JPWO2020055758A5 - - Google Patents
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- JPWO2020055758A5 JPWO2020055758A5 JP2021513334A JP2021513334A JPWO2020055758A5 JP WO2020055758 A5 JPWO2020055758 A5 JP WO2020055758A5 JP 2021513334 A JP2021513334 A JP 2021513334A JP 2021513334 A JP2021513334 A JP 2021513334A JP WO2020055758 A5 JPWO2020055758 A5 JP WO2020055758A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- inhibitor
- alkyl
- kras
- optionally substituted
- 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
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- 239000008194 pharmaceutical composition Substances 0.000 claims 78
- 230000002401 inhibitory effect Effects 0.000 claims 48
- 239000003112 inhibitor Substances 0.000 claims 45
- 102200006538 KRAS G12C Human genes 0.000 claims 30
- -1 dialkylaminylalkyl Chemical group 0.000 claims 29
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 101700008359 CDK4 Proteins 0.000 claims 21
- 125000001188 haloalkyl group Chemical group 0.000 claims 21
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000004404 heteroalkyl group Chemical group 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 20
- 201000011510 cancer Diseases 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 14
- 239000011780 sodium chloride Substances 0.000 claims 14
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 210000004027 cells Anatomy 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 7
- 208000009956 Adenocarcinoma Diseases 0.000 claims 7
- 206010025323 Lymphomas Diseases 0.000 claims 7
- 206010025310 Other lymphomas Diseases 0.000 claims 7
- 206010039491 Sarcoma Diseases 0.000 claims 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000004043 oxo group Chemical group O=* 0.000 claims 7
- 201000009030 carcinoma Diseases 0.000 claims 6
- XEEYBQQBJWHFJM-UHFFFAOYSA-N iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 6
- 206010041823 Squamous cell carcinoma Diseases 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 206010024612 Lipoma Diseases 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000005418 aryl aryl group Chemical group 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 230000035945 sensitivity Effects 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 3
- 206010016629 Fibroma Diseases 0.000 claims 3
- 206010018338 Glioma Diseases 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atoms Chemical group C* 0.000 claims 3
- 201000008808 fibrosarcoma Diseases 0.000 claims 3
- 201000011066 hemangioma Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 2
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims 2
- 229950001573 Abemaciclib Drugs 0.000 claims 2
- 208000002458 Carcinoid Tumor Diseases 0.000 claims 2
- 206010007275 Carcinoid tumour Diseases 0.000 claims 2
- 208000002927 Hamartoma Diseases 0.000 claims 2
- 206010024190 Leiomyosarcomas Diseases 0.000 claims 2
- 206010025650 Malignant melanoma Diseases 0.000 claims 2
- 206010027191 Meningioma Diseases 0.000 claims 2
- UZWDCWONPYILKI-UHFFFAOYSA-N N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical group C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- AHJRHEGDXFFMBM-UHFFFAOYSA-N Palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims 2
- 229960004390 Palbociclib Drugs 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 229950003687 Ribociclib Drugs 0.000 claims 2
- 206010043276 Teratoma Diseases 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000002489 hematologic Effects 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 201000010260 leiomyoma Diseases 0.000 claims 2
- 231100000682 maximum tolerated dose Toxicity 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 201000009251 multiple myeloma Diseases 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 201000004404 neurofibroma Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 239000000546 pharmaceutic aid Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- 230000004083 survival Effects 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 230000004614 tumor growth Effects 0.000 claims 2
- 125000006699 (C1-C3) hydroxyalkyl group Chemical group 0.000 claims 1
- KEFBAMRFXYKOBI-UHFFFAOYSA-N 1,4$l^{2}-thiazinane 1,1-dioxide Chemical compound O=S1(=O)CC[N]CC1 KEFBAMRFXYKOBI-UHFFFAOYSA-N 0.000 claims 1
- 125000005962 1,4-oxazepanyl group Chemical group 0.000 claims 1
- PDGKHKMBHVFCMG-UHFFFAOYSA-N 2-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[7,8-dihydropyrazino[5,6]pyrrolo[1,2-d]pyrimidine-9,1'-cyclohexane]-6-one Chemical compound C1CN(C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C2N3C4(CCCCC4)CNC2=O)C3=N1 PDGKHKMBHVFCMG-UHFFFAOYSA-N 0.000 claims 1
- 241000321096 Adenoides Species 0.000 claims 1
- 210000002534 Adenoids Anatomy 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 210000004100 Adrenal Glands Anatomy 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 210000000013 Bile Ducts Anatomy 0.000 claims 1
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- 206010073106 Bone giant cell tumour malignant Diseases 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 208000003362 Bronchogenic Carcinoma Diseases 0.000 claims 1
- 208000009458 Carcinoma in Situ Diseases 0.000 claims 1
- 208000006990 Cholangiocarcinoma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims 1
- 210000001072 Colon Anatomy 0.000 claims 1
- 206010048832 Colon adenoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000007033 Dysgerminoma Diseases 0.000 claims 1
- 206010058314 Dysplasia Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 210000003238 Esophagus Anatomy 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 208000005917 Exostosis Diseases 0.000 claims 1
- 208000007659 Fibroadenoma Diseases 0.000 claims 1
- 206010053717 Fibrous histiocytoma Diseases 0.000 claims 1
- 210000001035 Gastrointestinal Tract Anatomy 0.000 claims 1
- 208000000527 Germinoma Diseases 0.000 claims 1
- 208000007569 Giant Cell Tumors Diseases 0.000 claims 1
- 206010018404 Glucagonoma Diseases 0.000 claims 1
- 206010018691 Granuloma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 206010020243 Hodgkin's disease Diseases 0.000 claims 1
- 206010022498 Insulinoma Diseases 0.000 claims 1
- 208000007766 Kaposi Sarcoma Diseases 0.000 claims 1
- 210000001117 Keloid Anatomy 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 208000000429 Leukemia, Lymphocytic, Chronic, B-Cell Diseases 0.000 claims 1
- 206010024627 Liposarcoma Diseases 0.000 claims 1
- 210000004072 Lung Anatomy 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 210000002418 Meninges Anatomy 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000010492 Mucinous Cystadenocarcinoma Diseases 0.000 claims 1
- 206010028549 Myeloid leukaemia Diseases 0.000 claims 1
- 206010028576 Myeloproliferative disease Diseases 0.000 claims 1
- 208000009091 Myxoma Diseases 0.000 claims 1
- 208000007538 Neurilemmoma Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000007256 Nevus Diseases 0.000 claims 1
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims 1
- 208000002154 Non-Small-Cell Lung Carcinoma Diseases 0.000 claims 1
- 108009000071 Non-small cell lung cancer Proteins 0.000 claims 1
- 206010031149 Osteitis Diseases 0.000 claims 1
- 208000000035 Osteochondroma Diseases 0.000 claims 1
- 208000008798 Osteoma Diseases 0.000 claims 1
- 210000000496 Pancreas Anatomy 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 210000002307 Prostate Anatomy 0.000 claims 1
- 208000005678 Rhabdomyoma Diseases 0.000 claims 1
- 206010039667 Schwannoma Diseases 0.000 claims 1
- 208000004548 Serous Cystadenocarcinoma Diseases 0.000 claims 1
- 208000000097 Sertoli-Leydig Cell Tumor Diseases 0.000 claims 1
- 210000002784 Stomach Anatomy 0.000 claims 1
- 210000002536 Stromal Cells Anatomy 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N THP Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 208000001608 Teratocarcinoma Diseases 0.000 claims 1
- 210000001550 Testis Anatomy 0.000 claims 1
- 206010044412 Transitional cell carcinoma Diseases 0.000 claims 1
- 210000003708 Urethra Anatomy 0.000 claims 1
- 210000003932 Urinary Bladder Anatomy 0.000 claims 1
- 210000004291 Uterus Anatomy 0.000 claims 1
- 210000001215 Vagina Anatomy 0.000 claims 1
- 208000009540 Villous Adenoma Diseases 0.000 claims 1
- 208000009311 Vipoma Diseases 0.000 claims 1
- 240000006365 Vitis vinifera Species 0.000 claims 1
- 235000014787 Vitis vinifera Nutrition 0.000 claims 1
- 210000003905 Vulva Anatomy 0.000 claims 1
- 206010048214 Xanthoma Diseases 0.000 claims 1
- 230000001154 acute Effects 0.000 claims 1
- 201000005510 acute lymphocytic leukemia Diseases 0.000 claims 1
- 201000003076 angiosarcoma Diseases 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000008975 bone inflammation disease Diseases 0.000 claims 1
- 201000003149 breast fibroadenoma Diseases 0.000 claims 1
- 201000002143 bronchus adenoma Diseases 0.000 claims 1
- 201000005217 chondroblastoma Diseases 0.000 claims 1
- 201000005262 chondroma Diseases 0.000 claims 1
- 201000009047 chordoma Diseases 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 201000010305 cutaneous fibrous histiocytoma Diseases 0.000 claims 1
- 125000002944 cyanoaryl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000013601 eggs Nutrition 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 201000009051 embryonal carcinoma Diseases 0.000 claims 1
- 201000009409 embryonal rhabdomyosarcoma Diseases 0.000 claims 1
- 201000003914 endometrial carcinoma Diseases 0.000 claims 1
- 201000010934 exostosis Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 201000000052 gastrinoma Diseases 0.000 claims 1
- 201000003115 germ cell cancer Diseases 0.000 claims 1
- 201000010915 glioblastoma multiforme Diseases 0.000 claims 1
- 235000009754 grape Nutrition 0.000 claims 1
- 235000012333 grape Nutrition 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 201000010985 invasive ductal carcinoma Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000004593 malignant giant cell tumor Diseases 0.000 claims 1
- 201000000289 malignant teratoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 201000003793 myelodysplastic syndrome Diseases 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 125000004929 pyrrolidonyl group Chemical group N1(C(CCC1)=O)* 0.000 claims 1
- 201000000582 retinoblastoma Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 201000010208 seminoma Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229950007127 trilaciclib Drugs 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862729205P | 2018-09-10 | 2018-09-10 | |
| US62/729,205 | 2018-09-10 | ||
| PCT/US2019/050233 WO2020055758A1 (en) | 2018-09-10 | 2019-09-09 | Combination therapies |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022500388A JP2022500388A (ja) | 2022-01-04 |
| JPWO2020055758A5 true JPWO2020055758A5 (ru) | 2022-09-16 |
Family
ID=69778101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021513334A Pending JP2022500388A (ja) | 2018-09-10 | 2019-09-09 | 組み合わせ療法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20220096482A1 (ru) |
| EP (1) | EP3849537A4 (ru) |
| JP (1) | JP2022500388A (ru) |
| AU (1) | AU2019340436A1 (ru) |
| CA (1) | CA3111977A1 (ru) |
| WO (1) | WO2020055758A1 (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3849538A4 (en) * | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849536A4 (en) * | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2021043322A1 (zh) * | 2019-09-06 | 2021-03-11 | 正大天晴药业集团南京顺欣制药有限公司 | 氮杂环庚烷并嘧啶类衍生物及其医药用途 |
| CN114555586B (zh) * | 2019-10-10 | 2023-06-23 | 信达生物制药(苏州)有限公司 | Krasg12c蛋白抑制剂及其制备方法和用途 |
| WO2021219072A1 (zh) * | 2020-04-30 | 2021-11-04 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| US20230233558A1 (en) * | 2020-06-25 | 2023-07-27 | Tolremo Therapeutics Ag | Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4205165B2 (ja) | 1996-05-08 | 2009-01-07 | サイクラセル リミテッド | Ｃｄｋ４活性の阻害のための方法と手段 |
| US7915301B2 (en) | 2002-07-08 | 2011-03-29 | Piramal Life Science Limited | Inhibitors of cyclin dependent kinases and their use |
| CN1956982A (zh) | 2004-05-21 | 2007-05-02 | 万有制药株式会社 | 具有氨基噻唑骨架的Cdk4、6选择性抑制剂 |
| ATE478852T1 (de) | 2005-09-09 | 2010-09-15 | Schering Corp | Neue 4-cyano-, 4-amino-, und 4- aminomethylderivative von pyrazoloä1,5- aüpyridinen, pyrazoloä1,5-cüpyrimidinen und 2h- indazolverbindungen und 5-cyano-, 5-amino- und 5- aminomethylderivative von imidazoä1,2-aüpyridinen,und imidazoä1,5-aüpyrazinverbindungen als inhibitoren der cyclinabhänggen kinase |
| WO2009034411A1 (en) | 2007-09-12 | 2009-03-19 | Centre National De La Recherche Scientifique | Perharidines as cdk inhibitors |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| EP2179991A1 (de) | 2008-10-21 | 2010-04-28 | Bayer Schering Pharma Aktiengesellschaft | Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| EP2179992A1 (de) | 2008-10-21 | 2010-04-28 | Bayer Schering Pharma Aktiengesellschaft | Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| JP2012509859A (ja) | 2008-11-24 | 2012-04-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | 中皮腫の治療のためのｃｄｋ阻害物質 |
| WO2010075542A1 (en) | 2008-12-23 | 2010-07-01 | Curis, Inc. | Cdk inhibitors |
| CA2761896A1 (en) | 2009-05-13 | 2010-11-18 | The University Of North Carolina At Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| KR101180030B1 (ko) | 2010-02-05 | 2012-09-05 | 광주과학기술원 | 사이클린-의존적 키나제 저해제로서 항암 활성을 지닌 인디루빈-3'-옥심 유도체 |
| WO2011130232A1 (en) * | 2010-04-13 | 2011-10-20 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor and an mtor inhibitor for treating cancer |
| US8566072B2 (en) | 2010-04-16 | 2013-10-22 | University Of South Carolina | Cyclin based inhibitors of CDK2 and CDK4 |
| CA2961937C (en) | 2010-10-25 | 2018-09-25 | G1 Therapeutics, Inc. | Cdk inhibitors |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| EP2636677B1 (en) | 2010-11-02 | 2016-01-13 | SNU R & DB Foundation | Cdk-inhibiting pyrrolopyrimidinone carboxamide derivative or pharmaceutically acceptable salt thereof, and pharmaceutical composition containing same as active ingredient for preventing or treating liver cell cancer |
| EP2714667B1 (en) | 2011-05-27 | 2020-11-25 | Laxman S. DESAI | Aminooxazole inhibitors of cyclin dependent kinases |
| US9376465B2 (en) | 2012-03-27 | 2016-06-28 | University Of South Carolina | Cyclin based inhibitors of CDK2 and CDK4 |
| US20130289240A1 (en) | 2012-03-27 | 2013-10-31 | Campbell McInnes | Cyclin Based Inhibitors of CDK2 and CDK4 |
| US20140296484A1 (en) | 2013-03-27 | 2014-10-02 | University Of South Carolina | Cyclin Based Inhibitors of CDK2 and CDK4 |
| CN106687454B8 (zh) | 2014-07-24 | 2019-08-30 | 贝达医药公司 | 作为细胞周期蛋白依赖性激酶(cdk)抑制剂的2h-吲唑衍生物及其医疗用途 |
| JO3556B1 (ar) * | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| AR102094A1 (es) * | 2014-09-25 | 2017-02-01 | Araxes Pharma Llc | Inhibidores de proteínas kras con una mutación g12c |
| US20170157212A1 (en) | 2015-12-03 | 2017-06-08 | Salk Institute For Biological Studies | Cdk modulators and methods for the treatment of cancer |
| SG11201810171SA (en) * | 2016-05-18 | 2018-12-28 | Mirati Therapeutics Inc | Kras g12c inhibitors |
| EP4001269A1 (en) * | 2016-12-22 | 2022-05-25 | Amgen Inc. | Benzoisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
| CN110382482A (zh) * | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| ES2944547T3 (es) | 2017-11-15 | 2023-06-22 | Mirati Therapeutics Inc | Inhibidores de KRas G12C |
-
2019
- 2019-09-09 EP EP19859991.2A patent/EP3849537A4/en active Pending
- 2019-09-09 JP JP2021513334A patent/JP2022500388A/ja active Pending
- 2019-09-09 US US17/275,177 patent/US20220096482A1/en active Pending
- 2019-09-09 WO PCT/US2019/050233 patent/WO2020055758A1/en unknown
- 2019-09-09 CA CA3111977A patent/CA3111977A1/en active Pending
- 2019-09-09 AU AU2019340436A patent/AU2019340436A1/en active Pending
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