WO2013136254A1 - Heterocyclyl compounds - Google Patents

Heterocyclyl compounds Download PDF

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Publication number
WO2013136254A1
WO2013136254A1 PCT/IB2013/051915 IB2013051915W WO2013136254A1 WO 2013136254 A1 WO2013136254 A1 WO 2013136254A1 IB 2013051915 W IB2013051915 W IB 2013051915W WO 2013136254 A1 WO2013136254 A1 WO 2013136254A1
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WO
WIPO (PCT)
Prior art keywords
alkyl
group
substituted
cycloalkyl
unsubstituted
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.)
Ceased
Application number
PCT/IB2013/051915
Other languages
English (en)
French (fr)
Inventor
Bhavesh Dave
Rakesh Kumar Banerjee
Samiron Phukan
Abhijit Datta Khoje
Rajkumar HANGARGE
Jitendra Sambhaji Jadhav
Venkata P. Palle
Rajender Kumar Kamboj
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.)
Lupin Ltd
Original Assignee
Lupin Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47997632&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2013136254(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to AU2013234014A priority Critical patent/AU2013234014B2/en
Priority to JP2014561567A priority patent/JP6093384B2/ja
Priority to US14/385,106 priority patent/US9573944B2/en
Priority to EA201491671A priority patent/EA029768B1/ru
Priority to DK13711973.1T priority patent/DK2834236T3/da
Priority to SG11201405007QA priority patent/SG11201405007QA/en
Priority to CN201380014210.XA priority patent/CN104203947A/zh
Priority to MX2014010925A priority patent/MX355526B/es
Priority to CA2865167A priority patent/CA2865167C/en
Priority to KR1020147028556A priority patent/KR20140138910A/ko
Priority to AP2014008008A priority patent/AP3834A/en
Priority to MA37405A priority patent/MA37405A1/fr
Priority to ES13711973T priority patent/ES2741896T3/es
Application filed by Lupin Ltd filed Critical Lupin Ltd
Priority to HK15106571.7A priority patent/HK1206020B/en
Priority to IN1754MUN2014 priority patent/IN2014MN01754A/en
Priority to EP13711973.1A priority patent/EP2834236B1/en
Priority to UAA201411011A priority patent/UA114906C2/uk
Priority to KR1020197017334A priority patent/KR102240101B1/ko
Priority to NZ629442A priority patent/NZ629442A/en
Priority to CUP2014000109A priority patent/CU24335B1/es
Publication of WO2013136254A1 publication Critical patent/WO2013136254A1/en
Priority to TNP2014000357A priority patent/TN2014000357A1/fr
Priority to IL234559A priority patent/IL234559A/en
Priority to PH12014502040A priority patent/PH12014502040B1/en
Anticipated expiration legal-status Critical
Priority to CR20140464A priority patent/CR20140464A/es
Priority to US15/400,627 priority patent/US9827247B2/en
Ceased legal-status Critical Current

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Classifications

    • 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
    • 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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P25/28—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
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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

Definitions

  • R 1 is selected from the group consisting of hydrogen, substituted- or unsubstituted-alkyl, substituted- or unsubstituted- cycloalkyl, and substituted- or unsubstituted- heterocyclyl;
  • alkenyl as used herein, means an 'alkyl' group as defined hereinabove containing 2 to 20 carbon atoms and containing at least one double bond.
  • alkenyl include, but are not limited to, pent-2-enyl, hex-3-enyl, allyl, vinyl, and the like.
  • Step-1 Synthesis of 3-(3-bromophenyl) oxetan-3-ol
  • Azetidin-3-ol hydrochloride (1.0 g, 9.13 mmol) was taken in DMSO and l-fluoro-3- nitrobenzene (1.0 g, 7.09 mmol) was added followed by K 2 C0 3 (2.449 g, 17.72 mmol).
  • the reaction mixture was heated to 100 °C for 16 hrs. After completion of the reaction, the reaction mixture was cooled and poured into water which was then extracted with ethyl acetate (3 x 8ml). The organic layers were combined, washed with water and brine, dried over sodium sulfate, and concentrated under vacuum.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Pathology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
PCT/IB2013/051915 2012-03-14 2013-03-11 Heterocyclyl compounds Ceased WO2013136254A1 (en)

Priority Applications (25)

Application Number Priority Date Filing Date Title
CUP2014000109A CU24335B1 (es) 2012-03-14 2013-03-11 Piridopirimidinas sustituidas como inhibidores de la quinasa mek y útiles para el tratamiento del cáncer
HK15106571.7A HK1206020B (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
US14/385,106 US9573944B2 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
EA201491671A EA029768B1 (ru) 2012-03-14 2013-03-11 Гетероциклильные соединения
DK13711973.1T DK2834236T3 (da) 2012-03-14 2013-03-11 Heterocyclylforbindelser
SG11201405007QA SG11201405007QA (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
CN201380014210.XA CN104203947A (zh) 2012-03-14 2013-03-11 杂环基化合物
MX2014010925A MX355526B (es) 2012-03-14 2013-03-11 Compuesto de heterociclilo.
CA2865167A CA2865167C (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
KR1020147028556A KR20140138910A (ko) 2012-03-14 2013-03-11 헤테로사이클릴 화합물
AP2014008008A AP3834A (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
MA37405A MA37405A1 (fr) 2012-03-14 2013-03-11 Composés hétérocyclyle
ES13711973T ES2741896T3 (es) 2012-03-14 2013-03-11 Compuestos de heterociclilo
AU2013234014A AU2013234014B2 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
EP13711973.1A EP2834236B1 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
NZ629442A NZ629442A (en) 2012-03-14 2013-03-11 Heterocyclyl compounds as mek inhibitors
IN1754MUN2014 IN2014MN01754A (enExample) 2012-03-14 2013-03-11
UAA201411011A UA114906C2 (uk) 2012-03-14 2013-03-11 Гетероциклільні сполуки як інгібітори мек
KR1020197017334A KR102240101B1 (ko) 2012-03-14 2013-03-11 헤테로사이클릴 화합물
JP2014561567A JP6093384B2 (ja) 2012-03-14 2013-03-11 ヘテロシクリル化合物
TNP2014000357A TN2014000357A1 (en) 2012-03-14 2014-08-18 Heterocyclyl compounds
IL234559A IL234559A (en) 2012-03-14 2014-09-09 Heterocyclic compounds
PH12014502040A PH12014502040B1 (en) 2012-03-14 2014-09-12 Heterocyclyl compounds
CR20140464A CR20140464A (es) 2012-03-14 2014-10-06 Compuestos de heterociclilo
US15/400,627 US9827247B2 (en) 2012-03-14 2017-01-06 Heterocyclyl compounds

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN288/KOL/2012 2012-03-14
IN288KO2012 2012-03-14

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US14/385,106 A-371-Of-International US9573944B2 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
US15/400,627 Continuation US9827247B2 (en) 2012-03-14 2017-01-06 Heterocyclyl compounds

Publications (1)

Publication Number Publication Date
WO2013136254A1 true WO2013136254A1 (en) 2013-09-19

Family

ID=47997632

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/IB2013/051915 Ceased WO2013136254A1 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds
PCT/IB2013/051908 Ceased WO2013136249A1 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds as mek inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/IB2013/051908 Ceased WO2013136249A1 (en) 2012-03-14 2013-03-11 Heterocyclyl compounds as mek inhibitors

Country Status (35)

Country Link
US (5) US9573944B2 (enExample)
EP (2) EP2834236B1 (enExample)
JP (3) JP6093384B2 (enExample)
KR (4) KR102240101B1 (enExample)
CN (4) CN104271577A (enExample)
AP (2) AP3834A (enExample)
AU (4) AU2013234014B2 (enExample)
BR (1) BR112014022713B1 (enExample)
CA (2) CA2865164C (enExample)
CL (2) CL2014002412A1 (enExample)
CO (2) CO7170131A2 (enExample)
CR (2) CR20140464A (enExample)
CU (2) CU24335B1 (enExample)
DK (2) DK2834237T3 (enExample)
DO (2) DOP2014000203A (enExample)
EA (2) EA028232B1 (enExample)
ES (2) ES2684517T3 (enExample)
GE (2) GEP201706774B (enExample)
GT (2) GT201400195A (enExample)
IL (2) IL234560A (enExample)
IN (2) IN2014MN01755A (enExample)
MA (2) MA37405A1 (enExample)
MX (3) MX355474B (enExample)
MY (2) MY174188A (enExample)
NI (2) NI201400107A (enExample)
NZ (2) NZ629432A (enExample)
PE (2) PE20141974A1 (enExample)
PH (2) PH12014502040B1 (enExample)
PL (1) PL2834237T3 (enExample)
SG (2) SG11201405006PA (enExample)
TN (2) TN2014000356A1 (enExample)
TR (1) TR201811976T4 (enExample)
UA (2) UA114907C2 (enExample)
WO (2) WO2013136254A1 (enExample)
ZA (1) ZA201406186B (enExample)

Cited By (21)

* Cited by examiner, † Cited by third party
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WO2016009306A1 (en) * 2014-07-15 2016-01-21 Lupin Limited Heterocyclyl compounds as mek inhibitors
WO2016035008A1 (en) * 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2020254451A1 (en) 2019-06-19 2020-12-24 Boehringer Ingelheim International Gmbh Anticancer combination therapy
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2022214594A1 (en) 2021-04-09 2022-10-13 Boehringer Ingelheim International Gmbh Anticancer therapy
WO2023099608A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099623A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099592A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099624A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099620A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
US11814380B2 (en) 2017-12-21 2023-11-14 Boehringer Ingelheim International Gmbh Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
US12053473B2 (en) 2016-12-22 2024-08-06 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
WO2024246099A1 (en) 2023-05-30 2024-12-05 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma
WO2026114916A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras inhibitors for the treatment of cancer
WO2026114958A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras degraders for the treatment of cancer
WO2026114957A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras degraders for the treatment of cancer
WO2026114918A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras inhibitors for the treatment of cancer

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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
MA37405A1 (fr) * 2012-03-14 2016-03-31 Lupin Ltd Composés hétérocyclyle
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
EP3061747B1 (en) 2013-10-25 2021-04-07 Shanghai Hengrui Pharmaceutical Co. Ltd. Pyridic ketone derivatives, method of preparing same, and pharmaceutical application thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
RS66310B1 (sr) 2018-05-04 2025-01-31 Incyte Corp Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu
KR102956194B1 (ko) 2018-05-04 2026-04-23 인사이트 코포레이션 Fgfr 억제제의 염
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
IL290033B2 (en) * 2019-07-30 2026-05-01 Edvince Ab MEK inhibitor for stroke treatment
EP3797899A1 (de) 2019-09-27 2021-03-31 Primetals Technologies Austria GmbH Vorrichtung und verfahren zum erkennen von einer bewegung eines körpers in einer industrieanlage
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TWI825637B (zh) * 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
AU2022258968A1 (en) * 2021-04-16 2023-10-19 Ikena Oncology, Inc. Mek inhibitors and uses thereof
JP2024521788A (ja) 2021-05-27 2024-06-04 ミラティ セラピューティクス, インコーポレイテッド 併用療法
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
TW202313610A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環
CN114605408B (zh) * 2022-03-30 2023-06-16 沈阳药科大学 5-羟基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制法和应用
CN114573581B (zh) * 2022-03-30 2023-09-01 沈阳药科大学 5-取代氨基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制备与应用
CN114573582B (zh) * 2022-03-30 2023-06-16 沈阳药科大学 1,2,3,4-四氢吡啶并[2,3-d]嘧啶类化合物及其制备方法和应用
CN114456166B (zh) * 2022-03-30 2023-06-16 沈阳药科大学 5-取代氨基-3-甲基吡啶并[2,3-d]嘧啶类化合物及其制备与应用
CN118973580A (zh) 2022-04-08 2024-11-15 米拉蒂治疗股份有限公司 包含sos1抑制剂和mek抑制剂的组合疗法
CN119768393A (zh) 2022-05-25 2025-04-04 医肯纳肿瘤学公司 Mek抑制剂和其用途
JP7854973B2 (ja) * 2022-09-26 2026-05-07 ファイザー・インク Mek阻害剤としての3,4-ジヒドロ-2,7-ナフチリジン-1,6(2h,7h)-ジオン

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005121142A1 (en) * 2004-06-11 2005-12-22 Japan Tobacco Inc. 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2h-pyrido’2,3-d! pyrimidine derivatives and related compounds for the treatment of cancer

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
UA72612C2 (en) * 2000-07-06 2005-03-15 Pyrido[2.3-d]pyrimidine and pyrimido[4.5-d]pyrimidine nucleoside analogues, prodrugs and method for inhibiting growth of neoplastic cells
US6825180B2 (en) * 2001-05-18 2004-11-30 Cell Therapeutics, Inc. Pyridopyrimidine compounds and their uses
GB0129099D0 (en) 2001-12-05 2002-01-23 Astrazeneca Ab Chemical compounds
NZ534069A (en) * 2002-01-22 2007-03-30 Warner Lambert Co 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones to be used to treat neurodegenerative disorders, viruses and cancer
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
KR101190912B1 (ko) 2003-11-19 2012-10-12 어레이 바이오파마 인크. Mek의 헤테로시클릭 억제제 및 그의 사용 방법
US7378423B2 (en) * 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
EP2421612A1 (en) 2009-04-21 2012-02-29 Novartis AG Heterocyclic compounds as mek inhibitors
MA37405A1 (fr) 2012-03-14 2016-03-31 Lupin Ltd Composés hétérocyclyle

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005121142A1 (en) * 2004-06-11 2005-12-22 Japan Tobacco Inc. 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2h-pyrido’2,3-d! pyrimidine derivatives and related compounds for the treatment of cancer

Cited By (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016009306A1 (en) * 2014-07-15 2016-01-21 Lupin Limited Heterocyclyl compounds as mek inhibitors
WO2016035008A1 (en) * 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
US12053473B2 (en) 2016-12-22 2024-08-06 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
US11814380B2 (en) 2017-12-21 2023-11-14 Boehringer Ingelheim International Gmbh Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2020254451A1 (en) 2019-06-19 2020-12-24 Boehringer Ingelheim International Gmbh Anticancer combination therapy
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2021245051A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2022214594A1 (en) 2021-04-09 2022-10-13 Boehringer Ingelheim International Gmbh Anticancer therapy
WO2023099592A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099624A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099620A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes
WO2023099623A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2023099608A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2024246099A1 (en) 2023-05-30 2024-12-05 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma
WO2026114916A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras inhibitors for the treatment of cancer
WO2026114958A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras degraders for the treatment of cancer
WO2026114957A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras degraders for the treatment of cancer
WO2026114918A1 (en) 2024-11-27 2026-06-04 Boehringer Ingelheim International Gmbh Spirocyclic annulated 2-amino-3-cyano thiophene derivatives as kras inhibitors for the treatment of cancer

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