HRP20191126T1 - Spojevi pirazolopirimidina ako inhibitori kinaze - Google Patents
Spojevi pirazolopirimidina ako inhibitori kinaze Download PDFInfo
- Publication number
- HRP20191126T1 HRP20191126T1 HRP20191126TT HRP20191126T HRP20191126T1 HR P20191126 T1 HRP20191126 T1 HR P20191126T1 HR P20191126T T HRP20191126T T HR P20191126TT HR P20191126 T HRP20191126 T HR P20191126T HR P20191126 T1 HRP20191126 T1 HR P20191126T1
- Authority
- HR
- Croatia
- Prior art keywords
- disease
- compound
- pharmaceutically acceptable
- phenoxyphenyl
- pyrazolo
- Prior art date
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- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical class C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 4
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 4
- 208000027866 inflammatory disease Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- LCFFREMLXLZNHE-GBOLQPHISA-N (e)-2-[(3r)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile Chemical compound C12=C(N)N=CN=C2N([C@@H]2CCCN(C2)C(=O)C(/C#N)=C/C(C)(C)N2CCN(CC2)C2COC2)N=C1C(C(=C1)F)=CC=C1OC1=CC=CC=C1 LCFFREMLXLZNHE-GBOLQPHISA-N 0.000 claims 1
- ISBHMJZRKAFTGE-ONEGZZNKSA-N (e)-pent-2-enenitrile Chemical compound CC\C=C\C#N ISBHMJZRKAFTGE-ONEGZZNKSA-N 0.000 claims 1
- LCFFREMLXLZNHE-VWLOTQADSA-N 2-[(3s)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile Chemical compound C12=C(N)N=CN=C2N([C@H]2CCCN(C2)C(=O)C(C#N)=CC(C)(C)N2CCN(CC2)C2COC2)N=C1C(C(=C1)F)=CC=C1OC1=CC=CC=C1 LCFFREMLXLZNHE-VWLOTQADSA-N 0.000 claims 1
- KVLHSLKAKZYMEZ-CLJLJLNGSA-N 4-[(9ar)-3,4,6,7,9,9a-hexahydro-1h-pyrazino[2,1-c][1,4]oxazin-8-yl]-2-[(3r)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methylpent-2-enenitrile Chemical compound C12=C(N)N=CN=C2N([C@@H]2CCCN(C2)C(=O)C(C#N)=CC(C)(C)N2C[C@@H]3COCCN3CC2)N=C1C(C(=C1)F)=CC=C1OC1=CC=CC=C1 KVLHSLKAKZYMEZ-CLJLJLNGSA-N 0.000 claims 1
- KVLHSLKAKZYMEZ-UIOOFZCWSA-N 4-[(9as)-3,4,6,7,9,9a-hexahydro-1h-pyrazino[2,1-c][1,4]oxazin-8-yl]-2-[(3s)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methylpent-2-enenitrile Chemical compound C12=C(N)N=CN=C2N([C@H]2CCCN(C2)C(=O)C(C#N)=CC(C)(C)N2C[C@H]3COCCN3CC2)N=C1C(C(=C1)F)=CC=C1OC1=CC=CC=C1 KVLHSLKAKZYMEZ-UIOOFZCWSA-N 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 206010001767 Alopecia universalis Diseases 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 206010002412 Angiocentric lymphomas Diseases 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 208000032467 Aplastic anaemia Diseases 0.000 claims 1
- 206010003011 Appendicitis Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 206010003840 Autonomic nervous system imbalance Diseases 0.000 claims 1
- 208000036170 B-Cell Marginal Zone Lymphoma Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000032568 B-cell prolymphocytic leukaemia Diseases 0.000 claims 1
- 208000025321 B-lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010006448 Bronchiolitis Diseases 0.000 claims 1
- 208000023611 Burkitt leukaemia Diseases 0.000 claims 1
- 206010006811 Bursitis Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 206010011841 Dacryoadenitis acquired Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000004145 Endometritis Diseases 0.000 claims 1
- 208000004232 Enteritis Diseases 0.000 claims 1
- 201000011275 Epicondylitis Diseases 0.000 claims 1
- 206010016228 Fasciitis Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 208000005577 Gastroenteritis Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 201000008197 Laryngitis Diseases 0.000 claims 1
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000003926 Myelitis Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 208000005890 Neuroma Diseases 0.000 claims 1
- 208000005225 Opsoclonus-Myoclonus Syndrome Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 206010031149 Osteitis Diseases 0.000 claims 1
- 208000005141 Otitis Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010034038 Parotitis Diseases 0.000 claims 1
- 201000007100 Pharyngitis Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 206010035742 Pneumonitis Diseases 0.000 claims 1
- 206010065857 Primary Effusion Lymphoma Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 206010036711 Primary mediastinal large B-cell lymphomas Diseases 0.000 claims 1
- 206010036774 Proctitis Diseases 0.000 claims 1
- 208000035416 Prolymphocytic B-Cell Leukemia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037596 Pyelonephritis Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000007893 Salpingitis Diseases 0.000 claims 1
- 208000001106 Takayasu Arteritis Diseases 0.000 claims 1
- 208000000491 Tendinopathy Diseases 0.000 claims 1
- 206010043255 Tendonitis Diseases 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 206010045240 Type I hypersensitivity Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000006374 Uterine Cervicitis Diseases 0.000 claims 1
- 206010046914 Vaginal infection Diseases 0.000 claims 1
- 201000008100 Vaginitis Diseases 0.000 claims 1
- 208000003728 Vulvodynia Diseases 0.000 claims 1
- 206010069055 Vulvovaginal pain Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000032775 alopecia universalis congenita Diseases 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 208000010217 blepharitis Diseases 0.000 claims 1
- 208000018339 bone inflammation disease Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 206010008323 cervicitis Diseases 0.000 claims 1
- 208000003167 cholangitis Diseases 0.000 claims 1
- 201000001352 cholecystitis Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 201000003146 cystitis Diseases 0.000 claims 1
- 201000004400 dacryoadenitis Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000019479 dysautonomia Diseases 0.000 claims 1
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- 201000010063 epididymitis Diseases 0.000 claims 1
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- 238000009472 formulation Methods 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000002557 hidradenitis Diseases 0.000 claims 1
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- 208000006116 lymphomatoid granulomatosis Diseases 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 1
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- 208000004396 mastitis Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
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- 208000008494 pericarditis Diseases 0.000 claims 1
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- 208000017426 precursor B-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000018290 primary dysautonomia Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000007094 prostatitis Diseases 0.000 claims 1
- 208000002574 reactive arthritis Diseases 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
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- 206010044008 tonsillitis Diseases 0.000 claims 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
-
- 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
- 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
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- 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
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- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
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- 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
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- 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
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- 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
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Claims (10)
1. Spoj i/ili njegova farmaceutski prihvatljiva sol, naznačen time što je spoj odabran iz niza koji sadrži:
(R)-2-(3-(4-amino-3-(2-fluror-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-11-karbonil)-4-metil-4-(4-(oksetan-3-il)piperazin-1-il)pent-2-enenitril;
(S)-2-(3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-11-karbonil)-4metil-4-(4-oksetan-3-il)piperazin-1-il)pent-2-enenitril;
2-((R)-3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-((R)-heksahidropirazino[2,1-c][1,4]oksazin-8(1H)-il)-4-metilpent-2-enenitril;
2-((S)-3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-((R)-heksahidropirazino[2,1-c][1,4oksazin-8(1H)-il)-4-metilpent-2-enenitril;
2-((R)-3-4(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-((s)-heksahidropirazino[2,1-c][1,4]oksazin-8(1H)-il)-4-metilpent-2-enenitril;
2-((S)-3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-((S)-heksahidropirazino[2,1-c][1,4]oksazin-8(1H)-il)-4-metilpent-2-enenitril;
(R)-2-(3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-(5,6-dihidroimisazo[1,2-a]pirazin-7(8H)-il)-4-metilpent-2-enenitril; i
(S)-2-(3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-(5,6-dihifroimidazo[1,2-a]pirazin-7*8H)-il)-4-metilpent-2-enenitril,
ili smjesa njihovih R i S izomera; ili
(E) ili (Z) izomer bilo kojeg od gore navedenih spojeva.
2. Spoj i/ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time što je spoj:
(R)-2-(3-(4-animo-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-11-karbonil)-4-metil-4-(4-(oksetan-3-il)piperazin-1-il)pent-2-enenitril;
(S)-2-(3-(4-amino-3-)2-fluoro-4-fenoksifenil)1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-11-karbonil)-4-metil-4-(4-oksetan-3-il)piperazin-1-il)pent-2-enenitil;ili
smjesa (R)-2-(3-(4-amino-3-(2-fluoro-4-fenoksifenil)1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-metil-4-(4-(oksetan-3-il)piperazin-1-il)pent-2-enenitrila i (S)-2-(3-(4-amino-3(-2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidin-1-karbonil)-4-metil-4-(4-(oksetan-3il)piperazin-1-il)pent-2-enenitrila;
ili pojendinačni (E) ili (Z) izomer bilo kojeg od gornjih spojeva.
3. Spoj i/ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1, naznačen time sto je spoj smjesa (E) izomera i (Z) izomera (R)-2-(3-(4-amino-3-(2-fluoro-4-fenoksifenil)-1H-pirazolo[3,4-d]pirimidin-1-il)piperidon-1-karbonil)-4-metil-4-(4-(oksetan-3-il)piperazin-1-il)pent-2-enenitrila koji ima strukturu:
4. Spoj i/ili njegovu farmaceutski prihvatljivu sol prema bilo kojen od zahtjeva 1 do 3; i farmaceutski prihvatljivo pomoćno sredstvo;
poželjno spoj i/ili njegovu farmaceutski prihvatljivu sol prema zahtjevu 2 ili 3, i farmaceutski prihvatljiv prihvatljivo pomoćno sredstvo.
5. Farmaceutski pripravak prema zahtjevu 4, naznačen time da je farmaceutski pripravak enterički premazan ili formulacija s odloženim otpuštanjem.
6. Spoj i/ili njegova farmaceutski prihvatljiva sol prema bilo kojen od zahtjeva 1 do 3, naznačen time što se koristi za liječenje bolesti odabrane od autoimunih bolesti, heteroimunih stanja ili bolesti, upalnih bolesti i raka, poželjno spoj i/ili njegova farmaceutski prihvatljiva sol prema zahtjevu 2 ili 3, za uporabu za liječenje bolesti odabrane od autoimunih bolesti, heteroimunskih stanja ili bolesti, upalnih bolesti i raka.
7. Spoj i/ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 6 naznačen time da je bolest odabrana od autoimunih bolesti, heteroimunih stanja ili bolesti, te upalnih bolesti, pri čemu:
se autoimune bolesti biraju iz skupa koji čine upalna bolest crijeva, ulcerativni kolitis, artritis, lupus, reumatoidni artritis, psorijazni artritis, osteoartritis, Stillova bolest, juvenilni artritis, dijabetes, miastenija gravis, Hashimotov tiroiditis, Ordov tiroiditis, Gravesova bolest, Sjogrenov sindrom, Sjogrenova bolest suhog oka, ne-Sjogrenova bolest suhog oka, multipla skleroza, Guillain-Barreov sindrom, akutni diseminirani encefalomijelitis, Addisonova bolest, sindrom opsoklonus- mioklonus, ankilozirajući spondilitis, sindrom protu-fosfolipidnog protutijela, aplastična anemija, autoimuni hepatitis, celijakija, Goodpastureov sindrom, idiopatska trombocitopenična purpura, optički neuritis, sklerodermija, primana bilijarna ciroza, Reiterov sindrom, Takayasuov arteritis, temporalni arteritis, topla autoimuna hemolitička anemija, Wegenerova granulomatoza, psorijaza, alopecija universalis, Behcetova bolest, kronični umor, disautonomija, endometrioza, intersticijski cistitis, neuromiotonija, sklerodermija, te vulvodinija; heteroimuno stanje ili bolest se bira iz skupa koji čine bolest presatka protiv domaćina, transplantacija, transfuzija, anafilaksa, alergija, hiperosjetljivost tip I, alergijski konjunktivitis, alergijski rinitis, i atopijski dermatitis; te pri čemu je upalna bolest odabrana iz skupa koji čine astma, apendicitis, blefaritis, bronhiolitis, bronhitis, bursitis, cervicitis, kolangitis, kolecistitis, kolitis, konjunktivitis, cistitis, dakrioadenitis, dermatitis, urtikarija, dermatomiozitis, encefalitis, endokarditis, endometritis, enteritis, enterokolitis, epikondilitis, epididimitis, fascitis, fibrozitis, gastritis, gastroenteritis, hepatitis, hidradenitis suppurativa, laringitis, mastitis, meningitis, mijelitis miokarditis, miozitis, nefritis, ooforitis, orhitis, osteitis, otitis, pankreatitis, parotitis, perikarditis, peritonitis, faringitis, pleuritis, flebitis, pneumonitis, upala pluća, proktitis, prostatitis, pijelonefritis, rinitis, salpingitis, sinusitis, stomatitis, sinovitis, tendonitis, tonzilitis, uveitis, vaginitis, vaskulitis, i vulvitis.
8. Spoj i/ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju bolesti prema zahtjevu 7, naznačen time da se bolest bira između reumatoidnog artritisa, psorijaznog artritisa, lupusa, sistemskog eritematoznog lupusa, uveitisa, urtikarije, atopijskog dermatitisa, vaskulitisa uključujući Wegenerovu granulomatozu, Sjogrenov sindrom, ankilozirajućeg spondilitisa, te astme.
9. Spoj i/ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 6 naznačen time da bolest je rak izabran od limfoma difuznih velikih B-stanica, folikularnog limfoma, kroničnog limfocitnog limfoma, kronične limfocitne leukemije, B-ALL, prolifmocitne leukemije B-stanica, malog limfocitnog limfoma (SLL), multiplog mijeloma, ne-Hodgkinovog limfoma B-stanica, limfoplazmocitnog limfoma/Waldenströmove makroglobulinemije, limfoma marginalne zone prostate, mijeloma stanica plazme, plazmacitoma, ekstranodalnog B–staničnog limfoma marginalne zone, nodalnog B–staničnog limfoma marginalne zone, limfoma plaštenih stanica, medijastinalnog (timusnog) limfoma velikih B-stanica, intravaskularnog limfoma velikih B-stanica, primarnog efuzijskog limfoma, Burkittovog limfoma/leukemije, i limfomatoidne granulomatoze.
10. Spoj i/ili njegova farmaceutski prihvatljiva sol za uporabu prema bilo kojem od zahtjeva 6 do 9 naznačen time da se spoj i/ili farmaceutski prihvatljiva sol primjenjuje u kombinaciji s jednim ili više antikancerogenih ili protuupalnih sredstava.
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