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- Withdrawn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 (Direct) | 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 (Direct) |
| EP (1) | EP2197876A1 (Direct) |
| JP (1) | JP2010538003A (Direct) |
| WO (1) | WO2009032667A1 (Direct) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8865732B2 (en) | 2008-03-21 | 2014-10-21 | Novartis Ag | Heterocyclic compounds and uses thereof |
| AU2012203026B2 (en) * | 2008-03-21 | 2014-06-12 | Novartis Ag | Novel 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 |
| WO2013169864A2 (en) | 2012-05-08 | 2013-11-14 | Lycera Corporation | TETRAHYDRO[1,8]NAPHTHYRIDINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORƴ AND THE TREATMENT OF DISEASE |
| CA2871514C (en) | 2012-05-08 | 2020-08-25 | Merck Sharp & Dohme Corp. | Tetrahydronaphthyridine and related bicyclic compounds for inhibition of ror.gamma.activity and the treatment of disease |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| ES2786925T3 (es) | 2013-03-14 | 2020-10-14 | Brigham & Womens Hospital Inc | Composiciones y procedimientos para la expansión y el cultivo de células madre epiteliales |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| CA2927182A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | Quinolinyl modulators of ror.gamma.t |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| 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 |
| 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 |
| WO2015095788A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | 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 |
| EP3110429A4 (en) | 2014-02-27 | 2018-02-21 | Lycera Corporation | Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma & related therapeutic methods |
| AU2015256190B2 (en) | 2014-05-05 | 2019-08-15 | Lycera Corporation | Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| WO2015171558A2 (en) | 2014-05-05 | 2015-11-12 | Lycera Corporation | BENZENESULFONAMIDO AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATEMENT 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 |
| KR20230019500A (ko) | 2014-09-03 | 2023-02-08 | 더 브리검 앤드 우먼즈 하스피털, 인크. | 청력 손실의 치료를 위해 내이 털세포를 생성하기 위한 조성물, 시스템, 및 방법 |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| JP2018510135A (ja) | 2015-02-11 | 2018-04-12 | 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阻害剤としての置換ピラゾール化合物及びその使用 |
| 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 |
| EP3307738B1 (en) | 2015-06-11 | 2022-04-20 | The Regents of the University of Michigan | Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease |
| JP6980534B2 (ja) | 2015-06-25 | 2021-12-15 | ザ チルドレンズ メディカル センター コーポレーション | 造血幹細胞の増大、富化、および維持に関する方法および組成物 |
| PT3365346T (pt) | 2015-10-23 | 2020-03-05 | Esteve Pharmaceuticals Sa | Compostos de oxa-diazaspiro tendo atividade contra a dor |
| CA3002850A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as rorgammat inhibitors and uses thereof |
| WO2017075178A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| CA3002853A1 (en) | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| EP3377500B1 (en) | 2015-11-16 | 2022-10-19 | Esteve Pharmaceuticals, S.A. | Oxadiazaspiro compounds for the treatment of drug abuse and addiction |
| EP3400286A1 (en) | 2016-01-08 | 2018-11-14 | 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 |
| 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 |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| JP7080179B2 (ja) | 2016-03-15 | 2022-06-03 | ザ チルドレンズ メディカル センター コーポレーション | 造血幹細胞の増大に関する方法および組成物 |
| CN109715163B (zh) | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
| JP7109446B2 (ja) | 2016-12-30 | 2022-07-29 | 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 | 幹細胞／前駆支持細胞の自己複製を誘導するための１ｈ－ピロール－２，５－ジオン化合物およびその使用方法 |
| JP7309614B2 (ja) | 2017-05-02 | 2023-07-18 | ノバルティス アーゲー | 組み合わせ療法 |
| BR112020007359A2 (pt) | 2017-10-17 | 2020-09-29 | Esteve Pharmaceuticals, S.A. | sais de (r)-9-(2,5-difluorofenetil)-4-etil-2-metil-1-oxa-4,9-diazaespiro[5.5]undecan-3-ona |
| CN112135613A (zh) | 2018-03-20 | 2020-12-25 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| WO2019236766A1 (en) | 2018-06-06 | 2019-12-12 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
| CA3109647A1 (en) | 2018-08-17 | 2020-02-20 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by upregulating jag-1 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| CN113508111A (zh) | 2018-12-31 | 2021-10-15 | 西奈山伊坎医学院 | 激酶抑制剂化合物和组合物及使用方法 |
| CN113795490A (zh) | 2019-05-13 | 2021-12-14 | 诺华股份有限公司 | N-(3-(2-(2-羟基乙氧基)-6-吗啉代吡啶-4-基)-4-甲基苯基)-2(三氟甲基)异烟酰胺的新结晶形式作为Raf抑制剂治疗癌症 |
| US20250368635A1 (en) * | 2022-11-15 | 2025-12-04 | 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 |
| US20070179125A1 (en) * | 2005-11-16 | 2007-08-02 | Damien Fraysse | Aminopyrimidines useful as kinase inhibitors |
-
2008
- 2008-08-27 EP EP08829568A patent/EP2197876A1/en not_active Withdrawn
- 2008-08-27 JP JP2010523102A patent/JP2010538003A/ja not_active Withdrawn
- 2008-08-27 US US12/674,016 patent/US20110190280A1/en not_active Abandoned
- 2008-08-27 WO PCT/US2008/074389 patent/WO2009032667A1/en not_active Ceased
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