JP2017505808A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017505808A5 JP2017505808A5 JP2016562078A JP2016562078A JP2017505808A5 JP 2017505808 A5 JP2017505808 A5 JP 2017505808A5 JP 2016562078 A JP2016562078 A JP 2016562078A JP 2016562078 A JP2016562078 A JP 2016562078A JP 2017505808 A5 JP2017505808 A5 JP 2017505808A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- thiadiazol
- acetamido
- pyridin
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 14
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- -1 nitro, amino Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 102000009127 Glutaminase Human genes 0.000 claims 4
- 108010073324 Glutaminase Proteins 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 4
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 206010047115 Vasculitis Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 201000002481 Myositis Diseases 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 239000000730 antalgic agent Substances 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 239000000739 antihistaminic agent Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 229940125721 immunosuppressive agent Drugs 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000030767 Autoimmune encephalitis Diseases 0.000 claims 1
- 208000015338 Autoimmune hepatitis type 1 Diseases 0.000 claims 1
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000023514 Barrett esophagus Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010014612 Encephalitis viral Diseases 0.000 claims 1
- 208000010334 End Stage Liver Disease Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000003923 Hereditary Corneal Dystrophies Diseases 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome 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
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 241000243985 Onchocerca volvulus Species 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 208000031845 Pernicious anaemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010058141 Skin graft rejection Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010046914 Vaginal infection Diseases 0.000 claims 1
- 201000008100 Vaginitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000000735 allogeneic effect Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 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
- 230000001363 autoimmune Effects 0.000 claims 1
- 201000004982 autoimmune uveitis Diseases 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000011444 chronic liver failure Diseases 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 206010011005 corneal dystrophy Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000002491 encephalomyelitis Diseases 0.000 claims 1
- 206010014801 endophthalmitis Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000007565 gingivitis Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 208000009326 ileitis Diseases 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 201000001371 inclusion conjunctivitis Diseases 0.000 claims 1
- 208000013256 infectious meningitis Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000010982 kidney cancer 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
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000009928 nephrosis Diseases 0.000 claims 1
- 231100001027 nephrosis Toxicity 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000002042 onchocerciasis Diseases 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
- 229940127084 other anti-cancer agent Drugs 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 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
- 201000001245 periodontitis Diseases 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004550 quinolin-6-yl group Chemical group N1=CC=CC2=CC(=CC=C12)* 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 210000004116 schwann cell Anatomy 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 206010044325 trachoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 210000002700 urine Anatomy 0.000 claims 1
- 201000002498 viral encephalitis Diseases 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Applications Claiming Priority (19)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN36CH2014 | 2014-01-06 | ||
| IN39/CHE/2014 | 2014-01-06 | ||
| IN39CH2014 | 2014-01-06 | ||
| IN36/CHE/2014 | 2014-01-06 | ||
| IN2639/CHE/2014 | 2014-05-29 | ||
| IN2639CH2014 | 2014-05-29 | ||
| IN2647/CHE/2014 | 2014-05-29 | ||
| IN2647CH2014 | 2014-05-29 | ||
| IN2783/CHE/2014 | 2014-06-06 | ||
| IN2783CH2014 | 2014-06-06 | ||
| IN3525CH2014 | 2014-07-18 | ||
| IN3525/CHE/2014 | 2014-07-18 | ||
| IN3612CH2014 | 2014-07-24 | ||
| IN3613/CHE/2014 | 2014-07-24 | ||
| IN3613CH2014 | 2014-07-24 | ||
| IN3612/CHE/2014 | 2014-07-24 | ||
| IN5438/CHE/2014 | 2014-10-31 | ||
| IN5438CH2014 | 2014-10-31 | ||
| PCT/IB2015/050075 WO2015101957A2 (en) | 2014-01-06 | 2015-01-05 | Novel glutaminase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019090711A Division JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505808A JP2017505808A (ja) | 2017-02-23 |
| JP2017505808A5 true JP2017505808A5 (cg-RX-API-DMAC7.html) | 2018-01-25 |
| JP6783663B2 JP6783663B2 (ja) | 2020-11-11 |
Family
ID=52478027
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016562079A Expired - Fee Related JP6666263B2 (ja) | 2014-01-06 | 2015-01-05 | グルタミナーゼの新規阻害剤 |
| JP2016562078A Expired - Fee Related JP6783663B2 (ja) | 2014-01-06 | 2015-01-05 | 新規グルタミナーゼ阻害剤 |
| JP2019090711A Pending JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016562079A Expired - Fee Related JP6666263B2 (ja) | 2014-01-06 | 2015-01-05 | グルタミナーゼの新規阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019090711A Pending JP2019163290A (ja) | 2014-01-06 | 2019-05-13 | 新規グルタミナーゼ阻害剤 |
Country Status (16)
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20150085078A (ko) | 2012-11-21 | 2015-07-22 | 아지오스 파마슈티컬스 아이엔씨. | 글루타마제 억제제 및 사용 방법 |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| CN105960405B (zh) * | 2014-01-06 | 2021-02-19 | 理森制药股份公司 | 谷氨酰胺酶抑制剂 |
| CA2943339A1 (en) * | 2014-03-21 | 2015-09-24 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| PE20161436A1 (es) * | 2014-04-30 | 2017-01-08 | Pfizer | Derivados de diheterociclo enlazado a cicloalquilo |
| PT3164394T (pt) | 2014-07-03 | 2020-05-08 | Univ Texas | Inibidores gls1 para o tratamento de doenças |
| WO2016007647A1 (en) | 2014-07-09 | 2016-01-14 | The Johns Hopkins University | Glutaminase inhibitor discovery and nanoparticle-enhanced delivery for cancer therapy |
| AU2016287661B2 (en) * | 2015-06-30 | 2020-07-16 | Board Of Regents, University Of Texas System | GLS1 inhibitors for treating disease |
| US10842763B2 (en) | 2015-07-31 | 2020-11-24 | The Johns Hopkins University | Methods for cancer and immunotherapy using prodrugs of glutamine analogs |
| EP3328376A4 (en) * | 2015-07-31 | 2019-03-13 | The Johns Hopkins University | Methods and compositions for treating metabolic reprogramming disorders |
| JP6863981B2 (ja) | 2015-07-31 | 2021-04-21 | ザ・ジョンズ・ホプキンス・ユニバーシティー | グルタミン類似体のプロドラッグ |
| WO2017021177A1 (en) * | 2015-08-04 | 2017-02-09 | Universitat De Barcelona | Pharmaceutical combinations for use in the treatment of cancer |
| GB201520959D0 (en) | 2015-11-27 | 2016-01-13 | Astrazeneca Ab And Cancer Res Technology Ltd | Bis-pyridazine compounds and their use in treating cancer |
| TW201731511A (zh) | 2015-11-30 | 2017-09-16 | 阿斯特捷利康公司 | １，３，４-噻二唑化合物及其在治療癌症中之用途 |
| TW201733587A (zh) * | 2015-11-30 | 2017-10-01 | 阿斯特捷利康公司 | 1,3,4-噻二唑化合物及其在治療癌症中之用途 |
| TW201730188A (zh) * | 2015-11-30 | 2017-09-01 | 阿斯特捷利康公司 | 1,3,4-噻二唑化合物及其在治療癌症中之用途 |
| EP3394054B1 (en) | 2015-12-21 | 2019-11-06 | Council of Scientific and Industrial Research | Novel 1,2,3 triazole-thiazole compounds, process for preparation and use thereof |
| KR102777513B1 (ko) | 2015-12-22 | 2025-03-06 | 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 | (ｒ)-1-(4-(6-(2-(4-(3,3-디플루오로시클로부톡시)-6-메틸피리딘-2-일)아세트아미도)피리다진-3-일)-2-플루오로부틸)-ｎ-메틸-1ｈ-1,2,3-트리아졸-4-카르복사미드의 염 형태 및 다형체 |
| CN107474024B (zh) * | 2016-06-08 | 2022-12-13 | 北京赛林泰医药技术有限公司 | 一种谷氨酰酶抑制剂及其组合物和用途 |
| WO2018102715A1 (en) * | 2016-12-02 | 2018-06-07 | Indiana University Research And Technology Corporation | Compositions and methods for treating and/or reducing corneal dystrophy |
| MX2019008388A (es) * | 2017-01-27 | 2019-12-02 | Univ Cornell | Polímeros e hidrogeles zwitteriónicamente modificados. |
| CN110741003B (zh) * | 2017-06-13 | 2021-07-23 | 南京明德新药研发有限公司 | 作为gls1抑制剂的化合物 |
| WO2019079632A1 (en) | 2017-10-18 | 2019-04-25 | Board Of Regents, The University Of Texas System | GLUTAMINASE INHIBITOR THERAPY |
| JP7217273B6 (ja) | 2017-10-27 | 2024-02-08 | 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 | ピリジンカルボニル誘導体およびｔｒｐｃ６阻害剤としてのその治療的使用 |
| US20190269705A1 (en) * | 2017-11-27 | 2019-09-05 | Regents Of The University Of Minnesota | Methods and materials for treating graft versus host disease |
| WO2020028115A1 (en) * | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | 5-methyl-4-fluoro-thiazol-2-yl compounds |
| CN113166137B (zh) | 2018-09-19 | 2024-08-16 | 比奥根Ma公司 | O-糖蛋白-2-乙酰氨基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂 |
| EP3878470A4 (en) * | 2018-11-08 | 2022-08-31 | The University of Tokyo | METHOD FOR ELIMINATING SENESCENE CELLS AND METHOD FOR PREPARING SENESCENE CELLS |
| CN109223778B (zh) * | 2018-11-16 | 2021-07-27 | 上海市肺科医院 | C24h24n6o2s3在制备抗结核菌药物中的用途 |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| WO2020223267A1 (en) | 2019-05-01 | 2020-11-05 | Boehringer Ingelheim International Gmbh | (r)-(2-methyloxiran-2-yl)methyl 4-bromobenzenesulfonate |
| CN110746416A (zh) * | 2019-09-05 | 2020-02-04 | 中国药科大学 | 含有三氮唑结构的谷氨酰胺酶gls1抑制剂或其可药用的盐、其制备方法及用途 |
| JP2023509452A (ja) | 2020-01-03 | 2023-03-08 | バーグ エルエルシー | がんを処置するためのｕｂｅ２ｋモジュレータとしての多環式アミド |
| CN111643669A (zh) * | 2020-06-30 | 2020-09-11 | 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） | 谷氨酰胺酶抑制剂在制备治疗银屑病的药物中的应用 |
| EP4196118A1 (en) | 2020-08-13 | 2023-06-21 | Boehringer Ingelheim International GmbH | Treatment of cognitive impairement associated with schizophrenia |
| CN116348108A (zh) | 2020-10-13 | 2023-06-27 | 勃林格殷格翰国际有限公司 | 再加工方法 |
| CA3194868A1 (en) * | 2020-10-16 | 2022-04-21 | Georg Winter | Heterocyclic cullin ring ubiquitin ligase compounds and uses thereof |
| IL308122A (en) | 2021-06-16 | 2023-12-01 | Celgene Corp | Azetidinyl compounds consisting of a carboxylic acid group for the treatment of neurodegenerative diseases |
| CN114805346A (zh) * | 2021-07-08 | 2022-07-29 | 成都硕德药业有限公司 | 杂环类衍生物、其制备方法及用途 |
| CN116023375A (zh) * | 2021-10-25 | 2023-04-28 | 成都苑东生物制药股份有限公司 | 一种杂环类衍生物、其制备方法及用途 |
| WO2023114170A1 (en) | 2021-12-14 | 2023-06-22 | Boehringer Ingelheim International Gmbh | Aldosterone synthase inhibitors for treating chronic kidney disease |
| US20250288577A1 (en) * | 2022-04-29 | 2025-09-18 | Cornell University | Methods of treating a virus infection and methods of inhibiting viral replication |
| CN114874186B (zh) * | 2022-05-16 | 2023-07-11 | 深圳大学 | 一种谷氨酰胺酰基环化酶同工酶抑制剂及其制备方法与应用 |
| WO2024233839A1 (en) * | 2023-05-10 | 2024-11-14 | Leal Therapeutics, Inc. | Small molecule inhibitors of glutaminase |
| WO2025082274A1 (zh) * | 2023-10-17 | 2025-04-24 | 楚浦创制（武汉）医药科技有限公司 | 硫代羰基化合物及其应用 |
| CN119192178B (zh) * | 2024-09-23 | 2025-08-05 | 浙江师范大学行知学院 | 一种氨基脲衍生物及其制备方法与应用 |
| CN119656315B (zh) * | 2024-12-23 | 2025-10-17 | 重庆医科大学 | Gls1抑制剂在缓解溃疡性结肠炎中的应用 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2104783A1 (en) * | 1970-07-14 | 1972-04-21 | Berlin Chemie Veb | 2,5-disubstd 2-amino-1,3,4-thiadiazoles-from 4-substd 1-acylthiosemic - virustatics |
| JPH0358980A (ja) * | 1989-07-28 | 1991-03-14 | Canon Inc | 液晶性化合物、これを含む液晶組成物、およびこれを使用した液晶素子 |
| EP0656210A1 (en) | 1993-11-19 | 1995-06-07 | Takeda Chemical Industries, Ltd. | Imidazole derivatives as glutaminose inhibitors |
| WO1999009825A1 (en) | 1997-08-29 | 1999-03-04 | Elan Pharmaceuticals, Inc. | Method of preventing neuronal death |
| WO2000059533A1 (en) | 1999-04-02 | 2000-10-12 | Children's Hospital Los Angeles | Use of asparaginase and glutaminase to treat autoimmune disease and graft versus host disease |
| US6451828B1 (en) | 2000-08-10 | 2002-09-17 | Elan Pharmaceuticals, Inc. | Selective inhibition of glutaminase by bis-thiadiazoles |
| NO315152B1 (no) | 2001-06-28 | 2003-07-21 | Tomm Slater | Anordning for rensing av luft |
| US7288246B2 (en) | 2001-09-13 | 2007-10-30 | The Board Of Regents Of The University Of Oklahoma | Method of alleviating chronic pain via peripheral glutaminase regulation |
| SE0300456D0 (sv) * | 2003-02-19 | 2003-02-19 | Astrazeneca Ab | Novel compounds |
| EP1597256A1 (en) * | 2003-02-21 | 2005-11-23 | Pfizer Inc. | N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors |
| DE10326821A1 (de) | 2003-06-11 | 2005-01-05 | Medical Enzymes Ag | Pharmazeutische Kombinationspräparate zur Krebstherapie |
| US20060276438A1 (en) | 2004-10-04 | 2006-12-07 | Natarajan Sethuraman | Prevention and treatment of influenza with glutamine antagonist agents |
| AP2008004410A0 (en) | 2005-10-06 | 2008-04-30 | Nippon Soda Co | Cross-linked cyclic amine compounds and agents forpest control |
| CA2651691A1 (en) | 2006-05-10 | 2007-11-15 | Medical Enzymes Ag | Glutaminase and 6-diazo-5-oxo-l-norleucine (don) for cancer therapy |
| TW200819437A (en) * | 2006-08-17 | 2008-05-01 | Astrazeneca Ab | Chemical compounds |
| TWI414523B (zh) * | 2006-12-28 | 2013-11-11 | Metabolex Inc | 用於治療糖尿病及代謝病症之雜環受體促效劑 |
| US7638541B2 (en) * | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| CA2693169C (en) | 2007-07-19 | 2016-01-12 | Metabolex, Inc. | N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders |
| AU2009233984B2 (en) * | 2008-04-07 | 2012-11-22 | Irm Llc | Compounds and compositions as modulators of GPR119 activity |
| CN102066337A (zh) | 2008-04-22 | 2011-05-18 | 第一三共株式会社 | 5-羟基嘧啶-4-甲酰胺化合物 |
| US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| WO2010013849A1 (ja) * | 2008-08-01 | 2010-02-04 | 日本ケミファ株式会社 | Ｇｐｒ１１９作動薬 |
| WO2010033871A2 (en) | 2008-09-18 | 2010-03-25 | The Johns Hopkins University | Compositions and methods targeting glutaminase |
| WO2010045303A2 (en) * | 2008-10-16 | 2010-04-22 | Schering Corporation | Pyrrolidine, piperidine and piperazine derivatives and methods of use thereof |
| WO2010048149A2 (en) * | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| JP2010138082A (ja) * | 2008-12-09 | 2010-06-24 | Nippon Soda Co Ltd | 環状アミン化合物またはその塩、並びに有害生物防除剤 |
| WO2010111504A2 (en) | 2009-03-25 | 2010-09-30 | Cornell University | Inhibition of glutaminase c |
| WO2011025006A1 (ja) * | 2009-08-31 | 2011-03-03 | 日本ケミファ株式会社 | Ｇｐｒ１１９作動薬 |
| EP2496567B1 (en) * | 2009-11-05 | 2017-07-12 | Rhizen Pharmaceuticals S.A. | Novel benzopyran kinase modulators |
| ES2362770B1 (es) | 2009-12-24 | 2012-05-22 | Universidad De Sevilla | Uso de compuesto n-fenil-n'-(3-metil-2-butenil)tiourea para la elaboración de medicamentos destinados al tratamiento de la encefalopatía hepática. |
| KR20120130104A (ko) * | 2010-02-01 | 2012-11-28 | 닛뽕 케미파 가부시키가이샤 | Ｇｐｒ119 작동약 |
| US20130109643A1 (en) | 2010-05-10 | 2013-05-02 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| CA2798080C (en) * | 2010-05-17 | 2020-08-25 | Incozen Therapeutics Pvt. Ltd. | 3,5-disubstitued-3h-imidazo[4,5-b]pyridine and 3,5- disubstitued -3h-[1,2,3]triazolo[4,5-b] pyridine compounds as modulators of protein kinases |
| WO2012006506A1 (en) | 2010-07-09 | 2012-01-12 | Massachusetts Institute Of Technology | Metabolic gene, enzyme, and flux targets for cancer therapy |
| US20130252983A1 (en) | 2010-09-10 | 2013-09-26 | Cornell University | Activating phosphorylation site on glutaminase c |
| JP2014094886A (ja) * | 2011-02-28 | 2014-05-22 | Nippon Chemiphar Co Ltd | Ｇｐｒ１１９作動薬 |
| CN103030597B (zh) | 2011-09-30 | 2014-10-01 | 南昌滨西科技有限公司 | 肾脏型谷氨酰胺酶抑制剂及其制备方法和用途 |
| TW201321353A (zh) | 2011-10-08 | 2013-06-01 | Novartis Ag | 胺基甲酸酯／尿素衍生物 |
| SG11201402305WA (en) | 2011-11-21 | 2014-06-27 | Calithera Biosciences Inc | Heterocyclic inhibitors of glutaminase |
| US8604016B2 (en) | 2011-11-21 | 2013-12-10 | Calithera Biosciences Inc. | Heterocyclic inhibitors of glutaminase |
| WO2014043633A1 (en) | 2012-09-17 | 2014-03-20 | Agios Pharmaceuticals, Inc. | Use of e-cadherin and vimentin for selection of treatment responsive patients |
| US10793535B2 (en) | 2012-11-16 | 2020-10-06 | Calithera Biosciences, Inc. | Heterocyclic glutaminase inhibitors |
| KR20150085078A (ko) | 2012-11-21 | 2015-07-22 | 아지오스 파마슈티컬스 아이엔씨. | 글루타마제 억제제 및 사용 방법 |
| US9029531B2 (en) * | 2012-11-22 | 2015-05-12 | Agios Pharmaceuticals, Inc. | Compounds and their methods of use |
| WO2014079011A1 (en) * | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| CN105283182A (zh) | 2012-12-03 | 2016-01-27 | 卡利泰拉生物科技公司 | 用谷氨酰胺酶的杂环抑制剂治疗癌症 |
| CN105960405B (zh) * | 2014-01-06 | 2021-02-19 | 理森制药股份公司 | 谷氨酰胺酶抑制剂 |
| PE20161436A1 (es) * | 2014-04-30 | 2017-01-08 | Pfizer | Derivados de diheterociclo enlazado a cicloalquilo |
-
2015
- 2015-01-05 CN CN201580006698.0A patent/CN105960405B/zh not_active Expired - Fee Related
- 2015-01-05 SG SG11201605478XA patent/SG11201605478XA/en unknown
- 2015-01-05 EA EA201691135A patent/EA033163B1/ru unknown
- 2015-01-05 EP EP15705845.4A patent/EP3092236B1/en not_active Not-in-force
- 2015-01-05 EA EA201991183A patent/EA201991183A1/ru unknown
- 2015-01-05 AU AU2015204210A patent/AU2015204210B2/en not_active Ceased
- 2015-01-05 EP EP15705095.6A patent/EP3092235A2/en not_active Withdrawn
- 2015-01-05 WO PCT/IB2015/050075 patent/WO2015101957A2/en not_active Ceased
- 2015-01-05 ES ES15705845T patent/ES2833576T3/es active Active
- 2015-01-05 CN CN201580009614.9A patent/CN106029659B/zh not_active Expired - Fee Related
- 2015-01-05 BR BR112016015706A patent/BR112016015706A8/pt not_active Application Discontinuation
- 2015-01-05 CN CN202010256915.4A patent/CN111393431A/zh active Pending
- 2015-01-05 EA EA201691134A patent/EA035499B1/ru unknown
- 2015-01-05 KR KR1020167021582A patent/KR20160100408A/ko not_active Ceased
- 2015-01-05 KR KR1020227001963A patent/KR20220013017A/ko not_active Ceased
- 2015-01-05 CN CN202110114920.6A patent/CN112920180A/zh active Pending
- 2015-01-05 CN CN202010671865.6A patent/CN111892589A/zh active Pending
- 2015-01-05 CA CA2934700A patent/CA2934700A1/en not_active Abandoned
- 2015-01-05 CA CA2934702A patent/CA2934702A1/en not_active Abandoned
- 2015-01-05 KR KR1020167021580A patent/KR20160100407A/ko not_active Ceased
- 2015-01-05 DK DK15705845.4T patent/DK3092236T3/da active
- 2015-01-05 US US14/769,365 patent/US20160297761A1/en not_active Abandoned
- 2015-01-05 US US14/769,331 patent/US9783533B2/en not_active Expired - Fee Related
- 2015-01-05 WO PCT/IB2015/050076 patent/WO2015101958A2/en not_active Ceased
- 2015-01-05 JP JP2016562079A patent/JP6666263B2/ja not_active Expired - Fee Related
- 2015-01-05 JP JP2016562078A patent/JP6783663B2/ja not_active Expired - Fee Related
-
2016
- 2016-06-21 IL IL246362A patent/IL246362B/en unknown
- 2016-06-23 ZA ZA2016/04272A patent/ZA201604272B/en unknown
- 2016-07-05 CL CL2016001715A patent/CL2016001715A1/es unknown
-
2017
- 2017-08-31 US US15/693,291 patent/US10611759B2/en not_active Expired - Fee Related
-
2019
- 2019-05-13 JP JP2019090711A patent/JP2019163290A/ja active Pending
-
2020
- 2020-03-20 US US16/825,755 patent/US20210032236A1/en not_active Abandoned