JP2010538003A5 - - Google Patents
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- JP2010538003A5 JP2010538003A5 JP2010523102A JP2010523102A JP2010538003A5 JP 2010538003 A5 JP2010538003 A5 JP 2010538003A5 JP 2010523102 A JP2010523102 A JP 2010523102A JP 2010523102 A JP2010523102 A JP 2010523102A JP 2010538003 A5 JP2010538003 A5 JP 2010538003A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- compound
- salt
- tumors
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 24
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 16
- 206010028980 Neoplasm Diseases 0.000 claims 12
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 11
- 206010009944 Colon cancer Diseases 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 210000003169 central nervous system Anatomy 0.000 claims 8
- 208000005017 glioblastoma Diseases 0.000 claims 8
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 208000032839 leukemia Diseases 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 208000017604 Hodgkin disease Diseases 0.000 claims 6
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 6
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 5
- 208000026310 Breast neoplasm Diseases 0.000 claims 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 5
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 5
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 5
- 201000001441 melanoma Diseases 0.000 claims 5
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 5
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 4
- 206010003571 Astrocytoma Diseases 0.000 claims 4
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 4
- 206010008342 Cervix carcinoma Diseases 0.000 claims 4
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 4
- 206010014733 Endometrial cancer Diseases 0.000 claims 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 4
- 206010014967 Ependymoma Diseases 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 4
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims 4
- 206010041067 Small cell lung cancer Diseases 0.000 claims 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 4
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 4
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 4
- 201000010881 cervical cancer Diseases 0.000 claims 4
- 208000029742 colonic neoplasm Diseases 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 201000003911 head and neck carcinoma Diseases 0.000 claims 4
- 201000005202 lung cancer Diseases 0.000 claims 4
- 208000020816 lung neoplasm Diseases 0.000 claims 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 4
- 201000002528 pancreatic cancer Diseases 0.000 claims 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 4
- 201000000849 skin cancer Diseases 0.000 claims 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 4
- 201000011549 stomach cancer Diseases 0.000 claims 4
- 201000002510 thyroid cancer Diseases 0.000 claims 4
- 208000029862 Barrett adenocarcinoma Diseases 0.000 claims 3
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 201000007455 central nervous system cancer Diseases 0.000 claims 3
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims 2
- 208000036566 Erythroleukaemia Diseases 0.000 claims 2
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 208000007913 Pituitary Neoplasms 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
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000021841 acute erythroid leukemia Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 125000000066 S-methyl group Chemical group [H]C([H])([H])S* 0.000 claims 1
- 208000034254 Squamous cell carcinoma of the cervix uteri Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 201000006612 cervical squamous cell carcinoma Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- AEOCXXJPGCBFJA-UHFFFAOYSA-N ethionamide Chemical compound CCC1=CC(C(N)=S)=CC=N1 AEOCXXJPGCBFJA-UHFFFAOYSA-N 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 210000003593 megakaryocyte Anatomy 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- -1 optionally Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US96868707P | 2007-08-29 | 2007-08-29 | |
| PCT/US2008/074389 WO2009032667A1 (en) | 2007-08-29 | 2008-08-27 | Thiazole and oxazole kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010538003A JP2010538003A (ja) | 2010-12-09 |
| JP2010538003A5 true JP2010538003A5 (cg-RX-API-DMAC7.html) | 2011-09-29 |
Family
ID=40029314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010523102A Withdrawn JP2010538003A (ja) | 2007-08-29 | 2008-08-27 | チアゾールおよびオキサゾールキナーゼ阻害薬 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20110190280A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2197876A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2010538003A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009032667A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012203026B2 (en) * | 2008-03-21 | 2014-06-12 | Novartis Ag | Novel heterocyclic compounds and uses thereof |
| US8865732B2 (en) | 2008-03-21 | 2014-10-21 | Novartis Ag | Heterocyclic compounds and uses thereof |
| US9512111B2 (en) | 2010-11-08 | 2016-12-06 | Lycera Corporation | N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease |
| BR112014028017A2 (pt) | 2012-05-08 | 2017-06-27 | Lycera Corp | composto, composição farmacêutica, método para tratar um distúrbio, método para reduzir a quantidade il-17 em um indivíduo e método para inibir a atividade de ror |
| US9394315B2 (en) | 2012-05-08 | 2016-07-19 | Lycera Corporation | Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| BR112015023261A2 (pt) | 2013-03-14 | 2017-07-18 | Massachusetts Inst Technology | composições e métodos para expansão e cultura de células-tronco epiteliais |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| WO2015057626A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | QUINOLINYL MODULATORS OF RORyT |
| WO2015095792A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease |
| US9809561B2 (en) | 2013-12-20 | 2017-11-07 | Merck Sharp & Dohme Corp. | Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease |
| US9663502B2 (en) | 2013-12-20 | 2017-05-30 | Lycera Corporation | 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease |
| EP2980088A1 (en) | 2014-07-28 | 2016-02-03 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| AU2015222917A1 (en) | 2014-02-27 | 2016-09-15 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods |
| EP3209641A4 (en) | 2014-05-05 | 2018-06-06 | Lycera Corporation | Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease |
| EP3140291A4 (en) | 2014-05-05 | 2018-01-10 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| TW201615643A (zh) | 2014-06-02 | 2016-05-01 | 伊史帝夫博士實驗室股份有限公司 | 具有多重模式抗疼痛活性之１－氧雜－４，９－二氮雜螺十一烷化合物之烷基與芳基衍生物 |
| TWI685497B (zh) | 2014-06-02 | 2020-02-21 | 西班牙商伊史帝夫製藥公司 | 具有多重模式抗疼痛活性的１-氧雜-４,９-二氮雜螺十一烷化合物之烷基衍生物 |
| JP6773645B2 (ja) | 2014-09-03 | 2020-10-21 | ザ ブリガム アンド ウィミンズ ホスピタル，インコーポレイテッド | 聴覚障害の治療のための内耳毛細胞を生成するための組成物、システムおよび方法 |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| EP3256450B1 (en) | 2015-02-11 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof |
| CA2982847A1 (en) | 2015-05-05 | 2016-11-10 | Lycera Corporation | Dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease |
| US10611740B2 (en) | 2015-06-11 | 2020-04-07 | Lycera Corporation | Aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| EP3313420B1 (en) | 2015-06-25 | 2024-03-13 | The Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| CN108349998B (zh) | 2015-10-23 | 2021-10-29 | 埃斯蒂文制药股份有限公司 | 具有抗疼痛活性的氧杂-二氮杂螺环化合物 |
| JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ＲＯＲγＴ阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
| EP3368539B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as ror gamma t inhibitors and uses thereof |
| JP2018531957A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ＲＯＲγＴ阻害薬としての置換二環式ピラゾール化合物及びその使用 |
| US10927128B2 (en) | 2015-11-16 | 2021-02-23 | Esteve Pharmaceuticals. S.A. | Oxadiazaspiro compounds for the treatment of drug abuse and addiction |
| WO2017120543A1 (en) | 2016-01-08 | 2017-07-13 | Massachusetts Institute Of Technology | Production of differentiated enteroendocrine cells and insulin producing cells |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| AU2017235461B2 (en) | 2016-03-15 | 2023-02-23 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| EP3515446B1 (en) | 2016-09-19 | 2023-12-20 | Novartis AG | Therapeutic combinations comprising a raf inhibitor and a erk inhibitor |
| AU2017386417B2 (en) | 2016-12-30 | 2022-07-14 | Frequency Therapeutics, Inc. | 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| DK3618875T3 (da) | 2017-05-02 | 2023-07-10 | Novartis Ag | Kombinationsterapi omfattende en raf-inhibitor og trametinib |
| US11236110B2 (en) | 2017-10-17 | 2022-02-01 | Esteve Pharmaceuticals, S.A. | Salts of (R)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one |
| AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| US20210254006A1 (en) | 2018-06-06 | 2021-08-19 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| JP2021533788A (ja) | 2018-08-17 | 2021-12-09 | フリークエンシー セラピューティクス インコーポレイテッド | Ｊａｇ−１を上方制御することにより有毛細胞を生成するための組成物及び方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| EP3906233B1 (en) | 2018-12-31 | 2024-01-31 | Icahn School of Medicine at Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| KR102881316B1 (ko) | 2019-05-13 | 2025-11-05 | 노파르티스 아게 | 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태 |
| CN120187724A (zh) * | 2022-11-15 | 2025-06-20 | 株式会社沃若诺伊 | 杂芳基衍生物化合物、及其用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0411791D0 (en) * | 2004-05-26 | 2004-06-30 | Cyclacel Ltd | Compounds |
| CN101360740A (zh) * | 2005-11-16 | 2009-02-04 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶 |
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2008
- 2008-08-27 WO PCT/US2008/074389 patent/WO2009032667A1/en not_active Ceased
- 2008-08-27 EP EP08829568A patent/EP2197876A1/en not_active Withdrawn
- 2008-08-27 US US12/674,016 patent/US20110190280A1/en not_active Abandoned
- 2008-08-27 JP JP2010523102A patent/JP2010538003A/ja not_active Withdrawn