HRP20140541T4 - Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila - Google Patents
Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila Download PDFInfo
- Publication number
- HRP20140541T4 HRP20140541T4 HRP20140541TT HRP20140541T HRP20140541T4 HR P20140541 T4 HRP20140541 T4 HR P20140541T4 HR P20140541T T HRP20140541T T HR P20140541TT HR P20140541 T HRP20140541 T HR P20140541T HR P20140541 T4 HRP20140541 T4 HR P20140541T4
- Authority
- HR
- Croatia
- Prior art keywords
- disease
- fact
- cancer
- salt
- inflammatory
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title claims 15
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 201000010099 disease Diseases 0.000 claims 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 14
- 201000011510 cancer Diseases 0.000 claims 13
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 9
- 208000037244 polycythemia vera Diseases 0.000 claims 9
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 8
- 208000027866 inflammatory disease Diseases 0.000 claims 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 6
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 5
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 5
- 210000002345 respiratory system Anatomy 0.000 claims 5
- 208000017520 skin disease Diseases 0.000 claims 5
- 206010028561 Myeloid metaplasia Diseases 0.000 claims 4
- 206010028537 myelofibrosis Diseases 0.000 claims 4
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical class C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 3
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 3
- 230000002489 hematologic effect Effects 0.000 claims 3
- 210000003491 skin Anatomy 0.000 claims 3
- LGJWVXWQCTZSGC-XFULWGLBSA-N (3r)-3-cyclopentyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile;sulfuric acid Chemical compound OS(O)(=O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 LGJWVXWQCTZSGC-XFULWGLBSA-N 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 241000701085 Human alphaherpesvirus 3 Species 0.000 claims 2
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000009525 Myocarditis Diseases 0.000 claims 2
- 206010034277 Pemphigoid Diseases 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 208000000594 bullous pemphigoid Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 230000009610 hypersensitivity Effects 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 2
- 239000011976 maleic acid Substances 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 230000000699 topical effect Effects 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- WOJBKXOVBVZSET-HFNHQGOYSA-N (z)-but-2-enedioic acid;(3r)-3-cyclopentyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound OC(=O)\C=C/C(O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 WOJBKXOVBVZSET-HFNHQGOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012441 Dermatitis bullous Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 241000598436 Human T-cell lymphotropic virus Species 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102000042838 JAK family Human genes 0.000 claims 1
- 108091082332 JAK family Proteins 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 229940084434 fungoid Drugs 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 201000004614 iritis Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000005962 mycosis fungoides Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 1
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- JFMWPOCYMYGEDM-XFULWGLBSA-N ruxolitinib phosphate Chemical compound OP(O)(O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 JFMWPOCYMYGEDM-XFULWGLBSA-N 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 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
- A61K31/519—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
- 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
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- 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
- A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- C07B2200/07—Optical isomers
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Biotechnology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
Claims (17)
1. Sol izabrana iz grupe koju čine:
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol maleinske kiseline;
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol sumporne kiseline; i
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol fosforne kiseline.
2. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilnu sol maleinske kiseline.
3. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilnu sol sumporne kiseline.
4. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilnu sol fosforne kiseline.
5. Sol prema patentnom zahtjevu 1, koja je značajno izolirana.
6. Postupak pripreme soli prema bilo kojem od patentnih zahtjeva od 1 do 5 koji podrazumijeva kombiniranje (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrila sa maleinskom kiselinom, sumpornom kiselinom ili fosfornom kiselinom.
7. Pripravak koji sadrži najmanje jednu sol prema bilo kojem od patentnih zahtjeva od 1 do 5 i najmanje jedan farmaceutski prihvatljiv nosač.
8. Pripravak prema patentnom zahtjevu 7 koji je pogodan za oralnu ili topičku primjenu.
9. Pripravak prema patentnom zahtjevu 7 koji je pogodan za topičku primjenu.
10. Sol prema bilo kojem od patentnih zahtjeva od 1 do 5 za upotrebu u tretmanu bolesti kod pacijenta, naznačenu time, što bolest predstavlja bolest koju karakterizira poremećena aktivnost JAK.
11. Sol za upotrebu prema patentnom zahtjevu 10,
naznačenu time, što navedena bolest predstavlja odbacivanje alotransplanta ili oboljenje transplatat-protiv domaćina; ili
naznačenu time, što navedena bolest predstavlja autoimunu bolest; ili
naznačenu time, što navedena bolest predstavlja poremećaj kože; ili
naznačenu time, što navedena bolest predstavlja virusnu bolest; ili
naznačenu time, što navedena bolest predstavlja rak; ili
naznačenu time, što navedenu bolest karakterizira mutirani JAK2; ili
naznačenu time, što navedena bolest predstavlja mijeloproliferativni poremećaj; ili
naznačenu time, što navedena bolest predstavlja upalnu bolest; ili
naznačenu time, što navedena bolest predstavlja ishemičku reperfuzijsku povredu ili neki drugi događaj koji je posljedica ishemije; ili
naznačenu time, što navedena bolest predstavlja anoreksiju ili kaheksiju koja nastaje kao posljedica ili prati rak; ili
naznačenu time, što navedena bolest predstavlja zamor koji nastaje kao posljedica ili prati rak.
12. Sol za upotrebu prema patentnom zahtjevu 11,
naznačenu time, što navedena autoimuna bolest predstavlja poremećaj kože, multiplu sklerozu, reumatoidni artritis, juvenilni artritis, dijabetes tipa I, lupus, upalnu bolest creva, Kronovu bolest, mijasteniju gravis, imunoglobulinsku nefropatiju, miokarditis ili autoimuni poremećaj štitne žlijezde; ili
naznačenu time, što navedena autoimuna bolest predstavlja bulozni poremećaj kože; ili
naznačenu time, što navedeni poremećaj kože predstavlja atopijski dermatitis, psorijazu, preosjetljivost kože, iritaciju kože, osip, kontaktni dermatitis ili alergijsku kontaktnu preosjetljivost kože; ili
naznačenu time, što navedena virusna bolest predstavlja bolest izazvanu Epstein-Bar virusom (EBV), Hepatitis B, Hepatitis C, HIV, HTLV 1, Varicella-Zoster virusom (VZV) ili humanim papiloma virusom (HPV); ili
naznačenu time, što navedeni rak predstavlja solidan tumor; ili
naznačenu time, što navedeni rak predstavlja rak prostate, renalni rak, rak jetre, rak dojke, rak pluća, rak štitne žlijezde, Kaposijevu sarkomu, Kastelmanovu bolest ili rak gušterače; ili
naznačenu time, što navedeni rak predstavlja hematološki rak; ili
naznačenu time, što navedeni rak predstavlja rak kože; ili
naznačenu time, što navedeni rak predstavlja multipli mijelom; ili
naznačenu time, što se najmanje jedna mutacija spomenutog mutiranog JAK2 nalazi u pseudo-kinaznoj domeni navedenog JAK2; ili
naznačenu time, što navedeni mijeloproliferativni poremećaj (MPD) predstavlja policitemiju vera (PV), esencijalnu trombocitemiju (ET), mijeloidnu metaplaziju sa mijelofibrozom (MMM), kroničnu mijelogenu leukemiju (CML), hroničnu mijelomonocitnu leukemiju (CMML), hipereozinofilni sindrom (HES) ili sistemsku bolest mast ćelija (SMCD); ili
naznačenu time, što navedena upalna bolest predstavlja upalnu bolest oka; ili
naznačenu time, što navedena upalna bolest predstavlja upalnu bolest dišnih puteva; ili
naznačenu time, što navedena upalna bolest predstavlja upalnu miopatiju; ili
naznačenu time, što navedena upalna bolest predstavlja miokarditis.
13. Sol za upotrebu prema patentnom zahtjevu 12, naznačenu time, što navedeni bulozni poremećaj kože predstavlja pemfigus vulgaris (PV) ili bulozni pemfigoid (BP) ; ili
naznačenu time, što navedeni rak predstavlja rak prostate; ili
naznačenu time, što navedeni hematološki rak predstavlja limfom, leukemiju ili multipli mijelom; ili
naznačenu time, što navedeni rak kože predstavlja kožni T-ćelijski limfom ili kožni B-ćelijski limfom; ili
naznačenu time, što navedeno upalno oboljenje oka predstavlja iritis, uveitis, skleritis ili konjuktivitis; ili
naznačenu time, što se navedeno upalno oboljenje dišnih puteva odnosi na gornji respiratorni trakt; ili
naznačenu time, što se navedeno upalno oboljenje dišnih puteva odnosi na donji respiratorni trakt.
14. Sol prema bilo kojem od patentnih zahtjeva 1 do 5 za upotrebu u tretmanu raka; poremećaja kože; upalnog procesa; reumatoidnog artritisa; raka prostate; psorijaze; multiplog mijeloma; mijeloidne metaplazije sa mijelofibrozom (MMM); policitemije vera (PV); esencijalne trombocitemije (ET); fungoidne mikoze; hematološkog raka; kronične mijeloidne leukemije (CML); akutne limfoblasne leukemije (ALL); ili kronične mijelomonocitne leukemije (CMML).
15. Sol prema bilo kojem od patentnih zahtjeva od 1 do 5 za upotrebu u tretmanu mijeloidne metaplazije sa mijelofibrozom (MMM); policitemije vera (PV) ili esencijalne trombocitemije (ET).
16. (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna kisela sol fosforne kiseline za upotrebu u tretmanu mijeloproliferativnog poremećaja.
17. Spoj za upotrebu prema patentnom zahtjevu 16, naznačen time, što spomenuti mijeloproliferativni poremećaj predstavlja mijeloidna metaplazija sa mijelofibrozom (MMM); policitemija vera (PV) ili esencijalna trombocitemija (ET).
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US94370507P | 2007-06-13 | 2007-06-13 | |
EP08770794.9A EP2173752B2 (en) | 2007-06-13 | 2008-06-12 | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
PCT/US2008/066662 WO2008157208A2 (en) | 2007-06-13 | 2008-06-12 | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
Publications (2)
Publication Number | Publication Date |
---|---|
HRP20140541T1 HRP20140541T1 (hr) | 2014-07-18 |
HRP20140541T4 true HRP20140541T4 (hr) | 2022-08-19 |
Family
ID=40029273
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20140541TT HRP20140541T4 (hr) | 2007-06-13 | 2014-06-09 | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila |
HRP20160717TT HRP20160717T1 (hr) | 2007-06-13 | 2016-06-21 | Kristalne soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1 h-pirazol-1-il)-3- ciklopentilpropionitril |
HRP20190385TT HRP20190385T1 (hr) | 2007-06-13 | 2019-02-28 | Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3- ciklopentilpropionitrila |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20160717TT HRP20160717T1 (hr) | 2007-06-13 | 2016-06-21 | Kristalne soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1 h-pirazol-1-il)-3- ciklopentilpropionitril |
HRP20190385TT HRP20190385T1 (hr) | 2007-06-13 | 2019-02-28 | Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3- ciklopentilpropionitrila |
Country Status (42)
Families Citing this family (118)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005105814A1 (en) * | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
PT1951684T (pt) | 2005-11-01 | 2016-10-13 | Targegen Inc | Inibidores de cinases de tipo biaril-meta-pirimidina |
US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
PT3184526T (pt) | 2005-12-13 | 2018-12-19 | Incyte Holdings Corp | Derivados de pirrolo[2,3-d]pirimidina como inibidores da cinase janus |
EP2121692B1 (en) | 2006-12-22 | 2013-04-10 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
US20080312259A1 (en) | 2007-06-13 | 2008-12-18 | Incyte Corporation | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE |
EA020777B1 (ru) * | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
TWI444382B (zh) | 2008-03-11 | 2014-07-11 | Incyte Corp | 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物 |
JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
CN105837560A (zh) | 2009-02-27 | 2016-08-10 | 埃姆比特生物科学公司 | 调控jak激酶的喹唑啉衍生物和其使用方法 |
CN106967070A (zh) | 2009-05-22 | 2017-07-21 | 因塞特控股公司 | 作为jak抑制剂的化合物 |
ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
BR112012008267B1 (pt) * | 2009-10-09 | 2022-10-04 | Incyte Holdings Corporation | Derivados hidroxila, ceto e glucuronida de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1- il)-3-ciclopentilpropanonitrila |
SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
CA2790070C (en) * | 2010-02-18 | 2018-03-06 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
TWI766281B (zh) | 2010-03-10 | 2022-06-01 | 美商英塞特控股公司 | 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物 |
PE20130216A1 (es) * | 2010-05-21 | 2013-02-27 | Incyte Corp | Formulacion topica para un inhibidor de jak |
MX2013002384A (es) | 2010-09-01 | 2013-07-05 | Ambit Biosciences Corp | Compuestos quinazolina y metodos para utilizarlos. |
PT2635299T (pt) * | 2010-11-02 | 2019-10-14 | Univ Columbia | Métodos de tratamento de distúrbios de perda de cabelo |
WO2012060847A1 (en) | 2010-11-07 | 2012-05-10 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | Novartis Pharma Ag | mTOR/JAK inhibitor combination therapy |
MX344580B (es) * | 2011-06-14 | 2016-12-20 | Novartis Ag | Combinacion de panobinostat y ruxolitinib en el tratamiento del cancer tal como una neoplasia mieloproliferativa. |
EA201490042A1 (ru) | 2011-06-20 | 2014-10-30 | Инсайт Корпорейшн | Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak |
CN102921007B (zh) * | 2011-08-09 | 2014-12-10 | 中国科学院上海生命科学研究院 | 防治胰岛素抵抗和糖尿病的方法和试剂 |
WO2013023119A1 (en) * | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | JAK P13K/mTOR COMBINATION THERAPY |
TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
US10821111B2 (en) | 2011-11-30 | 2020-11-03 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
US9089574B2 (en) | 2011-11-30 | 2015-07-28 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
US20130310340A1 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
AR091079A1 (es) | 2012-05-18 | 2014-12-30 | Incyte Corp | Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak |
WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
CA2879603A1 (en) | 2012-07-27 | 2014-01-30 | Ratiopharm Gmbh | Oral dosage forms for modified release comprising ruxolitinib |
CN107936039A (zh) | 2012-11-01 | 2018-04-20 | 因赛特公司 | 作为jak抑制剂的三环稠合噻吩衍生物 |
SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
HUE057262T2 (hu) | 2013-03-06 | 2022-04-28 | Incyte Holdings Corp | Eljárás és köztitermékek JAK inhibitor elõállítására |
US20140343034A1 (en) * | 2013-04-25 | 2014-11-20 | Japan Tobacco Inc. | Skin barrier function improving agent |
PL3786162T3 (pl) | 2013-05-17 | 2024-04-08 | Incyte Holdings Corporation | Pochodne bipirazolu jako inhibitory jak |
US9655854B2 (en) * | 2013-08-07 | 2017-05-23 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
EP3049110A2 (en) * | 2013-09-23 | 2016-08-03 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for targeting tumor microenvironment and for preventing metastasis |
CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
MA39987A (fr) | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
CN105218548A (zh) * | 2014-06-09 | 2016-01-06 | 上海海和药物研究开发有限公司 | 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途 |
WO2016024232A1 (en) | 2014-08-11 | 2016-02-18 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor, a jak-2 inhibitor and/or a cdk 4/6 inhibitor |
HRP20220738T1 (hr) | 2014-08-11 | 2022-08-19 | Acerta Pharma B.V. | Terapijske kombinacije inhibitora btk, inhibitora pd-1 i/ili inhibitora pd-l1 |
HUE056329T2 (hu) | 2014-08-11 | 2022-02-28 | Acerta Pharma Bv | BTK-inhibitor és BCL-2-inhibitor terápiás kombinációi |
ES2874537T3 (es) * | 2014-08-21 | 2021-11-05 | Ratiopharm Gmbh | Sal oxalato de ruxolitinib |
EP3183253B1 (en) * | 2014-08-21 | 2018-06-27 | ratiopharm GmbH | Salt of (r)-3-(4-(7h-pyrrolo [2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3-cyclopentylpropanenitrile with benzenesulfonic acid |
WO2016035014A1 (en) * | 2014-09-01 | 2016-03-10 | Sun Pharmaceutical Industries Limited | Processes for the preparation of ruxolitinib phosphate |
WO2016063294A2 (en) * | 2014-10-20 | 2016-04-28 | Msn Laboratories Private Limited | Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof |
CZ2014773A3 (cs) | 2014-11-10 | 2016-05-18 | Zentiva, K.S. | Soli (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu |
WO2016077595A1 (en) | 2014-11-12 | 2016-05-19 | The General Hospital Corporation | Methods for treating neurodegenerative diseases |
CZ2015496A3 (cs) | 2015-07-14 | 2017-01-25 | Zentiva, K.S. | Krystalické formy solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a jejich příprava |
ES2898329T3 (es) | 2016-01-12 | 2022-03-07 | Oncotracker Inc | Métodos mejorados para supervisar el estado inmunitario de un sujeto |
CZ201629A3 (cs) | 2016-01-22 | 2017-08-02 | Zentiva, K.S. | Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy |
CN107573348B (zh) * | 2016-01-29 | 2019-09-03 | 上海宣创生物科技有限公司 | 巴瑞克替尼三氟乙酸盐b晶型及其制备方法 |
CN107641125A (zh) * | 2016-02-01 | 2018-01-30 | 上海宣创生物科技有限公司 | 巴瑞克替尼磷酸盐i晶型及其制备方法 |
WO2017173451A1 (en) * | 2016-04-01 | 2017-10-05 | The General Hospital Corporation | Targeting innate immune signaling in neuroinflammation and neurodegeneration |
CN107759600A (zh) * | 2016-06-16 | 2018-03-06 | 正大天晴药业集团股份有限公司 | 作为jak抑制剂的吡咯并嘧啶化合物的结晶 |
WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
RU2644155C1 (ru) * | 2016-12-12 | 2018-02-08 | Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") | 2-(3-(4-(7H-пирроло[2,3-d]пиримидин-4-ил)-1H-пиразол-1-ил)-1-(этилсульфонил)азетидин-3-ил)ацетонитрила геминафтилдисульфонат в качестве ингибитора Янус киназ |
WO2018231944A1 (en) | 2017-06-13 | 2018-12-20 | Berenson James R | Diagnostic, prognostic, and monitoring methods for solid tumor cancers |
US10981906B2 (en) | 2017-11-03 | 2021-04-20 | Aclaris Therapeutics, Inc. | Substituted pyrrolopyridine JAK inhibitors and methods of making and using the same |
US10800775B2 (en) | 2017-11-03 | 2020-10-13 | Aclaris Therapeutics, Inc. | Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same |
AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
CN112105608B (zh) | 2018-01-30 | 2023-07-14 | 因赛特公司 | 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法 |
EP3752146A1 (en) | 2018-02-16 | 2020-12-23 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
KR20210003086A (ko) | 2018-03-08 | 2021-01-11 | 노파르티스 아게 | 항-p-셀렉틴 항체의 용도 |
AU2019245420A1 (en) | 2018-03-30 | 2020-11-12 | Incyte Corporation | Treatment of hidradenitis suppurativa using JAK inhibitors |
WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
MA52208A (fr) | 2018-04-13 | 2021-02-17 | Incyte Corp | Biomarqueurs pour une maladie du greffon contre l'hôte |
AU2019314302A1 (en) | 2018-07-31 | 2021-01-28 | Loxo Oncology, Inc. | Spray-dried dispersions and formulations of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1H-pyrazole-4-carboxamide |
JP2021534244A (ja) | 2018-08-10 | 2021-12-09 | アクラリス セラピューティクス,インコーポレイテッド | ピロロピリミジンitk阻害剤 |
WO2020039401A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | Treatment comprising il-1βeta binding antibodies and combinations thereof |
AU2019335200A1 (en) | 2018-09-04 | 2021-03-11 | Theravance Biopharma R&D Ip, Llc | 5 to 7 membered heterocyclic amides as JAK inhibitors |
CA3117969A1 (en) | 2018-10-31 | 2020-05-07 | Incyte Corporation | Combination therapy for treatment of hematological diseases |
US20220041579A1 (en) | 2018-12-19 | 2022-02-10 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of fgfr tyrosine kinases |
CN113490666A (zh) | 2018-12-19 | 2021-10-08 | 奥瑞生物药品公司 | 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物 |
CN114007621A (zh) | 2019-03-05 | 2022-02-01 | 因赛特公司 | 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂 |
JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
US20220202820A1 (en) | 2019-04-16 | 2022-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
KR20220004726A (ko) | 2019-05-02 | 2022-01-11 | 어클라리스 쎄라퓨틱스, 인코포레이티드 | Jak 억제제로서의 치환된 피롤로피리딘 |
US20200405627A1 (en) | 2019-06-10 | 2020-12-31 | Incyte Corporation | Topical treatment of vitiligo by a jak inhibitor |
CA3144871A1 (en) | 2019-06-27 | 2020-12-30 | Crispr Therapeutics Ag | Use of chimeric antigen receptor t cells and nk cell inhibitors for treating cancer |
CN114599364A (zh) | 2019-09-05 | 2022-06-07 | 因赛特公司 | 用于减少特应性皮炎瘙痒的鲁索替尼制剂 |
WO2021053490A1 (en) | 2019-09-16 | 2021-03-25 | Novartis Ag | Use of high-affinity, ligand-blocking, humanized anti-t-cell immunoglobulin domain and mucin domain-3 (tim-3) igg4 antibody for the treatment of myelofibrosis |
JP2022547311A (ja) | 2019-09-16 | 2022-11-11 | ノバルティス アーゲー | 骨髄線維症の治療のためのmdm2阻害剤の使用 |
US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
JP2023506118A (ja) | 2019-10-16 | 2023-02-15 | インサイト・コーポレイション | 皮膚エリテマトーデス及び扁平苔癬(lp)の治療のためのjak1阻害剤の使用 |
IL293085A (en) | 2019-11-22 | 2022-07-01 | Incyte Corp | Combined treatment that includes an alk2 inhibitor and a jak2 inhibitor |
EP3892280A3 (en) | 2020-04-09 | 2022-01-12 | Children's Hospital Medical Center | Sars-cov-2 infection biomarkers and uses thereof |
WO2021206766A1 (en) | 2020-04-09 | 2021-10-14 | Children's Hospital Medical Center | Sars-cov-2 infection biomarkers and uses thereof |
US11324750B2 (en) | 2020-04-09 | 2022-05-10 | Children's Hospital Medical Center | Compositions and methods for the treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection |
PE20231102A1 (es) | 2020-06-02 | 2023-07-19 | Incyte Corp | Procesos para preparar un inhibidor de jak1 |
CA3184633A1 (en) | 2020-06-03 | 2021-12-09 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
US20220023344A1 (en) | 2020-06-26 | 2022-01-27 | Crispr Therapeutics Ag | Allogeneic cell therapy of acute lymphoblastic leukemia using genetically engineered t cells targeting cd19 |
KR20230096973A (ko) | 2020-08-18 | 2023-06-30 | 인사이트 코포레이션 | Jak 저해제를 제조하기 위한 방법 및 중간체 |
US11897889B2 (en) | 2020-08-18 | 2024-02-13 | Incyte Corporation | Process and intermediates for preparing a JAK1 inhibitor |
CN116261447A (zh) | 2020-09-16 | 2023-06-13 | 因赛特公司 | 局部治疗白癜风 |
CA3197645A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Topical ruxolitinib for treating lichen planus |
WO2022074599A1 (en) | 2020-10-08 | 2022-04-14 | Novartis Ag | Use of an erk inhibitor for the treatment of myelofibrosis |
US20240000777A1 (en) | 2020-10-08 | 2024-01-04 | Novartis Ag | Use of an erk inhibitor for the treatment of myelofibrosis |
MX2023006638A (es) | 2020-12-04 | 2023-08-22 | Incyte Corp | Inhibidor de la cinasa janus (jak) con un análogo de la vitamina d para el tratamiento de enfermedades de la piel. |
MX2023006542A (es) | 2020-12-08 | 2023-08-25 | Incyte Corp | Inhibidores de la vía cinasa jano 1 (jak1) para el tratamiento del vitiligo. |
JP2024503021A (ja) | 2021-01-11 | 2024-01-24 | インサイト・コーポレイション | Jak経路阻害剤及びrock阻害剤を含む併用療法 |
WO2022182857A1 (en) | 2021-02-25 | 2022-09-01 | Impact Biomedicines, Inc. | Use of a bet inhibitor alone or in combination with fedratinib or ruxolitinib for treating a hematological malignancy such as myelofibrosis |
WO2023102559A1 (en) | 2021-12-03 | 2023-06-08 | Incyte Corporation | Topical formulations of ruxolitinib with an organic amine ph adjusting agent for treatment of skin diseases |
WO2023222565A1 (en) | 2022-05-16 | 2023-11-23 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation |
US20230399331A1 (en) | 2022-06-14 | 2023-12-14 | Incyte Corporation | Solid forms of jak inhibitor and process of preparing the same |
WO2024028193A1 (en) | 2022-08-03 | 2024-02-08 | Medichem, S.A. | Stable oral pharmaceutical formulation containing ruxolitinib hemifumarate |
WO2024099396A1 (zh) * | 2022-11-11 | 2024-05-16 | 浙江奥翔药业股份有限公司 | 芦可替尼晶体及其药物组合物 |
Family Cites Families (286)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2985589A (en) | 1957-05-22 | 1961-05-23 | Universal Oil Prod Co | Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets |
US3832460A (en) * | 1971-03-19 | 1974-08-27 | C Kosti | Anesthetic-vasoconstrictor-antihistamine composition for the treatment of hypertrophied oral tissue |
US4140755A (en) | 1976-02-13 | 1979-02-20 | Hoffmann-La Roche Inc. | Sustained release tablet formulations |
GB2030584B (en) | 1978-10-03 | 1983-03-23 | Lankro Chem Ltd | Photopolymerisable solder resist compositions |
JPS5553537A (en) | 1978-10-13 | 1980-04-19 | Barron Robert Michael | Abrasive foam material and its preparation |
DE3036390A1 (de) | 1980-09-26 | 1982-05-13 | Troponwerke GmbH & Co KG, 5000 Köln | Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen |
DE3220113A1 (de) | 1982-05-28 | 1983-12-01 | Basf Ag, 6700 Ludwigshafen | Difluormethoxiphenylthiophosphorsaeureester |
US4402832A (en) | 1982-08-12 | 1983-09-06 | Uop Inc. | High efficiency continuous separation process |
US4548990A (en) | 1983-08-15 | 1985-10-22 | Ciba-Geigy Corporation | Crosslinked, porous polymers for controlled drug delivery |
US4498991A (en) | 1984-06-18 | 1985-02-12 | Uop Inc. | Serial flow continuous separation process |
NL8403224A (nl) | 1984-10-24 | 1986-05-16 | Oce Andeno Bv | Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen. |
CA1306260C (en) | 1985-10-18 | 1992-08-11 | Shionogi & Co., Ltd. | Condensed imidazopyridine derivatives |
JPH0781138B2 (ja) | 1986-12-02 | 1995-08-30 | 株式会社資生堂 | 抗酸化剤 |
ES2087916T3 (es) | 1989-10-11 | 1996-08-01 | Teijin Ltd | Derivado de pirimidina biciclico, metodo para producir el mismo, y preparacion farmaceutica que contiene el mismo como ingrediente activo. |
IT1258781B (it) | 1992-01-16 | 1996-02-29 | Zambon Spa | Composizione farmaceutica oftalmica contenente n-acetilcisteina e polivinilalcol |
US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
AU671491B2 (en) | 1992-12-18 | 1996-08-29 | F. Hoffmann-La Roche Ag | N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines |
US6638905B2 (en) | 1993-06-18 | 2003-10-28 | The Salk Institute For Biological Studies | Cloning and recombinant production of CFR receptor(s) |
JPH0710876A (ja) | 1993-06-24 | 1995-01-13 | Teijin Ltd | 4位に環状アミノ基を有するピロロ[2,3―d]ピリミジン |
EP0727217A3 (en) | 1995-02-10 | 1997-01-15 | Suntory Ltd | Pharmaceutical and cosmetic compositions containing God-type ellagitannin as an active ingredient |
IL117580A0 (en) | 1995-03-29 | 1996-07-23 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them |
US5856326A (en) | 1995-03-29 | 1999-01-05 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
MX9800136A (es) | 1995-07-05 | 1998-03-29 | Du Pont | Pirimidinonas fungicidas. |
SK398A3 (en) | 1995-07-06 | 1998-07-08 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
US5630943A (en) | 1995-11-30 | 1997-05-20 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Discontinuous countercurrent chromatographic process and apparatus |
GB9604361D0 (en) | 1996-02-29 | 1996-05-01 | Pharmacia Spa | 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors |
AU727939B2 (en) | 1996-04-03 | 2001-01-04 | Merck & Co., Inc. | A method of treating cancer |
WO1997038664A2 (en) | 1996-04-18 | 1997-10-23 | Merck & Co., Inc. | A method of treating cancer |
US5795909A (en) * | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
WO1997045412A1 (en) | 1996-05-30 | 1997-12-04 | Merck & Co., Inc. | A method of treating cancer |
US6624138B1 (en) * | 2001-09-27 | 2003-09-23 | Gp Medical | Drug-loaded biological material chemically treated with genipin |
CA2286239A1 (en) | 1997-04-07 | 1998-10-15 | Merck & Co., Inc. | A method of treating cancer |
US6063284A (en) | 1997-05-15 | 2000-05-16 | Em Industries, Inc. | Single column closed-loop recycling with periodic intra-profile injection |
US6060038A (en) | 1997-05-15 | 2000-05-09 | Merck & Co., Inc. | Radiolabeled farnesyl-protein transferase inhibitors |
WO1999007379A1 (en) | 1997-08-11 | 1999-02-18 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,6-HETEROARYL-DIPYRIDO[2,3-b:3',2'-f]AZEPINES AND THEIR USE IN THE PREVENTION OR TREATMENT OF HIV INFECTION |
US6075056A (en) | 1997-10-03 | 2000-06-13 | Penederm, Inc. | Antifungal/steroid topical compositions |
US6025366A (en) | 1998-04-02 | 2000-02-15 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
US6232320B1 (en) * | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
SK18542000A3 (sk) | 1998-06-04 | 2001-12-03 | Abbott Laboratories | Protizápalové zlúčeniny inhibujúce bunkovú adhéziu |
PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
EA005852B1 (ru) | 1998-06-19 | 2005-06-30 | Пфайзер Продактс Инк. | ПИРРОЛО[2,3-d]ПИРИМИДИНЫ |
ATE459616T1 (de) | 1998-08-11 | 2010-03-15 | Novartis Ag | Isochinoline derivate mit angiogenesis-hemmender wirkung |
JP2000119271A (ja) | 1998-08-12 | 2000-04-25 | Hokuriku Seiyaku Co Ltd | 1h―イミダゾピリジン誘導体 |
CA2343148C (en) * | 1998-09-10 | 2005-11-15 | Nycomed Danmark A/S | Quick release pharmaceutical compositions of drug substances |
JP3869128B2 (ja) | 1998-09-11 | 2007-01-17 | 株式会社ルネサステクノロジ | 半導体集積回路装置の製造方法 |
US6375839B1 (en) | 1998-10-29 | 2002-04-23 | Institut Francais Du Petrole | Process and device for separation with variable-length chromatographic zones |
FR2785196B1 (fr) | 1998-10-29 | 2000-12-15 | Inst Francais Du Petrole | Procede et dispositif de separation avec des zones chromatographiques a longueur variable |
US6413419B1 (en) | 1998-10-29 | 2002-07-02 | Institut Francais Du Petrole | Process and device for separation with variable-length chromatographic |
US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
JP2002538121A (ja) | 1999-03-03 | 2002-11-12 | メルク エンド カムパニー インコーポレーテッド | プレニルタンパク質トランスフェラーゼの阻害剤 |
GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
US6217895B1 (en) | 1999-03-22 | 2001-04-17 | Control Delivery Systems | Method for treating and/or preventing retinal diseases with sustained release corticosteroids |
US6239113B1 (en) | 1999-03-31 | 2001-05-29 | Insite Vision, Incorporated | Topical treatment or prevention of ocular infections |
WO2000063168A1 (en) | 1999-04-16 | 2000-10-26 | Coelacanth Chemical Corporation | Synthesis of azetidine derivatives |
US6921763B2 (en) | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
US6699880B1 (en) | 1999-10-13 | 2004-03-02 | Banyu Pharmaceutical Co., Ltd. | Substituted imidazolidinone derivatives |
CN1195755C (zh) * | 1999-12-10 | 2005-04-06 | 辉瑞产品公司 | 吡咯并[2,3-d]嘧啶化合物 |
IL150388A0 (en) * | 1999-12-24 | 2002-12-01 | Aventis Pharma Ltd | Azaindoles |
GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
US7235551B2 (en) | 2000-03-02 | 2007-06-26 | Smithkline Beecham Corporation | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases |
DK1142566T3 (da) | 2000-04-07 | 2004-02-09 | Medidom Lab | Oftalmologiske formuleringer på basis af ciclosporin, hyaluronsyre og polysorbat |
AU4878601A (en) | 2000-04-20 | 2001-11-07 | Mitsubishi Corporation | Aromatic amide compounds |
MXPA02010618A (es) | 2000-04-25 | 2004-05-05 | Icos Corp | Inhibidores de fosfatidilinositol 3-quinasa delta. |
US7498304B2 (en) | 2000-06-16 | 2009-03-03 | Curis, Inc. | Angiogenesis-modulating compositions and uses |
CA2412215A1 (en) | 2000-06-16 | 2001-12-27 | Curis, Inc. | Angiogenesis-modulating compositions and uses |
US6335342B1 (en) * | 2000-06-19 | 2002-01-01 | Pharmacia & Upjohn S.P.A. | Azaindole derivatives, process for their preparation, and their use as antitumor agents |
AU2001274598A1 (en) * | 2000-06-23 | 2002-01-02 | Mitsubishi Pharma Corporation | Antitumor effect potentiators |
MXPA03000068A (es) | 2000-06-26 | 2003-09-25 | Pfizer Prod Inc | Compuestos de pirrolo (2,3-d)pirimidina como agentes inmunosupresores. |
IL153231A0 (en) | 2000-06-28 | 2003-07-06 | Smithkline Beecham Plc | Wet milling process |
EP1343781B1 (en) | 2000-12-05 | 2008-09-03 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
GB0100622D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds V111 |
US20040077654A1 (en) | 2001-01-15 | 2004-04-22 | Bouillot Anne Marie Jeanne | Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression |
WO2002060492A1 (en) | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
AU2002308748A1 (en) | 2001-05-16 | 2002-11-25 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
US7301023B2 (en) | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
GB0115393D0 (en) | 2001-06-23 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
ES2274986T3 (es) * | 2001-08-01 | 2007-06-01 | MERCK & CO., INC. | Derivados de benzimidazo 4,5-f/isoquinolinona. |
IL160915A0 (en) | 2001-09-19 | 2004-08-31 | Aventis Pharma Sa | Indolizines inhibiting kinase proteins |
US6429231B1 (en) | 2001-09-24 | 2002-08-06 | Bradley Pharmaceuticals, Inc. | Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use |
RU2337692C3 (ru) | 2001-10-30 | 2020-11-09 | Новартис Аг | Производные стауроспорина в качестве ингибиторов активности рецепторной тирозинкиназы flt3 |
JP2003155285A (ja) | 2001-11-19 | 2003-05-27 | Toray Ind Inc | 環状含窒素誘導体 |
AU2002224131A1 (en) | 2001-11-30 | 2003-06-17 | Teijin Limited | Process for producing 5-(3-cyanophenyl)-3-formylbenzoic acid compound |
GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
US6995144B2 (en) | 2002-03-14 | 2006-02-07 | Eisai Co., Ltd. | Nitrogen containing heterocyclic compounds and medicines containing the same |
TW200403058A (en) * | 2002-04-19 | 2004-03-01 | Bristol Myers Squibb Co | Heterocyclo inhibitors of potassium channel function |
AU2003237121A1 (en) * | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
DE60318198T2 (de) | 2002-05-02 | 2008-12-04 | Merck & Co., Inc. | Tyrosinkinase-hemmer |
BR0309844A (pt) | 2002-05-07 | 2005-02-15 | Control Delivery Sys Inc | Processos para formação de um dispositivo para a distribuição de droga |
CA2486183C (en) | 2002-05-23 | 2012-01-10 | Cytopia Pty Ltd. | Protein kinase inhibitors |
TW200406374A (en) | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
WO2004003026A1 (ja) | 2002-06-26 | 2004-01-08 | Idemitsu Kosan Co., Ltd. | 共重合体水素添加物、その製造方法及びそれを用いたホットメルト接着剤組成物 |
GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
GB0215844D0 (en) | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
AU2003252478A1 (en) | 2002-07-10 | 2004-02-02 | Ono Pharmaceutical Co., Ltd. | Ccr4 antagonist and medicinal use thereof |
PL374700A1 (en) | 2002-09-20 | 2005-10-31 | Alcon, Inc. | Use of cytokine synthesis inhibitors for the treatment of dry eye disorders |
US20040204404A1 (en) | 2002-09-30 | 2004-10-14 | Robert Zelle | Human N-type calcium channel blockers |
CA2506773A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
PL378246A1 (pl) | 2002-11-26 | 2006-03-20 | Pfizer Products Inc. | Sposób leczenia odrzucania przeszczepu |
UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
UY28126A1 (es) | 2002-12-24 | 2004-06-30 | Alcon Inc | Uso de glucocorticoides selectivos para la superficie ocular en el tratamiento de la sequedad ocular |
US7135493B2 (en) | 2003-01-13 | 2006-11-14 | Astellas Pharma Inc. | HDAC inhibitor |
US7444183B2 (en) * | 2003-02-03 | 2008-10-28 | Enteromedics, Inc. | Intraluminal electrode apparatus and method |
JP2006518381A (ja) | 2003-02-07 | 2006-08-10 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール |
GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
US7547794B2 (en) | 2003-04-03 | 2009-06-16 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
SE0301373D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
SE0301372D0 (sv) | 2003-05-09 | 2003-05-09 | Astrazeneca Ab | Novel compounds |
FR2857454B1 (fr) | 2003-07-08 | 2006-08-11 | Aventis Pasteur | Dosage des acides techoiques des bacteries gram+ |
US20050043346A1 (en) | 2003-08-08 | 2005-02-24 | Pharmacia Italia S.P.A. | Pyridylpyrrole derivatives active as kinase inhibitors |
EP1663204B1 (en) | 2003-08-29 | 2014-05-07 | Exelixis, Inc. | C-kit modulators and methods of use |
WO2005026129A1 (en) | 2003-09-15 | 2005-03-24 | Gpc Biotech Ag | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
AR045944A1 (es) | 2003-09-24 | 2005-11-16 | Novartis Ag | Derivados de isoquinolina 1.4-disustituidas |
TWI343256B (en) | 2003-10-24 | 2011-06-11 | Santen Pharmaceutical Co Ltd | Cornea-conjunctiva disorder treating agent |
MY141220A (en) | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
MXPA06005882A (es) | 2003-11-25 | 2006-06-27 | Pfizer Prod Inc | Metodo de tratamiento de la aterosclerosis. |
JP2007514729A (ja) | 2003-12-17 | 2007-06-07 | ファイザー・プロダクツ・インク | 移植拒絶反応の治療方法 |
PL1696920T3 (pl) | 2003-12-19 | 2015-03-31 | Plexxikon Inc | Związki i sposoby opracowywania modulatorów Ret |
CN1918138B (zh) | 2003-12-19 | 2011-05-04 | 先灵公司 | 作为cxc-和cc-趋化因子受体配体的噻二唑化合物 |
NZ547696A (en) | 2003-12-23 | 2009-12-24 | Astex Therapeutics Ltd | Pyrazole derivatives as protein kinase modulators |
WO2005067546A2 (en) * | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
EP1744751A4 (en) | 2004-03-18 | 2010-03-10 | Brigham & Womens Hospital | TREATMENT OF SYNUCLEINOPATHIES |
ATE508129T1 (de) | 2004-03-30 | 2011-05-15 | Vertex Pharma | Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole |
EP1750727A2 (en) | 2004-04-23 | 2007-02-14 | Exelixis, Inc. | Kinase modulators and methods of use |
WO2005105814A1 (en) | 2004-04-28 | 2005-11-10 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
US7558717B2 (en) | 2004-04-28 | 2009-07-07 | Vertex Pharmaceuticals Incorporated | Crystal structure of human JAK3 kinase domain complex and binding pockets thereof |
AU2005237254B2 (en) | 2004-05-03 | 2010-02-04 | Novartis Ag | Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor |
US20060074102A1 (en) | 2004-05-14 | 2006-04-06 | Kevin Cusack | Kinase inhibitors as therapeutic agents |
PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
ES2396135T3 (es) | 2004-06-10 | 2013-02-19 | Irm Llc | Compuestos y composiciones como inhibidores de proteínas cinasas |
JP5315611B2 (ja) | 2004-06-23 | 2013-10-16 | 小野薬品工業株式会社 | S1p受容体結合能を有する化合物およびその用途 |
EP1765819B1 (en) | 2004-06-30 | 2014-03-12 | Vertex Pharmaceuticals Inc. | Azaindoles useful as inhibitors of protein kinases |
US7138423B2 (en) * | 2004-07-20 | 2006-11-21 | Bristol-Myers Squibb Company | Arylpyrrolidine derivatives as NK-1 /SSRI antagonists |
FR2873691B1 (fr) | 2004-07-29 | 2006-10-06 | Sanofi Synthelabo | Derives d'amino-piperidine, leur preparation et leur application en therapeutique |
WO2006013114A1 (en) | 2004-08-06 | 2006-02-09 | Develogen Aktiengesellschaft | Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome |
CN101006186A (zh) | 2004-08-23 | 2007-07-25 | 财团法人牧岩生命工学研究所 | 用于检测sars冠状病毒的引物和探针,包括该引物和/或探针的试剂盒及其检测方法 |
US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
KR100858262B1 (ko) | 2004-10-13 | 2008-09-11 | 에프. 호프만-라 로슈 아게 | Cdk2 및 혈관신생에 대한 저해제로서 유용하고, 유방암,대장암, 폐암 및 전립선암의 치료용으로 유용한이중치환된 피라졸로벤조디아제핀 |
UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
ES2354824T3 (es) | 2004-11-04 | 2011-03-18 | Vertex Pharmaceuticals, Inc. | Pirazolo[1,5-a]pirimidinas útiles como inhibidores de proteínas cinasas. |
EP1885352A2 (en) | 2004-11-24 | 2008-02-13 | Novartis AG | Combinations comprising jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors |
US7517870B2 (en) | 2004-12-03 | 2009-04-14 | Fondazione Telethon | Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization |
US20060128803A1 (en) | 2004-12-14 | 2006-06-15 | Alcon, Inc. | Method of treating dry eye disorders using 13(S)-HODE and its analogs |
US7981065B2 (en) | 2004-12-20 | 2011-07-19 | Cardiac Pacemakers, Inc. | Lead electrode incorporating extracellular matrix |
AR054416A1 (es) | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
TW200635899A (en) | 2004-12-22 | 2006-10-16 | Astrazeneca Ab | Chemical compounds |
EP1844037A1 (en) | 2005-01-20 | 2007-10-17 | Pfizer Limited | Chemical compounds |
US8633205B2 (en) * | 2005-02-03 | 2014-01-21 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases |
US7683171B2 (en) | 2005-02-04 | 2010-03-23 | Bristol-Myers Squibb Company | 1H-imidazo[4,5-d]thieno[3,2-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same |
JP2008533145A (ja) | 2005-03-15 | 2008-08-21 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
WO2006108103A1 (en) | 2005-04-05 | 2006-10-12 | Pharmacopeia, Inc. | Purine and imidazopyridine derivatives for immunosuppression |
GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
CN101228161B (zh) | 2005-05-20 | 2012-10-10 | 沃泰克斯药物股份有限公司 | 适用作蛋白激酶抑制剂的吡咯并吡啶类 |
ES2651349T3 (es) | 2005-06-08 | 2018-01-25 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta JAK |
AU2006254825A1 (en) | 2005-06-08 | 2006-12-14 | Targegen, Inc. | Methods and compositions for the treatment of ocular disorders |
WO2006136823A1 (en) | 2005-06-21 | 2006-12-28 | Astex Therapeutics Limited | Heterocyclic containing amines as kinase b inhibitors |
BRPI0611863B1 (pt) | 2005-06-22 | 2021-11-23 | Plexxikon, Inc | Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo |
JP2007010876A (ja) | 2005-06-29 | 2007-01-18 | Fujinon Corp | レンズ駆動装置 |
EP2251341A1 (en) | 2005-07-14 | 2010-11-17 | Astellas Pharma Inc. | Heterocyclic Janus kinase 3 inhibitors |
FR2889662B1 (fr) | 2005-08-11 | 2011-01-14 | Galderma Res & Dev | Emulsion de type huile-dans-eau pour application topique en dermatologie |
US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
CA2621261C (en) | 2005-09-22 | 2014-05-20 | Incyte Corporation | Azepine inhibitors of janus kinases |
EP2532667A1 (en) | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
WO2007044894A2 (en) | 2005-10-11 | 2007-04-19 | Chembridge Research Laboratories, Inc. | Cell-free protein expression systems and methods of use thereof |
BRPI0617221B1 (pt) | 2005-10-14 | 2016-07-12 | Sumitomo Chemical Co | composto de hidrazida, seu uso, pesticida e método de controlar uma peste |
EP1945631B8 (en) | 2005-10-28 | 2013-01-02 | AstraZeneca AB | 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer |
PT1951684T (pt) | 2005-11-01 | 2016-10-13 | Targegen Inc | Inibidores de cinases de tipo biaril-meta-pirimidina |
WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
PT3184526T (pt) | 2005-12-13 | 2018-12-19 | Incyte Holdings Corp | Derivados de pirrolo[2,3-d]pirimidina como inibidores da cinase janus |
US20130137681A1 (en) | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
WO2007076423A2 (en) | 2005-12-22 | 2007-07-05 | Smithkline Beecham Corporation | INHIBITORS OF Akt ACTIVITY |
CN101389324A (zh) | 2005-12-23 | 2009-03-18 | 史密丝克莱恩比彻姆公司 | Aurora激酶的氮杂吲哚抑制剂 |
BRPI0722364A2 (pt) | 2006-01-17 | 2011-08-16 | Vertex Pharma | azaindóis, composição farmacêutica e usos dos referidos compostos |
US20070208053A1 (en) * | 2006-01-19 | 2007-09-06 | Arnold Lee D | Fused heterobicyclic kinase inhibitors |
WO2007090141A2 (en) | 2006-02-01 | 2007-08-09 | Smithkline Beecham Corporation | Pyrrolo [2, 3, b] pyridine derivatives useful as raf kinase inhibitors |
US7745477B2 (en) | 2006-02-07 | 2010-06-29 | Hoffman-La Roche Inc. | Heteroaryl and benzyl amide compounds |
AU2007225836A1 (en) | 2006-03-10 | 2007-09-20 | Ono Pharmaceutical Co., Ltd. | Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient |
BRPI0709866B8 (pt) | 2006-04-03 | 2021-05-25 | Astellas Pharma Inc | compostos héteros e composição farmacêutica compreendendo ditos compostos |
AU2007235487A1 (en) * | 2006-04-05 | 2007-10-18 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
WO2007116313A2 (en) | 2006-04-12 | 2007-10-18 | Pfizer Limited | Pyrrolidine derivatives as modulators of chemokine ccr5 receptors |
WO2007129195A2 (en) | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
US7691811B2 (en) | 2006-05-25 | 2010-04-06 | Bodor Nicholas S | Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye |
TWI398252B (zh) | 2006-05-26 | 2013-06-11 | Novartis Ag | 吡咯并嘧啶化合物及其用途 |
JP2009544625A (ja) | 2006-07-20 | 2009-12-17 | メーメット・カーラマン | Rhoキナーゼのベンゾチオフェン阻害剤 |
WO2008013622A2 (en) | 2006-07-27 | 2008-01-31 | E. I. Du Pont De Nemours And Company | Fungicidal azocyclic amides |
WO2008016123A1 (fr) | 2006-08-03 | 2008-02-07 | Takeda Pharmaceutical Company Limited | INHIBITEUR DE LA GSK-3β |
JP5252404B2 (ja) | 2006-08-16 | 2013-07-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ピラジン化合物、その使用及び調製方法 |
KR20090060333A (ko) | 2006-09-08 | 2009-06-11 | 노파르티스 아게 | 림프구 상호작용에 의해 매개되는 질환의 치료에 유용한 n-바이아릴 (헤테로)아릴술폰아미드 유도체 |
WO2008035376A2 (en) | 2006-09-19 | 2008-03-27 | Council Of Scientific & Industrial Research | A novel bio-erodible insert for ophthalmic applications and a process for the preparation thereof |
CL2007002866A1 (es) | 2006-10-04 | 2008-07-04 | Pharmacopeia Inc | Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m |
CL2007002867A1 (es) | 2006-10-04 | 2008-06-27 | Pharmacopeia Inc | Compuestos derivados de 2-(bencimidazolil)purina, inhibidores de janus quinasa 3; composicion farmaceutica que los contiene; y su uso para tratar enfermedades autoinmune, inflamatorias, cardiovasculares, rechazo de implante, entre otras. |
US20120225057A1 (en) | 2006-10-11 | 2012-09-06 | Deciphera Pharmaceuticals, Llc | Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases |
AU2007316417B2 (en) | 2006-11-06 | 2013-08-22 | Tolero Pharmaceuticals, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
US20080119496A1 (en) | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
ME02372B (me) | 2006-11-22 | 2016-06-20 | Incyte Holdings Corp | Imidazotriazini i imidazopiramidini kao inhibitori kinaze |
WO2008067119A2 (en) | 2006-11-27 | 2008-06-05 | Smithkline Beecham Corporation | Novel compounds |
NZ577111A (en) | 2006-12-15 | 2012-05-25 | Abbott Lab | Novel oxadiazole compounds |
AU2007338793B2 (en) | 2006-12-20 | 2012-05-03 | Amgen Inc. | Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer |
WO2008079291A2 (en) | 2006-12-20 | 2008-07-03 | Amgen Inc. | Substituted heterocycles and methods of use |
EP2121692B1 (en) | 2006-12-22 | 2013-04-10 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
WO2008077712A1 (en) | 2006-12-22 | 2008-07-03 | Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. | Gel useful for the delivery of ophthalmic drugs |
KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
WO2008082839A2 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
WO2008082840A1 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
EP2132177B1 (en) | 2007-03-01 | 2013-07-17 | Novartis AG | Pim kinase inhibitors and methods of their use |
WO2008124323A1 (en) | 2007-04-03 | 2008-10-16 | Array Biopharma Inc. | Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors |
GB0709031D0 (en) | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
CA2687931C (en) | 2007-05-31 | 2016-05-24 | Boehringer Ingelheim International Gmbh | Ccr2 receptor antagonists and uses thereof |
GB0710528D0 (en) | 2007-06-01 | 2007-07-11 | Glaxo Group Ltd | Novel compounds |
US20080312259A1 (en) | 2007-06-13 | 2008-12-18 | Incyte Corporation | SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE |
CL2008001709A1 (es) * | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
KR20120115413A (ko) | 2007-07-11 | 2012-10-17 | 화이자 인코포레이티드 | 안구 건조증 치료용 약학 조성물 및 방법 |
BRPI0815042A2 (pt) | 2007-08-01 | 2015-02-10 | Pfizer | Compostos de pirazol |
WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
US20110263664A1 (en) | 2007-11-15 | 2011-10-27 | Musc Foundation For Research Development | Inhibitors of PIM-1 Protein Kinases, Compositions and Methods for Treating Prostate Cancer |
EA020777B1 (ru) | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
GB0723815D0 (en) | 2007-12-05 | 2008-01-16 | Glaxo Group Ltd | Compounds |
DK3133080T3 (en) | 2008-01-18 | 2018-11-26 | Inst Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | PRESENT UNKNOWN CYTOSTATIC 7-DEAZAPURIN NUCLEOSIDES |
US8273744B2 (en) | 2008-02-04 | 2012-09-25 | Mercury Therapeutics, Inc. | AMPK modulators |
PE20091577A1 (es) | 2008-03-03 | 2009-11-05 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
TWI444382B (zh) | 2008-03-11 | 2014-07-11 | Incyte Corp | 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物 |
KR101408517B1 (ko) | 2008-03-21 | 2014-06-17 | 노파르티스 아게 | 신규한 헤테로시클릭 화합물 및 그의 용도 |
US20110212157A1 (en) | 2008-06-26 | 2011-09-01 | Anterios, Inc. | Dermal delivery |
UY31952A (es) | 2008-07-02 | 2010-01-29 | Astrazeneca Ab | 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim |
FR2933409B1 (fr) | 2008-07-03 | 2010-08-27 | Centre Nat Rech Scient | NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM |
WO2010022081A1 (en) | 2008-08-19 | 2010-02-25 | Array Biopharma Inc. | Triazolopyridine compounds as pim kinase inhibitors |
TWI496779B (zh) | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為pim激酶抑制劑之三唑吡啶化合物 |
PT2384326E (pt) | 2008-08-20 | 2014-06-09 | Zoetis Llc | Compostos de pirrolo[2,3-d]pirimidina |
WO2010026124A1 (en) | 2008-09-02 | 2010-03-11 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
JP5584215B2 (ja) | 2008-09-02 | 2014-09-03 | ノバルティス アーゲー | ヘテロ環pimキナーゼ阻害剤 |
EA201100426A1 (ru) | 2008-09-02 | 2011-10-31 | Новартис Аг | Бициклические ингибиторы киназы |
CL2009001884A1 (es) | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
EP2210890A1 (en) | 2009-01-19 | 2010-07-28 | Almirall, S.A. | Oxadiazole derivatives as S1P1 receptor agonists |
US8263601B2 (en) | 2009-02-27 | 2012-09-11 | Concert Pharmaceuticals, Inc. | Deuterium substituted xanthine derivatives |
CN106967070A (zh) | 2009-05-22 | 2017-07-21 | 因塞特控股公司 | 作为jak抑制剂的化合物 |
ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
US20120157500A1 (en) | 2009-08-24 | 2012-06-21 | Weikang Tao | Jak inhibition blocks rna interference associated toxicities |
TW201111385A (en) | 2009-08-27 | 2011-04-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
JP5567136B2 (ja) | 2009-09-08 | 2014-08-06 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 4−置換ピリジン−3−イル−カルボキサミド化合物及び使用方法 |
EP2305660A1 (en) | 2009-09-25 | 2011-04-06 | Almirall, S.A. | New thiadiazole derivatives |
BR112012008267B1 (pt) | 2009-10-09 | 2022-10-04 | Incyte Holdings Corporation | Derivados hidroxila, ceto e glucuronida de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1- il)-3-ciclopentilpropanonitrila |
CN102666545B (zh) | 2009-10-20 | 2016-04-06 | 塞尔卓姆有限公司 | 作为jak抑制剂的杂环吡唑并嘧啶类似物 |
EP2332917B1 (en) | 2009-11-11 | 2012-08-01 | Sygnis Bioscience GmbH & Co. KG | Compounds for PIM kinase inhibition and for treating malignancy |
KR20120118088A (ko) | 2009-11-24 | 2012-10-25 | 앨더바이오 홀딩스 엘엘씨 | Ⅰl-6에 대한 항체 및 이들의 용도 |
US20130129675A1 (en) | 2009-12-04 | 2013-05-23 | Board Of Regents, The University Of Texas System | Interferon therapies in combination with blockade of stat3 activation |
MX2012008049A (es) | 2010-01-12 | 2012-08-01 | Hoffmann La Roche | Compuestos heterociclicos triciclicos, composiciones y metodos de uso de los mismos,. |
SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
CA2790070C (en) | 2010-02-18 | 2018-03-06 | Incyte Corporation | Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors |
TWI766281B (zh) | 2010-03-10 | 2022-06-01 | 美商英塞特控股公司 | 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物 |
WO2011130146A1 (en) | 2010-04-14 | 2011-10-20 | Array Biopharma Inc. | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
EP2390252A1 (en) | 2010-05-19 | 2011-11-30 | Almirall, S.A. | New pyrazole derivatives |
PE20130216A1 (es) | 2010-05-21 | 2013-02-27 | Incyte Corp | Formulacion topica para un inhibidor de jak |
US8637529B2 (en) | 2010-06-11 | 2014-01-28 | AbbYie Inc. | Pyrazolo[3,4-d]pyrimidine compounds |
US9351943B2 (en) | 2010-07-01 | 2016-05-31 | Matthew T. McLeay | Anti-fibroblastic fluorochemical emulsion therapies |
EP2621489A1 (en) | 2010-09-30 | 2013-08-07 | Portola Pharmaceuticals, Inc. | Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine |
CN101974161B (zh) | 2010-09-30 | 2012-10-31 | 中国科学院西双版纳热带植物园 | 一种溶解和快速水解木质纤维素生物质的方法及其设备和应用 |
AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
CN103370068A (zh) | 2010-12-03 | 2013-10-23 | Ym生物科学澳大利亚私人有限公司 | Jak-2 介导的病症的治疗 |
US9993480B2 (en) | 2011-02-18 | 2018-06-12 | Novartis Pharma Ag | mTOR/JAK inhibitor combination therapy |
EA201490042A1 (ru) | 2011-06-20 | 2014-10-30 | Инсайт Корпорейшн | Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak |
WO2013023119A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | JAK P13K/mTOR COMBINATION THERAPY |
TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
AR091079A1 (es) | 2012-05-18 | 2014-12-30 | Incyte Corp | Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak |
US10155987B2 (en) | 2012-06-12 | 2018-12-18 | Dana-Farber Cancer Institute, Inc. | Methods of predicting resistance to JAK inhibitor therapy |
WO2014036016A1 (en) | 2012-08-31 | 2014-03-06 | Principia Biopharma Inc. | Benzimidazole derivatives as itk inhibitors |
US9263059B2 (en) | 2012-09-28 | 2016-02-16 | International Business Machines Corporation | Deep tagging background noises |
US20140095210A1 (en) | 2012-10-02 | 2014-04-03 | CareRev, Inc. | Computer-implemented method and system for facilitating information sharing, communication, and collaboration in a healthcare facility |
CN107936039A (zh) | 2012-11-01 | 2018-04-20 | 因赛特公司 | 作为jak抑制剂的三环稠合噻吩衍生物 |
SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
HUE057262T2 (hu) | 2013-03-06 | 2022-04-28 | Incyte Holdings Corp | Eljárás és köztitermékek JAK inhibitor elõállítására |
PL3786162T3 (pl) | 2013-05-17 | 2024-04-08 | Incyte Holdings Corporation | Pochodne bipirazolu jako inhibitory jak |
TWI503855B (zh) | 2013-07-05 | 2015-10-11 | Timotion Technology Co Ltd | 極限開關及具有該開關之線性致動器 |
US9655854B2 (en) | 2013-08-07 | 2017-05-23 | Incyte Corporation | Sustained release dosage forms for a JAK1 inhibitor |
US20150065447A1 (en) | 2013-08-20 | 2015-03-05 | Incyte Corporation | Survival benefit in patients with solid tumors with elevated c-reactive protein levels |
PE20161388A1 (es) | 2014-02-28 | 2016-12-28 | Incyte Corp | Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos |
CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
MA39987A (fr) | 2014-04-30 | 2017-03-08 | Incyte Corp | Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées |
US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
-
2008
- 2008-06-12 US US12/137,892 patent/US20080312259A1/en not_active Abandoned
- 2008-06-12 DK DK13198120.1T patent/DK2740731T3/en active
- 2008-06-12 KR KR1020157002074A patent/KR20150036210A/ko active Search and Examination
- 2008-06-12 CU CU20120155A patent/CU24179B1/es active IP Right Grant
- 2008-06-12 CN CN201310367212.9A patent/CN103524509B/zh active Active
- 2008-06-12 PL PL13198120.1T patent/PL2740731T3/pl unknown
- 2008-06-12 RS RS20160375A patent/RS54878B1/sr unknown
- 2008-06-12 PL PL16152794T patent/PL3070090T3/pl unknown
- 2008-06-12 CA CA2689663A patent/CA2689663C/en active Active
- 2008-06-12 PL PL08770794.9T patent/PL2173752T5/pl unknown
- 2008-06-12 SI SI200832042T patent/SI3070090T1/sl unknown
- 2008-06-12 SG SG2012043428A patent/SG182198A1/en unknown
- 2008-06-12 PT PT16152794T patent/PT3070090T/pt unknown
- 2008-06-12 EA EA201070013A patent/EA019784B1/ru unknown
- 2008-06-12 SI SI200831621A patent/SI2740731T1/sl unknown
- 2008-06-12 EP EP08770794.9A patent/EP2173752B2/en active Active
- 2008-06-12 TR TR2019/03488T patent/TR201903488T4/tr unknown
- 2008-06-12 CN CN2008801029033A patent/CN101932582B/zh active Active
- 2008-06-12 DK DK16152794.0T patent/DK3070090T3/en active
- 2008-06-12 MX MX2013005828A patent/MX342814B/es unknown
- 2008-06-12 HU HUE16152794A patent/HUE043732T2/hu unknown
- 2008-06-12 UA UAA201000232A patent/UA99467C2/ru unknown
- 2008-06-12 EP EP21200662.1A patent/EP4011883A1/en active Pending
- 2008-06-12 MY MYPI20095311A patent/MY154969A/en unknown
- 2008-06-12 PT PT87707949T patent/PT2173752E/pt unknown
- 2008-06-12 JP JP2010512343A patent/JP5475653B2/ja active Active
- 2008-06-12 SI SI200831217T patent/SI2173752T2/sl unknown
- 2008-06-12 EP EP13198120.1A patent/EP2740731B1/en active Active
- 2008-06-12 ME MEP-2009-345A patent/ME00960B/me unknown
- 2008-06-12 HU HUE13198120A patent/HUE029236T2/en unknown
- 2008-06-12 GE GEAP200811637A patent/GEP20125533B/en unknown
- 2008-06-12 BR BRPI0814254A patent/BRPI0814254B8/pt active IP Right Grant
- 2008-06-12 LT LTEP16152794.0T patent/LT3070090T/lt unknown
- 2008-06-12 RS RS20190251A patent/RS58449B1/sr unknown
- 2008-06-12 KR KR1020107000805A patent/KR101549876B1/ko active IP Right Grant
- 2008-06-12 RS RS20140152A patent/RS53245B2/sr unknown
- 2008-06-12 ES ES16152794T patent/ES2714092T3/es active Active
- 2008-06-12 EP EP18203965.1A patent/EP3495369B1/en active Active
- 2008-06-12 SG SG10201912675VA patent/SG10201912675VA/en unknown
- 2008-06-12 SG SG10201509887UA patent/SG10201509887UA/en unknown
- 2008-06-12 DK DK08770794.9T patent/DK2173752T4/da active
- 2008-06-12 MX MX2009013402A patent/MX2009013402A/es active IP Right Grant
- 2008-06-12 AU AU2008266183A patent/AU2008266183B2/en active Active
- 2008-06-12 ES ES18203965T patent/ES2903444T3/es active Active
- 2008-06-12 WO PCT/US2008/066662 patent/WO2008157208A2/en active Application Filing
- 2008-06-12 EP EP16152794.0A patent/EP3070090B1/en not_active Revoked
- 2008-06-12 ES ES08770794T patent/ES2467665T5/es active Active
- 2008-06-12 ES ES13198120.1T patent/ES2575797T3/es active Active
- 2008-06-12 NZ NZ581803A patent/NZ581803A/en unknown
-
2009
- 2009-12-06 IL IL202524A patent/IL202524A/en active IP Right Grant
- 2009-12-09 CR CR11151A patent/CR11151A/es unknown
- 2009-12-10 TN TNP2009000514A patent/TN2009000514A1/fr unknown
- 2009-12-10 ZA ZA2009/08826A patent/ZA200908826B/en unknown
- 2009-12-10 DO DO2009000280A patent/DOP2009000280A/es unknown
- 2009-12-10 GT GT200900314A patent/GT200900314A/es unknown
- 2009-12-11 NI NI200900216A patent/NI200900216A/es unknown
- 2009-12-11 CU CU2009000213A patent/CU23933B1/es active IP Right Grant
- 2009-12-14 EC EC2009009802A patent/ECSP099802A/es unknown
- 2009-12-16 CO CO09144142A patent/CO6251256A2/es active IP Right Grant
-
2010
- 2010-01-08 SM SM201000002T patent/SMP201000002B/it unknown
- 2010-01-12 MA MA32505A patent/MA31517B1/fr unknown
- 2010-10-14 HK HK10109728.8A patent/HK1143161A1/xx unknown
-
2013
- 2013-12-05 US US14/097,588 patent/US8722693B2/en active Active
- 2013-12-05 US US14/097,598 patent/US20140094477A1/en not_active Abandoned
-
2014
- 2014-04-18 US US14/256,311 patent/US8829013B1/en active Active
- 2014-04-18 US US14/256,383 patent/US8822481B1/en active Active
- 2014-05-01 IL IL232410A patent/IL232410A0/en active IP Right Grant
- 2014-05-06 US US14/270,915 patent/US9376439B2/en active Active
- 2014-05-07 CY CY20141100323T patent/CY1115145T1/el unknown
- 2014-06-09 HR HRP20140541TT patent/HRP20140541T4/hr unknown
- 2014-12-03 HK HK14112206.9A patent/HK1198652A1/zh unknown
-
2016
- 2016-05-25 US US15/164,518 patent/US10016429B2/en active Active
- 2016-06-13 CY CY20161100513T patent/CY1117693T1/el unknown
- 2016-06-21 HR HRP20160717TT patent/HRP20160717T1/hr unknown
-
2018
- 2018-06-08 US US16/003,210 patent/US10610530B2/en active Active
-
2019
- 2019-01-16 IL IL264276A patent/IL264276B/en active IP Right Grant
- 2019-02-28 HR HRP20190385TT patent/HRP20190385T1/hr unknown
- 2019-03-07 CY CY20191100273T patent/CY1121338T1/el unknown
- 2019-06-11 NO NO2019025C patent/NO2019025I1/no unknown
-
2020
- 2020-03-02 US US16/806,244 patent/US11213528B2/en active Active
-
2021
- 2021-01-26 IL IL280401A patent/IL280401B/en unknown
- 2021-10-31 IL IL287708A patent/IL287708B1/en unknown
- 2021-11-29 US US17/536,925 patent/US20220288078A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20140541T4 (hr) | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila | |
HRP20192203T1 (hr) | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori | |
JP2010529209A5 (hr) | ||
JP2010529208A5 (hr) | ||
JP2014520146A5 (hr) | ||
JP2016040271A5 (hr) | ||
US10463667B2 (en) | Metabolites of the janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile | |
JP2015537030A5 (hr) | ||
EP3183247B9 (en) | Aminopyrimidinyl compounds as jak inhibitors | |
TWI354554B (en) | Substituted pyrimidines | |
HRP20210036T1 (hr) | Soli inhibitora pi3k i postupci za njihovo dobivanje | |
RU2015101647A (ru) | Кристаллы соли | |
HRP20221221T1 (hr) | Pirimidinski spoj kao inhibitor jak kinaze | |
HRP20161390T1 (hr) | Derivati azetidina i ciklobutana kao inhibitori jak | |
HRP20171610T1 (hr) | Selektivni inhibitori pi3k delta | |
HRP20151250T1 (hr) | Derivati izoksazolo-piridina | |
SI2892900T1 (en) | Compounds of pyrazolopyrimidine, as kinase inhibitors | |
JP2011252024A5 (hr) | ||
JP2013515729A5 (hr) | ||
JP2015527401A5 (hr) | ||
MX2015001715A (es) | Compuestos de pirrolopirimidina novedosos como inhibidores de proteinas quinasas. | |
RU2015156142A (ru) | Бисульфат ингибитора янус-киназы (jak) и способ его получения | |
CA2656507A1 (en) | Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors | |
JP2017520538A5 (hr) | ||
TW201040148A (en) | Quinazolinedione derivatives, preparation thereof and various therapeutic uses thereof |