DK2603081T3 - Besylatsalt af en btk-inhibitor - Google Patents

Besylatsalt af en btk-inhibitor Download PDF

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Publication number
DK2603081T3
DK2603081T3 DK11816874.9T DK11816874T DK2603081T3 DK 2603081 T3 DK2603081 T3 DK 2603081T3 DK 11816874 T DK11816874 T DK 11816874T DK 2603081 T3 DK2603081 T3 DK 2603081T3
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compound
theta
degrees
disease
mold
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DK11816874.9T
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English (en)
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Steven Richard Witowski
Iii William Frederick Westlin
Richland Wayne Tester
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Celgene Avilomics Res Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Claims (14)

1. Forbindelse 2:
2. Forbindelse ifølge krav 1, hvor forbindelsen er på fast form.
3. Forbindelse ifølge krav 2, hvor forbindelsen er krystallinsk.
4. Forbindelse ifølge krav 3, hvor forbindelsen er et krystallinsk faststof, som i det væsentlige er uden amorf forbindelse 2.
5. Forbindelse ifølge krav 1, hvor forbindelsen i det væsentlige er uden urenheder.
6. Fast form ifølge krav 2, hvor formen er form P1, hvor form P1 er kendetegnet ved at have et eller flere peaks i sit PXRD-mønster udvalgt blandt dem ved 6,21 ± 0,1 grader 2-theta, 9,48 ± 0,1 grader 2-theta og 13,29 ± 0,1 grader 2-theta.
7. Fast form ifølge krav 6, med mindst to peaks i sit PXRD-mønster udvalgt blandt dem ved 6,21 ± 0,1 grader 2-theta, 9,48 ± 0,1 grader 2-theta og 13,29 ± 0,1 grader 2-theta.
8. Fast form ifølge krav 2, hvor formen er form P22, hvor form P22 er kendetegnet ved at have et eller flere peaks i sit PXRD-mønster udvalgt blandt dem ved 7,29 ± 0,1 grader 2-theta, 8,38 ± 0,1 grader 2-theta og 11,12 ± 0,1 grader 2-theta.
9. Fast form ifølge krav 8, med mindst to peaks i sit PXRD-mønster udvalgt blandt dem ved 7,29 ± 0,1 grader 2-theta, 8,38 ± 0,1 grader 2-theta og 11,12 ± 0,1 grader 2-theta.
10. Sammensætning omfattende forbindelsen ifølge krav 1 og en farmaceutisk acceptabel bærer eller excipiens.
11. Forbindelse ifølge krav 1 eller sammensætning deraf til anvendelse ved behandling af en BTK-medieret lidelse hos en patient.
12. Forbindelse eller sammensætning til anvendelse ifølge krav 11, hvor lidelsen er udvalgt blandt en autoimmun sygdom, en heteroimmun sygdom, en inflammatorisk sygdom, en cancer, en sygdom i knogle og led eller en trom-boembolisk lidelse, fortrinsvis hvor lidelsen er udvalgt blandt reumatoid artri-tis, multipel sklerose, diabetes, kronisk lymfatisk B-celle-leukæmi, akut lymfa-tisk leukæmi, hårcelleleukæmi, non-Hodgkins lymfom, Hodgkins lymfom, myelomatose, kolorektal cancer, pancreascancer, knoglecancer, knoglemetastase, osteoporose, irritabel tyktarm, Crohns sygdom, systemisk lupus erythematosus eller lidelser, der er forbundet med nyretransplantation.
13. Fast form ifølge krav 6, som har et PXRD-mønster, der i det væsentlige ligner det, der er vist i figur 2.
14. Fast form ifølge krav 8, som har et PXRD-mønster, der i det væsentlige ligner det, der er vist i figur 6.
DK11816874.9T 2010-08-10 2011-08-08 Besylatsalt af en btk-inhibitor DK2603081T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37234910P 2010-08-10 2010-08-10
PCT/US2011/046926 WO2012021444A1 (en) 2010-08-10 2011-08-08 Besylate salt of a btk inhibitor

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DK2603081T3 true DK2603081T3 (da) 2017-01-16

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US (2) US8563568B2 (da)
EP (2) EP3144298A1 (da)
JP (1) JP6068340B2 (da)
KR (1) KR20130099040A (da)
CN (2) CN105566229A (da)
AR (1) AR082600A1 (da)
AU (1) AU2011289604C1 (da)
BR (1) BR112013003388A2 (da)
CA (1) CA2807051A1 (da)
DK (1) DK2603081T3 (da)
ES (1) ES2617763T3 (da)
IL (1) IL224271A (da)
MX (1) MX336875B (da)
MY (1) MY160734A (da)
NZ (1) NZ607845A (da)
PT (1) PT2603081T (da)
RU (1) RU2013109393A (da)
SG (1) SG187796A1 (da)
TW (1) TWI533872B (da)
WO (1) WO2012021444A1 (da)
ZA (1) ZA201301802B (da)

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