CA2906542A1 - Combination of kinase inhibitors and uses thereof - Google Patents

Combination of kinase inhibitors and uses thereof Download PDF

Info

Publication number
CA2906542A1
CA2906542A1 CA2906542A CA2906542A CA2906542A1 CA 2906542 A1 CA2906542 A1 CA 2906542A1 CA 2906542 A CA2906542 A CA 2906542A CA 2906542 A CA2906542 A CA 2906542A CA 2906542 A1 CA2906542 A1 CA 2906542A1
Authority
CA
Canada
Prior art keywords
kinase
aryl
inhibitor
10alkyl
alpha
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
CA2906542A
Other languages
English (en)
French (fr)
Inventor
Yi Liu
Pingda Ren
Katayoun JESSEN
Xin Guo
Christian Rommel
Troy Edward Wilson
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.)
Intellikine LLC
Original Assignee
Intellikine LLC
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 Intellikine LLC filed Critical Intellikine LLC
Publication of CA2906542A1 publication Critical patent/CA2906542A1/en
Abandoned legal-status Critical Current

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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/435—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
    • A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2906542A 2013-03-15 2014-03-12 Combination of kinase inhibitors and uses thereof Abandoned CA2906542A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201313843816A 2013-03-15 2013-03-15
US13/843,816 2013-03-15
US201314099644A 2013-12-06 2013-12-06
US14/099,644 2013-12-06
PCT/US2014/025090 WO2014151147A1 (en) 2013-03-15 2014-03-12 Combination of kinase inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
CA2906542A1 true CA2906542A1 (en) 2014-09-25

Family

ID=51580899

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2906542A Abandoned CA2906542A1 (en) 2013-03-15 2014-03-12 Combination of kinase inhibitors and uses thereof

Country Status (6)

Country Link
EP (1) EP2968340A4 (https=)
JP (1) JP2016512835A (https=)
CN (1) CN105246482A (https=)
CA (1) CA2906542A1 (https=)
HK (1) HK1219421A1 (https=)
WO (1) WO2014151147A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017132235A1 (en) * 2016-01-26 2017-08-03 Dana-Farber Cancer Institute, Inc. METHODS FOR TREATING BRAIN METASTASES USING COMBINATIONS OF ANTI-P13K AND ANTI-mTOR AGENTS

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201613919A (en) 2014-07-02 2016-04-16 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
GB201506933D0 (en) * 2015-04-23 2015-06-10 Sentinel Oncology Ltd Pharmaceutical compounds
EP3344039A4 (en) * 2015-09-03 2019-08-28 Arizona Board of Regents on behalf of the University of Arizona LOW MOLECULAR DYRK1A INHIBITORS AND USES THEREOF
LT3442535T (lt) 2016-04-15 2022-10-25 Cancer Research Technology Limited Heterocikliniai junginiai kaip ret kinazės inhibitoriai
DK3442980T3 (da) 2016-04-15 2021-08-30 Cancer Research Tech Ltd Heterocykliske forbindelser som ret-kinase-hæmmere
CN106632351A (zh) * 2016-11-18 2017-05-10 山东友帮生化科技有限公司 6‑溴咪唑并[1,2‑a]吡嗪‑3‑羧酸乙酯的制法
CN106831782A (zh) * 2016-11-23 2017-06-13 山东友帮生化科技有限公司 6‑氯咪唑并[1,2‑b]哒嗪‑3‑甲酸的合成方法
CN108239067A (zh) * 2016-12-27 2018-07-03 沈阳药科大学 喹唑啉酮类衍生物及其制备方法和用途
GB201705971D0 (en) 2017-04-13 2017-05-31 Cancer Res Tech Ltd Inhibitor compounds
CN111655228B (zh) 2017-05-03 2024-02-09 听治疗有限责任公司 预防和治疗听力损失的组合物和方法
SG11202004361SA (en) * 2017-11-13 2020-06-29 Luoxin Pharmaceutical Shanghai Co Ltd Quinazolinone compound and application thereof
US12528810B2 (en) 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
CN112469707B (zh) 2018-06-27 2024-06-21 利伯纳生物科学株式会社 脊髓性肌萎缩症的预防剂或治疗剂
GEP20237548B (en) * 2018-07-05 2023-10-10 Incyte Corp Fused pyrazine derivatives as a2a /a2b inhibitors
US12187721B2 (en) 2018-10-17 2025-01-07 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
JP7629200B2 (ja) * 2018-11-20 2025-02-13 ジョージタウン ユニバーシティ 神経変性、筋変性及びリソソーム蓄積障害を治療するための組成物及び方法
MX2022012678A (es) * 2020-04-08 2023-01-11 Remix Therapeutics Inc Compuestos y metodos para modular el corte y empalme.
IL298760A (en) 2020-06-05 2023-02-01 Kinnate Biopharma Inc Fibroblast growth factor receptor kinase inhibitors
CN115611883B (zh) * 2021-07-13 2025-03-28 生物岛实验室 一种双环结构的PI3Kα抑制剂及其制备方法和用途
WO2024057013A1 (en) * 2022-09-12 2024-03-21 Exscientia Ai Limited Nlrp3 modulators
CN116425743B (zh) * 2022-12-30 2025-06-17 贵州医科大学 一种作为PI3Kα激酶抑制剂的苯并杂环类化合物及其制备方法与应用
CN121816181A (zh) 2023-06-30 2026-04-07 柏林合作研究学会 噻唑并四氢喹啉化合物作为ii类磷酸肌醇3-激酶抑制剂

Family Cites Families (167)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
US3657744A (en) 1970-05-08 1972-04-25 Univ Minnesota Method for fixing prosthetic implants in a living body
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5350395A (en) 1986-04-15 1994-09-27 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5061273A (en) 1989-06-01 1991-10-29 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5040548A (en) 1989-06-01 1991-08-20 Yock Paul G Angioplasty mehtod
US4748982A (en) 1987-01-06 1988-06-07 Advanced Cardiovascular Systems, Inc. Reinforced balloon dilatation catheter with slitted exchange sleeve and method
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
CA1322628C (en) 1988-10-04 1993-10-05 Richard A. Schatz Expandable intraluminal graft
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
US5292331A (en) 1989-08-24 1994-03-08 Applied Vascular Engineering, Inc. Endovascular support device
US5674278A (en) 1989-08-24 1997-10-07 Arterial Vascular Engineering, Inc. Endovascular support device
US6344053B1 (en) 1993-12-22 2002-02-05 Medtronic Ave, Inc. Endovascular support device and method
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
EP0636026B1 (en) 1992-04-02 2001-12-05 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
HU225869B1 (en) 1992-04-02 2007-11-28 Smithkline Beecham Corp Compounds with antiallergic and antiinflammatory activity and pharmaceutical compns. contg. them
JP3192424B2 (ja) 1992-04-02 2001-07-30 スミスクライン・ビーチャム・コーポレイション アレルギーまたは炎症疾患の治療用化合物
TW225528B (https=) 1992-04-03 1994-06-21 Ciba Geigy Ag
BR9207175A (pt) 1992-10-28 1995-12-12 Genentech Inc Composição contendo antagonista de fator de crescimento de célula endotelial vascular sequência aminoácida de anticorpo monoclonal polipeptídeo e método de tratamento de tumor em mamífero
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
MX9800215A (es) 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
EP0907642B1 (en) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
EP0923585B1 (en) 1996-07-18 2002-05-08 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
WO1998007697A1 (en) 1996-08-23 1998-02-26 Pfizer Inc. Arylsulfonylamino hydroxamic acid derivatives
US5759787A (en) 1996-08-26 1998-06-02 Tularik Inc. Kinase assay
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
WO1998030566A1 (en) 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
EP0977733B1 (en) 1997-02-03 2003-09-03 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク Ｎ−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EA002546B1 (ru) 1997-02-11 2002-06-27 Пфайзер Инк. Производные арилсульфонилгидроксамовой кислоты
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
PE20000270A1 (es) 1998-02-14 2000-05-20 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
AU750462B2 (en) 1998-06-23 2002-07-18 Glaxo Group Limited 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
KR100563395B1 (ko) 1998-06-30 2006-03-23 다우 글로벌 테크놀로지스 인크. 중합체 폴리올 및 이의 제조방법
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
AU5879299A (en) 1998-10-16 2000-05-08 Monaghan, Sandra Marina Adenine derivatives
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
WO2000037502A2 (en) 1998-12-22 2000-06-29 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
WO2000059509A1 (en) 1999-03-30 2000-10-12 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
CA2371583C (en) 1999-05-04 2005-09-13 Schering Corporation Piperazine derivatives useful as ccr5 antagonists
HK1039330B (en) 1999-05-04 2005-12-09 Schering Corporation Piperidine derivatives useful as ccr5 antagonists
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
EP1212089B1 (en) 1999-08-21 2006-03-22 ALTANA Pharma AG Synergistic combination of roflumilast and salmeterol
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
CZ294251B6 (cs) 2000-06-27 2004-11-10 Laboratorios S. A. L. V. A. T., S. A. Karbamáty a jejich použití pro výrobu farmaceutického prostředku
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
WO2002012266A1 (en) 2000-08-05 2002-02-14 Glaxo Group Limited 17.beta.-carbothioate 17.alpha.-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
JP4445704B2 (ja) 2000-12-22 2010-04-07 アルミラル・ソシエダッド・アノニマ キヌクリジンカルバメート誘導体およびｍ３アンダゴニストとしてのそれらの使用
IL156558A0 (en) 2000-12-28 2004-01-04 Almirall Prodesfarma Ag Novel quinuclidine derivatives and medicinal compositions containing the same
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
PT1383786E (pt) 2001-04-30 2008-12-30 Glaxo Group Ltd Derivados anti-inflamatórios de éster 17.beta-carbotioato de androstano com um grupo éster ciclíco na posição 17.alfa
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
CZ20033126A3 (cs) 2001-05-25 2004-09-15 Pfizer Inc. Kombinace agonistu adenosin A2a receptoru a anticholinergického činidla pro ošetřování obstruktivních nemocí dýchacích cest
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
EP2319919B1 (en) 2001-06-21 2015-08-12 BASF Enzymes LLC Nitrilases
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
JP2005512974A (ja) 2001-10-17 2005-05-12 ユ セ ベ ソシエテ アノニム キヌクリジン誘導体、その調製方法、及びｍ２及び／又はｍ３ムスカリン受容体阻害剤としてのその使用
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
WO2003048181A1 (en) 2001-12-01 2003-06-12 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
EP1461336B1 (en) 2001-12-20 2013-05-22 CHIESI FARMACEUTICI S.p.A. 1-alkyl-1-azoniabicyclo (2.2.2) octane carbamate derivatives and their use as muscarinic receptor antagonists
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
WO2003062259A2 (en) 2002-01-21 2003-07-31 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
CA2477764A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
UA80120C2 (en) 2002-03-26 2007-08-27 Boehringer Ingelheim Pharma Glucocorticoid mimetics, pharmaceutical composition based thereon
AU2003234716A1 (en) 2002-04-10 2003-10-27 Joel M. Linden Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
EP1519922A1 (en) 2002-07-02 2005-04-06 Merck Frosst Canada & Co. Di-aryl-substituted ethane pyridone pde4 inhibitors
SI1521733T1 (sl) 2002-07-08 2014-10-30 Pfizer Products Inc. Modulatorji glukokortikoidnega receptorja
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
CA2494613C (en) 2002-08-10 2011-06-28 Altana Pharma Ag Pyrrolidinedione substituted piperidine-phthalazones as pde4 inhibitors
WO2004018451A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
WO2004018450A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-n-oxide-derivatives
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
AU2003253408A1 (en) 2002-08-17 2004-03-11 Nycomed Gmbh Novel phenanthridines
EP1581533A2 (en) 2002-08-17 2005-10-05 ALTANA Pharma AG Novel benzonaphthyridines
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
JP2006501236A (ja) 2002-08-23 2006-01-12 ランバクシー ラボラトリーズ リミテッド ムスカリン性レセプター拮抗薬としてのフルオロおよびスルホニルアミノ含有３，６−二置換アザビシクロ（３．１．０）ヘキサン誘導体
CA2495827C (en) 2002-08-29 2012-05-08 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
ES2281658T3 (es) 2002-08-29 2007-10-01 Nycomed Gmbh 3-hidroxi-6-fenilfenantridinas como inhibidores de pde-4.
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤
EP1541574A4 (en) 2002-09-18 2007-06-20 Ono Pharmaceutical Co TRIAZASPIRO DERIVATIVES 5.5 | UNDECANS AND DRUGS CONTAINING THEM AS AN ACTIVE INGREDIENT
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EA010408B1 (ru) 2002-10-23 2008-08-29 Гленмарк Фармасьютикалс Лтд. Трициклические соединения для лечения воспалительных и аллергических нарушений, способы их приготовления и содержащие их фармацевтические составы
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
JP2010523566A (ja) 2007-04-05 2010-07-15 ワイス エルエルシー ワートマニン−ラパマイシンコンジュゲートおよびその使用
EP2303890A4 (en) * 2008-06-19 2012-04-11 Progenics Pharm Inc INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE
US20110224223A1 (en) * 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP5788316B2 (ja) * 2008-07-08 2015-09-30 インテリカイン， エルエルシー キナーゼインヒビターおよび使用方法
PE20121148A1 (es) * 2009-08-17 2012-09-07 Intellikine Llc Compuestos heterociclicos y usos de los mismos
EP2475375A4 (en) * 2009-09-09 2013-02-20 Avila Therapeutics Inc PI3 KINASE INHIBITORS AND USES THEREOF
US9096590B2 (en) * 2010-05-24 2015-08-04 Intellikine Llc Substituted benzoxazoles as PI3 kinase inhibitors
EP2640367A2 (en) * 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
US9295673B2 (en) * 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
PE20140601A1 (es) * 2011-04-25 2014-05-24 Novartis Ag COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K) Y UN INHIBIDOR DE mTOR
WO2012154610A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive pi3k kinase inhibitors and uses thereof
WO2014046617A1 (en) * 2012-09-19 2014-03-27 Agency For Science, Technology And Research Compositions and methods for treating cancer

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017132235A1 (en) * 2016-01-26 2017-08-03 Dana-Farber Cancer Institute, Inc. METHODS FOR TREATING BRAIN METASTASES USING COMBINATIONS OF ANTI-P13K AND ANTI-mTOR AGENTS
US11318139B2 (en) 2016-01-26 2022-05-03 Dana-Farber Cancer Institute, Inc. Methods for treating brain metastases using combinations of anti-P13K and anti-mTOR agents

Also Published As

Publication number Publication date
WO2014151147A1 (en) 2014-09-25
HK1219421A1 (zh) 2017-04-07
EP2968340A1 (en) 2016-01-20
JP2016512835A (ja) 2016-05-09
EP2968340A4 (en) 2016-08-10
CN105246482A (zh) 2016-01-13

Similar Documents

Publication Publication Date Title
CA2906542A1 (en) Combination of kinase inhibitors and uses thereof
US11654143B2 (en) Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor, a JAK-2 inhibitor, and/or a BCL-2 inhibitor
US11485745B2 (en) Amido spirocyclic amide and sulfonamide derivatives
AU2009310364B2 (en) Benzoxazole kinase inhibitors and methods of use
AU2009204487C1 (en) Certain chemical entities, compositions and methods
RU2665462C2 (ru) Соединения 5-азаиндазола и способы их применения
WO2012148540A1 (en) Combination of kanase inhibitors and uses threof
CA2836769C (en) The combination of paclitaxel and an mtor inhibitor for the treatment of a proliferative disorder
CA2856803A1 (en) Enhanced treatment regimens using mtor inhibitors
US20180207154A1 (en) Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor and/or a JAK-2 Inhibitor
CA2855666A1 (en) Combination of kinase inhibitors and uses thereof
KR101660664B1 (ko) 도파민 d1 리간드로서의 헤테로방향족 화합물
CA3121408A1 (en) Heteroaromatic derivatives for use as regulator, preparation method therefor and use thereof
AU2009259867A1 (en) Triazolopyridine JAK inhibitor compounds and methods
MX2011000216A (es) Inhibidores de cinasa y metodos para su uso.
KR20140071361A (ko) 피라졸로[3,4-c]피리딘 화합물 및 사용 방법
KR20130001272A (ko) 이미다조피리딘 및 푸린 화합물, 조성물 및 사용 방법
WO2016024232A1 (en) Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor
KR20120135270A (ko) 피리도［3,2-ｄ］피리미딘 ｐｉ3ｋ 델타 억제제 화합물 및 이의 용도
US20160089371A1 (en) Combination of Kinase Inhibitors and Uses Thereof
WO2016055982A1 (en) Quinoline and quinazoline compounds
WO2012154608A1 (en) Reactive mtor and pi3 kinase inhibitors and uses thereof
US20180318304A1 (en) Methods of Using BTK Inhibitors to Treat Dermatoses

Legal Events

Date Code Title Description
FZDE Dead

Effective date: 20200312