DK2501384T3 - Fremgangsmåde til behandling af proliferative lidelser og andre patologiske tilstande formidlede af BCR-ABL, C-KIT, DDR1, DDR2, eller PDGF-R-kinaseaktivitet - Google Patents
Fremgangsmåde til behandling af proliferative lidelser og andre patologiske tilstande formidlede af BCR-ABL, C-KIT, DDR1, DDR2, eller PDGF-R-kinaseaktivitet Download PDFInfo
- Publication number
- DK2501384T3 DK2501384T3 DK10781781.9T DK10781781T DK2501384T3 DK 2501384 T3 DK2501384 T3 DK 2501384T3 DK 10781781 T DK10781781 T DK 10781781T DK 2501384 T3 DK2501384 T3 DK 2501384T3
- Authority
- DK
- Denmark
- Prior art keywords
- nilotinib
- formula
- treatment
- pyrimidylaminobenzamide
- pharmaceutically acceptable
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims description 22
- 230000000694 effects Effects 0.000 title claims description 11
- 230000001575 pathological effect Effects 0.000 title claims description 9
- 230000002062 proliferating effect Effects 0.000 title claims description 8
- -1 DDR2 Proteins 0.000 title claims description 6
- 102100036725 Epithelial discoidin domain-containing receptor 1 Human genes 0.000 title description 9
- 101710131668 Epithelial discoidin domain-containing receptor 1 Proteins 0.000 title description 9
- 108091008606 PDGF receptors Proteins 0.000 title description 9
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 title description 8
- 230000001404 mediated effect Effects 0.000 title description 7
- 238000000034 method Methods 0.000 title description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 208000035475 disorder Diseases 0.000 claims description 13
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 11
- 150000001875 compounds Chemical class 0.000 claims description 8
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 7
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 6
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims description 6
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 6
- 201000008736 Systemic mastocytosis Diseases 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 5
- 201000001441 melanoma Diseases 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 4
- 208000009905 Neurofibromatoses Diseases 0.000 claims description 4
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims description 4
- DKAGJZJALZXOOV-UHFFFAOYSA-N hydrate;hydrochloride Chemical compound O.Cl DKAGJZJALZXOOV-UHFFFAOYSA-N 0.000 claims description 4
- 201000004931 neurofibromatosis Diseases 0.000 claims description 4
- 206010016654 Fibrosis Diseases 0.000 claims description 3
- 206010039710 Scleroderma Diseases 0.000 claims description 3
- 230000004761 fibrosis Effects 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 230000035772 mutation Effects 0.000 claims description 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000007033 Dysgerminoma Diseases 0.000 claims description 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 206010036030 Polyarthritis Diseases 0.000 claims description 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 201000010208 Seminoma Diseases 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 210000004214 philadelphia chromosome Anatomy 0.000 claims description 2
- 208000030428 polyarticular arthritis Diseases 0.000 claims description 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 235000015197 apple juice Nutrition 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 239000005536 L01XE08 - Nilotinib Substances 0.000 description 58
- 229960001346 nilotinib Drugs 0.000 description 58
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 description 57
- 239000002775 capsule Substances 0.000 description 19
- 235000013399 edible fruits Nutrition 0.000 description 9
- 102100036723 Discoidin domain-containing receptor 2 Human genes 0.000 description 8
- 101710127786 Discoidin domain-containing receptor 2 Proteins 0.000 description 8
- 102000011653 Platelet-Derived Growth Factor Receptors Human genes 0.000 description 8
- 210000002966 serum Anatomy 0.000 description 8
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 description 7
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
- 206010028980 Neoplasm Diseases 0.000 description 6
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 6
- 235000015067 sauces Nutrition 0.000 description 5
- 235000013618 yogurt Nutrition 0.000 description 5
- 241000220225 Malus Species 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 3
- 240000000560 Citrus x paradisi Species 0.000 description 3
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 3
- 210000004369 blood Anatomy 0.000 description 3
- 239000008280 blood Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 235000013861 fat-free Nutrition 0.000 description 3
- 235000019253 formic acid Nutrition 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 235000021152 breakfast Nutrition 0.000 description 2
- 238000005119 centrifugation Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 230000009246 food effect Effects 0.000 description 2
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 235000015201 grapefruit juice Nutrition 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000001294 liquid chromatography-tandem mass spectrometry Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 235000012054 meals Nutrition 0.000 description 2
- 238000012552 review Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- YCBPQSYLYYBPDW-UHFFFAOYSA-N 4-methyl-n-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide;hydrate;hydrochloride Chemical compound O.Cl.C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 YCBPQSYLYYBPDW-UHFFFAOYSA-N 0.000 description 1
- 206010019668 Hepatic fibrosis Diseases 0.000 description 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 208000037656 Respiratory Sounds Diseases 0.000 description 1
- 201000009594 Systemic Scleroderma Diseases 0.000 description 1
- 206010042953 Systemic sclerosis Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- VZTDIZULWFCMLS-UHFFFAOYSA-N ammonium formate Chemical compound [NH4+].[O-]C=O VZTDIZULWFCMLS-UHFFFAOYSA-N 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 235000021016 apples Nutrition 0.000 description 1
- 238000013475 authorization Methods 0.000 description 1
- 235000013361 beverage Nutrition 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 208000029640 digestive system melanoma Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229960002411 imatinib Drugs 0.000 description 1
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 239000002050 international nonproprietary name Substances 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 238000010829 isocratic elution Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000002552 multiple reaction monitoring Methods 0.000 description 1
- 230000001613 neoplastic effect Effects 0.000 description 1
- 102000027450 oncoproteins Human genes 0.000 description 1
- 108091008819 oncoproteins Proteins 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 201000001514 prostate carcinoma Diseases 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 206010037833 rales Diseases 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000004885 tandem mass spectrometry Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
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
- A61K31/395—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
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P17/06—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
- 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
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D239/69—Benzenesulfonamido-pyrimidines
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (3)
1. Pyrimidylaminobenzamid af formlen (I)
(i), hvor Py betegner 3-pyridyl, Ri repræsenterer hydrogen, R2 repræsenterer 5-(4-methyl-1 H-imidazol-1-yl)-3-(trifluormethyl)-phenyl; og R4 repræsenterer methyl; eller et farmaceutisk acceptabelt salt deraf, til behandling af en proliferativ lidelse eller anden patologisk tilstand valgt blandt melanom, især melanom omfattende c-KIT-mutationer, brystcancer, tyktarmscancer, lungecancer, prostatacancer eller Kaposi's sarcom, gastrointestinale stromatumorer (GIST), akut myeloid leukæmi (AML), leukæmi, som reagerer på en inhibering af Abl-tyrosinkinaseaktiviteten, kronisk myeloid leukæmi (CML), Philadelphia chromosom-positiv akut lymfoblastisk leukæmi (Ph+ ALL), mesothelioma, systemisk mastocytose, hypereosinofil syndrom (HES), fibrose, leverfibrose, nyrefibrose, rheumatoid arthritis, polyarthritis, sclerodermi, lupus erythematosus, graft versus host-sygdom, neurofibromatose, pulmonal hypertension, pulmonal arteriel hypertension, Alzheimer's sygdom, seminom, dysgerminom og psoriasis, hvor forbindelsen af formel (I) eller et farmaceutisk acceptabelt salt deraf og eventuelt, farmaceutisk acceptable bærere, indgives oralt dispergeret i æblemos.
2. Pyrimidylaminobenzamid af formlen (I) til anvendelse i overensstemmelse med krav 1 i form af dets monohydrochlorid-monohydratsalt.
3. Pyrimidylaminobenzamid af formlen (I) elleret pyrimidylaminobenzamid af formlen (I) i form af dets monohydrochlorid-monohydratsalt til anvendelse i overensstemmelse med krav 1, hvor den patologiske tilstand vælges blandt CML og Ph+ ALL.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26181209P | 2009-11-17 | 2009-11-17 | |
| PCT/US2010/056926 WO2011062927A1 (en) | 2009-11-17 | 2010-11-17 | Method of treating proliferative disorders and other pathological conditions mediated by bcr-abl, c-kit, ddr1, ddr2 or pdgf-r kinase activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DK2501384T3 true DK2501384T3 (da) | 2016-05-17 |
| DK2501384T4 DK2501384T4 (da) | 2024-01-02 |
Family
ID=43513643
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK10781781.9T DK2501384T4 (da) | 2009-11-17 | 2010-11-17 | Fremgangsmåde til behandling af proliferative lidelser og andre patologiske tilstande formidlede af BCR-ABL, C-KIT, DDR1, DDR2, eller PDGF-R-kinaseaktivitet |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US9061029B2 (da) |
| EP (1) | EP2501384B2 (da) |
| JP (2) | JP5829615B2 (da) |
| KR (1) | KR101743315B1 (da) |
| CN (1) | CN102612368B (da) |
| AR (1) | AR079029A1 (da) |
| AU (1) | AU2010322102B2 (da) |
| BR (1) | BR112012011693A2 (da) |
| CA (1) | CA2779490C (da) |
| CL (1) | CL2012001270A1 (da) |
| CO (1) | CO6551690A2 (da) |
| DK (1) | DK2501384T4 (da) |
| EC (1) | ECSP12011903A (da) |
| ES (1) | ES2572128T5 (da) |
| FI (1) | FI2501384T4 (da) |
| GT (1) | GT201200150A (da) |
| HR (1) | HRP20160472T4 (da) |
| HU (1) | HUE027307T2 (da) |
| IL (1) | IL219727A (da) |
| JO (1) | JO3634B1 (da) |
| MA (1) | MA33738B1 (da) |
| ME (1) | ME02413B (da) |
| MX (1) | MX2012005694A (da) |
| MY (1) | MY169956A (da) |
| NZ (1) | NZ599968A (da) |
| PE (1) | PE20121476A1 (da) |
| PH (1) | PH12012500965A1 (da) |
| PL (1) | PL2501384T5 (da) |
| RS (1) | RS54747B2 (da) |
| RU (1) | RU2625835C2 (da) |
| SG (1) | SG10201501169VA (da) |
| SI (1) | SI2501384T2 (da) |
| SM (1) | SMT201600143B (da) |
| TN (1) | TN2012000206A1 (da) |
| TW (1) | TWI498116B (da) |
| WO (1) | WO2011062927A1 (da) |
| ZA (1) | ZA201203328B (da) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2776130A1 (en) | 2011-11-07 | 2014-09-17 | Institut National de la Sante et de la Recherche Medicale (INSERM) | A ddr1 antagonist or an inhibitor of ddr1 gene expression for use in the prevention or treatment of crescentic glomerulonephritis |
| AR090835A1 (es) | 2012-04-24 | 2014-12-10 | Chugai Pharmaceutical Co Ltd | Derivados de quinazolindiona |
| CA2871237A1 (en) | 2012-04-24 | 2013-10-31 | Chugai Seiyaku Kabushiki Kaisha | Benzamide derivative |
| CA2911040C (en) | 2012-05-02 | 2021-11-16 | Georgetown University | Treating an .alpha.-synucleinopathy with tyrosine kinase inhibitors |
| PE20161416A1 (es) * | 2012-05-15 | 2017-01-08 | Novartis Ag | Derivados de benzamida para la inhibicion de la actividad abl1, abl2 y bcr-abl1 |
| US20140080772A1 (en) * | 2012-09-06 | 2014-03-20 | The Board Of Regents Of The University Of Texas System | Treatments for melanoma |
| US9561245B2 (en) | 2012-09-06 | 2017-02-07 | The Board Of Regents Of The University Of Texas System | Combination treatments for melanoma |
| US9572828B2 (en) | 2013-07-18 | 2017-02-21 | The Board Of Regents Of The University Of Texas System | Treatment for melanoma |
| US10005739B2 (en) | 2013-10-23 | 2018-06-26 | Chugai Seiyaku Kabushiki Kaisha | Quinazolinone and isoquinolinone derivative |
| HK1248208A1 (zh) * | 2015-08-31 | 2018-10-12 | 东丽株式会社 | 尿素衍生物和其用途 |
| CN108103186B (zh) * | 2018-02-28 | 2021-07-02 | 固安博健生物技术有限公司 | 诊断类风湿性关节炎和骨关节炎的分子标志物 |
| TWI831259B (zh) | 2018-06-15 | 2024-02-01 | 漢達生技醫藥股份有限公司 | 包含達沙替尼十二烷基硫酸鹽組合物的膠囊 |
| CN120040470A (zh) | 2018-11-20 | 2025-05-27 | 乔治敦大学 | 用于治疗神经退行性、肌退行性和溶酶体贮积病症的组合物和方法 |
| WO2020144650A1 (en) * | 2019-01-10 | 2020-07-16 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of prostate cancer |
| EP4096791A1 (en) | 2020-01-31 | 2022-12-07 | Nanocopoeia LLC | Amorphous nilotinib microparticles and uses thereof |
| WO2021222739A1 (en) | 2020-04-30 | 2021-11-04 | Nanocopoeia, Llc | Orally disintegrating tablet comprising amorphous solid dispersion of nilotinib |
| MX2023003556A (es) | 2020-09-29 | 2023-06-13 | Shenzhen Pharmacin Co Ltd | Composiciones farmaceuticas. |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2337995T3 (es) | 2002-06-28 | 2010-05-03 | Nippon Shinyaku Co., Ltd. | Derivado de amida. |
| GB0215676D0 (en) * | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| CA2493764C (en) * | 2002-08-01 | 2011-05-24 | Aesgen, Inc. | Improved treatment of cancer with glutamine |
| CA2606716C (en) * | 2005-05-02 | 2013-07-23 | Novartis Ag | Use of pyrimidylaminobenzamide derivatives for the treatment of systematic mastocytosis |
| SA06270147B1 (ar) | 2005-06-09 | 2009-12-22 | نوفارتيس ايه جي | عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين |
| GT200600316A (es) | 2005-07-20 | 2007-04-02 | Sales de 4-metilo-n-(3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo)-3-(4-piridina-3-ilo-pirimidina-2-iloamino)- benzamida. | |
| GT200600315A (es) | 2005-07-20 | 2007-03-19 | Formas cristalinas de 4-metilo-n-[3-(4-metilo-imidazol-1-ilo)-5-trifluorometilo-fenilo]-3-(4-pyridina-3-ilo-pirimidina-2-iloamino)-benzamida | |
| EP1923053A1 (en) | 2006-09-27 | 2008-05-21 | Novartis AG | Pharmaceutical compositions comprising nilotinib or its salt |
| KR100925559B1 (ko) * | 2007-10-26 | 2009-11-05 | 한국과학기술연구원 | 악티노마이신 d를 유효성분으로 하는 ddr과 콜라겐결합 저해제 |
-
2010
- 2010-11-14 JO JOP/2010/0396A patent/JO3634B1/ar active
- 2010-11-15 AR ARP100104212A patent/AR079029A1/es not_active Application Discontinuation
- 2010-11-16 TW TW099139425A patent/TWI498116B/zh active
- 2010-11-17 SG SG10201501169VA patent/SG10201501169VA/en unknown
- 2010-11-17 FI FIEP10781781.9T patent/FI2501384T4/fi active
- 2010-11-17 PH PH1/2012/500965A patent/PH12012500965A1/en unknown
- 2010-11-17 US US13/509,626 patent/US9061029B2/en active Active
- 2010-11-17 CN CN201080051819.0A patent/CN102612368B/zh not_active Ceased
- 2010-11-17 MX MX2012005694A patent/MX2012005694A/es active IP Right Grant
- 2010-11-17 HU HUE10781781A patent/HUE027307T2/hu unknown
- 2010-11-17 SI SI201031172T patent/SI2501384T2/sl unknown
- 2010-11-17 JP JP2012539982A patent/JP5829615B2/ja active Active
- 2010-11-17 HR HRP20160472TT patent/HRP20160472T4/hr unknown
- 2010-11-17 PL PL10781781.9T patent/PL2501384T5/pl unknown
- 2010-11-17 MY MYPI2012001993A patent/MY169956A/en unknown
- 2010-11-17 WO PCT/US2010/056926 patent/WO2011062927A1/en not_active Ceased
- 2010-11-17 EP EP10781781.9A patent/EP2501384B2/en active Active
- 2010-11-17 AU AU2010322102A patent/AU2010322102B2/en active Active
- 2010-11-17 ES ES10781781T patent/ES2572128T5/es active Active
- 2010-11-17 PE PE2012000667A patent/PE20121476A1/es not_active Application Discontinuation
- 2010-11-17 KR KR1020127012603A patent/KR101743315B1/ko active Active
- 2010-11-17 RS RS20160303A patent/RS54747B2/sr unknown
- 2010-11-17 ME MEP-2016-89A patent/ME02413B/me unknown
- 2010-11-17 BR BR112012011693A patent/BR112012011693A2/pt not_active Application Discontinuation
- 2010-11-17 NZ NZ599968A patent/NZ599968A/en not_active IP Right Cessation
- 2010-11-17 RU RU2012124811A patent/RU2625835C2/ru active
- 2010-11-17 DK DK10781781.9T patent/DK2501384T4/da active
- 2010-11-17 CA CA2779490A patent/CA2779490C/en active Active
-
2012
- 2012-05-07 TN TNP2012000206A patent/TN2012000206A1/en unknown
- 2012-05-08 ZA ZA2012/03328A patent/ZA201203328B/en unknown
- 2012-05-10 IL IL219727A patent/IL219727A/en active IP Right Grant
- 2012-05-11 MA MA34855A patent/MA33738B1/fr unknown
- 2012-05-16 EC ECSP12011903 patent/ECSP12011903A/es unknown
- 2012-05-16 CL CL2012001270A patent/CL2012001270A1/es unknown
- 2012-05-17 GT GT201200150A patent/GT201200150A/es unknown
- 2012-05-17 CO CO12081907A patent/CO6551690A2/es not_active Application Discontinuation
-
2015
- 2015-04-28 JP JP2015091857A patent/JP2015180636A/ja active Pending
-
2016
- 2016-05-23 SM SM201600143T patent/SMT201600143B/it unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK2501384T3 (da) | Fremgangsmåde til behandling af proliferative lidelser og andre patologiske tilstande formidlede af BCR-ABL, C-KIT, DDR1, DDR2, eller PDGF-R-kinaseaktivitet | |
| KR102708049B1 (ko) | N-(3,5-디메톡시페닐)-n'-(1-메틸에틸)-n-[3-(1-메틸-1h-피라졸-4-일)퀴녹살린-6-일]에탄-1,2-디아민을 포함하는 제약 조성물 | |
| JP5992049B2 (ja) | 置換されたキナゾリノンのための経口速放性製剤 | |
| US20170143716A1 (en) | Method of treating proliferative disorders and other pathological conditions mediated by bcr-abl, c-kit, ddr1, ddr2 or pdgf-r kinase activity | |
| JP6621534B2 (ja) | 慢性咳の処置のためのオルブピタント | |
| KR20250069693A (ko) | 암 치료 | |
| EP2608792B1 (en) | Methods of administering an egfr inhibitor | |
| BR112021012255A2 (pt) | Método para o tratamento de um câncer em um paciente, método para reduzir efeitos colaterais do tratamento de um câncer em um paciente, combinação de um inibidor de cyp3a e docetaxel para uso em um tratamento médico de um câncer, docetaxel para uso em uma terapia de combinação no tratamento de câncer, inibidor de cyp3a para uso em uma terapia de combinação no tratamento de câncer, uso e kit que compreende uma composição farmacêutica para administração oral que compreende docetaxel e uma composição farmacêutica que compreende um inibidor de cyp3a | |
| BR112021004527A2 (pt) | kits e métodos para tratamento contra câncer | |
| AU2017221673A1 (en) | Novel indole derivative and anti-cancer composition containing same | |
| HK1169950B (en) | Method of treating proliferative disorders and other pathological conditions mediated by bcr-abl, c-kit, ddr1, ddr2 or pdgf-r kinase activity | |
| Dutt et al. | Evaluation of Donepezil Hydrochloride Using Various Physical Parameters | |
| JP2024509269A (ja) | 脳がんの治療における使用のためのベルバラフェニブ | |
| WO2025265030A1 (en) | Concomitant administration of selective glucocorticoid receptor modulator relacorilant and p-glycoprotein substrates | |
| Arunkumar et al. | Formulation and evaluation of bilayer matrix tablets of nebivolol hydrochloride and valsartan | |
| TW200524595A (en) | Methods for treating IGF1R-inhibitor induced hyperglycemia |