JP2017501200A5 - - Google Patents
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- JP2017501200A5 JP2017501200A5 JP2016544111A JP2016544111A JP2017501200A5 JP 2017501200 A5 JP2017501200 A5 JP 2017501200A5 JP 2016544111 A JP2016544111 A JP 2016544111A JP 2016544111 A JP2016544111 A JP 2016544111A JP 2017501200 A5 JP2017501200 A5 JP 2017501200A5
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- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- pharmaceutical composition
- disease
- treating
- 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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- 206010028980 Neoplasm Diseases 0.000 claims 16
- 201000011510 cancer Diseases 0.000 claims 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims 7
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 7
- 239000002955 immunomodulating agent Substances 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- 229940000425 combination drug Drugs 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 4
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 230000001419 dependent effect Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical group N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 102000009618 Transforming Growth Factors Human genes 0.000 claims 1
- 108010009583 Transforming Growth Factors Proteins 0.000 claims 1
- 238000009175 antibody therapy Methods 0.000 claims 1
- 238000002619 cancer immunotherapy Methods 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- -1 3-dihydroindolinyl Chemical group 0.000 description 15
- 125000000623 heterocyclic group Chemical group 0.000 description 8
- 125000001072 heteroaryl group Chemical group 0.000 description 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 5
- 125000002619 bicyclic group Chemical group 0.000 description 4
- 125000004122 cyclic group Chemical group 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
- 125000003118 aryl group Chemical group 0.000 description 3
- 125000004429 atom Chemical group 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 239000002131 composite material Substances 0.000 description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 125000006413 ring segment Chemical group 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 239000011593 sulfur Substances 0.000 description 2
- 125000001544 thienyl group Chemical group 0.000 description 2
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical compound N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 description 1
- 125000001698 2H-pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 125000002393 azetidinyl group Chemical group 0.000 description 1
- 125000004069 aziridinyl group Chemical group 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000005874 benzothiadiazolyl group Chemical group 0.000 description 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 1
- 125000002636 imidazolinyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 description 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 1
- 125000001041 indolyl group Chemical group 0.000 description 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 description 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 1
- 125000005956 isoquinolyl group Chemical group 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000003566 oxetanyl group Chemical group 0.000 description 1
- 125000000466 oxiranyl group Chemical group 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000004525 thiadiazinyl group Chemical group S1NN=C(C=C1)* 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000005307 thiatriazolyl group Chemical group S1N=NN=C1* 0.000 description 1
- 125000004305 thiazinyl group Chemical group S1NC(=CC=C1)* 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN6/DEL/2014 | 2014-01-01 | ||
| IN6DE2014 | 2014-01-01 | ||
| PCT/US2014/072922 WO2015103355A1 (en) | 2014-01-01 | 2014-12-31 | Compounds and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019000208A Division JP2019048899A (ja) | 2014-01-01 | 2019-01-04 | 化合物及び使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017501200A JP2017501200A (ja) | 2017-01-12 |
| JP2017501200A5 true JP2017501200A5 (https=) | 2019-02-14 |
| JP6474166B2 JP6474166B2 (ja) | 2019-02-27 |
Family
ID=52293317
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016544111A Expired - Fee Related JP6474166B2 (ja) | 2014-01-01 | 2014-12-31 | 化合物及び使用方法 |
| JP2019000208A Pending JP2019048899A (ja) | 2014-01-01 | 2019-01-04 | 化合物及び使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019000208A Pending JP2019048899A (ja) | 2014-01-01 | 2019-01-04 | 化合物及び使用方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10030004B2 (https=) |
| EP (1) | EP3089971B1 (https=) |
| JP (2) | JP6474166B2 (https=) |
| CN (2) | CN106132950B (https=) |
| AU (2) | AU2014373773C1 (https=) |
| CA (1) | CA2935392C (https=) |
| CY (1) | CY1123290T1 (https=) |
| DK (1) | DK3089971T3 (https=) |
| ES (1) | ES2813875T3 (https=) |
| HR (1) | HRP20201384T1 (https=) |
| HU (1) | HUE050761T2 (https=) |
| LT (1) | LT3089971T (https=) |
| PL (1) | PL3089971T3 (https=) |
| PT (1) | PT3089971T (https=) |
| RS (1) | RS60718B1 (https=) |
| SI (1) | SI3089971T1 (https=) |
| WO (1) | WO2015103355A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
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| PL3089971T3 (pl) | 2014-01-01 | 2021-01-25 | Medivation Technologies Llc | Związki i sposoby ich zastosowania |
| JP6952747B2 (ja) | 2018-09-18 | 2021-10-20 | ファイザー・インク | がん処置のためのＴＧＦβ阻害剤およびＣＤＫ阻害剤の組合せ |
| US12427147B2 (en) | 2018-10-31 | 2025-09-30 | Senju Pharmaceutical Co., Ltd. | Retinal ganglion cell death inhibitor |
| MA54526A (fr) * | 2018-12-20 | 2022-03-30 | Pfizer | NOUVELLES FORMES POLYMORPHES D'UN INHIBITEUR DE TGFBeta |
| AU2019417418B2 (en) * | 2018-12-27 | 2025-02-27 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as ΤGFβR1 (Alk5) inhibitors for the treatment of cancer |
| EP4041399A1 (en) | 2019-10-02 | 2022-08-17 | Tolremo Therapeutics AG | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer |
| CN111116565B (zh) * | 2020-04-01 | 2020-07-14 | 中科利健制药(广州)有限公司 | 2-芳基-4-（4-吡唑氧基）吡啶类化合物、其制备方法、药物组合物与应用 |
| KR20230028798A (ko) | 2020-06-25 | 2023-03-02 | 톨레모 테라퓨틱스 아게 | 암 치료를 위한 CBP/p300 브로모도메인 억제제 및 KRAS 억제제의 조합물 |
| WO2021260110A1 (en) * | 2020-06-25 | 2021-12-30 | Tolremo Therapeutics Ag | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment, amelioration or prevention of fibrotic disease |
| EP4182308B1 (en) * | 2020-07-15 | 2024-09-04 | Chiesi Farmaceutici S.p.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| CN114369083B (zh) * | 2020-10-15 | 2026-02-27 | 四川科伦博泰生物医药股份有限公司 | 杂环类化合物、包含其的药物组合物、其制备方法及其用途 |
| EP4251625A4 (en) * | 2020-11-24 | 2024-10-09 | Aligos Therapeutics, Inc. | Tricyclic compounds |
| WO2022130206A1 (en) | 2020-12-16 | 2022-06-23 | Pfizer Inc. | TGFβr1 INHIBITOR COMBINATION THERAPIES |
| CN112843058A (zh) * | 2021-01-27 | 2021-05-28 | 复旦大学附属华山医院 | 烟酰胺类化合物在制备治疗抗脊索肿瘤药物中的应用 |
| IL307402A (en) | 2021-04-07 | 2023-12-01 | Tolremo Therapeutics Ag | The tercyclic derivatives, pharmaceutical compounds and their use in the treatment or amelioration of cancer |
| WO2022229846A1 (en) | 2021-04-29 | 2022-11-03 | Pfizer Inc. | Treatment of cancer using a transforming growth factor beta receptor type 1 inhibitor |
| WO2023054712A1 (ja) | 2021-09-30 | 2023-04-06 | ペプチドリーム株式会社 | ペプチド |
| CN115353326A (zh) * | 2022-07-27 | 2022-11-18 | 魏玉芝 | 一种反光防车印沥青及其制备方法 |
| CN116606244A (zh) * | 2023-05-26 | 2023-08-18 | 康化（上海）新药研发有限公司 | 一种6-溴-5-甲氧基吡啶-3-胺的合成方法 |
| CN117865965B (zh) * | 2024-01-08 | 2024-06-28 | 贵州省天然产物研究中心 | 吡咯并嘧啶-4-胺和吡唑并嘧啶-4-胺衍生物及制备方法和应用 |
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