JP2010538003A5 - - Google Patents
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- Publication number
- 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.)
- Withdrawn
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP2197876A1 (https=) |
| JP (1) | JP2010538003A (https=) |
| WO (1) | WO2009032667A1 (https=) |
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 |
| CA2816753A1 (en) | 2010-11-08 | 2012-05-18 | Lycera Corporation | N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of rory activity and the treatment of diseases |
| JP6242868B2 (ja) | 2012-05-08 | 2017-12-06 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ［１，８］ナフチリジンスルホンアミドおよび関連化合物 |
| AU2013259737A1 (en) | 2012-05-08 | 2014-10-02 | Lycera Corporation | Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease |
| LT2970890T (lt) | 2013-03-14 | 2020-07-10 | The Brigham And Women`S Hospital, Inc. | Kompozicijos ir būdai, skirti epitelinių kamieninių ląstelių padauginimui ir kultivavimui |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| ES2742843T3 (es) | 2013-10-15 | 2020-02-17 | Janssen Pharmaceutica Nv | Moduladores de quinolinilo de ROR(gamma)t |
| 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 |
| WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | 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 |
| US9783511B2 (en) | 2013-12-20 | 2017-10-10 | Lycera Corporation | Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease |
| EP2980088A1 (en) | 2014-07-28 | 2016-02-03 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| JP2017507950A (ja) | 2014-02-27 | 2017-03-23 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | レチノイン酸受容体関連オーファン受容体ガンマのアゴニストを使用する養子細胞療法及び関連治療方法 |
| US9896441B2 (en) | 2014-05-05 | 2018-02-20 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease |
| JP6523337B2 (ja) | 2014-05-05 | 2019-05-29 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγのアゴニストとしての使用及び疾患治療のためのベンゼンスルホンアミド及び関連化合物 |
| 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 |
| 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 |
| WO2016037016A1 (en) | 2014-09-03 | 2016-03-10 | The Brigham And Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| 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 |
| JP2018515491A (ja) | 2015-05-05 | 2018-06-14 | リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ | ＲＯＲγの作動薬及び疾患の療法として使用するジヒドロ−２Ｈ−ベンゾ［ｂ］［１，４］オキサジンスルホンアミド及び関連化合物 |
| KR20180025894A (ko) | 2015-06-11 | 2018-03-09 | 라이세라 코퍼레이션 | Rory의 작용제로서 사용하기 위한 아릴 디히드로-2h-벤조[b][1,4]옥사진 술폰아미드 및 관련 화합물 및 질환의 치료 |
| US10669528B2 (en) | 2015-06-25 | 2020-06-02 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| ME03636B (me) | 2015-10-23 | 2020-07-20 | Esteve Pharmaceuticals Sa | Oksa-diazaspiro jedinjenja која imaju aktivnost protiv bola |
| AU2016344118A1 (en) | 2015-10-27 | 2018-05-10 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| RU2018117503A (ru) | 2015-10-27 | 2019-11-28 | Мерк Шарп И Доум Корп. | ЗАМЕЩЕННЫЕ ИНДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ RORγТ И ИХ ПРИМЕНЕНИЕ |
| WO2017075178A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| AR106697A1 (es) | 2015-11-16 | 2018-02-07 | Esteve Labor Dr | Compuestos oxadiazoespíricos para el tratamiento del abuso y la adicción a las drogas |
| CN108779437A (zh) | 2016-01-08 | 2018-11-09 | 麻省理工学院 | 分化的肠内分泌细胞和胰岛素产生细胞的制备 |
| 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 |
| WO2017161001A1 (en) | 2016-03-15 | 2017-09-21 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| AU2017329090B9 (en) | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
| US11066419B2 (en) | 2016-12-30 | 2021-07-20 | Frequency Therapeutics, Inc. | 1H-pyrrole-2,5-dione compounds and methods of using same |
| ES2952265T3 (es) | 2017-05-02 | 2023-10-30 | Novartis Ag | Terapia combinada que comprende un inhibidor de Raf y trametinib |
| MY200894A (en) | 2017-10-17 | 2024-01-22 | Esteve Pharmaceuticals Sa | Salts of (r)-9-(2,5-difluorophenethyl)-4-ethyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one |
| JP2021518413A (ja) | 2018-03-20 | 2021-08-02 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
| 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 |
| CN113195707A (zh) | 2018-08-17 | 2021-07-30 | 频率治疗公司 | 用于通过上调jag-1来生成毛细胞的组合物和方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| WO2020142485A1 (en) | 2018-12-31 | 2020-07-09 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| ES3025633T3 (en) | 2019-05-13 | 2025-06-09 | Novartis Ag | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
| AU2023381004A1 (en) * | 2022-11-15 | 2025-04-10 | Voronoi, Inc. | Heteroaryl derivative compound, and uses thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0411791D0 (en) * | 2004-05-26 | 2004-06-30 | Cyclacel Ltd | Compounds |
| CA2629781A1 (en) * | 2005-11-16 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
-
2008
- 2008-08-27 US US12/674,016 patent/US20110190280A1/en not_active Abandoned
- 2008-08-27 JP JP2010523102A patent/JP2010538003A/ja not_active Withdrawn
- 2008-08-27 WO PCT/US2008/074389 patent/WO2009032667A1/en not_active Ceased
- 2008-08-27 EP EP08829568A patent/EP2197876A1/en not_active Withdrawn
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