AU2020407573A1 - Combinations - Google Patents
Combinations Download PDFInfo
- Publication number
- AU2020407573A1 AU2020407573A1 AU2020407573A AU2020407573A AU2020407573A1 AU 2020407573 A1 AU2020407573 A1 AU 2020407573A1 AU 2020407573 A AU2020407573 A AU 2020407573A AU 2020407573 A AU2020407573 A AU 2020407573A AU 2020407573 A1 AU2020407573 A1 AU 2020407573A1
- Authority
- AU
- Australia
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- group
- cancer
- 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.)
- Abandoned
Links
- 150000001875 compounds Chemical class 0.000 claims abstract description 287
- 150000003839 salts Chemical class 0.000 claims abstract description 194
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 40
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 35
- 201000010099 disease Diseases 0.000 claims abstract description 34
- 201000011510 cancer Diseases 0.000 claims abstract description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 232
- 125000000623 heterocyclic group Chemical group 0.000 claims description 106
- 125000001072 heteroaryl group Chemical group 0.000 claims description 90
- -1 SHR9549 Chemical compound 0.000 claims description 87
- 229910052739 hydrogen Inorganic materials 0.000 claims description 70
- 239000001257 hydrogen Substances 0.000 claims description 70
- 229910052736 halogen Inorganic materials 0.000 claims description 63
- 150000002367 halogens Chemical class 0.000 claims description 63
- 206010006187 Breast cancer Diseases 0.000 claims description 59
- 208000026310 Breast neoplasm Diseases 0.000 claims description 59
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 47
- 125000001424 substituent group Chemical group 0.000 claims description 42
- 102100038595 Estrogen receptor Human genes 0.000 claims description 41
- 108010007005 Estrogen Receptor alpha Proteins 0.000 claims description 39
- 150000001412 amines Chemical class 0.000 claims description 38
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 36
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 28
- 125000002950 monocyclic group Chemical group 0.000 claims description 27
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 230000035772 mutation Effects 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 125000001188 haloalkyl group Chemical group 0.000 claims description 23
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 23
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 21
- 229910052757 nitrogen Inorganic materials 0.000 claims description 20
- 239000003886 aromatase inhibitor Substances 0.000 claims description 18
- 238000011282 treatment Methods 0.000 claims description 18
- 125000002252 acyl group Chemical group 0.000 claims description 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 15
- 229940122815 Aromatase inhibitor Drugs 0.000 claims description 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 10
- 230000003637 steroidlike Effects 0.000 claims description 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 9
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 9
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 9
- BURHGPHDEVGCEZ-KJGLQBJMSA-N (e)-3-[4-[(e)-2-(2-chloro-4-fluorophenyl)-1-(1h-indazol-5-yl)but-1-enyl]phenyl]prop-2-enoic acid Chemical compound C=1C=C(F)C=C(Cl)C=1C(/CC)=C(C=1C=C2C=NNC2=CC=1)\C1=CC=C(\C=C\C(O)=O)C=C1 BURHGPHDEVGCEZ-KJGLQBJMSA-N 0.000 claims description 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 8
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 7
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 7
- 229960005309 estradiol Drugs 0.000 claims description 7
- 229930182833 estradiol Natural products 0.000 claims description 7
- 210000002966 serum Anatomy 0.000 claims description 7
- 125000003107 substituted aryl group Chemical group 0.000 claims description 7
- SIFNOOUKXBRGGB-AREMUKBSSA-N (6r)-6-[2-[ethyl-[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol Chemical compound C1=CC(CCNCC)=CC=C1CN(CC)C1=CC(OC)=CC=C1[C@H]1CC2=CC=C(O)C=C2CC1 SIFNOOUKXBRGGB-AREMUKBSSA-N 0.000 claims description 6
- KOAITBOFZOEDOC-BJMVGYQFSA-N (E)-3-[4-[[2-(4-fluoro-2,6-dimethylbenzoyl)-6-hydroxy-1-benzothiophen-3-yl]oxy]phenyl]prop-2-enoic acid Chemical compound FC1=CC(=C(C(=O)C2=C(C3=C(S2)C=C(C=C3)O)OC2=CC=C(C=C2)/C=C/C(=O)O)C(=C1)C)C KOAITBOFZOEDOC-BJMVGYQFSA-N 0.000 claims description 6
- 238000009261 endocrine therapy Methods 0.000 claims description 5
- 229960001603 tamoxifen Drugs 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- JPFTZIJTXCHJNE-HMOQVRKWSA-N (E)-N,N-dimethyl-4-[2-[5-[(Z)-4,4,4-trifluoro-1-(3-fluoro-2H-indazol-5-yl)-2-phenylbut-1-enyl]pyridin-2-yl]oxyethylamino]but-2-enamide Chemical compound CN(C(\C=C\CNCCOC1=NC=C(C=C1)\C(=C(\CC(F)(F)F)/C1=CC=CC=C1)\C=1C=C2C(=NNC2=CC=1)F)=O)C JPFTZIJTXCHJNE-HMOQVRKWSA-N 0.000 claims description 4
- GQCXHIKRWBIQMD-AKJBCIBTSA-N 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol Chemical compound FC1=C(C(=CC(=C1)NC1CN(C1)CCCF)F)[C@H]1N([C@@H](CC2=C1NC1=CC=CC=C21)C)CC(CO)(F)F GQCXHIKRWBIQMD-AKJBCIBTSA-N 0.000 claims description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 4
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 4
- 229940126088 GDC-9545 Drugs 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 4
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 4
- 206010047741 Vulval cancer Diseases 0.000 claims description 4
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims description 4
- 201000010881 cervical cancer Diseases 0.000 claims description 4
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 claims description 4
- 208000000649 small cell carcinoma Diseases 0.000 claims description 4
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 4
- 206010046766 uterine cancer Diseases 0.000 claims description 4
- 206010046885 vaginal cancer Diseases 0.000 claims description 4
- 208000013139 vaginal neoplasm Diseases 0.000 claims description 4
- 201000005102 vulva cancer Diseases 0.000 claims description 4
- TZZDVPMABRWKIZ-XMOGEVODSA-N (3S)-3-[6-[4-[[1-[4-[(1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl]phenyl]piperidin-4-yl]methyl]piperazin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione Chemical compound OC=1C=C2CC[C@@H]([C@@H](C2=CC=1)C1=CC=C(C=C1)N1CCC(CC1)CN1CCN(CC1)C=1C=C2CN(C(C2=CC=1)=O)[C@@H]1C(NC(CC1)=O)=O)C1=CC=CC=C1 TZZDVPMABRWKIZ-XMOGEVODSA-N 0.000 claims description 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 2
- SJXNPGGVGZXKKI-NYYWCZLTSA-N (E)-3-[4-[[2-[2-(1,1-difluoroethyl)-4-fluorophenyl]-6-hydroxy-1-benzothiophen-3-yl]oxy]phenyl]prop-2-enoic acid Chemical compound FC(C)(F)C1=C(C=CC(=C1)F)C1=C(C2=C(S1)C=C(C=C2)O)OC1=CC=C(C=C1)/C=C/C(=O)O SJXNPGGVGZXKKI-NYYWCZLTSA-N 0.000 claims description 2
- DFBDRVGWBHBJNR-BBNFHIFMSA-N (e)-3-[3,5-difluoro-4-[(1r,3r)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H](N2CC(C)(C)F)C)=C(F)C=C(\C=C\C(O)=O)C=C1F DFBDRVGWBHBJNR-BBNFHIFMSA-N 0.000 claims description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 2
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- KISZAGQTIXIVAR-VWLOTQADSA-N 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid Chemical compound ClC1=C(C=CC(=C1)Cl)C1=C(C2=C(CCC1)C=C(C=C2)C(=O)O)C1=CC=C(C=C1)O[C@@H]1CN(CC1)CCCF KISZAGQTIXIVAR-VWLOTQADSA-N 0.000 claims description 2
- 206010000830 Acute leukaemia Diseases 0.000 claims description 2
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims description 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010055113 Breast cancer metastatic Diseases 0.000 claims description 2
- 208000006332 Choriocarcinoma Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 2
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical group OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 claims description 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 208000002471 Penile Neoplasms Diseases 0.000 claims description 2
- 206010034299 Penile cancer Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 102220568068 Tetratricopeptide repeat protein 4_S47T_mutation Human genes 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000023915 Ureteral Neoplasms Diseases 0.000 claims description 2
- 206010046392 Ureteric cancer Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims description 2
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims description 2
- 229960000817 bazedoxifene Drugs 0.000 claims description 2
- UCJGJABZCDBEDK-UHFFFAOYSA-N bazedoxifene Chemical compound C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 UCJGJABZCDBEDK-UHFFFAOYSA-N 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 229950004948 brilanestrant Drugs 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 2
- 229950005473 elacestrant Drugs 0.000 claims description 2
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- 229960000255 exemestane Drugs 0.000 claims description 2
- 230000001605 fetal effect Effects 0.000 claims description 2
- 229960002258 fulvestrant Drugs 0.000 claims description 2
- 210000000232 gallbladder Anatomy 0.000 claims description 2
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- 229940126389 imlunestrant Drugs 0.000 claims description 2
- 210000000244 kidney pelvis Anatomy 0.000 claims description 2
- GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 claims description 2
- 229960002367 lasofoxifene Drugs 0.000 claims description 2
- 229960003881 letrozole Drugs 0.000 claims description 2
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 208000020984 malignant renal pelvis neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 229960003969 ospemifene Drugs 0.000 claims description 2
- LUMKNAVTFCDUIE-VHXPQNKSSA-N ospemifene Chemical compound C1=CC(OCCO)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 LUMKNAVTFCDUIE-VHXPQNKSSA-N 0.000 claims description 2
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- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
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- 208000037244 polycythemia vera Diseases 0.000 claims description 2
- 229960004622 raloxifene Drugs 0.000 claims description 2
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims description 2
- 206010038038 rectal cancer Diseases 0.000 claims description 2
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- 230000000306 recurrent effect Effects 0.000 claims description 2
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- 229940073462 rintodestrant Drugs 0.000 claims description 2
- 102200087501 rs104894110 Human genes 0.000 claims description 2
- 102200071658 rs111033601 Human genes 0.000 claims description 2
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- BPEWUONYVDABNZ-DZBHQSCQSA-N testolactone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(OC(=O)CC4)[C@@H]4[C@@H]3CCC2=C1 BPEWUONYVDABNZ-DZBHQSCQSA-N 0.000 claims description 2
- 229960005353 testolactone Drugs 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims description 2
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
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- 239000003112 inhibitor Substances 0.000 abstract description 7
- 101000621390 Homo sapiens Wee1-like protein kinase Proteins 0.000 abstract description 3
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- 125000003118 aryl group Chemical group 0.000 description 94
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- 125000004432 carbon atom Chemical group C* 0.000 description 50
- 150000002431 hydrogen Chemical class 0.000 description 42
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 36
- 125000003342 alkenyl group Chemical group 0.000 description 34
- 125000000304 alkynyl group Chemical group 0.000 description 34
- 125000005842 heteroatom Chemical group 0.000 description 30
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 28
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 11
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- 239000002904 solvent Substances 0.000 description 10
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- 125000004646 sulfenyl group Chemical group S(*)* 0.000 description 8
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- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 7
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 description 7
- 239000012458 free base Substances 0.000 description 7
- 238000000338 in vitro Methods 0.000 description 7
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- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 7
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- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 description 6
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- 239000003381 stabilizer Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000002626 targeted therapy Methods 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 150000003557 thiazoles Chemical class 0.000 description 1
- 150000003577 thiophenes Chemical class 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 230000004614 tumor growth Effects 0.000 description 1
- 230000036642 wellbeing Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Glass Compositions (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962952020P | 2019-12-20 | 2019-12-20 | |
| US62/952,020 | 2019-12-20 | ||
| US202063009788P | 2020-04-14 | 2020-04-14 | |
| US63/009,788 | 2020-04-14 | ||
| PCT/US2020/065415 WO2021127047A1 (en) | 2019-12-20 | 2020-12-16 | Combinations |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2020407573A1 true AU2020407573A1 (en) | 2022-07-14 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2020407573A Abandoned AU2020407573A1 (en) | 2019-12-20 | 2020-12-16 | Combinations |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20230087941A1 (enExample) |
| EP (1) | EP4069240A4 (enExample) |
| JP (1) | JP2023507797A (enExample) |
| KR (1) | KR20220119419A (enExample) |
| CN (1) | CN115038450A (enExample) |
| AU (1) | AU2020407573A1 (enExample) |
| BR (1) | BR112022012280A2 (enExample) |
| CA (1) | CA3165479A1 (enExample) |
| IL (1) | IL294078A (enExample) |
| MX (1) | MX2022007628A (enExample) |
| TW (1) | TW202135809A (enExample) |
| WO (1) | WO2021127047A1 (enExample) |
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| EP4566612A3 (en) | 2018-03-09 | 2025-08-20 | Recurium IP Holdings, LLC | Substituted 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidin-3-ones |
| AU2020384291A1 (en) | 2019-11-15 | 2022-05-26 | Recurium Ip Holdings, Llc | Chiral synthesis of a tertiary alcohol |
| WO2022011391A1 (en) | 2020-07-09 | 2022-01-13 | Recurium Ip Holdings, Llc | Salts and forms of a wee1 inhibitor |
| WO2023280180A1 (zh) * | 2021-07-05 | 2023-01-12 | 微境生物医药科技(上海)有限公司 | 作为Wee-1抑制剂的稠环化合物 |
| TW202340196A (zh) * | 2021-12-31 | 2023-10-16 | 大陸商正大天晴藥業集團股份有限公司 | 含有雜環的化合物及其應用 |
| WO2025193930A1 (en) * | 2024-03-14 | 2025-09-18 | Zeno Management, Inc. | Wee1 inhibitor combination therapy |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PE20080695A1 (es) * | 2006-04-27 | 2008-06-28 | Banyu Pharma Co Ltd | Derivados de dihidropirazolopirimidinona como inhibidores de quinasa weel |
| AU2010247397B2 (en) * | 2009-05-15 | 2012-07-12 | Novartis Ag | Combination of a phosphoinositide 3-kinase inhibitor and an antidiabetic compound |
| SG11201607339VA (en) * | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Methods and compositions for modulating estrogen receptor mutants |
| KR20220071293A (ko) * | 2016-04-01 | 2022-05-31 | 리커리엄 아이피 홀딩스, 엘엘씨 | 에스트로겐 수용체 조절제 |
| CN109422754A (zh) * | 2017-08-24 | 2019-03-05 | 上海迪诺医药科技有限公司 | 吡唑并[3,4-d]嘧啶-3-酮衍生物、其药物组合物及应用 |
| EP3694861A4 (en) * | 2017-10-09 | 2021-05-19 | Nuvation Bio Inc. | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| EP4566612A3 (en) * | 2018-03-09 | 2025-08-20 | Recurium IP Holdings, LLC | Substituted 1,2-dihydro-3h-pyrazolo[3,4-d]pyrimidin-3-ones |
-
2020
- 2020-12-16 JP JP2022538218A patent/JP2023507797A/ja active Pending
- 2020-12-16 MX MX2022007628A patent/MX2022007628A/es unknown
- 2020-12-16 US US17/757,486 patent/US20230087941A1/en not_active Abandoned
- 2020-12-16 KR KR1020227024700A patent/KR20220119419A/ko active Pending
- 2020-12-16 CN CN202080095297.8A patent/CN115038450A/zh active Pending
- 2020-12-16 CA CA3165479A patent/CA3165479A1/en active Pending
- 2020-12-16 IL IL294078A patent/IL294078A/en unknown
- 2020-12-16 BR BR112022012280A patent/BR112022012280A2/pt not_active IP Right Cessation
- 2020-12-16 WO PCT/US2020/065415 patent/WO2021127047A1/en not_active Ceased
- 2020-12-16 AU AU2020407573A patent/AU2020407573A1/en not_active Abandoned
- 2020-12-16 EP EP20901281.4A patent/EP4069240A4/en active Pending
- 2020-12-18 TW TW109145140A patent/TW202135809A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3165479A1 (en) | 2021-06-24 |
| KR20220119419A (ko) | 2022-08-29 |
| IL294078A (en) | 2022-08-01 |
| CN115038450A (zh) | 2022-09-09 |
| WO2021127047A1 (en) | 2021-06-24 |
| US20230087941A1 (en) | 2023-03-23 |
| MX2022007628A (es) | 2022-08-25 |
| TW202135809A (zh) | 2021-10-01 |
| JP2023507797A (ja) | 2023-02-27 |
| EP4069240A4 (en) | 2023-12-20 |
| BR112022012280A2 (pt) | 2022-08-30 |
| EP4069240A1 (en) | 2022-10-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK1 | Application lapsed section 142(2)(a) - no request for examination in relevant period |