CA2773848A1 - Pi3 kinase inhibitors and uses thereof - Google Patents

Pi3 kinase inhibitors and uses thereof Download PDF

Info

Publication number
CA2773848A1
CA2773848A1 CA2773848A CA2773848A CA2773848A1 CA 2773848 A1 CA2773848 A1 CA 2773848A1 CA 2773848 A CA2773848 A CA 2773848A CA 2773848 A CA2773848 A CA 2773848A CA 2773848 A1 CA2773848 A1 CA 2773848A1
Authority
CA
Canada
Prior art keywords
ring
nitrogen
oxygen
sulfur
independently selected
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2773848A
Other languages
English (en)
French (fr)
Inventor
Deqiang Niu
Russell C. Petter
Juswinder Singh
Arthur F. Kluge
Hormoz Mazdiyasni
Zhendong Zhu
Lixin Qiao
Kevin Kuntz
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Celgene Avilomics Research Inc
Original Assignee
Avila Therapeutics Inc
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 Avila Therapeutics Inc filed Critical Avila Therapeutics Inc
Publication of CA2773848A1 publication Critical patent/CA2773848A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P35/02—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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A61P7/06—Antianaemics
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Microbiology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
CA2773848A 2009-09-09 2010-09-09 Pi3 kinase inhibitors and uses thereof Abandoned CA2773848A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24094709P 2009-09-09 2009-09-09
US61/240,947 2009-09-09
US37139610P 2010-08-06 2010-08-06
US61/371,396 2010-08-06
PCT/US2010/048317 WO2011031896A2 (en) 2009-09-09 2010-09-09 Pi3 kinase inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
CA2773848A1 true CA2773848A1 (en) 2011-03-17

Family

ID=43733099

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2773848A Abandoned CA2773848A1 (en) 2009-09-09 2010-09-09 Pi3 kinase inhibitors and uses thereof

Country Status (16)

Country Link
US (1) US20110230476A1 (https=)
EP (1) EP2475375A4 (https=)
JP (1) JP2013504325A (https=)
KR (1) KR20120063515A (https=)
CN (1) CN102625708A (https=)
AU (1) AU2010292198A1 (https=)
BR (1) BR112012008385A2 (https=)
CA (1) CA2773848A1 (https=)
IL (1) IL218555A0 (https=)
MX (1) MX339584B (https=)
NZ (2) NZ598808A (https=)
PH (1) PH12012500491A1 (https=)
RU (1) RU2595718C2 (https=)
SG (2) SG10201405598QA (https=)
TW (2) TW201609747A (https=)
WO (1) WO2011031896A2 (https=)

Families Citing this family (139)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200801012A (en) * 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US8946197B2 (en) 2009-11-16 2015-02-03 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
CA2829558A1 (en) * 2011-03-09 2012-09-13 Celgene Avilomics Research, Inc. Pi3 kinase inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2012154608A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive mtor and pi3 kinase inhibitors and uses thereof
WO2012154610A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive pi3k kinase inhibitors and uses thereof
US8889716B2 (en) 2011-05-10 2014-11-18 Chdi Foundation, Inc. Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof
JP2014520863A (ja) 2011-07-13 2014-08-25 ファーマサイクリックス，インク． Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤
BR112014007310A2 (pt) 2011-09-27 2017-04-04 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
WO2013144180A1 (en) * 2012-03-28 2013-10-03 Intervet International B.V. Heteroaryl compounds with cyclic bridging unit for use in the treatment helminth infection
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
HUE051096T2 (hu) 2012-04-26 2021-03-01 Massachusetts Gen Hospital Ágensek és módszerek a sebészeti keratózis kezelésére és megelõzésére
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US20150204846A1 (en) * 2012-05-15 2015-07-23 New York University Phosphatidylinositol-3-kinase c2 beta modulators and methods of use thereof
WO2014012093A1 (en) * 2012-07-13 2014-01-16 Wake Forest University Health Sciences Prostate cancer targeted prodrugs and methods of use thereof
WO2014022569A1 (en) * 2012-08-03 2014-02-06 Principia Biopharma Inc. Treatment of dry eye
CA2879597C (en) 2012-08-21 2021-01-12 Opko Pharmaceuticals, Llc Ophthalmic liposome formulations for treating posterior segment disease
US11458199B2 (en) 2012-08-21 2022-10-04 Opko Pharmaceuticals, Llc Liposome formulations
SI2892900T1 (en) 2012-09-10 2018-01-31 Principia Biopharma Inc. Pyrazolopyrimidine compounds as kinase inhibitors
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
JP6207100B2 (ja) 2012-12-21 2017-10-04 ギリアード カリストガ エルエルシー イソキノリノンまたはキナゾリノンホスファチジルイノシトール３−キナーゼ阻害剤
AU2013364068B2 (en) 2012-12-21 2016-10-20 Gilead Calistoga Llc Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors
MX368903B (es) * 2013-02-20 2019-10-21 Kala Pharmaceuticals Inc Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas.
MX394360B (es) 2013-03-14 2025-03-24 Sumitomo Pharma Oncology Inc Inhibidores de jak2 y alk2 y metodos para su uso.
JP6387360B2 (ja) 2013-03-14 2018-09-05 ノバルティス アーゲー 変異ｉｄｈの阻害薬としての３−ピリミジン−４−イル−オキサゾリジン−２−オン
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
EP2968340A4 (en) * 2013-03-15 2016-08-10 Intellikine Llc COMBINING KINASE INHIBITORS AND USES THEREOF
CA2904393A1 (en) * 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
JP6378918B2 (ja) * 2013-04-03 2018-08-22 株式会社ヤクルト本社 チアゾリジン誘導体又はその塩を有効成分とするＰｉｍ阻害剤
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
AR096151A1 (es) * 2013-05-01 2015-12-09 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos
US10508309B2 (en) * 2013-05-17 2019-12-17 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
PL3008053T3 (pl) 2013-06-14 2018-08-31 Gilead Calistoga Llc Inhibitory 3-kinazy fosfatydyloinozytolu
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
BR112016006978A2 (pt) 2013-09-30 2017-08-01 Pharmacyclics Llc inibidores de tirosina quinase de bruton
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
ES2670550T3 (es) 2013-10-14 2018-05-30 Eisai R&D Management Co., Ltd. Derivados de quinolina selectivamente sustituidos
SG10202103278TA (en) 2013-10-14 2021-04-29 Eisai R&D Man Co Ltd Selectively substituted quinoline compounds
WO2015058126A1 (en) * 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
US10047084B2 (en) 2013-11-20 2018-08-14 Beijing Forelandpharma Co. Ltd. Imidazolone derivatives, pharmaceutical compositions and uses thereof
EP3076968B1 (en) 2013-12-02 2019-04-17 ChemoCentryx, Inc. Ccr6 compounds
CN112353806A (zh) 2014-02-21 2021-02-12 普林斯匹亚生物制药公司 Btk抑制剂的盐和固体形式
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
JP2017528498A (ja) * 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
SG11201704808VA (en) 2014-12-18 2017-07-28 Principia Biopharma Inc Treatment of pemphigus
ES2737227T3 (es) 2014-12-24 2020-01-10 Kither Biotech S R L Péptido inhibidor de gamma PI3K novedoso para el tratamiento de enfermedades del sistema respiratorio
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
WO2016172952A1 (zh) 2015-04-30 2016-11-03 江苏挪贝肽医药科技有限公司 PI4KIIIα蛋白及相关的膜蛋白复合体在治疗阿尔茨海默病中的应用
CA2986359A1 (en) 2015-05-20 2016-11-24 Novartis Ag Pharmaceutical combination of everolimus with dactolisib
WO2016210165A1 (en) 2015-06-24 2016-12-29 Principia Biopharma Inc. Tyrosine kinase inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058805A1 (en) * 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
RU2617409C1 (ru) * 2015-12-24 2017-04-25 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) Амиды акриловой и метакриловой кислот с n-алкилпиперазино-пиперидинами и способ их получения
RU2617694C1 (ru) * 2015-12-24 2017-04-26 Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) Амиды акриловой и метакриловой кислот с олигопиперидинами и способ их получения
GB201602527D0 (en) * 2016-02-12 2016-03-30 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
MX383920B (es) 2016-05-26 2025-03-14 Recurium Ip Holdings Llc Compuestos inhibidores de egfr.
CN115054586B (zh) 2016-06-29 2024-08-02 普林斯匹亚生物制药公司 改性的释放制剂
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
CN110114070A (zh) 2016-11-23 2019-08-09 诺华公司 使用依维莫司(everolimus)、达托里昔布(dactolisib)或二者增强免疫反应的方法
CN106755343A (zh) * 2016-12-01 2017-05-31 北京致成生物医学科技有限公司 胰腺癌预后诊断分子标记物
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US10858351B2 (en) * 2017-04-26 2020-12-08 Alberta Research Chemicals Inc. Substituted tetrahydropyridine derivatives as IDO-1 inhibitors and uses thereof
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
US10596165B2 (en) 2018-02-12 2020-03-24 resTORbio, Inc. Combination therapies
KR20210003780A (ko) 2018-04-05 2021-01-12 스미토모 다이니폰 파마 온콜로지, 인크. Axl 키나제 억제제 및 그의 용도
AU2019251363B2 (en) 2018-04-10 2024-03-07 Neuropore Therapies, Inc. Morpholine derivates as inhibitors of Vps34
KR102803762B1 (ko) 2018-04-10 2025-05-09 뉴로포레 테라피스, 인코포레이티드 Pi3-키나제 및 오토파지 경로의 조절인자로서의 트리-치환된 아릴 및 헤테로아릴 유도체
AU2019310590A1 (en) 2018-07-26 2021-01-14 Sumitomo Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
MX2021000887A (es) * 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
KR102328682B1 (ko) 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
EP3849545A1 (en) * 2018-09-10 2021-07-21 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of neurofibromatosis
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2021055747A1 (en) 2019-09-19 2021-03-25 Totus Medicines Inc. Therapeutic conjugates
US20210106584A1 (en) 2019-10-14 2021-04-15 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
US12590298B2 (en) 2019-10-18 2026-03-31 The Regents Of The University Of California Ex vivo tumor angiogenesis model
KR20220087497A (ko) 2019-10-18 2022-06-24 더 리전츠 오브 더 유니버시티 오브 캘리포니아 병원성 혈관을 표적화하기 위한 화합물 및 방법
US20210269434A1 (en) * 2020-01-10 2021-09-02 Incyte Corporation Tricyclic compounds as inhibitors of kras
WO2021150613A1 (en) 2020-01-20 2021-07-29 Incyte Corporation Spiro compounds as inhibitors of kras
US11814390B2 (en) 2020-01-22 2023-11-14 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
KR20250133471A (ko) 2020-02-18 2025-09-05 길리애드 사이언시즈, 인코포레이티드 항바이러스 화합물
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
EP4157281A4 (en) * 2020-05-27 2024-11-27 Duke University COMPOSITIONS AND METHODS FOR SENSITIZING ACUTE MYELOID LEUKEMIAS TO CHEMOTHERAPY
US11999752B2 (en) 2020-08-28 2024-06-04 Incyte Corporation Vinyl imidazole compounds as inhibitors of KRAS
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
CN113045582B (zh) * 2021-02-05 2022-12-23 中国药科大学 Parp-1/pi3k双靶点抑制剂或其药学上可接受的盐及其制备方法与用途
WO2022198024A1 (en) * 2021-03-18 2022-09-22 Totus Medicines Inc. Therapeutic conjugates
WO2022204112A1 (en) 2021-03-22 2022-09-29 Incyte Corporation Imidazole and triazole kras inhibitors
CN117396470A (zh) * 2021-04-09 2024-01-12 巴塞尔大学 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物
KR20240008312A (ko) * 2021-04-09 2024-01-18 유니버시타트 바셀 Pi3k의 가역적 및 비가역적 공유 억제제로서의 트리아진 유도체
CA3216162A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides
MX2024000357A (es) 2021-07-07 2024-02-12 Incyte Corp Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras).
WO2023287896A1 (en) 2021-07-14 2023-01-19 Incyte Corporation Tricyclic compounds as inhibitors of kras
TW202321191A (zh) * 2021-07-29 2023-06-01 美商賽迪拉治療股份有限公司 Ｔｅａｄ抑制劑及其用途
AU2022328698B2 (en) 2021-08-18 2025-02-20 Gilead Sciences, Inc. Phospholipid compounds and methods of making and using the same
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
CN113754680B (zh) * 2021-09-28 2022-07-22 云白药征武科技(上海)有限公司 一种α氟代酰基哌嗪衍生物及其制备和应用
CA3234375A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
CA3235146A1 (en) 2021-10-14 2023-04-20 Incyte Corporation Quinoline compounds as inhibitors of kras
KR102939621B1 (ko) * 2022-07-21 2026-03-17 주식회사 바오밥에이바이오 헤테로비시클릭 화합물 및 그를 포함하는 약제학적 조성물
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
WO2025188658A1 (en) * 2024-03-06 2025-09-12 Alterome Therapeutics, Inc. Akt1 modulators

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
ATE411996T1 (de) * 2002-09-30 2008-11-15 Bayer Healthcare Ag Kondensierte azolpyrimidinderivate
AR046845A1 (es) * 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
WO2005113556A1 (en) * 2004-05-13 2005-12-01 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
WO2006089106A2 (en) * 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
TW200801012A (en) * 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
TWI498332B (zh) * 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
GB0611152D0 (en) * 2006-06-06 2006-07-19 Ucb Sa Therapeutic agents
EP2050749B1 (en) * 2006-08-08 2017-11-22 Chugai Seiyaku Kabushiki Kaisha Pyrimidine derivative as pi3k inhibitor and use thereof
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
PE20090717A1 (es) * 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
TWI433677B (zh) * 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
EP2205242B1 (en) * 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
JP5348725B2 (ja) * 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
GB0805818D0 (en) * 2008-03-31 2008-04-30 Ucb Pharma Sa Therapeutic agents
EA024252B1 (ru) * 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой

Also Published As

Publication number Publication date
TWI499592B (zh) 2015-09-11
NZ626650A (en) 2015-12-24
WO2011031896A3 (en) 2011-05-12
TW201609747A (zh) 2016-03-16
KR20120063515A (ko) 2012-06-15
CN102625708A (zh) 2012-08-01
IL218555A0 (en) 2012-05-31
TW201120047A (en) 2011-06-16
WO2011031896A2 (en) 2011-03-17
MX2012002972A (es) 2012-06-25
RU2012110024A (ru) 2013-11-10
EP2475375A4 (en) 2013-02-20
PH12012500491A1 (en) 2018-03-21
MX339584B (es) 2016-06-01
AU2010292198A1 (en) 2012-04-05
JP2013504325A (ja) 2013-02-07
SG10201405598QA (en) 2014-11-27
US20110230476A1 (en) 2011-09-22
NZ598808A (en) 2014-07-25
RU2595718C2 (ru) 2016-08-27
SG179085A1 (en) 2012-04-27
BR112012008385A2 (pt) 2019-09-24
EP2475375A2 (en) 2012-07-18

Similar Documents

Publication Publication Date Title
CA2773848A1 (en) Pi3 kinase inhibitors and uses thereof
AU2012225382B2 (en) PI3 kinase inhibitors and uses thereof
US10968236B2 (en) TYK2 inhibitors and uses thereof
JP7530360B2 (ja) Ｔｙｋ２阻害剤およびその使用
JP2026035684A (ja) Ｔｙｋ２阻害剤およびその使用
JP5808826B2 (ja) 複素環化合物およびその使用
US12338242B2 (en) TYK2 inhibitors and uses thereof
TW200911810A (en) Substituted imidazopyridazines and pyrrolopyrimidines as lipid kinase inhibitors
KR20130031234A (ko) 헤테로사이클릭 화합물 및 이의 용도
CA2878040A1 (en) Irak inhibitors and uses thereof
AU2012310168B2 (en) 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
EP4194450A1 (en) Cdk9 inhibitor and use thereof
CN113493471A (zh) 杂芳环类激酶抑制剂

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20150901

FZDE Discontinued

Effective date: 20180717