ME02801B - Kristalni inhibitori bromodomena - Google Patents
Kristalni inhibitori bromodomenaInfo
- Publication number
- ME02801B ME02801B MEP-2017-170A MEP2017170A ME02801B ME 02801 B ME02801 B ME 02801B ME P2017170 A MEP2017170 A ME P2017170A ME 02801 B ME02801 B ME 02801B
- Authority
- ME
- Montenegro
- Prior art keywords
- crystalline form
- cancer
- difluorophenoxy
- pyrrolo
- dihydro
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title 1
- RDONXGFGWSSFMY-UHFFFAOYSA-N n-[4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-1h-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide Chemical compound C=1N(C)C(=O)C=2NC=CC=2C=1C1=CC(NS(=O)(=O)CC)=CC=C1OC1=CC=C(F)C=C1F RDONXGFGWSSFMY-UHFFFAOYSA-N 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 239000003937 drug carrier Substances 0.000 claims 15
- 238000000634 powder X-ray diffraction Methods 0.000 claims 15
- 208000017169 kidney disease Diseases 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000020832 chronic kidney disease Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 201000009030 Carcinoma Diseases 0.000 claims 3
- 208000017667 Chronic Disease Diseases 0.000 claims 3
- 230000001154 acute effect Effects 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 206010000830 Acute leukaemia Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 201000004253 NUT midline carcinoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims 2
- 208000009956 adenocarcinoma Diseases 0.000 claims 2
- 230000000747 cardiac effect Effects 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 238000001757 thermogravimetry curve Methods 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000007122 AIDS-Associated Nephropathy Diseases 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 201000009047 Chordoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000009798 Craniopharyngioma Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 206010058314 Dysplasia Diseases 0.000 claims 1
- 201000009051 Embryonal Carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims 1
- 208000036566 Erythroleukaemia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 206010018374 Glomerulonephritis minimal lesion Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims 1
- 206010062767 Hypophysitis Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000004883 Lipoid Nephrosis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000007054 Medullary Carcinoma Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010054949 Metaplasia Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000007641 Pinealoma Diseases 0.000 claims 1
- 206010035742 Pneumonitis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 201000000331 Testicular germ cell cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010044248 Toxic shock syndrome Diseases 0.000 claims 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000014070 Vestibular schwannoma Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 208000004064 acoustic neuroma Diseases 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 208000021841 acute erythroid leukemia Diseases 0.000 claims 1
- 206010003230 arteritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 201000007180 bile duct carcinoma Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 208000019748 bullous skin disease Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000024207 chronic leukemia Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000002445 cystadenocarcinoma Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 208000037828 epithelial carcinoma Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- RSOJSFYJLQADDM-UHFFFAOYSA-N ethanesulfonamide Chemical compound [CH2]CS(N)(=O)=O RSOJSFYJLQADDM-UHFFFAOYSA-N 0.000 claims 1
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims 1
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000002409 gliosarcoma Diseases 0.000 claims 1
- 208000025750 heavy chain disease Diseases 0.000 claims 1
- 201000002222 hemangioblastoma Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000003463 hyperproliferative effect Effects 0.000 claims 1
- 201000006334 interstitial nephritis Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000012804 lymphangiosarcoma Diseases 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 206010027191 meningioma Diseases 0.000 claims 1
- 230000015689 metaplastic ossification Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 208000004019 papillary adenocarcinoma Diseases 0.000 claims 1
- 201000010198 papillary carcinoma Diseases 0.000 claims 1
- 238000013146 percutaneous coronary intervention Methods 0.000 claims 1
- 208000008494 pericarditis Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000024724 pineal body neoplasm Diseases 0.000 claims 1
- 201000004123 pineal gland cancer Diseases 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 230000010410 reperfusion Effects 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 201000008407 sebaceous adenocarcinoma Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000010965 sweat gland carcinoma Diseases 0.000 claims 1
- 210000001258 synovial membrane Anatomy 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 208000012991 uterine carcinoma Diseases 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- AIDS & HIV (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
Claims (26)
1. Izolovana kristalna forma N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida gde kristalna forma ima šablon rendgenske praškaste difrakcije koji se sastoje od tri ili više 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine: 6.2°, 9.0°, 12.3°, 12.6°, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
2. Izolovana kristalna forma N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1, gde kristalna forma ima šablon rendgenske praškaste difrakcije koji se sastoje od sledećih 2θ vrednosti maksimuma ± 0.2: 6.2°, 9.0°, 11.0°, 12.3°, 12.6°, 13.1°, 14.1°, 15.6°, 16.4°, 16.5°, 16.9°, 17.8°, 18.1°, 18.3°, 18.9°, 20.4°, 21.1°, 21.6°, 21.8°, 22.1°, 22.9°, 23.2°, 24.4°, 24.7°, 25.6°, 26.3°, 27.0°, i 27.3°.
3. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji od tri, četiri, pet ili šest 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine 6.2°, 9.0°, 12.3°, 12.6, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
4. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji od šest 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine 6.2°, 9.0°, 12.3°, 12.6, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
5. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji od pet 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine 6.2°, 9.0°, 12.3°, 12.6, 15.6°, 22.1 °, 25.6°, 26.3°, 27.0°, i 27.3°.
6. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji od četiri 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine 6.2°, 9.0°, 12.3°, 12.6, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
7. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji od tri 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine 6.2°, 9.0°, 12.3°, 12.6, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
8. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz sledećih 2θ vrednosti maksimuma ± 0.2: 6.2°, 9.0°, 12.3°, 12.6°, i 15.6°.
9. Kristalna forma prema patentnom zahtevu 1 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz sledećih 2θ vrednosti maksimuma ± 0.2: 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
10. Kristalna forma prema patentnom zahtevu 2 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz vrednosti maksimuma ± 0.2 pri 2θ pozicijama 6.2°, 9.0°, 12.3°, 12.6°, 13.1°, 14.1°, 16.4°, 16.5°, 16.9°, 17.8°, 18.1°, 18.3°, i 18.9°.
11. Kristalna forma prema patentnom zahtevu 2 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz vrednosti maksimuma ± 0.2 pri 2θ pozicijama 6.2°, 9.0°, 12.3°, 12.6°, 13.1°, 14.1°, 18.1°, i 18.9°.
12. Kristalna forma prema patentnom zahtevu 2 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz vrednosti maksimuma ± 0.2 pri 2θ pozicijama 6.2°, 9.0°, 12.3°, 12.6°, 13.1 °, i 18.1°.
13. Kristalna forma prema patentnom zahtevu 2 koja ima šablon rendgenske praškaste difrakcije koji se sastoji iz vrednosti maksimuma ± 0.2 pri 2θ pozicijama 9.0°, 12.3°, 12.6°, 13.1°, i 18.1°.
14. Kristalna forma prema patentnom zahtevu 1 koja ima endotermu termograma diferencijalne skenirajuće kalorimetrije između 240 i 242 °C.
15. Kristalna forma prema patentnom zahtevu 1 koja ima endotermu termograma diferencijalne skenirajuće kalorimetrije približno 241 °C.
16. Farmaceutski sastav koji se sastoji od izolovane kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1, i bar jednog farmaceutski prihvatljivog nosača.
17. Farmaceutski sastav koji se sastoji od izolovane kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje kancera kod subjekta koja obuhvata davanje terapeutski efektivne količine farmaceutskog sastava koji se sastoji od kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu za njim.
18. Farmaceutski sastav za upotrebu prema patentnom zahtevu 17 gde je kancer izabran iz grupe koju čine: akustična neuroma, akutna leukemija, akutna limfocitna leukemija, akutna mijelocitna leukemija (monocitna, mijeloblastična, adenokarcinom, angiosarkom, astrocitom, mijelomonocitna i promijelocitna), akutna leukemija T-ćelija, karcinom bazalnih ćelija, karcinom žučnog kanala, kancer bubrega, kancer mozga, kancer dojke, bronhogeni karcinom, kancer grlića materice, hondrosarkom, hordom, horiokarcinom, hronična leukemija, hronična limfocitna leukemija, hronična mijelocitna (granulocitna) leukemija, hronična mijelogena leukemija, kancer debelog creva, kolorektalni kancer, kraniofaringiom, cistadenokarcinom, difuzni limfom velikih B-ćelija, disproliferativne promene (displazija i metaplazije), embrionalni karcinom, kancer endometrijuma, endoteliosarkom, ependimom, epitelni karcinom, eritroleukemija, kancer ezofagea, karcinom ezofagealnog receptora, esencijalna trombocitemija, Evingov tumor, fibrosarkom, folikularni limfom, kancer germinativnih ćelija testisa, glioblastom, gliosarkom, bolest teškog lanca, hemangioblastom, hepatom, hepatocelularni kancer, hormonski neosetljivi kancer prostate, leiomiosarkom, leukemija, liposarkom, kancer pluća, limfagioendoteliosarkom, limfangiosarkom, limfoblastna leukemija, limfom (Hodgkinov i ne-Hodgkinov), malignosti i hiperproliferativni poremećaji bešike, dojke, debelog creva, pluća, jajnika, pankreasa, prostata, kože i materice, limfoidne malignosti T-ćelijskog ili B-ćelijskog porekla, leukemija, limfom, medularni karcinom, meduloblastom, melanom, meningiom, mezoteliom, višestruki mijelom, mijelogenomna leukemija, mijelom, mikosarkom, neuroblastom, središnji karcinom NUT-a (NMC), kancer ne-malih ćelija pluća, oligodendrogliom, oralni kancer, osteogeni sarkom, kancer jajnika, kancer pankreasa, papilarni adenokarcinomi, papilarni karcinom, pinealom, policitemija vera, karcinom prostate, karcinom rektuma, karcinom bubrežnih ćelija, retinoblastom, rabdomiosarkom, sarkom, karcinomom lojne žlezde, karcinomom malih ćelija, karcinom malih ćelija pluća, čvrsti tumori (karcinomi i sarkomi), kancer malih ćelija pluća, kancer želuca, karcinom skvamoznih ćelija, sinoviom, karcinom znojne žlezde, tiroidni kancer, Valdenstromova makroglobulinemija, tumori testisa, karcinom materice i Vilmsov tumor.
19. Metoda za pravljenje farmaceutskog sastava koji se sastoji iz N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida i farmaceutski prihvatljivog nosača, koja se sastoji iz: mešanja izolovane kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida gde kristalna forma ima šablon rendgenske praškaste difrakcije koji se sastoji iz tri ili više 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine: 6.2°, 9.0°, 12.3°, 12.6°, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°, sa farmaceutski prihvatljivim nosačem.
20. Sastav koji se sastoji više od 90% (w/w) od kristalne forme II N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida gde kristalna forma ima šablon rendgenske praškaste difrakcije koji se sastoji iz tri ili više 2θ vrednosti maksimuma ± 0.2 izabranih iz grupe koju čine: 6.2°, 9.0°, 12.3°, 12.6°, 15.6°, 22.1°, 25.6°, 26.3°, 27.0°, i 27.3°.
21. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2.4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje akutne bolesti bubrega ili stanja kod subjekta koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu za njim, gde navedene akutna bolesti bubrega ili stanje je izabrano iz grupe koju čine: bolest bubrega izazvana ishemijom i reperfuzijom, bolesti bubrega izazvane srčanim i glavnim zahvatima, bolesti bubrega izazvane perkutanom koronarnom intervencijom, bolesti bubrega izazvane radioaktivnim kontrastom, bolesti bubrega izazvane sepsom, bolesti izazvane pneumonijom i bolesti bubrega izazvane lekovima.
22. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje hronične bolesti bubrega ili stanja kod subjekta koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu uza njim, gde navedena hronična bolest bubrega ili stanje je izabrana iz grupe koju čine: Dijabetična nefropatija, hipertenzivna nefropatija, nefropatija povezana sa HIV-om, glomerulonefritis, lupusni nefritis, IgA nefropatija, fokalna segmentarna glomeruloskleroza, membranski glomerulonefritis, bolest minimalnih promena, bolest policističkih bubrega i tubularni intersticijski nefritis.
23. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-r6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje bolesti ili stanja kod subjekta koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu uza njim, gde navedena hronična bolest bubrega ili stanje je izabrana iz grupe koju čine Adisonova bolest, akutni giht, ankilozni spondilitis, astma, ateroskleroza, Behcetova bolest, bulozne kožne bolesti, srčana miopatija, srčana hipertrofija, hronična opstruktivna plućna bolest (KOPB), Kronova bolest, dermatitis, ekcem, arteritis gigantnih ćelija, glomerulonefritis, hepatitis, hipofizitis, inflamatorna bolest creva, Kavasaki bolest, lupus nefritis, multipla skleroza, miokarditis, miozitis, nefritis, odbacivanje transplantata organa, osteoartritis, pankreatitis, perikarditis, nodoza poliarteritisa, pneumonitis, primarna bilijarna ciroza, psorijaza, psoriatični artritis, reumatoidni artritis, skleritis, sklerozni holangitis, sepsa, sistemski lupus eritematozus, Takaiasuov arteritis, toksični šok, tiroiditis, dijabetes tipa I, ulcerativni kolitis, uveitis, vitiligo, vaskulitis i Vegenerova granulomatoza.
24. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje stečenog sindroma imunodeficijencije (AIDS) kod subjekta koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koju ima potrebu za njim.
25. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i bar jednog farmaceutski prihvatljivog nosača za upotrebu u metodi za tretiranje bolesti ili stanja kod subjekta koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu uza njim, gde navedena hronična bolest bubrega ili stanje je izabrana iz grupe koju čine: gojaznost, dislipidemija, hiperholesterolemija, Alchajmerova bolest, metabolički sindrom, hepatična steatoza, dijabetes tipa II, otpornost na inzulin, dijabetska retinopatija i dijabetska neuropatija.
26. Farmaceutski sastav koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača za upotrebu u metodi kontracepcije kod muških subjekata koja se sastoji iz davanja terapeutski efektivne količine farmaceutskog sastava koji se sastoji iz kristalne forme N-[4-(2,4-difluorofenoksi)-3-(6-metil-7-okso-6,7-dihidro-1H-pirolo[2,3-c]piridin-4-il)fenil]etanesulfonamida prema patentnom zahtevu 1 i barem jednog farmaceutski prihvatljivog nosača, subjektu koji ima potrebu uza njim.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361840777P | 2013-06-28 | 2013-06-28 | |
| EP14745267.6A EP3013826B1 (en) | 2013-06-28 | 2014-06-27 | Crystalline bromodomain inhibitors |
| PCT/US2014/044513 WO2014210425A1 (en) | 2013-06-28 | 2014-06-27 | Crystalline bromodomain inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02801B true ME02801B (me) | 2018-01-20 |
Family
ID=51261220
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2017-170A ME02801B (me) | 2013-06-28 | 2014-06-27 | Kristalni inhibitori bromodomena |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US9321765B2 (me) |
| EP (1) | EP3013826B1 (me) |
| JP (1) | JP6423425B2 (me) |
| KR (1) | KR102323829B1 (me) |
| CN (1) | CN105473586B (me) |
| AR (1) | AR096758A1 (me) |
| AU (2) | AU2014302252B2 (me) |
| BR (1) | BR112015032736A2 (me) |
| CA (1) | CA2916221C (me) |
| CL (1) | CL2015003722A1 (me) |
| CR (1) | CR20160036A (me) |
| CY (1) | CY1119066T1 (me) |
| DK (1) | DK3013826T3 (me) |
| DO (1) | DOP2015000304A (me) |
| ES (1) | ES2636939T3 (me) |
| HR (1) | HRP20171154T1 (me) |
| IL (1) | IL243202B (me) |
| LT (1) | LT3013826T (me) |
| ME (1) | ME02801B (me) |
| MX (1) | MX360065B (me) |
| NZ (1) | NZ631112A (me) |
| PE (1) | PE20160287A1 (me) |
| PH (1) | PH12015502792A1 (me) |
| PL (1) | PL3013826T3 (me) |
| PT (1) | PT3013826T (me) |
| RS (1) | RS56318B1 (me) |
| RU (1) | RU2675268C2 (me) |
| SG (1) | SG11201510692TA (me) |
| SI (1) | SI3013826T1 (me) |
| SM (1) | SMT201700363T1 (me) |
| TW (1) | TWI639594B (me) |
| UY (1) | UY35632A (me) |
| WO (1) | WO2014210425A1 (me) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| SG11201506924YA (en) | 2013-03-15 | 2015-09-29 | Incyte Corp | Tricyclic heterocycles as bet protein inhibitors |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| JP6461118B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| SG10201804471PA (en) | 2013-10-18 | 2018-07-30 | Celgene Quanticel Research Inc | Bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| WO2016092375A1 (en) | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| US20180200261A1 (en) * | 2015-07-20 | 2018-07-19 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| PT3442972T (pt) | 2016-04-15 | 2020-05-29 | Abbvie Inc | Inibidores de bromodomínio |
| CA3028689A1 (en) * | 2016-06-20 | 2017-12-28 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| WO2018106988A1 (en) * | 2016-12-09 | 2018-06-14 | Smet Pharmaceutical Inc. | Biologically active compositions containing two different classes of chemical compounds for treating solid tumors |
| CN109384784B (zh) * | 2017-08-10 | 2021-01-12 | 浙江海正药业股份有限公司 | 磺酰胺类衍生物、其制备方法及其在医药上的用途 |
| CA3097750A1 (en) | 2018-05-15 | 2019-11-21 | Abbvie Inc. | Treating solid tumors with bromodomain inhibitors |
| WO2020136650A1 (en) | 2018-12-25 | 2020-07-02 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an egfr inhibitor |
| WO2020232214A1 (en) | 2019-05-14 | 2020-11-19 | Abbvie Inc. | Treating acute myeloid leukemia (aml) with mivebresib, a bromodomain inhibitor |
| EP4058456A1 (en) * | 2019-11-13 | 2022-09-21 | RAPT Therapeutics, Inc. | Crystalline forms of c-c chemokine receptor type 4 antagonist and uses thereof |
| CN110964691B (zh) * | 2019-12-31 | 2020-10-30 | 深圳新赛尔生物科技有限公司 | 子宫内膜干细胞的定向成脂分化培养 |
| JP7840853B2 (ja) | 2020-01-19 | 2026-04-06 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | ブロモドメインタンパク質阻害剤の結晶形、塩形態及びその製造方法 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US11746932B2 (en) | 2020-07-02 | 2023-09-05 | Hempvana, Llc | Expandable and retractable hose reinforced with hemp |
| JP2023554521A (ja) * | 2020-12-22 | 2023-12-27 | ファイザー・インク | Ｅｉｆ４ｅ阻害剤の固体形態 |
| EP4358847A4 (en) | 2021-06-23 | 2025-05-21 | Kimtron, Inc. | System and method for ultra-close irradiation of rotating biomass |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6271380B1 (en) * | 1998-12-30 | 2001-08-07 | Dupont Pharmaceuticals Company | 1H-imidazo[4,5-d]pyridazin-7-ones, 3H-imidazo-[4,5-c]pyridin-4-ones and corresponding thiones as corticotropin releasing factor (CRF) receptor ligands |
| AU2003241960B2 (en) * | 2002-06-06 | 2009-07-30 | Eisai R&D Management Co., Ltd. | Novel fused imidazole derivative |
| TWI339206B (en) * | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| AU2010314395B2 (en) * | 2009-11-05 | 2015-04-09 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| PL2902030T3 (pl) | 2010-05-14 | 2017-07-31 | Dana-Farber Cancer Institute, Inc. | Związki tienotriazolodiazepinowe do leczenia nowotworu |
| CN103119160B (zh) * | 2010-05-14 | 2016-06-01 | 达那-法伯癌症研究所 | 用于调节代谢的组合物和方法 |
| AT510136B1 (de) * | 2010-07-12 | 2016-11-15 | Primetals Technologies Austria GmbH | Verfahren zur herstellung von kohlepartikeln enthaltenden presslingen |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
-
2014
- 2014-06-26 AR ARP140102431A patent/AR096758A1/es unknown
- 2014-06-27 NZ NZ631112A patent/NZ631112A/en unknown
- 2014-06-27 BR BR112015032736A patent/BR112015032736A2/pt not_active Application Discontinuation
- 2014-06-27 CN CN201480042976.3A patent/CN105473586B/zh active Active
- 2014-06-27 WO PCT/US2014/044513 patent/WO2014210425A1/en not_active Ceased
- 2014-06-27 CA CA2916221A patent/CA2916221C/en active Active
- 2014-06-27 SG SG11201510692TA patent/SG11201510692TA/en unknown
- 2014-06-27 DK DK14745267.6T patent/DK3013826T3/en active
- 2014-06-27 PL PL14745267T patent/PL3013826T3/pl unknown
- 2014-06-27 RS RS20170763A patent/RS56318B1/sr unknown
- 2014-06-27 RU RU2016102591A patent/RU2675268C2/ru active
- 2014-06-27 AU AU2014302252A patent/AU2014302252B2/en not_active Ceased
- 2014-06-27 TW TW103122417A patent/TWI639594B/zh not_active IP Right Cessation
- 2014-06-27 PT PT147452676T patent/PT3013826T/pt unknown
- 2014-06-27 SM SM20170363T patent/SMT201700363T1/it unknown
- 2014-06-27 HR HRP20171154TT patent/HRP20171154T1/hr unknown
- 2014-06-27 US US14/317,029 patent/US9321765B2/en active Active
- 2014-06-27 SI SI201430310T patent/SI3013826T1/sl unknown
- 2014-06-27 KR KR1020167002396A patent/KR102323829B1/ko not_active Expired - Fee Related
- 2014-06-27 ME MEP-2017-170A patent/ME02801B/me unknown
- 2014-06-27 PE PE2015002664A patent/PE20160287A1/es not_active Application Discontinuation
- 2014-06-27 MX MX2015017435A patent/MX360065B/es active IP Right Grant
- 2014-06-27 JP JP2016524230A patent/JP6423425B2/ja not_active Expired - Fee Related
- 2014-06-27 EP EP14745267.6A patent/EP3013826B1/en active Active
- 2014-06-27 LT LTEP14745267.6T patent/LT3013826T/lt unknown
- 2014-06-27 UY UY0001035632A patent/UY35632A/es not_active Application Discontinuation
- 2014-06-27 ES ES14745267.6T patent/ES2636939T3/es active Active
-
2015
- 2015-12-16 PH PH12015502792A patent/PH12015502792A1/en unknown
- 2015-12-17 IL IL243202A patent/IL243202B/en active IP Right Grant
- 2015-12-22 DO DO2015000304A patent/DOP2015000304A/es unknown
- 2015-12-23 CL CL2015003722A patent/CL2015003722A1/es unknown
-
2016
- 2016-01-19 CR CR20160036A patent/CR20160036A/es unknown
- 2016-04-25 US US15/137,816 patent/US20160237085A1/en not_active Abandoned
- 2016-11-18 US US15/355,876 patent/US20170066765A1/en not_active Abandoned
-
2017
- 2017-07-03 CY CY20171100702T patent/CY1119066T1/el unknown
-
2018
- 2018-03-20 AU AU2018201986A patent/AU2018201986A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME02801B (me) | Kristalni inhibitori bromodomena | |
| RU2018140061A (ru) | Ингибиторы бромодомена | |
| JP2019511482A5 (me) | ||
| SI2956452T1 (en) | Heterocyclic amides as kinase inhibitors | |
| HRP20250864T1 (hr) | Kristalni oblici p2x3 modulatora metil (s)‑2‑((2‑(2,6‑difluoro‑4‑(metilkarbamoil)fenil)‑7‑metilimidazo[1,2‑a] piridin‑3‑il)metil)morfolin‑4‑karboksilata | |
| Yang et al. | Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility | |
| JP2009530283A5 (me) | ||
| JP2023539931A5 (me) | ||
| JP2016513704A5 (me) | ||
| JP2011513485A5 (me) | ||
| JP2017510641A5 (me) | ||
| CN116113633A (zh) | 一种作为可透脑的btk或her2抑制剂的化合物及其制备方法与用途 | |
| HRP20240695T1 (hr) | Novi polimorfi kalcijeve soli kao protuupalna, imunomodulatorna i anti-proliferacijska sredstva | |
| JP2017516785A5 (me) | ||
| JP2017526696A5 (me) | ||
| JP2016540749A5 (me) | ||
| Richter et al. | Selective addition of amines to 5-trifluoromethyl-2, 4-dichloropyrimidine induced by Lewis acids | |
| CA2987563C (en) | Production method of enzalutamide crystal form | |
| HRP20210667T1 (hr) | Kristalni oblici antagonista androgenog receptora, postupak pripreme i njihova upotreba | |
| HRP20211151T1 (hr) | Kristalinska tosilatna sol pi3k delta selektivnog inhibitora za uporabu u farmaceutskim formulacijama | |
| HRP20192286T1 (hr) | Hidroksieitil sulfonat od ciklina ovisnog inhibitora kinaze proteina, njegov kristalni oblik, i postupak njegovog dobivanja | |
| JP2018510131A5 (me) | ||
| CN111278820A (zh) | 一种吡啶酮化合物的晶型、盐型及其制备方法 | |
| PE20210157A1 (es) | Polimorfos y formas solidas de un compuesto de pirimidinilamino-pirazol y metodos de produccion | |
| KR102588109B1 (ko) | 암 치료에 유용한 1-(사이클로) 알킬 피리딘-2-온의 트리사이클릭 융합 유도체 |