WO2012021444A8 - Besylate salt of a btk inhibitor - Google Patents

Besylate salt of a btk inhibitor Download PDF

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Publication number
WO2012021444A8
WO2012021444A8 PCT/US2011/046926 US2011046926W WO2012021444A8 WO 2012021444 A8 WO2012021444 A8 WO 2012021444A8 US 2011046926 W US2011046926 W US 2011046926W WO 2012021444 A8 WO2012021444 A8 WO 2012021444A8
Authority
WO
WIPO (PCT)
Prior art keywords
btk inhibitor
besylate salt
inhibitor
salt
besylate
Prior art date
Application number
PCT/US2011/046926
Other languages
French (fr)
Other versions
WO2012021444A1 (en
Inventor
Steven Richard Witowski
William Frederick Westlin Iii
Richland Wayne Tester
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
Priority to CN201180039445.5A priority Critical patent/CN103096716B/en
Priority to BR112013003388A priority patent/BR112013003388A2/en
Priority to ES11816874.9T priority patent/ES2617763T3/en
Priority to JP2013524147A priority patent/JP6068340B2/en
Priority to SG2013009972A priority patent/SG187796A1/en
Priority to NZ607845A priority patent/NZ607845A/en
Priority to EP11816874.9A priority patent/EP2603081B1/en
Priority to DK11816874.9T priority patent/DK2603081T3/en
Application filed by Avila Therapeutics, Inc. filed Critical Avila Therapeutics, Inc.
Priority to MX2013001126A priority patent/MX336875B/en
Priority to RU2013109393/04A priority patent/RU2013109393A/en
Priority to KR1020137006114A priority patent/KR20130099040A/en
Priority to AU2011289604A priority patent/AU2011289604C1/en
Priority to CA2807051A priority patent/CA2807051A1/en
Publication of WO2012021444A1 publication Critical patent/WO2012021444A1/en
Publication of WO2012021444A8 publication Critical patent/WO2012021444A8/en
Priority to IL224271A priority patent/IL224271A/en
Priority to ZA2013/01802A priority patent/ZA201301802B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same.
PCT/US2011/046926 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor WO2012021444A1 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
MX2013001126A MX336875B (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor.
BR112013003388A BR112013003388A2 (en) 2010-08-10 2011-08-08 besylate salt of a btk inhibitor
RU2013109393/04A RU2013109393A (en) 2010-08-10 2011-08-08 BTK INHIBITOR SALT
SG2013009972A SG187796A1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor
NZ607845A NZ607845A (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor
EP11816874.9A EP2603081B1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor
DK11816874.9T DK2603081T3 (en) 2010-08-10 2011-08-08 COLLECTED BY A BTK INHIBITOR
CN201180039445.5A CN103096716B (en) 2010-08-10 2011-08-08 The benzene sulfonate of BTK inhibitor
ES11816874.9T ES2617763T3 (en) 2010-08-10 2011-08-08 Besylate salt of a BTK inhibitor
JP2013524147A JP6068340B2 (en) 2010-08-10 2011-08-08 Besylate of BTK inhibitor
KR1020137006114A KR20130099040A (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor
AU2011289604A AU2011289604C1 (en) 2010-08-10 2011-08-08 Besylate salt of a BTK inhibitor
CA2807051A CA2807051A1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor
IL224271A IL224271A (en) 2010-08-10 2013-01-17 Besylate salt of a btk inhibitor
ZA2013/01802A ZA201301802B (en) 2010-08-10 2013-03-08 Besylate salt of a btk inhibitor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37234910P 2010-08-10 2010-08-10
US61/372,349 2010-08-10

Publications (2)

Publication Number Publication Date
WO2012021444A1 WO2012021444A1 (en) 2012-02-16
WO2012021444A8 true WO2012021444A8 (en) 2012-05-31

Family

ID=45567913

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/046926 WO2012021444A1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor

Country Status (21)

Country Link
US (2) US8563568B2 (en)
EP (2) EP3144298A1 (en)
JP (1) JP6068340B2 (en)
KR (1) KR20130099040A (en)
CN (2) CN103096716B (en)
AR (1) AR082600A1 (en)
AU (1) AU2011289604C1 (en)
BR (1) BR112013003388A2 (en)
CA (1) CA2807051A1 (en)
DK (1) DK2603081T3 (en)
ES (1) ES2617763T3 (en)
IL (1) IL224271A (en)
MX (1) MX336875B (en)
MY (1) MY160734A (en)
NZ (1) NZ607845A (en)
PT (1) PT2603081T (en)
RU (1) RU2013109393A (en)
SG (1) SG187796A1 (en)
TW (1) TWI533872B (en)
WO (1) WO2012021444A1 (en)
ZA (1) ZA201301802B (en)

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US11590167B2 (en) 2016-12-03 2023-02-28 Juno Therapeutic, Inc. Methods and compositions for use of therapeutic T cells in combination with kinase inhibitors

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