JP2019505597A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019505597A5 JP2019505597A5 JP2018563393A JP2018563393A JP2019505597A5 JP 2019505597 A5 JP2019505597 A5 JP 2019505597A5 JP 2018563393 A JP2018563393 A JP 2018563393A JP 2018563393 A JP2018563393 A JP 2018563393A JP 2019505597 A5 JP2019505597 A5 JP 2019505597A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- syndrome
- ring
- pharmaceutically acceptable
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 206010061218 Inflammation Diseases 0.000 claims 7
- 230000004054 inflammatory process Effects 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 101100406797 Arabidopsis thaliana PAD4 gene Proteins 0.000 claims 5
- 101150094373 Padi4 gene Proteins 0.000 claims 5
- 102100035731 Protein-arginine deiminase type-4 Human genes 0.000 claims 5
- 201000004681 Psoriasis Diseases 0.000 claims 5
- 125000001931 aliphatic group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 206010035664 Pneumonia Diseases 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 208000006673 asthma Diseases 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 208000017169 kidney disease Diseases 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 239000001301 oxygen Chemical group 0.000 claims 4
- 229910052717 sulfur Chemical group 0.000 claims 4
- 239000011593 sulfur Chemical group 0.000 claims 4
- 208000004852 Lung Injury Diseases 0.000 claims 3
- 208000019693 Lung disease Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 206010069363 Traumatic lung injury Diseases 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 231100000515 lung injury Toxicity 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 238000002054 transplantation Methods 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 208000032467 Aplastic anaemia Diseases 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000027932 Collagen disease Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010011878 Deafness Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- 208000037487 Endotoxemia Diseases 0.000 claims 2
- 201000005569 Gout Diseases 0.000 claims 2
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 2
- 208000007514 Herpes zoster Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000018208 Hyperimmunoglobulinemia D with periodic fever Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 208000030852 Parasitic disease Diseases 0.000 claims 2
- 206010035742 Pneumonitis Diseases 0.000 claims 2
- 206010037660 Pyrexia Diseases 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 208000002353 alcoholic hepatitis Diseases 0.000 claims 2
- 206010002022 amyloidosis Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 239000003814 drug Chemical group 0.000 claims 2
- 208000016354 hearing loss disease Diseases 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000007794 irritation Effects 0.000 claims 2
- 201000005962 mycosis fungoides Diseases 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000007056 sickle cell anemia Diseases 0.000 claims 2
- RMTXUPIIESNLPW-UHFFFAOYSA-N 1,2-dihydroxy-3-(pentadeca-8,11-dienyl)benzene Natural products CCCC=CCC=CCCCCCCCC1=CC=CC(O)=C1O RMTXUPIIESNLPW-UHFFFAOYSA-N 0.000 claims 1
- QARRXYBJLBIVAK-UEMSJJPVSA-N 3-[(8e,11e)-pentadeca-8,11-dienyl]benzene-1,2-diol;3-[(8e,11e)-pentadeca-8,11,14-trienyl]benzene-1,2-diol;3-[(8e,11e,13e)-pentadeca-8,11,13-trienyl]benzene-1,2-diol;3-[(e)-pentadec-8-enyl]benzene-1,2-diol;3-pentadecylbenzene-1,2-diol Chemical compound CCCCCCCCCCCCCCCC1=CC=CC(O)=C1O.CCCCCC\C=C\CCCCCCCC1=CC=CC(O)=C1O.CCC\C=C\C\C=C\CCCCCCCC1=CC=CC(O)=C1O.C\C=C\C=C\C\C=C\CCCCCCCC1=CC=CC(O)=C1O.OC1=CC=CC(CCCCCCC\C=C\C\C=C\CC=C)=C1O QARRXYBJLBIVAK-UEMSJJPVSA-N 0.000 claims 1
- IYROWZYPEIMDDN-UHFFFAOYSA-N 3-n-pentadec-8,11,13-trienyl catechol Natural products CC=CC=CCC=CCCCCCCCC1=CC=CC(O)=C1O IYROWZYPEIMDDN-UHFFFAOYSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 208000020576 Adrenal disease Diseases 0.000 claims 1
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 206010003011 Appendicitis Diseases 0.000 claims 1
- 206010003402 Arthropod sting Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 208000006373 Bell palsy Diseases 0.000 claims 1
- 208000009766 Blau syndrome Diseases 0.000 claims 1
- 206010006002 Bone pain Diseases 0.000 claims 1
- 206010006448 Bronchiolitis Diseases 0.000 claims 1
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 claims 1
- 206010006811 Bursitis Diseases 0.000 claims 1
- 241000282461 Canis lupus Species 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000023890 Complex Regional Pain Syndromes Diseases 0.000 claims 1
- 208000008448 Congenital adrenal hyperplasia Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000007336 Cryptococcosis Diseases 0.000 claims 1
- 241000221204 Cryptococcus neoformans Species 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 241001475178 Dira Species 0.000 claims 1
- 241000196324 Embryophyta Species 0.000 claims 1
- 201000011275 Epicondylitis Diseases 0.000 claims 1
- 208000034846 Familial Amyloid Neuropathies Diseases 0.000 claims 1
- 206010016207 Familial Mediterranean fever Diseases 0.000 claims 1
- 208000035690 Familial cold urticaria Diseases 0.000 claims 1
- 208000001362 Fetal Growth Retardation Diseases 0.000 claims 1
- 206010070531 Foetal growth restriction Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000022461 Glomerular disease Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010019233 Headaches Diseases 0.000 claims 1
- 206010019889 Hereditary neuropathic amyloidosis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101001076407 Homo sapiens Interleukin-1 receptor antagonist protein Proteins 0.000 claims 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000000203 Hyaline Membrane Disease Diseases 0.000 claims 1
- 206010020565 Hyperaemia Diseases 0.000 claims 1
- 208000037147 Hypercalcaemia Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000032571 Infant acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000006877 Insect Bites and Stings Diseases 0.000 claims 1
- 229940119178 Interleukin 1 receptor antagonist Drugs 0.000 claims 1
- 102000051628 Interleukin-1 receptor antagonist Human genes 0.000 claims 1
- 201000008450 Intracranial aneurysm Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 206010024238 Leptospirosis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 206010049565 Muscle fatigue Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 102100022691 NACHT, LRR and PYD domains-containing protein 3 Human genes 0.000 claims 1
- 101710126825 NACHT, LRR and PYD domains-containing protein 3 Proteins 0.000 claims 1
- 206010051606 Necrotising colitis Diseases 0.000 claims 1
- 206010028974 Neonatal respiratory distress syndrome Diseases 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 206010029240 Neuritis Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 208000010191 Osteitis Deformans Diseases 0.000 claims 1
- 206010033078 Otitis media Diseases 0.000 claims 1
- 206010070594 PFAPA syndrome Diseases 0.000 claims 1
- 208000027868 Paget disease Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 241001442654 Percnon planissimum Species 0.000 claims 1
- 201000005702 Pertussis Diseases 0.000 claims 1
- 201000007100 Pharyngitis Diseases 0.000 claims 1
- 208000005384 Pneumocystis Pneumonia Diseases 0.000 claims 1
- 206010073755 Pneumocystis jirovecii pneumonia Diseases 0.000 claims 1
- 206010065159 Polychondritis Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010037549 Purpura Diseases 0.000 claims 1
- 241001672981 Purpura Species 0.000 claims 1
- 208000006311 Pyoderma Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010038687 Respiratory distress Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 206010039792 Seborrhoea Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 claims 1
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 claims 1
- 208000013200 Stress disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000032851 Subarachnoid Hemorrhage Diseases 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 208000004760 Tenosynovitis Diseases 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 241000159243 Toxicodendron radicans Species 0.000 claims 1
- 201000005485 Toxoplasmosis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010064996 Ulcerative keratitis Diseases 0.000 claims 1
- 208000036826 VIIth nerve paralysis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 208000002399 aphthous stomatitis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 229910052790 beryllium Inorganic materials 0.000 claims 1
- ATBAMAFKBVZNFJ-UHFFFAOYSA-N beryllium atom Chemical compound [Be] ATBAMAFKBVZNFJ-UHFFFAOYSA-N 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 208000003295 carpal tunnel syndrome Diseases 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 239000002561 chemical irritant Substances 0.000 claims 1
- 201000004018 childhood brain stem glioma Diseases 0.000 claims 1
- 201000004709 chorioretinitis Diseases 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000025302 chronic primary adrenal insufficiency Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 201000007717 corneal ulcer Diseases 0.000 claims 1
- 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 claims 1
- 208000004921 cutaneous lupus erythematosus Diseases 0.000 claims 1
- 231100000895 deafness Toxicity 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000002169 ectodermal dysplasia Diseases 0.000 claims 1
- 208000030941 fetal growth restriction Diseases 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 231100000852 glomerular disease Toxicity 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 231100000869 headache Toxicity 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 230000010370 hearing loss Effects 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000025070 hereditary periodic fever syndrome Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000000148 hypercalcaemia Effects 0.000 claims 1
- 208000030915 hypercalcemia disease Diseases 0.000 claims 1
- 201000003535 hypohidrotic ectodermal dysplasia Diseases 0.000 claims 1
- 208000035128 hypohidrotic/hair/tooth type autosomal recessive ectodermal dysplasia 10B Diseases 0.000 claims 1
- 208000032771 hypohidrotic/hair/tooth type autosomal recessive ectodermal dysplasia 11B Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 201000006747 infectious mononucleosis Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000003407 interleukin 1 receptor blocking agent Substances 0.000 claims 1
- 230000035987 intoxication Effects 0.000 claims 1
- 231100000566 intoxication Toxicity 0.000 claims 1
- 201000004614 iritis Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000003265 lymphadenitis Diseases 0.000 claims 1
- 208000027202 mammary Paget disease Diseases 0.000 claims 1
- 235000013372 meat Nutrition 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000004995 necrotizing enterocolitis Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 201000002652 newborn respiratory distress syndrome Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 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
- GTUJJVSZIHQLHA-XPWFQUROSA-N pApA Chemical compound C1=NC2=C(N)N=CN=C2N1[C@@H]([C@@H]1O)O[C@H](COP(O)(O)=O)[C@H]1OP(O)(=O)OC[C@H]([C@@H](O)[C@H]1O)O[C@H]1N1C(N=CN=C2N)=C2N=C1 GTUJJVSZIHQLHA-XPWFQUROSA-N 0.000 claims 1
- 208000008494 pericarditis Diseases 0.000 claims 1
- 201000006195 perinatal necrotizing enterocolitis Diseases 0.000 claims 1
- 230000000737 periodic effect Effects 0.000 claims 1
- 208000025487 periodic fever syndrome Diseases 0.000 claims 1
- 201000001245 periodontitis Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000000317 pneumocystosis Diseases 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000010346 psychosocial stress Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 230000010410 reperfusion Effects 0.000 claims 1
- 208000004124 rheumatic heart disease Diseases 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 208000008742 seborrheic dermatitis Diseases 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 claims 1
- 208000026082 sterile multifocal osteomyelitis with periostitis and pustulosis Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 201000007905 transthyretin amyloidosis Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
- DQTMTQZSOJMZSF-UHFFFAOYSA-N urushiol Natural products CCCCCCCCCCCCCCCC1=CC=CC(O)=C1O DQTMTQZSOJMZSF-UHFFFAOYSA-N 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- 208000016261 weight loss Diseases 0.000 claims 1
- 0 C*ICC(C)(CC1)CC(CC(C)(C)*)CCC1C(*(*)C1=C)=*C1=CC(C(CC1CCCCCCCCC1)=O)=C* Chemical compound C*ICC(C)(CC1)CC(CC(C)(C)*)CCC1C(*(*)C1=C)=*C1=CC(C(CC1CCCCCCCCC1)=O)=C* 0.000 description 5
- YSHLVNOVNXNSQS-UHFFFAOYSA-N CN(CC(C1)N)CC1F Chemical compound CN(CC(C1)N)CC1F YSHLVNOVNXNSQS-UHFFFAOYSA-N 0.000 description 1
- QZSACHHNFDNCNB-UHFFFAOYSA-N CN(CCC1)CC1N Chemical compound CN(CCC1)CC1N QZSACHHNFDNCNB-UHFFFAOYSA-N 0.000 description 1
- DYXHMBATAKKMTQ-OAQYLSRUSA-N N[C@H](CCC1)CN1C(c(cc1)cc2c1[n](C=[IH])c(-c1cc(-c3ccccc3)n[n]1CC1CC1)n2)=O Chemical compound N[C@H](CCC1)CN1C(c(cc1)cc2c1[n](C=[IH])c(-c1cc(-c3ccccc3)n[n]1CC1CC1)n2)=O DYXHMBATAKKMTQ-OAQYLSRUSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662298726P | 2016-02-23 | 2016-02-23 | |
| US62/298,726 | 2016-02-23 | ||
| PCT/US2017/018790 WO2017147102A1 (en) | 2016-02-23 | 2017-02-22 | Heteroaryl inhibitors of pad4 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019505597A JP2019505597A (ja) | 2019-02-28 |
| JP2019505597A5 true JP2019505597A5 (enExample) | 2020-04-02 |
| JP6926126B2 JP6926126B2 (ja) | 2021-08-25 |
Family
ID=58191708
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018563393A Active JP6926126B2 (ja) | 2016-02-23 | 2017-02-22 | Ｐａｄ４のヘテロアリール阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11198681B2 (enExample) |
| EP (1) | EP3419969B1 (enExample) |
| JP (1) | JP6926126B2 (enExample) |
| KR (1) | KR102759005B1 (enExample) |
| CN (1) | CN109071497B (enExample) |
| AR (1) | AR107694A1 (enExample) |
| AU (1) | AU2017223416A1 (enExample) |
| BR (1) | BR112018016433A2 (enExample) |
| CA (1) | CA3015482A1 (enExample) |
| EA (1) | EA201891910A1 (enExample) |
| ES (1) | ES2770102T3 (enExample) |
| IL (1) | IL261167A (enExample) |
| MX (1) | MX2018009773A (enExample) |
| SG (1) | SG11201807021UA (enExample) |
| TW (1) | TW201825476A (enExample) |
| UY (1) | UY37134A (enExample) |
| WO (1) | WO2017147102A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3419969B1 (en) | 2016-02-23 | 2019-12-18 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| WO2018022897A1 (en) | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| CN110248934B (zh) | 2016-09-12 | 2022-05-24 | 帕德罗科治疗公司 | 杂芳基pad4抑制剂 |
| JP7504349B2 (ja) * | 2017-09-19 | 2024-06-24 | 三菱瓦斯化学株式会社 | 半導体リソグラフィー膜形成組成物、並びにレジストパターン形成方法及びデバイス |
| JP7065951B2 (ja) | 2017-09-22 | 2022-05-12 | ジュビラント エピパッド エルエルシー | Ｐａｄ阻害剤としての複素環式化合物 |
| WO2019077631A1 (en) | 2017-10-18 | 2019-04-25 | Jubilant Biosys Limited | IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS |
| EP3707135A1 (en) | 2017-11-06 | 2020-09-16 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation |
| IL274762B2 (en) | 2017-11-24 | 2023-10-01 | Jubilant Episcribe Llc | Novel heterocyclic compounds as prmt5 inhibitors |
| WO2019122202A1 (en) * | 2017-12-20 | 2019-06-27 | Ecole Polytechnique Federale De Lausanne (Epfl) | Sting inhibitors |
| WO2019175897A1 (en) | 2018-03-13 | 2019-09-19 | Jubilant Biosys Limited | Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation |
| CN112566916B (zh) * | 2018-08-08 | 2023-10-20 | 百时美施贵宝公司 | 作为pad4抑制剂的经取代的噻吩并吡咯 |
| KR20210042933A (ko) * | 2018-08-08 | 2021-04-20 | 브리스톨-마이어스 스큅 컴퍼니 | Pad 효소의 벤즈이미다졸 억제제 |
| EP3833440A1 (en) | 2018-08-08 | 2021-06-16 | Bristol-Myers Squibb Company | Indole and azaindole inhibitors of pad enzymes |
| WO2021040502A1 (ko) * | 2019-08-30 | 2021-03-04 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
| TW202115083A (zh) * | 2019-09-27 | 2021-04-16 | 大陸商南京藥捷安康生物科技有限公司 | 肽醯精胺酸脫亞胺酶抑制劑及其用途 |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| WO2021158840A1 (en) | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| CN113248507A (zh) * | 2020-02-09 | 2021-08-13 | 上海茂晟康慧科技有限公司 | 瑞德西韦关键中间体7-卤代吡咯并[1,2-f][1,2,4]三嗪-4-胺的合成方法 |
| TW202140477A (zh) | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環ｐａｄ４抑制劑 |
| PE20230488A1 (es) | 2020-04-30 | 2023-03-21 | Gilead Sciences Inc | Inhibidores macrociclicos de las peptidilarginina deiminasas |
| EP4267562A1 (en) | 2020-12-22 | 2023-11-01 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| US12240862B2 (en) | 2020-12-22 | 2025-03-04 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| CN112618546B (zh) * | 2020-12-22 | 2022-03-01 | 陈昊 | Pad4抑制剂在制备放射治疗增敏药物方面的应用 |
| KR20220122879A (ko) * | 2021-02-26 | 2022-09-05 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
| TW202446377A (zh) | 2023-04-18 | 2024-12-01 | 美商克力歐普股份有限公司 | Nk3調節劑及其用途 |
| WO2025006962A1 (en) | 2023-06-30 | 2025-01-02 | Bristol-Myers Squibb Company | Kras inhibitors |
| WO2025024265A1 (en) | 2023-07-21 | 2025-01-30 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad4 modulators |
| WO2025080781A1 (en) * | 2023-10-12 | 2025-04-17 | Kallyope, Inc. | Nk3 modulators and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014015905A1 (en) * | 2012-07-26 | 2014-01-30 | Glaxo Group Limited | 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors |
| CA3199601A1 (en) * | 2015-05-21 | 2016-11-24 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as pad4 inhibitors |
| AR107030A1 (es) * | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores aza-bencimidazol de pad4 |
| AR107032A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| EP3419969B1 (en) | 2016-02-23 | 2019-12-18 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| WO2018022897A1 (en) | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| CN110248934B (zh) | 2016-09-12 | 2022-05-24 | 帕德罗科治疗公司 | 杂芳基pad4抑制剂 |
-
2017
- 2017-02-22 EP EP17708142.9A patent/EP3419969B1/en active Active
- 2017-02-22 AU AU2017223416A patent/AU2017223416A1/en not_active Abandoned
- 2017-02-22 US US16/078,376 patent/US11198681B2/en active Active
- 2017-02-22 AR ARP170100442A patent/AR107694A1/es unknown
- 2017-02-22 UY UY0001037134A patent/UY37134A/es unknown
- 2017-02-22 CA CA3015482A patent/CA3015482A1/en not_active Abandoned
- 2017-02-22 TW TW106105844A patent/TW201825476A/zh unknown
- 2017-02-22 MX MX2018009773A patent/MX2018009773A/es unknown
- 2017-02-22 EA EA201891910A patent/EA201891910A1/ru unknown
- 2017-02-22 ES ES17708142T patent/ES2770102T3/es active Active
- 2017-02-22 BR BR112018016433-0A patent/BR112018016433A2/pt not_active IP Right Cessation
- 2017-02-22 SG SG11201807021UA patent/SG11201807021UA/en unknown
- 2017-02-22 WO PCT/US2017/018790 patent/WO2017147102A1/en not_active Ceased
- 2017-02-22 JP JP2018563393A patent/JP6926126B2/ja active Active
- 2017-02-22 CN CN201780025089.9A patent/CN109071497B/zh active Active
- 2017-02-22 KR KR1020187027136A patent/KR102759005B1/ko active Active
-
2018
- 2018-08-15 IL IL261167A patent/IL261167A/en unknown
-
2021
- 2021-11-09 US US17/522,348 patent/US11897866B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019505597A5 (enExample) | ||
| JP2019505568A5 (enExample) | ||
| JP2019526606A5 (enExample) | ||
| RU2673889C1 (ru) | Стабильная кристаллическая форма ii апремиласта, не содержащая сольваты, и способ ее получения | |
| CN109790162A (zh) | Pad4的共价抑制剂 | |
| ES2295682T3 (es) | Derivados de pirimidina y su uso como modulares de cb2. | |
| US20250205251A1 (en) | Aqueous oral pharmaceutical suspension compositions | |
| JP5346292B2 (ja) | ５−ｈｔ２ａセロトニン受容体に関連する障害の処置に有用な５−ｈｔ２ａセロトニン受容体の調整因子としてのピラゾール誘導体 | |
| ES2617671T3 (es) | Forma cristalina de un derivado de carbamoil ciclohexano | |
| BRPI0714062A2 (pt) | n-fenil-metil-5-oxo-prolina-2-amidas substituìdas como antagonistas do receptor da p2x, e os seus métodos de uso | |
| US20100190812A1 (en) | Nilotinib hcl crystalline forms | |
| ES2971478T3 (es) | Formas en estado sólido de sofosbuvir | |
| CN109071497A (zh) | Pad4杂芳基抑制剂 | |
| CN101945655A (zh) | 作为p2x7调节剂的5-氧代-3-吡咯烷甲酰胺衍生物 | |
| BR112014020416B1 (pt) | Cristal de 1-(2-desoxi-2-flúor-4-tio-ß-darabinofuranosil)citosina e composição farmacêutica contendo o referido cristal | |
| BR112012023649B1 (pt) | Método para produção de cristais de forma ii de monoidrato de n1 -(5-cloropiridin-2-il)-n2 -((1s,2r,4s)-4-[(dimetilamino) carbonil]-2-{[(5-metil-4,5,6,7-tetrahidrotiazol[5,4-c]piridin-2-il) carbonil] amino}ciclohexil)etanodiamida p-toluenossulfonato | |
| BR112017007953B1 (pt) | Forma cristalina ii do bissulfato inibidor de jak quinase, seu uso e seu método de preparação, e composição farmacêutica | |
| JP2001523712A (ja) | Ｐｄｅ−ｉｖのベンゼンスルホンアミド阻害剤およびそれらの治療的使用 | |
| WO2020254697A1 (en) | Fused 1,2 thiazoles and 1,2 thiazines which act as nl3p3 modulators | |
| JP2024095561A (ja) | ６－［（３Ｓ，４Ｓ）－４－メチル－ｌ－（ピリミジン－２－イルメチル）ピロリジン－３－イル］－３－テトラヒドロピラン－４－イル－７Ｈ－イミダゾ［ｌ，５－Ａ］ピラジン－８－オンの一水和物および結晶形態 | |
| SU1588284A3 (ru) | Способ получени производных 1Н, 3Н-пирроло [1,2-с] тиазола в форме рацематов или энантиомеров | |
| BRPI0619851A2 (pt) | formas cristalinas de 1-benzoil-4[2-[4-metóxi-7-(3-metil-1h-1,2,4-triazol-1il)-1-[( fosfonoóxi)metil]-1h-pirrol [2,3-c]piridin-3-il]-1,2-dioxoetil]-piperazina, composição que as compreende e uso das mesmas | |
| EA031671B1 (ru) | Твердые формы 2-(трет-бутиламино)-4-((1r,3r,4r)-3-гидрокси-4-метилциклогексиламино)пиримидин-5-карбоксамида, его композиции и способы его применения | |
| CN112313233A (zh) | Jak家族激酶的小分子抑制剂 | |
| ES2336363T3 (es) | Procedimiento de preparacion de sales de 4-((5-((ciclopropilamino)carbnil)-2-metilfenil)amino)-5-metil-n-propilpirrolo(2,1-f)(1,2,4)triazinacarboxamida y nuevas formas estables pruducidas en dicho procedimiento. |