BRPI0918496A2 (pt) 2008-09-02 2019-09-24 Novartis Ag composto inibidor bicíclico de quinase, uso do mesmo, composição farmacêutica e método para inibir a atividade da quinase pim em uma célula
CN104311480A (zh) 2008-09-02 2015-01-28 诺华股份有限公司 作为激酶抑制剂的吡啶甲酰胺衍生物
PT3106463T (pt) 2008-10-22 2018-05-18 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk
GB0821307D0 (en) 2008-11-21 2008-12-31 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
WO2010071885A1 (en) 2008-12-19 2010-06-24 Cephalon, Inc. Pyrrolotriazines as alk and jak2 inhibitors
CA3025627C (en) 2009-04-20 2021-08-31 Auspex Pharmaceuticals, Inc. Piperidine inhibitors of janus kinase 3
US20120128631A1 (en) 2009-05-19 2012-05-24 San Diego State University (SDSU) Foundation, dba San Diego State University (SDSU) Research Compositions and methods for kinase-mediated cytoprotection and enhanced cellular engraftment and persistence
WO2010135571A1 (en) 2009-05-20 2010-11-25 Cylene Pharmaceuticals, Inc. Novel protein kinase modulators
AU2010249493A1 (en) 2009-05-20 2011-12-08 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
WO2010148351A1 (en) 2009-06-18 2010-12-23 Cylene Pharmaceuticals, Inc. Rhodanines and related heterocycles as kinase inhibitors
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
JP2013503178A (ja) 2009-08-26 2013-01-31 サイリーン ファーマシューティカルズ インコーポレーティッド タンパク質キナーゼ調節物質としての縮合キノリン
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
US8435976B2 (en) 2009-09-08 2013-05-07 F. Hoffmann-La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
SG10201405568UA (en) 2009-09-08 2014-11-27 Hoffmann La Roche 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
CA2773854A1 (en) 2009-09-11 2011-03-17 Cylene Pharmaceuticals Inc. Pharmaceutically useful heterocycle-substituted lactams
SG179163A1 (en) 2009-09-16 2012-05-30 Cylene Pharmaceuticals Inc Novel tricyclic protein kinase modulators
AU2010295622A1 (en) 2009-09-16 2012-05-10 Cylene Pharmaceuticals, Inc. Tricyclic compounds and pharmaceutical uses thereof
ES2658290T3 (es) 2009-10-29 2018-03-09 Genosco Inhibidores de cinasa
EP2332917B1 (en) 2009-11-11 2012-08-01 Sygnis Bioscience GmbH & Co. KG Compounds for PIM kinase inhibition and for treating malignancy
JP2013510824A (ja) 2009-11-12 2013-03-28 セルビタ エス．エー． セリン／トレオニンキナーゼを調節または制御するための化合物、その調製のための方法、医薬組成物、化合物の使用、方法ならびにセリン／トレオニンキナーゼ調節剤
JP5740409B2 (ja) 2009-11-13 2015-06-24 ジェノスコ キナーゼ阻害剤
WO2011063398A1 (en) 2009-11-23 2011-05-26 Cylene Pharamaceuticals, Inc. Polymorphs and salts of a kinase inhibitor
KR101851130B1 (ko) 2009-12-04 2018-04-23 센화 바이오사이언시즈 인코포레이티드 Ｃｋ2 억제제로서 피라졸로피리미딘 및 관련된 헤테로사이클
AR079529A1 (es) 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
WO2011075613A1 (en) 2009-12-18 2011-06-23 Sanofi Azaindole derivatives, their preparation and their therapeutic application
US8563539B2 (en) 2009-12-23 2013-10-22 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
GB201002861D0 (en) 2010-02-19 2010-04-07 Cxr Biosciences Ltd Compositions
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
SG184475A1 (en) 2010-04-07 2012-11-29 Hoffmann La Roche Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP2013530199A (ja) 2010-07-06 2013-07-25 ノバルティス アーゲー キナーゼ阻害剤として有用な環状エーテル化合物
KR101995013B1 (ko) 2010-07-13 2019-07-02 에프. 호프만-라 로슈 아게 Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체
US8227773B2 (en) 2010-07-29 2012-07-24 Axcelis Technologies, Inc. Versatile beam glitch detection system
CA2806341C (en) 2010-07-29 2020-03-24 Rigel Pharmaceuticals, Inc. Ampk-activating heterocyclic compounds and methods for using the same
EP2637650A2 (en) 2010-11-10 2013-09-18 National Jewish Health Methods to test allergic conditions
WO2012065297A1 (en) 2010-11-16 2012-05-24 Impact Therapeutics, Inc. 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
MX2013006467A (es) 2010-12-09 2013-10-01 Amgen Inc Compuestos biciclicos como inhibidores pim.
RU2652638C2 (ru) 2010-12-17 2018-04-28 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пиразолхиназолиновые производные в качестве ингибиторов киназы
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
EP2668188B1 (en) 2011-01-26 2016-05-18 Nerviano Medical Sciences S.r.l. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
CN103339134B (zh) 2011-01-26 2015-12-23 内尔维阿诺医学科学有限公司 三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用
PH12013501754A1 (en) 2011-02-25 2013-10-14 Array Biopharma Inc Triazolopyridine compounds as pim kinase inhibitors
UY33930A (es) 2011-03-04 2012-10-31 Novartis Ag Inhibidores novedosos de quinasas
UY33929A (es) 2011-03-04 2012-10-31 Novartis Ag Compuestos de ciclohexilo tetrasustituido como inhibidores de quinasas
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
EP2688886A1 (en) 2011-03-22 2014-01-29 Amgen Inc. Azole compounds as pim inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
PE20141050A1 (es) 2011-04-05 2014-08-30 Pfizer Ltd Inhibidores de quinasa relacionados con pirrolo (2,3-d) pirimidina tropomiosina
EP2702055A1 (en) 2011-04-11 2014-03-05 Nerviano Medical Sciences S.r.l. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
EP2699569B1 (en) 2011-04-22 2017-08-30 Jasco Pharmaceuticals, LLC Aminopyrimidine kinase inhibitors
GB201107197D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Compounds
GB201107176D0 (en) 2011-04-28 2011-06-15 Cxr Biosciences Ltd Pyrrolnitrin derivatives
CA2834166A1 (en) 2011-04-29 2012-11-01 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
WO2012156367A1 (en) 2011-05-17 2012-11-22 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
KR101953210B1 (ko) 2011-05-19 2019-02-28 푼다시온 센트로 나시오날 드 인베스티가시오네스 온콜로기카스 카를로스Ⅲ 단백질 키나아제 억제제로서의 대환식 화합물
AU2012262489A1 (en) 2011-05-27 2013-04-04 Icahn School Of Medicine At Mount Sinai Substituted 2-benzylidene-2H-benzo[b][1,4]thiazin-3(4H)-ones, derivatives thereof, and therapeutic uses thereof
US9730929B2 (en) 2011-06-01 2017-08-15 Bayer Intellectual Property Gmbh Substituted aminoimidazopyridazines
WO2012170827A2 (en) 2011-06-08 2012-12-13 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as ck2 inhibitors
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
US9284319B2 (en) 2011-06-22 2016-03-15 Bayer Intellectual Property Gmbh Heterocyclyl aminoimidazopyridazines
PL3409278T3 (pl) 2011-07-21 2021-02-22 Sumitomo Pharma Oncology, Inc. Heterocykliczne inhibitory kinazy białkowej
CN102924444B (zh) 2011-08-11 2015-07-08 上海吉铠医药科技有限公司 Pim激酶抑制剂及其制备方法与在制药中的应用
BR112014003296A2 (pt) 2011-08-12 2017-03-14 Hoffmann La Roche composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, método para o tratamento de uma doença ou distúrbio, conjunto para o tratamento de uma condição mediada pela quinase pim e utilização do composto
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
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
JP5843524B2 (ja) 2011-09-02 2016-01-13 キヤノン株式会社 有機無機複合組成物、有機無機複合材料、光学素子および積層型回折光学素子
UA117092C2 (uk) 2011-09-06 2018-06-25 Байєр Інтеллектуал Проперті Гмбх Амінозаміщені імідазопіридазини
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2758400A1 (en) 2011-09-23 2014-07-30 Bayer Intellectual Property GmbH Substituted imidazopyridazines
US8614206B2 (en) 2011-09-27 2013-12-24 F. Hoffmann-La Roche Ag Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
US9145418B2 (en) 2011-10-07 2015-09-29 Nerviano Medical Sciences S.R.L. Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
WO2013050448A1 (en) 2011-10-07 2013-04-11 Nerviano Medical Sciences S.R.L. 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
ES2629690T3 (es) 2011-11-04 2017-08-14 Jasco Pharmaceuticals, LLC Inhibidores de aminopirimidina quinasa
WO2013130660A1 (en) 2012-02-28 2013-09-06 Amgen Inc. Amides as pim inhibitors
WO2013134079A1 (en) 2012-03-05 2013-09-12 Amgen Inc. Oxazolidinone compounds and derivatives thereof
US9777004B2 (en) 2012-03-29 2017-10-03 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
CA2869212A1 (en) 2012-04-04 2013-10-10 Bayer Pharma Aktiengesellschaft Amino-substituted imidazopyridazines
PT2841437T (pt) 2012-04-26 2017-09-28 Univ Montreal Derivados de imidazotiadiazol e imidazopirazina como inibidores de recetor 4 ativado por protease (par4) para o tratamento de agregação plaquetária
EP2852590B1 (en) 2012-04-27 2017-02-01 Novartis AG Cyclic bridgehead ether dgat1 inhibitors
SMT202000347T1 (it) 2012-05-09 2020-07-08 Biogen Ma Inc Modulatori di trasporto nucleare e loro usi
JP6078639B2 (ja) 2012-05-15 2017-02-08 ノバルティス アーゲー Ａｂｌ１、ａｂｌ２およびｂｃｒ−ａｂｌ１の活性を阻害するためのベンズアミド誘導体
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
CA2873672A1 (en) 2012-05-21 2013-11-28 Novartis Ag Novel ring-substituted n-pyridinyl amides as kinase inhibitors
GEP20176800B (en) 2012-05-22 2018-01-10 Idenix Pharmaceuticals Llk D-amino acid compounds for liver disease
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
EP2867232B1 (en) 2012-06-27 2018-08-08 F.Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
TW201408652A (zh) 2012-07-11 2014-03-01 Hoffmann La Roche 作爲ＲＯＲｃ調節劑之芳基磺內醯胺衍生物
TW201414737A (zh) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
WO2014022752A1 (en) 2012-08-03 2014-02-06 Amgen Inc. Macrocycles as pim inhibitors
WO2014033631A1 (en) 2012-08-31 2014-03-06 Novartis Ag N-(3-pyridyl) biarylamides as kinase inhibitors
WO2014033630A1 (en) 2012-08-31 2014-03-06 Novartis Ag Novel aminothiazole carboxamides as kinase inhibitors
CN103664878A (zh) 2012-09-12 2014-03-26 山东亨利医药科技有限责任公司 杂芳环及其衍生物类酪氨酸激酶抑制剂
US10118926B2 (en) 2012-09-14 2018-11-06 AbbVie Deutschland GmbH & Co. KG Tricyclic quinoline and quinoxaline derivatives
JP6666147B2 (ja) 2012-09-26 2020-03-13 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 環状エーテルピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物と使用方法
WO2014053568A1 (en) 2012-10-02 2014-04-10 Sanofi Indolyldihydroimidazopyrimidinone derivatives, preparation thereof and therapeutic use thereof
LT2909195T (lt) 2012-10-16 2017-09-25 Janssen Sciences Ireland Uc Antivirusiniai rsv junginiai
AU2013337824B2 (en) 2012-11-01 2018-03-08 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
US9783543B2 (en) 2012-11-19 2017-10-10 Bayer Pharma Aktiengesellschaft Aminoimidazopyridazines
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9598454B2 (en) 2012-12-18 2017-03-21 Vertex Pharmaceuticals Incorporated Mannose derivatives for treating bacterial infections
ES2715682T3 (es) 2012-12-19 2019-06-05 Novartis Ag Inhibidores de la autotaxina
US20150336960A1 (en) 2012-12-19 2015-11-26 Novartis Ag Aryl-substituted fused bicyclic pyridazine compounds
SI2822954T1 (sl) 2012-12-21 2016-07-29 Gilead Sciences, Inc. Policiklične karbamoilpiridonske spojine in njihova farmacevtska uporaba
PL2935222T3 (pl) 2012-12-21 2019-02-28 Epizyme Inc Inhibitory PRMT5 i ich zastosowania
FR3000569B1 (fr) 2013-01-03 2015-02-13 Peugeot Citroen Automobiles Sa Dispositif d'eclairage a ecran a bord(s) lumineux
CA2897200C (en) 2013-01-14 2021-07-06 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
PE20191245A1 (es) 2013-01-15 2019-09-18 Incyte Holdings Corp Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
JO3383B1 (ar) 2013-03-14 2019-03-13 Lilly Co Eli مثبطات cdc7
EP2968299B1 (en) 2013-03-15 2021-01-20 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
TWI742541B (zh) 2013-03-15 2021-10-11 英商邊緣生物科技有限公司 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物
EP3919056B1 (en) 2013-03-15 2024-08-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9308236B2 (en) 2013-03-15 2016-04-12 Bristol-Myers Squibb Company Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
AR095443A1 (es) 2013-03-15 2015-10-14 Fundación Centro Nac De Investig Oncológicas Carlos Iii Heterociclos condensados con acción sobre atr
RU2672584C2 (ru) 2013-03-15 2018-11-16 ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи 4-амино-6-(гетероциклил)пиколинаты и 6-амино-2-(гетероциклил)пиримидин-4-карбоксилаты и их применение в качестве гербицидов
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
JP6325078B2 (ja) 2013-03-15 2018-05-16 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ヘテロ環式化合物およびその使用
UY35421A (es) 2013-03-15 2014-10-31 Nihon Nohyaku Co Ltd Compuesto heterocíclico condensado o su sal, insecticida agrícola u hortícola que comprende el comp uesto y método de uso del insecticida
WO2014139145A1 (en) 2013-03-15 2014-09-18 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
MX363545B (es) 2013-03-15 2019-03-27 Idorsia Pharmaceuticals Ltd Derivados piridin-4-ilo.
JO3279B1 (ar) 2013-03-15 2018-09-16 Respivert Ltd مشتقات 2-((4- امينو -3- (3- فلورو-5- هيدروكسي فينيل)-h1- بيرازولو [d-3,4] بيرمدين-1-يل )ميثيل )- 3- (2- تراي فلورو ميثيل ) بينزيل ) كوينازولين -4 (h3)- واحد واستخدامها كمثبطات فوسفواينوسيتايد 3- كاينيز
US20140275108A1 (en) 2013-03-15 2014-09-18 Galderma Research & Development Novel benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
WO2014142290A1 (ja) 2013-03-15 2014-09-18 日本たばこ産業株式会社 ピラゾール－アミド化合物およびその医薬用途
TWI689490B (zh) 2013-03-15 2020-04-01 英商邊緣生物科技有限公司 用於治療纖維化之經取代之芳族化合物及相關方法
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
CA2940659C (en) 2014-02-28 2023-01-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
KR20240153401A (ko) 2014-04-08 2024-10-22 인사이트 홀딩스 코포레이션 Ｊａｋ 및 ｐｉ3ｋ 억제제 조합에 의한 ｂ-세포 악성종양의 치료
JP2017514832A (ja) 2014-04-30 2017-06-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ１抑制剤を調製する方法及びその新しい形態
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
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
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors

Also Published As

Publication number Publication date
HUE050215T2 (hu) 2020-11-30
US20150329534A1 (en) 2015-11-19
CR20150412A (es) 2015-10-27
AU2020201114A1 (en) 2020-03-05
ES2790419T3 (es) 2020-10-27
PT2945939T (pt) 2020-06-08
MX376306B (es) 2025-03-07
MX394082B (es) 2025-03-24
ES2941292T3 (es) 2023-05-19
US9550765B2 (en) 2017-01-24
IL239886A0 (en) 2015-08-31
PH12020500485A1 (en) 2021-06-14
AR094664A1 (es) 2015-08-19
JP2020200338A (ja) 2020-12-17
US9200004B2 (en) 2015-12-01
EP3670506A1 (en) 2020-06-24
AU2018217210B2 (en) 2020-02-20
DK2945939T3 (da) 2020-03-23
UA121098C2 (uk) 2020-04-10
SI2945939T1 (sl) 2020-08-31
CA2897333A1 (en) 2014-07-24
US10517858B2 (en) 2019-12-31
AU2014207691B2 (en) 2018-08-30
NZ749911A (en) 2020-02-28
JP2019206539A (ja) 2019-12-05
US20200405702A1 (en) 2020-12-31
TW201932456A (zh) 2019-08-16
CN108715590B (zh) 2022-03-08
EP4186897A1 (en) 2023-05-31
US20170182017A1 (en) 2017-06-29
PE20151448A1 (es) 2015-09-28
BR112015016793B1 (pt) 2021-12-28
US10828290B2 (en) 2020-11-10
TWI662030B (zh) 2019-06-11
MX2015009057A (es) 2015-10-05
HK1216424A1 (en) 2016-11-11
US20140200227A1 (en) 2014-07-17
CY1122933T1 (el) 2021-10-29
CN105051029A (zh) 2015-11-11
ZA202108141B (en) 2023-06-28
BR112015016793A2 (pt) 2017-07-11
KR102403306B1 (ko) 2022-06-02
SG11201505347VA (en) 2015-08-28
LT2945939T (lt) 2020-07-27
EP3670506B1 (en) 2023-01-04
AU2018217210C1 (en) 2020-08-27
AU2018217210A1 (en) 2018-08-30
KR102311840B1 (ko) 2021-10-14
US20180193323A1 (en) 2018-07-12
PH12015501567B1 (en) 2015-09-21
ECSP15035343A (es) 2017-03-31
US20190209537A1 (en) 2019-07-11
BR122019024759B1 (pt) 2022-02-08
JP6775645B2 (ja) 2020-10-28
EA201591339A1 (ru) 2015-12-30
RS60244B1 (sr) 2020-06-30
EA035929B1 (ru) 2020-09-02
TW201444823A (zh) 2014-12-01
PL2945939T3 (pl) 2020-08-24
US11229631B2 (en) 2022-01-25
JP6987937B2 (ja) 2022-01-05
MX2020011085A (es) 2022-07-20
EP2945939A1 (en) 2015-11-25
US20200155527A1 (en) 2020-05-21
CN108715590A (zh) 2018-10-30
EP2945939B1 (en) 2020-03-04
US9849120B2 (en) 2017-12-26
JP6554037B2 (ja) 2019-07-31
AU2014207691A1 (en) 2015-08-06
SG10201705662WA (en) 2017-08-30
CN105051029B (zh) 2018-07-31
SG10201912524QA (en) 2020-04-29
KR20210110754A (ko) 2021-09-08
PE20191245A1 (es) 2019-09-18
HRP20200770T1 (hr) 2020-07-24
AU2020201114B2 (en) 2021-03-25
KR20150113019A (ko) 2015-10-07
PH12015501567A1 (en) 2015-09-21
IL239886B (en) 2021-03-25
CA2897333C (en) 2021-07-06
JP2016505020A (ja) 2016-02-18
ME03780B (me) 2021-04-20
NZ710079A (en) 2020-01-31
US10265307B2 (en) 2019-04-23
CL2015001985A1 (es) 2015-10-02
WO2014113388A1 (en) 2014-07-24

Similar Documents

Publication Publication Date Title
ZA202108141B (en) Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
IL244224A0 (en) Pyro- and Thiane-Pyrimide Carboxamide Compounds for Use as Pim Kinase Inhibitors
IL256500B (en) Heterocyclic amides as kinase inhibitors
IL244240A0 (en) Aminoheteroaryl benzamides as kinase inhibitors
IL245660B (en) History of aminopyridines as tam family kinase inhibitors
HUE039504T2 (hu) Kináz inhibitor és alkalmazása
EP2968340A4 (en) COMBINING KINASE INHIBITORS AND USES THEREOF
PL3030561T3 (pl) N-cyjanometyloamidy jako inhibitory kinaz janusowych
HK1224673A1 (en) Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
GB201309603D0 (en) Novel compounds and their use as kinase inhibitors
GB201305741D0 (en) Novel compounds and their use as kinase inhibitors
GB201323021D0 (en) Use of kinase inhibitors
GB201321227D0 (en) Use of kinase inhibitors
GB201307155D0 (en) Kinase inhibitors