JP2017528461A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017528461A5 JP2017528461A5 JP2017512983A JP2017512983A JP2017528461A5 JP 2017528461 A5 JP2017528461 A5 JP 2017528461A5 JP 2017512983 A JP2017512983 A JP 2017512983A JP 2017512983 A JP2017512983 A JP 2017512983A JP 2017528461 A5 JP2017528461 A5 JP 2017528461A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- tumor
- cell
- alkyl
- lymphoma
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 54
- -1 1-imidazolyl Chemical group 0.000 claims 52
- 206010028980 Neoplasm Diseases 0.000 claims 36
- 150000003839 salts Chemical class 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 210000004027 cell Anatomy 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 10
- 125000003282 alkyl amino group Chemical group 0.000 claims 10
- 125000004663 dialkyl amino group Chemical group 0.000 claims 10
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 10
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 206010018338 Glioma Diseases 0.000 claims 8
- 208000032612 Glial tumor Diseases 0.000 claims 7
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 206010042971 T-cell lymphoma Diseases 0.000 claims 7
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 7
- 201000001441 melanoma Diseases 0.000 claims 7
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 6
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 6
- 201000000053 blastoma Diseases 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 201000008184 embryoma Diseases 0.000 claims 5
- 201000005962 mycosis fungoides Diseases 0.000 claims 5
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 208000003200 Adenoma Diseases 0.000 claims 4
- 206010001233 Adenoma benign Diseases 0.000 claims 4
- 206010003571 Astrocytoma Diseases 0.000 claims 4
- 208000036170 B-Cell Marginal Zone Lymphoma Diseases 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 4
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims 4
- 206010034811 Pharyngeal cancer Diseases 0.000 claims 4
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 206010039491 Sarcoma Diseases 0.000 claims 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 4
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 4
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 230000002710 gonadal effect Effects 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 4
- 208000007538 neurilemmoma Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 4
- 206010039667 schwannoma Diseases 0.000 claims 4
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 4
- 201000011549 stomach cancer Diseases 0.000 claims 4
- 201000002510 thyroid cancer Diseases 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 3
- 208000021309 Germ cell tumor Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 3
- 208000009956 adenocarcinoma Diseases 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 206010016629 fibroma Diseases 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 208000002008 AIDS-Related Lymphoma Diseases 0.000 claims 2
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 2
- 208000001794 Adipose Tissue Neoplasms Diseases 0.000 claims 2
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 claims 2
- 208000037540 Alveolar soft tissue sarcoma Diseases 0.000 claims 2
- 206010051810 Angiomyolipoma Diseases 0.000 claims 2
- 201000003076 Angiosarcoma Diseases 0.000 claims 2
- 201000008271 Atypical teratoid rhabdoid tumor Diseases 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 208000018084 Bone neoplasm Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000007690 Brenner tumor Diseases 0.000 claims 2
- 206010073258 Brenner tumour Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 208000009458 Carcinoma in Situ Diseases 0.000 claims 2
- 201000000274 Carcinosarcoma Diseases 0.000 claims 2
- 208000007389 Cementoma Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 201000005262 Chondroma Diseases 0.000 claims 2
- 201000009047 Chordoma Diseases 0.000 claims 2
- 208000006332 Choriocarcinoma Diseases 0.000 claims 2
- 208000004378 Choroid plexus papilloma Diseases 0.000 claims 2
- 206010009253 Clear cell sarcoma of the kidney Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000009798 Craniopharyngioma Diseases 0.000 claims 2
- 208000008334 Dermatofibrosarcoma Diseases 0.000 claims 2
- 201000009051 Embryonal Carcinoma Diseases 0.000 claims 2
- 208000033832 Eosinophilic Acute Leukemia Diseases 0.000 claims 2
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims 2
- 208000036566 Erythroleukaemia Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 206010061850 Extranodal marginal zone B-cell lymphoma (MALT type) Diseases 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 2
- 102000051325 Glucagon Human genes 0.000 claims 2
- 108060003199 Glucagon Proteins 0.000 claims 2
- 208000005234 Granulosa Cell Tumor Diseases 0.000 claims 2
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 2
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims 2
- 201000004462 Leydig Cell Tumor Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025219 Lymphangioma Diseases 0.000 claims 2
- 206010025312 Lymphoma AIDS related Diseases 0.000 claims 2
- 201000003791 MALT lymphoma Diseases 0.000 claims 2
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 2
- 206010064281 Malignant atrophic papulosis Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 208000009018 Medullary thyroid cancer Diseases 0.000 claims 2
- 208000000172 Medulloblastoma Diseases 0.000 claims 2
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims 2
- 208000002030 Merkel cell carcinoma Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims 2
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000007727 Muscle Tissue Neoplasms Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010073137 Myxoid liposarcoma Diseases 0.000 claims 2
- 208000002454 Nasopharyngeal Carcinoma Diseases 0.000 claims 2
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 2
- 206010028811 Natural killer-cell leukaemia Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010029266 Neuroendocrine carcinoma of the skin Diseases 0.000 claims 2
- 201000004404 Neurofibroma Diseases 0.000 claims 2
- 208000005890 Neuroma Diseases 0.000 claims 2
- 206010029488 Nodular melanoma Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010061872 Non-renal cell carcinoma of kidney Diseases 0.000 claims 2
- 208000007871 Odontogenic Tumors Diseases 0.000 claims 2
- 206010048757 Oncocytoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000002063 Oxyphilic Adenoma Diseases 0.000 claims 2
- 201000010630 Pancoast tumor Diseases 0.000 claims 2
- 208000015330 Pancoast tumour Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 2
- 208000037064 Papilloma of choroid plexus Diseases 0.000 claims 2
- 206010061332 Paraganglion neoplasm Diseases 0.000 claims 2
- 206010050487 Pinealoblastoma Diseases 0.000 claims 2
- 208000007641 Pinealoma Diseases 0.000 claims 2
- 201000005746 Pituitary adenoma Diseases 0.000 claims 2
- 206010061538 Pituitary tumour benign Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000007452 Plasmacytoma Diseases 0.000 claims 2
- 208000026149 Primary peritoneal carcinoma Diseases 0.000 claims 2
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000034541 Rare lymphatic malformation Diseases 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 208000033889 Renal medullary carcinoma Diseases 0.000 claims 2
- 201000000582 Retinoblastoma Diseases 0.000 claims 2
- 208000025316 Richter syndrome Diseases 0.000 claims 2
- 208000006938 Schwannomatosis Diseases 0.000 claims 2
- 201000010208 Seminoma Diseases 0.000 claims 2
- 208000003274 Sertoli cell tumor Diseases 0.000 claims 2
- 208000009359 Sezary Syndrome Diseases 0.000 claims 2
- 208000021388 Sezary disease Diseases 0.000 claims 2
- 208000003252 Signet Ring Cell Carcinoma Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 2
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 2
- 201000005969 Uveal melanoma Diseases 0.000 claims 2
- 208000014070 Vestibular schwannoma Diseases 0.000 claims 2
- 206010047741 Vulval cancer Diseases 0.000 claims 2
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 2
- 208000000260 Warts Diseases 0.000 claims 2
- 208000012018 Yolk sac tumor Diseases 0.000 claims 2
- 208000006336 acinar cell carcinoma Diseases 0.000 claims 2
- 208000004064 acoustic neuroma Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 208000021841 acute erythroid leukemia Diseases 0.000 claims 2
- 208000013593 acute megakaryoblastic leukemia Diseases 0.000 claims 2
- 208000020700 acute megakaryocytic leukemia Diseases 0.000 claims 2
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims 2
- 208000020990 adrenal cortex carcinoma Diseases 0.000 claims 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 2
- 208000007128 adrenocortical carcinoma Diseases 0.000 claims 2
- 201000006966 adult T-cell leukemia Diseases 0.000 claims 2
- 208000015230 aggressive NK-cell leukemia Diseases 0.000 claims 2
- 206010065867 alveolar rhabdomyosarcoma Diseases 0.000 claims 2
- 201000009076 bladder urachal carcinoma Diseases 0.000 claims 2
- 201000011143 bone giant cell tumor Diseases 0.000 claims 2
- 150000003857 carboxamides Chemical class 0.000 claims 2
- 210000000845 cartilage Anatomy 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 208000030748 clear cell sarcoma of kidney Diseases 0.000 claims 2
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 2
- 208000017763 cutaneous neuroendocrine carcinoma Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 230000002124 endocrine Effects 0.000 claims 2
- 208000001991 endodermal sinus tumor Diseases 0.000 claims 2
- 208000037902 enteropathy Diseases 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 208000024519 eye neoplasm Diseases 0.000 claims 2
- 210000003754 fetus Anatomy 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 201000010175 gallbladder cancer Diseases 0.000 claims 2
- 201000008822 gestational choriocarcinoma Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 2
- 229960004666 glucagon Drugs 0.000 claims 2
- 201000009277 hairy cell leukemia Diseases 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000002222 hemangioblastoma Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 208000006359 hepatoblastoma Diseases 0.000 claims 2
- 201000004933 in situ carcinoma Diseases 0.000 claims 2
- 201000002313 intestinal cancer Diseases 0.000 claims 2
- 208000028774 intestinal disease Diseases 0.000 claims 2
- 206010073096 invasive lobular breast carcinoma Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000020319 kidney medullary carcinoma Diseases 0.000 claims 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 2
- 231100000518 lethal Toxicity 0.000 claims 2
- 230000001665 lethal effect Effects 0.000 claims 2
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 2
- 206010024627 liposarcoma Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000012804 lymphangiosarcoma Diseases 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000015179 malignant superior sulcus neoplasm Diseases 0.000 claims 2
- 201000001117 malignant triton tumor Diseases 0.000 claims 2
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 2
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 2
- 208000000516 mast-cell leukemia Diseases 0.000 claims 2
- 208000029586 mediastinal germ cell tumor Diseases 0.000 claims 2
- 208000030163 medullary breast carcinoma Diseases 0.000 claims 2
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 2
- 230000001394 metastastic effect Effects 0.000 claims 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims 2
- 201000010225 mixed cell type cancer Diseases 0.000 claims 2
- 208000029638 mixed neoplasm Diseases 0.000 claims 2
- 208000022669 mucinous neoplasm Diseases 0.000 claims 2
- 201000009368 muscle benign neoplasm Diseases 0.000 claims 2
- 208000009091 myxoma Diseases 0.000 claims 2
- 208000001611 myxosarcoma Diseases 0.000 claims 2
- 208000014761 nasopharyngeal type undifferentiated carcinoma Diseases 0.000 claims 2
- 201000011216 nasopharynx carcinoma Diseases 0.000 claims 2
- 208000025189 neoplasm of testis Diseases 0.000 claims 2
- 230000009826 neoplastic cell growth Effects 0.000 claims 2
- 201000009494 neurilemmomatosis Diseases 0.000 claims 2
- 208000027831 neuroepithelial neoplasm Diseases 0.000 claims 2
- 201000000032 nodular malignant melanoma Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000008106 ocular cancer Diseases 0.000 claims 2
- 208000027825 odontogenic neoplasm Diseases 0.000 claims 2
- 208000027500 optic nerve neoplasm Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 230000002611 ovarian Effects 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 208000007312 paraganglioma Diseases 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 201000003113 pineoblastoma Diseases 0.000 claims 2
- 230000001817 pituitary effect Effects 0.000 claims 2
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 2
- 208000010916 pituitary tumor Diseases 0.000 claims 2
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 2
- 206010038038 rectal cancer Diseases 0.000 claims 2
- 201000001275 rectum cancer Diseases 0.000 claims 2
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims 2
- 201000008123 signet ring cell adenocarcinoma Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 201000010153 skin papilloma Diseases 0.000 claims 2
- 208000000649 small cell carcinoma Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 201000002314 small intestine cancer Diseases 0.000 claims 2
- 206010062113 splenic marginal zone lymphoma Diseases 0.000 claims 2
- 210000004243 sweat Anatomy 0.000 claims 2
- 206010042863 synovial sarcoma Diseases 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 2
- 210000001519 tissue Anatomy 0.000 claims 2
- 201000007363 trachea carcinoma Diseases 0.000 claims 2
- 208000025443 tumor of adipose tissue Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 206010046766 uterine cancer Diseases 0.000 claims 2
- 206010046885 vaginal cancer Diseases 0.000 claims 2
- 208000013139 vaginal neoplasm Diseases 0.000 claims 2
- 230000000007 visual effect Effects 0.000 claims 2
- 201000005102 vulva cancer Diseases 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004607 1,2,3,4-tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- MBIZXFATKUQOOA-UHFFFAOYSA-N 1,3,4-thiadiazole Chemical compound C1=NN=CS1 MBIZXFATKUQOOA-UHFFFAOYSA-N 0.000 claims 1
- KOFIDSXHWGFEMO-UHFFFAOYSA-N 1-(2-methylpropyl)pyrrolidine Chemical compound CC(C)CN1CCCC1 KOFIDSXHWGFEMO-UHFFFAOYSA-N 0.000 claims 1
- MCMFEZDRQOJKMN-UHFFFAOYSA-N 1-butylimidazole Chemical compound CCCCN1C=CN=C1 MCMFEZDRQOJKMN-UHFFFAOYSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- HYTIPJFUWHYQON-UHFFFAOYSA-N 3,4-dihydro-1h-quinoxalin-2-one Chemical compound C1=CC=C2NC(=O)CNC2=C1 HYTIPJFUWHYQON-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- QVTTWNXAJRQQHZ-UHFFFAOYSA-N 5-prop-1-enyl-1h-imidazole Chemical compound CC=CC1=CN=CN1 QVTTWNXAJRQQHZ-UHFFFAOYSA-N 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 241000321096 Adenoides Species 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 208000032568 B-cell prolymphocytic leukaemia Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005969 Bone giant cell tumour Diseases 0.000 claims 1
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010016935 Follicular thyroid cancer Diseases 0.000 claims 1
- 208000003098 Ganglion Cysts Diseases 0.000 claims 1
- 208000000527 Germinoma Diseases 0.000 claims 1
- 208000002966 Giant Cell Tumor of Bone Diseases 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 208000035416 Prolymphocytic B-Cell Leukemia Diseases 0.000 claims 1
- 102000005157 Somatostatin Human genes 0.000 claims 1
- 108010056088 Somatostatin Proteins 0.000 claims 1
- 206010041329 Somatostatinoma Diseases 0.000 claims 1
- 208000005400 Synovial Cyst Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 208000033781 Thyroid carcinoma Diseases 0.000 claims 1
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- SZPWXAOBLNYOHY-UHFFFAOYSA-N [C]1=CC=NC2=CC=CC=C12 Chemical group [C]1=CC=NC2=CC=CC=C12 SZPWXAOBLNYOHY-UHFFFAOYSA-N 0.000 claims 1
- 206010000583 acral lentiginous melanoma Diseases 0.000 claims 1
- 210000002534 adenoid Anatomy 0.000 claims 1
- 201000008395 adenosquamous carcinoma Diseases 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 230000002707 ameloblastic effect Effects 0.000 claims 1
- 206010002449 angioimmunoblastic T-cell lymphoma Diseases 0.000 claims 1
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- INSSHDIMRIMVLZ-UHFFFAOYSA-N butan-2-ylcyclopropane Chemical compound CCC(C)C1CC1 INSSHDIMRIMVLZ-UHFFFAOYSA-N 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 210000004720 cerebrum Anatomy 0.000 claims 1
- 210000003298 dental enamel Anatomy 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000014616 embryonal neoplasm Diseases 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 230000001605 fetal effect Effects 0.000 claims 1
- 239000000835 fiber Substances 0.000 claims 1
- 230000003352 fibrogenic effect Effects 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 201000003115 germ cell cancer Diseases 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 230000001401 hemangioblastic effect Effects 0.000 claims 1
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 210000002751 lymph Anatomy 0.000 claims 1
- 201000000564 macroglobulinemia Diseases 0.000 claims 1
- 201000011614 malignant glioma Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 206010027191 meningioma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 210000004248 oligodendroglia Anatomy 0.000 claims 1
- 210000001328 optic nerve Anatomy 0.000 claims 1
- 201000011130 optic nerve sheath meningioma Diseases 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims 1
- 229960000553 somatostatin Drugs 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 208000013077 thyroid gland carcinoma Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000013706 tumor of meninges Diseases 0.000 claims 1
- 208000023747 urothelial carcinoma Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462048763P | 2014-09-10 | 2014-09-10 | |
| US62/048,763 | 2014-09-10 | ||
| US201562146804P | 2015-04-13 | 2015-04-13 | |
| US62/146,804 | 2015-04-13 | ||
| PCT/US2015/049225 WO2016040508A1 (en) | 2014-09-10 | 2015-09-09 | Substituted pyrrolidine carboxamide compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017528461A JP2017528461A (ja) | 2017-09-28 |
| JP2017528461A5 true JP2017528461A5 (enExample) | 2018-10-18 |
Family
ID=55459531
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017512983A Pending JP2017528461A (ja) | 2014-09-10 | 2015-09-09 | 置換ピロリジンカルボキサミド化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20170247326A1 (enExample) |
| EP (1) | EP3193609A4 (enExample) |
| JP (1) | JP2017528461A (enExample) |
| AU (1) | AU2015315177A1 (enExample) |
| CA (1) | CA2960277A1 (enExample) |
| WO (1) | WO2016040508A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2017526706A (ja) | 2014-09-10 | 2017-09-14 | エピザイム,インコーポレイティド | イソオキサゾールカルボキサミド化合物 |
| AU2015315171A1 (en) | 2014-09-10 | 2017-03-16 | Epizyme, Inc. | Substituted cyclohexylamine compounds |
| MX2017002986A (es) | 2014-09-10 | 2017-10-24 | Epizyme Inc | Compuestos de piperidina sustituidos. |
| KR102496364B1 (ko) | 2014-09-10 | 2023-02-06 | 에피자임, 인코포레이티드 | Smyd 억제제 |
| JP2017528460A (ja) | 2014-09-10 | 2017-09-28 | エピザイム インコーポレイテッド | 不可逆的smyd阻害剤としてのイソオキサゾールカルボキサミド |
| CN111315735B (zh) | 2017-09-04 | 2024-03-08 | C4医药公司 | 二氢苯并咪唑酮 |
| EP4470618A3 (en) | 2019-03-06 | 2025-03-05 | C4 Therapeutics, Inc. | Heterocyclic compounds for medical treatment |
| GB201912674D0 (en) * | 2019-09-04 | 2019-10-16 | Mission Therapeutics Ltd | Novel compounds |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1428493A (en) * | 1973-05-02 | 1976-03-17 | Science Union & Cie | Heterocyclic amides processes for their preparation and pharma ceutical compositions containing them |
| JPS52128368A (en) * | 1976-04-15 | 1977-10-27 | Yamanouchi Pharmaceut Co Ltd | Novel carboxylic acid amide derivatives and their preparation |
| GR66581B (enExample) * | 1978-02-21 | 1981-03-27 | Delalande Sa | |
| EP1013276A1 (en) * | 1998-12-23 | 2000-06-28 | Pfizer Inc. | Aminoazacycloalkanes as CCR5 modulators |
| DE10148290A1 (de) * | 2001-09-29 | 2003-04-17 | Bayer Cropscience Gmbh | Heterocyclische Amide, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und ihre Verwendung |
| ATE455104T1 (de) * | 2001-11-01 | 2010-01-15 | Icagen Inc | Pyrazolamide zur anwendung in der behandlung von schmerz |
| MXPA05009245A (es) * | 2003-03-11 | 2005-10-19 | Pfizer Prod Inc | Nuevos compuestos de pirazina como inhibidores del factor de crecimiento transformante (tgf). |
| DK1603917T3 (da) * | 2003-03-14 | 2011-02-28 | Medigene Ag | Immunmodulerende heterocycliske forbindelser |
| TW200526641A (en) * | 2003-12-26 | 2005-08-16 | Daiichi Seiyaku Co | Amidopyrazole derivatives |
| MXPA06011328A (es) * | 2004-04-02 | 2006-12-15 | Vertex Pharma | Azaindoles utiles como inhibidotes de roca y otras proteinas cinasas. |
| WO2006086609A2 (en) * | 2005-02-10 | 2006-08-17 | Axys Pharmaceuticals, Inc. | Inhibitors of tryptase |
| WO2006107923A1 (en) * | 2005-04-05 | 2006-10-12 | Boehringer Ingelheim International Gmbh | Substituted benzylimidazoles useful for the treatment of inflammatory diseases |
| CA2604356A1 (en) * | 2005-04-12 | 2006-10-19 | Solvay Pharmaceuticals Gmbh | Aminoalkyl-amidomethyl-substituted 2-(4-sulphonylamino)-3-hydroxy-3,4-dihydro-2h-chromen-6-yl derivatives and their use as potassium channel blockers |
| WO2007011760A2 (en) * | 2005-07-15 | 2007-01-25 | Kalypsys, Inc. | Inhibitors of mitotic kinesin |
| JP5525261B2 (ja) * | 2006-10-24 | 2014-06-18 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Mtp阻害性テトラヒドロ−ナフタレン−1−カルボン酸誘導体 |
| EP1975165A1 (de) * | 2007-03-27 | 2008-10-01 | Boehringer Ingelheim Pharma GmbH & Co. KG | Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel |
| KR20100020487A (ko) * | 2007-05-24 | 2010-02-22 | 와이어쓰 엘엘씨 | 히스타민-3 길항제로서 아자시클릴벤즈아미드 유도체 |
| WO2009014620A1 (en) * | 2007-07-20 | 2009-01-29 | Merck & Co., Inc. | Pyrazolo[1,5-a]pyrimidine derivatives |
| US20110306597A1 (en) * | 2008-06-18 | 2011-12-15 | James Michael Crawforth | Nicotinamide Derivatives |
| WO2010017046A1 (en) * | 2008-08-05 | 2010-02-11 | Merck & Co., Inc. | Pyrazolo[1,5-a]pyridines as mark inhibitors |
| JP2013028538A (ja) * | 2009-11-13 | 2013-02-07 | Dainippon Sumitomo Pharma Co Ltd | 新規アミド誘導体 |
| CA2892042C (en) * | 2012-11-29 | 2022-06-14 | Chemocentryx, Inc. | Cxcr7 antagonists |
-
2015
- 2015-09-09 US US15/510,583 patent/US20170247326A1/en not_active Abandoned
- 2015-09-09 CA CA2960277A patent/CA2960277A1/en not_active Abandoned
- 2015-09-09 AU AU2015315177A patent/AU2015315177A1/en not_active Abandoned
- 2015-09-09 WO PCT/US2015/049225 patent/WO2016040508A1/en not_active Ceased
- 2015-09-09 JP JP2017512983A patent/JP2017528461A/ja active Pending
- 2015-09-09 EP EP15839644.0A patent/EP3193609A4/en not_active Withdrawn
-
2019
- 2019-05-28 US US16/423,618 patent/US20200048195A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017528461A5 (enExample) | ||
| JP2017538659A5 (enExample) | ||
| JP2017511801A5 (enExample) | ||
| AU2017221802B2 (en) | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain | |
| CA2807620C (en) | Pharmaceutically active compounds as axl inhibitors | |
| JP2017528464A5 (enExample) | ||
| US9546156B2 (en) | N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors | |
| US9790210B2 (en) | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors | |
| Garella et al. | Microwave-assisted synthesis of N-heterocycles in medicinal chemistry | |
| JP5256047B2 (ja) | ピロロ[3,2−c]ピリジン−4−オン2−インドリノン(indolinone)プロテインキナーゼ阻害剤 | |
| US9969694B2 (en) | N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors | |
| CN112601747B (zh) | 作为malt1抑制剂的吡唑衍生物 | |
| JP2017528460A5 (enExample) | ||
| KR20100110344A (ko) | C―met의 저해제로서 활성을 나타내는 융합 피리딘 | |
| JP2017538659A (ja) | Smyd阻害剤 | |
| JP2017528461A (ja) | 置換ピロリジンカルボキサミド化合物 | |
| JP2017527577A (ja) | 置換ピロリジン化合物 | |
| JP2017526706A5 (enExample) | ||
| JP2017527576A5 (enExample) | ||
| KR20150047609A (ko) | 피리딘 유도체 및 의약 | |
| US20230095520A1 (en) | Pharmaceutical composition for preventing or treating cancer comprising azole derivatives or pharmaceutically acceptable salt thereof | |
| JP2024514539A (ja) | 医薬化合物 | |
| HK40040495A (en) | Pyrazole derivatives as malt1 inhibitors | |
| KR20250113344A (ko) | CBP/p300 저해제로 사용되는 신규 화합물, 및 이를 유효성분으로 포함하는 암, 염증성 장애 또는 자가면역 질환의 예방 또는 치료용 약학 조성물 | |
| CN117396468A (zh) | 作为ron抑制剂的新型吡啶衍生化合物 |