CN105452226B - 四氢‑和二氢‑异喹啉prmt5抑制剂及其用途 - Google Patents
四氢‑和二氢‑异喹啉prmt5抑制剂及其用途 Download PDFInfo
- Publication number
- CN105452226B CN105452226B CN201380070441.2A CN201380070441A CN105452226B CN 105452226 B CN105452226 B CN 105452226B CN 201380070441 A CN201380070441 A CN 201380070441A CN 105452226 B CN105452226 B CN 105452226B
- Authority
- CN
- China
- Prior art keywords
- compound
- optionally substituted
- pharmaceutically acceptable
- alkyl
- formula
- 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.)
- Active
Links
- 0 CC=CC1=C(C)CC=CN(C[C@@](CNC(C2NC=*(C*)C=C2)=O)O)C1 Chemical compound CC=CC1=C(C)CC=CN(C[C@@](CNC(C2NC=*(C*)C=C2)=O)O)C1 0.000 description 44
- ZAMODMPUQSDENV-IBGZPJMESA-N CC(N(C1)CC1Nc1ncnc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O Chemical compound CC(N(C1)CC1Nc1ncnc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O ZAMODMPUQSDENV-IBGZPJMESA-N 0.000 description 2
- BEFPHTPKPJOWRZ-DEOSSOPVSA-N C/C(/NC(CC1)CCN1C(C)=O)=N\C=N/C(C(NC[C@@H](CN(CC1)Cc2c1cccc2)O)=O)=C Chemical compound C/C(/NC(CC1)CCN1C(C)=O)=N\C=N/C(C(NC[C@@H](CN(CC1)Cc2c1cccc2)O)=O)=C BEFPHTPKPJOWRZ-DEOSSOPVSA-N 0.000 description 1
- WMZFVCDVEVWOMM-NIDLAPIMSA-N C/C=C/C(/CC1CCOCC1)=C\C Chemical compound C/C=C/C(/CC1CCOCC1)=C\C WMZFVCDVEVWOMM-NIDLAPIMSA-N 0.000 description 1
- VPLREIUIVRTGMS-LIMHQNJXSA-N C/C=C\C1=C(C)CN(C[C@H](CNC(c2ncnc(NC3COC3)c2)=O)O)CC1 Chemical compound C/C=C\C1=C(C)CN(C[C@H](CNC(c2ncnc(NC3COC3)c2)=O)O)CC1 VPLREIUIVRTGMS-LIMHQNJXSA-N 0.000 description 1
- CAMFPSPROHIZAH-FPLPWBNLSA-N CC(/C(/C)=N\C#C)=C Chemical compound CC(/C(/C)=N\C#C)=C CAMFPSPROHIZAH-FPLPWBNLSA-N 0.000 description 1
- UBVMWNLJDDCBHD-UHFFFAOYSA-N CC(C)(C)C(N(C)N1)=C2N1N=CN=C2 Chemical compound CC(C)(C)C(N(C)N1)=C2N1N=CN=C2 UBVMWNLJDDCBHD-UHFFFAOYSA-N 0.000 description 1
- FWECVBOZGCYUHP-UHFFFAOYSA-N CC(C)(C)c1cc(-c2c[nH]cn2)ccc1 Chemical compound CC(C)(C)c1cc(-c2c[nH]cn2)ccc1 FWECVBOZGCYUHP-UHFFFAOYSA-N 0.000 description 1
- FFVBXDUYIITUST-UHFFFAOYSA-N CC(C)(C)c1cnc2nn[s]c2c1 Chemical compound CC(C)(C)c1cnc2nn[s]c2c1 FFVBXDUYIITUST-UHFFFAOYSA-N 0.000 description 1
- YBKHVMBSQIPHBT-UHFFFAOYSA-O CC(C)C(N)=C1N=CN=CN1[NH3+] Chemical compound CC(C)C(N)=C1N=CN=CN1[NH3+] YBKHVMBSQIPHBT-UHFFFAOYSA-O 0.000 description 1
- ONCOHEYXUDKXPO-UHFFFAOYSA-N CC(C)CC(CCC=C1)C1S(N(CC1)CC1N)(=O)=O Chemical compound CC(C)CC(CCC=C1)C1S(N(CC1)CC1N)(=O)=O ONCOHEYXUDKXPO-UHFFFAOYSA-N 0.000 description 1
- GAMCXFNSHKAREG-UHFFFAOYSA-N CC(C)c(cc1NC2CCOCC2)ccc1OC Chemical compound CC(C)c(cc1NC2CCOCC2)ccc1OC GAMCXFNSHKAREG-UHFFFAOYSA-N 0.000 description 1
- TUYAGRNRCPZEGB-XDXAGZTOSA-N CC(CCN(C[C@H](CNC(c1cc(NC2COC2)ncn1)=O)O)C1)=C1/C=C\C=C Chemical compound CC(CCN(C[C@H](CNC(c1cc(NC2COC2)ncn1)=O)O)C1)=C1/C=C\C=C TUYAGRNRCPZEGB-XDXAGZTOSA-N 0.000 description 1
- SMIGOWPKZAHIOE-DEOSSOPVSA-N CC(CN(CC1)CCC1Nc1nccc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O Chemical compound CC(CN(CC1)CCC1Nc1nccc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O SMIGOWPKZAHIOE-DEOSSOPVSA-N 0.000 description 1
- NQPJRXPUBKLFQV-QHCPKHFHSA-N CC(N(CC1)CCC1Nc1nccc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O Chemical compound CC(N(CC1)CCC1Nc1nccc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=O NQPJRXPUBKLFQV-QHCPKHFHSA-N 0.000 description 1
- GHBCDNURRBILMZ-QFIPXVFZSA-N CC(N(CC1)CCC1Nc1ncnc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=C Chemical compound CC(N(CC1)CCC1Nc1ncnc(C(NC[C@@H](CN(CC2)Cc3c2cccc3)O)=O)c1)=C GHBCDNURRBILMZ-QFIPXVFZSA-N 0.000 description 1
- IKZZNFNODBVCBO-UHFFFAOYSA-N CC(Nc(cc1)ccc1C(NCC(CN(CC1)Cc2c1cccc2)O)=O)O Chemical compound CC(Nc(cc1)ccc1C(NCC(CN(CC1)Cc2c1cccc2)O)=O)O IKZZNFNODBVCBO-UHFFFAOYSA-N 0.000 description 1
- CSQVVAHXCMAVBT-UHFFFAOYSA-N CCC(c1ncc2[n]1ncnc2)N(C)C Chemical compound CCC(c1ncc2[n]1ncnc2)N(C)C CSQVVAHXCMAVBT-UHFFFAOYSA-N 0.000 description 1
- ASQFBXYYBSHXSG-UHFFFAOYSA-N CCC1=C(CCN)CC=CC=C1 Chemical compound CCC1=C(CCN)CC=CC=C1 ASQFBXYYBSHXSG-UHFFFAOYSA-N 0.000 description 1
- DILGEBDXHMSANB-UHFFFAOYSA-N CCN(CCC(CCNC([AlH2])=O)O)CCc1c(C)cccc1 Chemical compound CCN(CCC(CCNC([AlH2])=O)O)CCc1c(C)cccc1 DILGEBDXHMSANB-UHFFFAOYSA-N 0.000 description 1
- NIVGSSBLFPADDF-UHFFFAOYSA-N CCc(c(C)c1)cc(SN)c1N Chemical compound CCc(c(C)c1)cc(SN)c1N NIVGSSBLFPADDF-UHFFFAOYSA-N 0.000 description 1
- FQPXMQIDNCPQCU-UHFFFAOYSA-N CCc1c(C(C)(C)C)[n](cnnc2)c2c1 Chemical compound CCc1c(C(C)(C)C)[n](cnnc2)c2c1 FQPXMQIDNCPQCU-UHFFFAOYSA-N 0.000 description 1
- NYVDLPIZBOJDIK-UHFFFAOYSA-N CCc1c(CCNCC(CNC(c(cc2)ccc2-c2ncccc2)=O)O)cccc1 Chemical compound CCc1c(CCNCC(CNC(c(cc2)ccc2-c2ncccc2)=O)O)cccc1 NYVDLPIZBOJDIK-UHFFFAOYSA-N 0.000 description 1
- CIVXQEHQUVADKX-UHFFFAOYSA-N CCc1nc(cc(cc2)F)c2[nH]1 Chemical compound CCc1nc(cc(cc2)F)c2[nH]1 CIVXQEHQUVADKX-UHFFFAOYSA-N 0.000 description 1
- XFRGEXAHJNIBCP-XPKXGTFLSA-O CN(C)c([nH]1)ncc1/N=C\C=[NH2+] Chemical compound CN(C)c([nH]1)ncc1/N=C\C=[NH2+] XFRGEXAHJNIBCP-XPKXGTFLSA-O 0.000 description 1
- RXWXPSLVKDNZAC-UHFFFAOYSA-N CN(C)c1n[s]c2c1ccnn2 Chemical compound CN(C)c1n[s]c2c1ccnn2 RXWXPSLVKDNZAC-UHFFFAOYSA-N 0.000 description 1
- HYALEYIYHOPNCA-UHFFFAOYSA-N CNc1n[s]c2c1ncnc2 Chemical compound CNc1n[s]c2c1ncnc2 HYALEYIYHOPNCA-UHFFFAOYSA-N 0.000 description 1
- DNAFPFUFCPIUKH-UHFFFAOYSA-N COC(c1cc(C2NC2CC2CCOCC2)ccn1)=O Chemical compound COC(c1cc(C2NC2CC2CCOCC2)ccn1)=O DNAFPFUFCPIUKH-UHFFFAOYSA-N 0.000 description 1
- LRJKAKFRLUGCMH-UHFFFAOYSA-N Cc([nH]c1ccc2)nc1c2Cl Chemical compound Cc([nH]c1ccc2)nc1c2Cl LRJKAKFRLUGCMH-UHFFFAOYSA-N 0.000 description 1
- DEIPVSXYIOFSCU-UHFFFAOYSA-N Cc1c[n](cncn2)c2n1 Chemical compound Cc1c[n](cncn2)c2n1 DEIPVSXYIOFSCU-UHFFFAOYSA-N 0.000 description 1
- YQFKROZYTRVSSK-UHFFFAOYSA-N Cc1cc2n[o]nc2cn1 Chemical compound Cc1cc2n[o]nc2cn1 YQFKROZYTRVSSK-UHFFFAOYSA-N 0.000 description 1
- NWUUMWKLDHQQEP-UHFFFAOYSA-N Cc1ncc2ncnc[n]12 Chemical compound Cc1ncc2ncnc[n]12 NWUUMWKLDHQQEP-UHFFFAOYSA-N 0.000 description 1
- FOGLBIJCADVSHC-UHFFFAOYSA-N Cc1ncc2nncc[n]12 Chemical compound Cc1ncc2nncc[n]12 FOGLBIJCADVSHC-UHFFFAOYSA-N 0.000 description 1
- SNTGWEFJDCUSJZ-UHFFFAOYSA-N Ic1nnc2nccc[n]12 Chemical compound Ic1nnc2nccc[n]12 SNTGWEFJDCUSJZ-UHFFFAOYSA-N 0.000 description 1
- BYWDGTKESWRSML-UHFFFAOYSA-N NCC(CN(CC1)Cc2c1cccc2)O Chemical compound NCC(CN(CC1)Cc2c1cccc2)O BYWDGTKESWRSML-UHFFFAOYSA-N 0.000 description 1
- HQZREDHOWCMDHT-UHFFFAOYSA-N NS(c(cc1)ccc1C(NCC(CN(CC1)Cc2c1cccc2)O)=O)(=O)=O Chemical compound NS(c(cc1)ccc1C(NCC(CN(CC1)Cc2c1cccc2)O)=O)(=O)=O HQZREDHOWCMDHT-UHFFFAOYSA-N 0.000 description 1
- HEQAPJIMOPCOIH-UHFFFAOYSA-N Nc1nnc2[n]1cncc2 Chemical compound Nc1nnc2[n]1cncc2 HEQAPJIMOPCOIH-UHFFFAOYSA-N 0.000 description 1
- RWSPRTBXAXZIOS-UHFFFAOYSA-N OC(c1cc(Cl)ncn1)=O Chemical compound OC(c1cc(Cl)ncn1)=O RWSPRTBXAXZIOS-UHFFFAOYSA-N 0.000 description 1
- NTGYTIJDOVSIRO-UHFFFAOYSA-N OCCNCCNC(c1ccccc1)=O Chemical compound OCCNCCNC(c1ccccc1)=O NTGYTIJDOVSIRO-UHFFFAOYSA-N 0.000 description 1
- ZKXZLIFRWWKZRY-KRWDZBQOSA-N O[C@@H](CNC(c1cc(NC2COC2)ncn1)=O)CN(CC1)Cc2c1cccc2 Chemical compound O[C@@H](CNC(c1cc(NC2COC2)ncn1)=O)CN(CC1)Cc2c1cccc2 ZKXZLIFRWWKZRY-KRWDZBQOSA-N 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
- C12N9/1007—Methyltransferases (general) (2.1.1.)
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Obesity (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745485P | 2012-12-21 | 2012-12-21 | |
| US61/745,485 | 2012-12-21 | ||
| US201361790525P | 2013-03-15 | 2013-03-15 | |
| US61/790,525 | 2013-03-15 | ||
| PCT/US2013/077235 WO2014100719A2 (en) | 2012-12-21 | 2013-12-20 | Prmt5 inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105452226A CN105452226A (zh) | 2016-03-30 |
| CN105452226B true CN105452226B (zh) | 2017-09-12 |
Family
ID=49958717
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380070441.2A Active CN105452226B (zh) | 2012-12-21 | 2013-12-20 | 四氢‑和二氢‑异喹啉prmt5抑制剂及其用途 |
Country Status (31)
| Country | Link |
|---|---|
| US (10) | US8993555B2 (enExample) |
| EP (3) | EP4219465A3 (enExample) |
| JP (1) | JP6678455B2 (enExample) |
| KR (2) | KR102024417B1 (enExample) |
| CN (1) | CN105452226B (enExample) |
| AU (1) | AU2018202150B2 (enExample) |
| BR (1) | BR112015014590B1 (enExample) |
| CA (1) | CA2894228C (enExample) |
| CL (1) | CL2015001790A1 (enExample) |
| CR (1) | CR20150371A (enExample) |
| CY (1) | CY1121625T1 (enExample) |
| DK (1) | DK2935222T3 (enExample) |
| DO (1) | DOP2015000158A (enExample) |
| EA (1) | EA027908B1 (enExample) |
| ES (1) | ES2701069T3 (enExample) |
| HR (1) | HRP20182037T1 (enExample) |
| HU (1) | HUE040323T2 (enExample) |
| IL (3) | IL239296B (enExample) |
| LT (1) | LT2935222T (enExample) |
| MX (1) | MX375184B (enExample) |
| MY (1) | MY199894A (enExample) |
| PE (1) | PE20151501A1 (enExample) |
| PH (2) | PH12015501351A1 (enExample) |
| PL (1) | PL2935222T3 (enExample) |
| PT (1) | PT2935222T (enExample) |
| RS (1) | RS58040B1 (enExample) |
| SI (1) | SI2935222T1 (enExample) |
| SM (1) | SMT201800669T1 (enExample) |
| UA (1) | UA118548C2 (enExample) |
| WO (1) | WO2014100719A2 (enExample) |
| ZA (1) | ZA201505212B (enExample) |
Families Citing this family (128)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9288251B2 (en) * | 2011-06-10 | 2016-03-15 | Citrix Systems, Inc. | Adaptive bitrate management on progressive download with indexed media files |
| TWI568722B (zh) | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲mPGES-1抑制劑之三唑酮化合物 |
| SI2935222T1 (sl) | 2012-12-21 | 2019-02-28 | Epizyme Inc. | Inhibitorji PRMT5 in njihove uporabe |
| CA2899363A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP2935243B1 (en) | 2012-12-21 | 2018-03-14 | Epizyme, Inc. | Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
| EP3912984A1 (en) | 2012-12-21 | 2021-11-24 | Janssen BioPharma, Inc. | 4'-fluoro-nucleosides, 4'-fluoro-nucleotides and analogs thereof for the treatment of hcv |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| CA2894157A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| US8906900B2 (en) | 2012-12-21 | 2014-12-09 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| CA2897333C (en) | 2013-01-15 | 2021-07-06 | Incyte Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153172A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9765035B2 (en) | 2013-03-14 | 2017-09-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| BR112015022785A2 (pt) | 2013-03-14 | 2017-07-18 | Epizyme Inc | composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt |
| US9133189B2 (en) | 2013-03-14 | 2015-09-15 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| WO2014178954A1 (en) | 2013-03-14 | 2014-11-06 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| US9738651B2 (en) | 2013-03-15 | 2017-08-22 | Epizyme, Inc. | CARM1 inhibitors and uses thereof |
| WO2014144455A1 (en) | 2013-03-15 | 2014-09-18 | Epizyme, Inc. | 1 -phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof |
| US9346802B2 (en) | 2013-03-15 | 2016-05-24 | Epizyme, Inc. | CARM1 inhibitors and uses thereof |
| CR20160135A (es) | 2013-08-23 | 2016-08-05 | Incyte Corp | Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de cinasas pim |
| PE20161552A1 (es) | 2014-06-17 | 2017-01-11 | Pfizer | Compuestos de dihidroisoquinolinona sustituida |
| WO2015200677A2 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP3160477A4 (en) * | 2014-06-25 | 2018-07-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| SMT202100260T1 (it) * | 2014-06-25 | 2021-07-12 | Glaxosmithkline Ip Dev Ltd | Sali cristallini di (s)-6-((1-acetilpiperidin-4-il)ammino)-n-(3-(3,4-diidroisochinolin-2(1h)-il)-2-idrossipropil) pirimidin-4-carbossammide. |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| EP3177288A4 (en) * | 2014-08-04 | 2018-04-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| GB201415573D0 (en) * | 2014-09-03 | 2014-10-15 | Cancer Therapeutics Crc Pty Ltd | Compounds |
| US10005792B2 (en) | 2014-09-03 | 2018-06-26 | Ctxt Pty. Ltd. | Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors |
| WO2016034673A1 (en) * | 2014-09-03 | 2016-03-10 | Ctxt Pty Ltd | Tetrahydroisoquinoline derived prmt5-inhibitors |
| US20180010132A1 (en) | 2014-09-11 | 2018-01-11 | Novartis Ag | Inhibition of prmt5 to treat mtap-deficiency-related diseases |
| US10479997B2 (en) | 2014-12-01 | 2019-11-19 | Novartis Ag | Compositions and methods for diagnosis and treatment of prostate cancer |
| AR104326A1 (es) | 2015-05-04 | 2017-07-12 | Lilly Co Eli | Compuestos nucleósidos 5-sustituidos |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| TWI791251B (zh) * | 2015-08-26 | 2023-02-01 | 比利時商健生藥品公司 | 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物 |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
| TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
| CN105497034B (zh) * | 2015-12-08 | 2018-08-07 | 暨南大学 | 一种通过靶向prmt5抑制骨肉瘤生长的组合物及其制备方法 |
| GB201604031D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| GB201604022D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| GB201604027D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| GB201604030D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| GB201604020D0 (en) * | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| GB201604029D0 (en) | 2016-03-09 | 2016-04-20 | Ctxt Pty Ltd | Compounds |
| WO2017153186A1 (en) | 2016-03-10 | 2017-09-14 | Janssen Pharmaceutica Nv | Substituted nucleoside analogues for use as prmt5 inhibitors |
| US10898504B2 (en) | 2016-03-10 | 2021-01-26 | Janssen Pharmaceutica Nv | Substituted nucleoside analogues for use as PRMT5 inhibitors |
| CA2969295A1 (en) * | 2016-06-06 | 2017-12-06 | Pfizer Inc. | Substituted carbonucleoside derivatives, and use thereof as a prmt5 inhibitor |
| US20180072718A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine compounds and uses thereof |
| US10611778B2 (en) | 2016-09-14 | 2020-04-07 | Janssen Pharmaceutica Nv | Fused bicyclic inhibitors of menin-MLL interaction |
| US12084462B2 (en) | 2016-09-14 | 2024-09-10 | Janssen Pharmaceutica Nv | Spiro bicyclic inhibitors of menin-MLL interaction |
| LT3512857T (lt) | 2016-09-14 | 2021-04-12 | Janssen Pharmaceutica Nv | Menin-mll sąveikos spirobicikliniai inhibitoriai |
| EP3519413A1 (en) | 2016-10-03 | 2019-08-07 | Janssen Pharmaceutica NV | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
| WO2018065365A1 (en) | 2016-10-03 | 2018-04-12 | Janssen Pharmaceutica Nv | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| US11197857B2 (en) | 2016-12-01 | 2021-12-14 | Glaxosmithkline Intellectual Property Development Limited | Combination therapy |
| WO2018100535A1 (en) * | 2016-12-01 | 2018-06-07 | Glaxosmithkline Intellectual Property Development Limited | Combination therapy |
| AU2017370694A1 (en) | 2016-12-08 | 2019-07-25 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating CDK4/6-mediated cancer |
| MX391405B (es) | 2016-12-15 | 2025-03-21 | Janssen Pharmaceutica Nv | Inhibidores de azepano de la interacción menina-mll. |
| PE20191359A1 (es) | 2017-02-27 | 2019-10-01 | Janssen Pharmaceutica Nv | Uso de biomarcadores en la identificacion de pacientes con cancer que seran sensibles al tratamiento con un inhibidor de prmt5 |
| CN108570059B (zh) * | 2017-03-09 | 2022-02-08 | 中国科学院上海药物研究所 | 一种具有prmt5抑制活性的化合物及其制备和应用 |
| GB201704327D0 (en) * | 2017-03-17 | 2017-05-03 | Argonaut Therapeutics Ltd | Compounds |
| BR112020002736A2 (pt) * | 2017-08-09 | 2020-07-28 | Prelude Therapeutics, Incorporated | inibidores seletivos da proteína arginina metiltransferase 5 (prmt5) |
| WO2019058393A1 (en) | 2017-09-22 | 2019-03-28 | Jubilant Biosys Limited | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF PAD |
| FI3697785T3 (fi) | 2017-10-18 | 2023-04-03 | Jubilant Epipad LLC | Imidatsopyridiiniyhdisteitä pad:n estäjinä |
| AU2018362046B2 (en) | 2017-11-06 | 2023-04-13 | Jubilant Prodel LLC | Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| BR112020010322A2 (pt) * | 2017-11-24 | 2020-11-17 | Jubilant Episcribe Llc | composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer |
| MX2020005944A (es) | 2017-12-08 | 2020-08-24 | Janssen Pharmaceutica Nv | Analogos espirobiciclicos novedosos. |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3724190B1 (en) | 2017-12-13 | 2022-07-06 | Lupin Limited | Substituted bicyclic heterocyclic compounds as prmt5 inhibitors |
| US11396517B1 (en) | 2017-12-20 | 2022-07-26 | Janssen Pharmaceutica Nv | Exo-aza spiro inhibitors of menin-MLL interaction |
| SMT202200294T1 (it) | 2018-02-20 | 2022-11-18 | Incyte Corp | Derivati di n-(fenil)-2-(fenil)pirimidina-4-carbossammide e composti correlati come inibitori di hpk1 per trattare il cancro |
| WO2019165189A1 (en) * | 2018-02-22 | 2019-08-29 | Icahn School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
| AU2019231689A1 (en) | 2018-03-06 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (AKT) degradation / disruption compounds and methods of use |
| KR102522856B1 (ko) | 2018-03-09 | 2023-04-19 | 파마블럭 사이언시스 (난징), 인코포레이티드 | 단백질 아르기닌 메틸전이효소 5(prmt 5)의 억제제, 이의 약학적 제품 및 이의 방법 |
| CN112105610B (zh) | 2018-03-13 | 2024-01-26 | 朱比连特普罗德尔有限责任公司 | 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物 |
| DK3765461T3 (da) * | 2018-03-14 | 2023-11-20 | Prelude Therapeutics Inc | Selektive protein argininmethyltransferase 5 (prmt5)-hæmmere |
| EP3768670A4 (en) * | 2018-03-22 | 2021-11-24 | Aurigene Discovery Technologies Limited | IMIDAZOLIDIN-2-ONE COMPOUNDS AS PRMT5 MODULATORS |
| MY203159A (en) * | 2018-03-22 | 2024-06-12 | Aurigene Discovery Tech Ltd | Substituted imidazolidin-2-one derivatives as prmt5 inhibitors |
| WO2019219805A1 (en) | 2018-05-16 | 2019-11-21 | Ctxone Pty Ltd | Combination therapy |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| US11077101B1 (en) * | 2018-07-18 | 2021-08-03 | Tango Therapeutics, Inc. | Compounds and methods of use |
| MA53287A (fr) | 2018-08-07 | 2022-05-11 | Merck Sharp & Dohme | Inhibiteurs de prmt5 |
| US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
| JP2022506718A (ja) * | 2018-11-08 | 2022-01-17 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | Prmt5阻害剤及びbcl-2阻害剤の組合せ |
| WO2020182018A1 (zh) * | 2019-03-12 | 2020-09-17 | 四川科伦博泰生物医药股份有限公司 | 氮杂环化合物、其制备方法及用途 |
| WO2020205660A1 (en) * | 2019-03-29 | 2020-10-08 | University Of Florida Research Foundation, Incorporated | Prmt5 inhibitor compounds |
| CN111825656B (zh) * | 2019-04-15 | 2023-03-31 | 南京药石科技股份有限公司 | 蛋白质精氨酸甲基转移酶5(prmt5)的抑制剂、其药学产品及其方法 |
| CA3137916A1 (en) | 2019-05-06 | 2020-11-12 | Ichan School Of Medicine At Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| TW202112375A (zh) | 2019-06-06 | 2021-04-01 | 比利時商健生藥品公司 | 使用prmt5抑制劑治療癌症之方法 |
| ES2967457T3 (es) | 2019-06-10 | 2024-04-30 | Lupin Ltd | Inhibidores de PRMT5 |
| JOP20210327A1 (ar) | 2019-06-12 | 2023-01-30 | Janssen Pharmaceutica Nv | مركبات وسيطة سبيرو ثنائية الحلقة جديدة |
| MX2021015911A (es) | 2019-06-28 | 2022-08-04 | Als Therapy Development Inst | Inhibicion de proteinas de repeticiones dipeptidicas. |
| CN110585434B (zh) * | 2019-10-11 | 2021-04-09 | 山东大学 | Prmt5抑制剂在抗病毒中的应用 |
| CN114466846B (zh) | 2019-10-12 | 2024-08-20 | 南京圣和药业股份有限公司 | 作为prmt5抑制剂的取代三环类化合物及其应用 |
| US12447152B2 (en) | 2019-10-22 | 2025-10-21 | Lupin Limited | Pharmaceutical combination of PRMT5 inhibitors |
| US12403137B2 (en) | 2019-10-28 | 2025-09-02 | Tango Therapeutics, Inc. | Compounds and methods of use |
| CN112778275B (zh) * | 2019-11-11 | 2023-05-12 | 石药集团中奇制药技术(石家庄)有限公司 | 金刚烷基prmt5抑制剂及其应用 |
| CN110950841A (zh) * | 2019-11-22 | 2020-04-03 | 济南大学 | 一类新型三唑类化合物的合成及应用 |
| CN111018832A (zh) * | 2019-11-26 | 2020-04-17 | 济南大学 | 一类含有四氢异喹啉结构的咪唑酮类化合物的制备及应用 |
| KR102514245B1 (ko) * | 2019-12-03 | 2023-03-29 | 한양대학교 에리카산학협력단 | 단백질 인산화 효소 저해 활성을 갖는 신규한 피라졸 유도체 및 이의 용도 |
| EP4069698A1 (en) | 2019-12-03 | 2022-10-12 | Lupin Limited | Substituted nucleoside analogs as prmt5 inhibitors |
| US20230108114A1 (en) * | 2019-12-17 | 2023-04-06 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
| WO2021126731A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| UA129208C2 (uk) | 2019-12-19 | 2025-02-05 | Янссен Фармацевтика Нв | Заміщені спіропохідні з прямим ланцюгом |
| CN113045543B (zh) * | 2019-12-26 | 2023-05-12 | 石药集团中奇制药技术(石家庄)有限公司 | 一种prmt5抑制剂及其应用 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| KR20230012041A (ko) * | 2020-06-02 | 2023-01-25 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | 3,4-디하이드로이소퀴놀린계 화합물 및 그 사용 |
| CN113754541B (zh) * | 2020-06-02 | 2025-01-03 | 深圳湾实验室 | 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用 |
| CN111592522B (zh) * | 2020-06-17 | 2022-09-09 | 郑州大学 | 一种精氨酸甲基化转移酶5小分子抑制剂及其制备方法和用途 |
| IL300147A (en) | 2020-07-31 | 2023-03-01 | Tango Therapeutics Inc | History Piperidin-1-yl-N-pyridin-3-yl-2-oxaacetamide is useful for the treatment of MTAP-deficient and/or MTA-accumulating cancer |
| JP2023540548A (ja) * | 2020-09-04 | 2023-09-25 | イノブストーン セラピューティクス リミテッド | 抗腫瘍活性を有する化合物及びその使用 |
| WO2022063094A1 (zh) | 2020-09-22 | 2022-03-31 | 南京明德新药研发有限公司 | 四氢异喹啉衍生物及其应用 |
| US20250206717A1 (en) | 2021-05-13 | 2025-06-26 | Innovstone Therapeutics Limited | Compound having anti-tumor activity and use thereof |
| GB202117230D0 (en) | 2021-11-29 | 2022-01-12 | Argonaut Therapeutics Ltd | Peptide vaccine |
| CA3240466A1 (en) | 2021-12-08 | 2023-06-15 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | Salt of 3,4-dihydroisoquinoline compound and use thereof |
| GB202203588D0 (en) | 2022-03-15 | 2022-04-27 | Argonaut Therapeutics Ltd | Cancer diagnostic |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| CN119101034B (zh) * | 2023-06-07 | 2025-10-17 | 石药集团中奇制药技术(石家庄)有限公司 | 固体形式的3,4-二氢异喹啉类化合物及其制备方法和用途 |
| CN119101035B (zh) * | 2023-06-07 | 2025-10-17 | 石药集团中奇制药技术(石家庄)有限公司 | 3,4-二氢异喹啉类化合物的盐及其制备方法和用途 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1370170A (zh) * | 1999-05-25 | 2002-09-18 | 宾夕法尼亚州研究基金会 | Dna甲基转移酶抑制剂 |
| CN101157929A (zh) * | 2007-02-02 | 2008-04-09 | 中国科学院上海有机化学研究所 | 番红霉素的生物合成基因簇 |
| CN102099338A (zh) * | 2008-07-18 | 2011-06-15 | 国家科学研究中心 | 用于治疗神经退行性疾病的杂环衍生物 |
| WO2011079236A1 (en) * | 2009-12-22 | 2011-06-30 | The Ohio State University Research Foundation | Compositions and methods for cancer detection and treatment |
Family Cites Families (179)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE63776C (de) | A. RUPERT, Eisenbahn - Werkmeister, in Köln - Nippes, Escherstrafse 14 | Verfahren und Vorrichtung eiserne Rohrwände mit Messing zu überziehen | ||
| DD68906A (enExample) | ||||
| GB1374366A (en) | 1972-07-21 | 1974-11-20 | Science Union & Cie | Propanol derivatives and a process for their preparation |
| DE2361390A1 (de) * | 1973-12-10 | 1975-06-19 | Merck Patent Gmbh | Isochinolinderivate und verfahren zu ihrer herstellung |
| US4026897A (en) | 1974-01-31 | 1977-05-31 | Otsuka Pharmaceutical Company | 5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-hydroxycarbostyril derivatives |
| CA1072359A (en) | 1974-10-08 | 1980-02-26 | Hiroyuki Konishi | Method for controlling the growth of plants |
| HU179951B (en) | 1979-10-11 | 1983-01-28 | Chinoin Gyogyszer Es Vegyeszet | Process for preparing 1,2,4-oxadiazolin-5-one derivatives and pharmaceutical compositions containing thereof |
| US4270537A (en) | 1979-11-19 | 1981-06-02 | Romaine Richard A | Automatic hypodermic syringe |
| NZ204589A (en) | 1982-06-16 | 1985-12-13 | May & Baker Ltd | 3-(n,n-dimethylcarbamoyl)-pyrazolo(1,5-a)pyridine and pharmaceutical compositions |
| DE3303344A1 (de) | 1983-02-02 | 1984-08-02 | Hoechst Ag, 6230 Frankfurt | Verfahren zur herstellung von n-alkylierten aminosaeuren und deren estern |
| US4684459A (en) | 1985-11-29 | 1987-08-04 | The Dow Chemical Company | Collector compositions for the froth flotation of mineral values |
| US4596556A (en) | 1985-03-25 | 1986-06-24 | Bioject, Inc. | Hypodermic injection apparatus |
| JPH07100688B2 (ja) * | 1986-02-12 | 1995-11-01 | 大日本製薬株式会社 | 環状アミン誘導体 |
| DE3631013A1 (de) * | 1986-09-12 | 1988-03-24 | Thomae Gmbh Dr K | Neue naphthylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| DE3640641A1 (de) | 1986-11-28 | 1988-07-14 | Thomae Gmbh Dr K | Neue heteroaromatische aminderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| US4886499A (en) | 1986-12-18 | 1989-12-12 | Hoffmann-La Roche Inc. | Portable injection appliance |
| GB8704027D0 (en) | 1987-02-20 | 1987-03-25 | Owen Mumford Ltd | Syringe needle combination |
| US4746655A (en) | 1987-06-10 | 1988-05-24 | A. H. Robins Company, Incorporated | Fused aromatic-spiropiperidine oxazepinones(and thiones) |
| US4941880A (en) | 1987-06-19 | 1990-07-17 | Bioject, Inc. | Pre-filled ampule and non-invasive hypodermic injection device assembly |
| US4940460A (en) | 1987-06-19 | 1990-07-10 | Bioject, Inc. | Patient-fillable and non-invasive hypodermic injection device assembly |
| US4790824A (en) | 1987-06-19 | 1988-12-13 | Bioject, Inc. | Non-invasive hypodermic injection device |
| DE3804793A1 (de) | 1988-02-16 | 1989-08-24 | Hoechst Ag | Renin-hemmende aminosaeurederivate |
| US5339163A (en) | 1988-03-16 | 1994-08-16 | Canon Kabushiki Kaisha | Automatic exposure control device using plural image plane detection areas |
| FR2638359A1 (fr) | 1988-11-03 | 1990-05-04 | Tino Dalto | Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau |
| DE3839126A1 (de) | 1988-11-19 | 1990-05-23 | Hoechst Ag | Renin-hemmende harnstoffderivate von dipeptiden, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung |
| US5776963A (en) | 1989-05-19 | 1998-07-07 | Hoechst Marion Roussel, Inc. | 3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility |
| US5312335A (en) | 1989-11-09 | 1994-05-17 | Bioject Inc. | Needleless hypodermic injection device |
| US5064413A (en) | 1989-11-09 | 1991-11-12 | Bioject, Inc. | Needleless hypodermic injection device |
| GB9005318D0 (en) | 1990-03-09 | 1990-05-02 | Isis Innovation | Antiarrhythmic agents |
| US5190521A (en) | 1990-08-22 | 1993-03-02 | Tecnol Medical Products, Inc. | Apparatus and method for raising a skin wheal and anesthetizing skin |
| US5527288A (en) | 1990-12-13 | 1996-06-18 | Elan Medical Technologies Limited | Intradermal drug delivery device and method for intradermal delivery of drugs |
| AU2228992A (en) | 1991-07-08 | 1993-02-11 | Glaxo Group Limited | Thiazolidine derivatives and their use as anti-viral compounds |
| GB9118204D0 (en) | 1991-08-23 | 1991-10-09 | Weston Terence E | Needle-less injector |
| SE9102652D0 (sv) | 1991-09-13 | 1991-09-13 | Kabi Pharmacia Ab | Injection needle arrangement |
| US5328483A (en) | 1992-02-27 | 1994-07-12 | Jacoby Richard M | Intradermal injection device with medication and needle guard |
| DK0649410T3 (da) | 1992-07-10 | 1997-09-15 | Glaxo Lab Sa | Anilidderivater. |
| US5383851A (en) | 1992-07-24 | 1995-01-24 | Bioject Inc. | Needleless hypodermic injection device |
| US5514694A (en) | 1992-09-21 | 1996-05-07 | Georgia Tech Research Corp | Peptidyl ketoamides |
| US5569189A (en) | 1992-09-28 | 1996-10-29 | Equidyne Systems, Inc. | hypodermic jet injector |
| US5294621A (en) | 1992-10-07 | 1994-03-15 | Ortho Pharmaceutical Corporation | Thieno tetrahydropyridines useful as class III antiarrhythmic agents |
| US5334144A (en) | 1992-10-30 | 1994-08-02 | Becton, Dickinson And Company | Single use disposable needleless injector |
| GB9402807D0 (en) * | 1994-02-14 | 1994-04-06 | Xenova Ltd | Pharmaceutical compounds |
| WO1995024176A1 (en) | 1994-03-07 | 1995-09-14 | Bioject, Inc. | Ampule filling device |
| US5466220A (en) | 1994-03-08 | 1995-11-14 | Bioject, Inc. | Drug vial mixing and transfer device |
| US5599302A (en) | 1995-01-09 | 1997-02-04 | Medi-Ject Corporation | Medical injection system and method, gas spring thereof and launching device using gas spring |
| US5693847A (en) | 1995-04-19 | 1997-12-02 | Vertex Pharmaceuticals Incorporated | Heteroatom functionalized α-methyl ketones |
| US5730723A (en) * | 1995-10-10 | 1998-03-24 | Visionary Medical Products Corporation, Inc. | Gas pressured needle-less injection device and method |
| US5554621A (en) * | 1995-06-07 | 1996-09-10 | Bristol-Myers Squibb Company | Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives |
| US6130217A (en) | 1995-09-20 | 2000-10-10 | Pfizer Inc | Compounds enhancing antitumor activity of other cytotoxic agents |
| US5893397A (en) | 1996-01-12 | 1999-04-13 | Bioject Inc. | Medication vial/syringe liquid-transfer apparatus |
| SE9600769D0 (sv) | 1996-02-28 | 1996-02-28 | Astra Ab | Compounds useful as analgesic |
| GB9607549D0 (en) * | 1996-04-11 | 1996-06-12 | Weston Medical Ltd | Spring-powered dispensing device |
| GB9717576D0 (en) | 1997-08-19 | 1997-10-22 | Xenova Ltd | Pharmaceutical compounds |
| US5874449A (en) | 1996-12-31 | 1999-02-23 | Gpi Nil Holdings, Inc. | N-linked sulfonamides of heterocyclic thioesters |
| US5993412A (en) | 1997-05-19 | 1999-11-30 | Bioject, Inc. | Injection apparatus |
| IT1298087B1 (it) | 1998-01-08 | 1999-12-20 | Fiderm S R L | Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni |
| US20020169101A1 (en) | 1999-05-10 | 2002-11-14 | Gonzalez Maria Isabel | Treatment of sexual dysfunction |
| IL148622A0 (en) | 1999-09-14 | 2002-09-12 | Aventis Pharm Prod Inc | Benzisoxazolyl-pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as d4 antagonists |
| US7125903B1 (en) | 1999-09-14 | 2006-10-24 | Aventis Pharmaceuticals Inc. | Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists |
| KR20020027647A (ko) | 1999-09-14 | 2002-04-13 | 게리 디. 스트리트, 스티븐 엘. 네스비트 | D4 길항제로서 유용한, 티에노이속사졸릴- 및티에닐피라졸릴-페녹시 치환된 프로필 유도체 |
| US7253165B2 (en) | 1999-09-14 | 2007-08-07 | Aventis Pharmaceuticals Inc. | Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists |
| MXPA02008797A (es) | 2000-03-14 | 2005-09-08 | Actelion Pharmaceuticals Ltd | Derivados de 1,2,3,4-tetrahidroisoquinolina. |
| WO2002014277A1 (en) | 2000-08-10 | 2002-02-21 | Tanabe Seiyaku Co., Ltd. | Biphenylcarboxamidoisoindoline compounds, processes for the preparation of the same and intermediates for the synthesis thereof |
| JP2004529132A (ja) * | 2001-03-27 | 2004-09-24 | アクテリオン ファマシューティカルズ リミテッド | 1,2,3,4−テトラヒドロイソキノリン誘導体 |
| MXPA04000334A (es) | 2001-07-11 | 2004-09-28 | Elan Pharm Inc | Compuestos de alquilamida n-(3-amino-2-hidroxi-propil) substituidos. |
| MXPA04001773A (es) | 2001-08-27 | 2004-05-31 | Arpida Ag | Derivados de 6,7-dihidroxitetrahidroisquinolinas 3-sustituidas parta uso como agentes antibacterianos. |
| TWI259081B (en) | 2001-10-26 | 2006-08-01 | Sugen Inc | Treatment of acute myeloid leukemia with indolinone compounds |
| SE0103644D0 (sv) | 2001-11-01 | 2001-11-01 | Astrazeneca Ab | Therapeutic isoquinoline compounds |
| IL161881A0 (en) | 2001-11-08 | 2005-11-20 | Upjohn Co | N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives |
| US7335779B2 (en) | 2002-03-08 | 2008-02-26 | Quonova, Llc | Modulation of pathogenicity |
| US7338969B2 (en) | 2002-03-08 | 2008-03-04 | Quonova, Llc | Modulation of pathogenicity |
| CA2479618A1 (en) | 2002-03-26 | 2003-10-09 | William K. Hagmann | Spirocyclic amides as cannabinoid receptor modulators |
| CA2480856A1 (en) | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Substituted aryl amides |
| US8013014B2 (en) | 2002-07-05 | 2011-09-06 | Georgia Tech Research Corporation | Aza-peptide epoxides |
| MXPA05002622A (es) | 2002-09-09 | 2005-09-08 | Johnson & Johnson | Derivados de 1,3,8,-triazaespiro [4.5]decan-4-ona sustituidos con hidroxialquilo utiles para el tratamiento de desordenes mediados por el receptor opioide huerfano. |
| SE0300010D0 (sv) | 2003-01-07 | 2003-01-07 | Astrazeneca Ab | Novel Compounds |
| EP1603884A4 (en) | 2003-02-28 | 2008-05-28 | Encysive Pharmaceuticals Inc | PYRIDINE, PYRIMIDINE, QUINOLINE, QUINAZOLINE AND NAPHTHALENE UROTENSIN II RECEPTOR ANTAGONISTS |
| WO2004078731A1 (en) * | 2003-03-06 | 2004-09-16 | 'chemical Diversity Research Institute', Ltd. | Quinoline-carboxylic acids and the derivatives thereof, a focused library |
| US7408008B2 (en) | 2003-12-09 | 2008-08-05 | Janssen Pharmaceutica, N.V. | Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support |
| JP2007526324A (ja) | 2004-03-02 | 2007-09-13 | スミスクライン・ビーチャム・コーポレイション | Akt活性のある阻害剤 |
| EP1735293A2 (en) | 2004-03-09 | 2006-12-27 | Elan Pharmaceuticals, Inc. | Substituted hydroxyethylamine aspartyl protease inhibitors |
| RU2266906C1 (ru) * | 2004-04-29 | 2005-12-27 | Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") | Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека |
| WO2005118543A1 (ja) | 2004-06-03 | 2005-12-15 | Ono Pharmaceutical Co., Ltd. | キナーゼ阻害薬およびその用途 |
| US8071624B2 (en) | 2004-06-24 | 2011-12-06 | Incyte Corporation | N-substituted piperidines and their use as pharmaceuticals |
| US20060009510A1 (en) | 2004-07-09 | 2006-01-12 | Pharmacia & Upjohn Company Llc | Method of synthesizing indolinone compounds |
| JP2008007405A (ja) * | 2004-12-07 | 2008-01-17 | Takeda Chem Ind Ltd | カルボキサミド誘導体 |
| US20100190788A1 (en) | 2005-07-11 | 2010-07-29 | Olivier Defert | Amide derivatives as kinase inhitors |
| EP1910317B1 (en) | 2005-07-20 | 2013-07-03 | Eli Lilly And Company | 1-amino linked compounds |
| GB0516723D0 (en) | 2005-08-15 | 2005-09-21 | Novartis Ag | Organic compounds |
| WO2007048042A2 (en) | 2005-10-21 | 2007-04-26 | University Of Alabama At Birmingham | Small molecule inhibitors of hiv-1 capsid assembly |
| EP1989188B1 (en) | 2006-02-28 | 2015-07-22 | Dart Neuroscience (Cayman) Ltd | Therapeutic piperazines as pde4 inhibitors |
| ES2569677T3 (es) | 2006-03-16 | 2016-05-12 | Second Genome, Inc. | Compuestos bicicloheteroarilo como moduladores de P2X7 y usos de los mismos |
| EP2027260B1 (en) | 2006-05-05 | 2013-12-11 | Cambridge Enterprise Limited | Epigenetic regulatory complex for control of gene expression |
| EP2394647A1 (en) | 2006-11-02 | 2011-12-14 | Aestus Therapeutics, Inc. | Methods of treating neuropathic pain by modulation of glycogenolysis or glycolysis pathways |
| CN101012223A (zh) | 2006-11-13 | 2007-08-08 | 西安新安医药科技有限公司 | 用于治疗的奥硝唑衍生物、制备方法及用途 |
| WO2008067756A1 (fr) | 2006-12-04 | 2008-06-12 | Jiangsu Simcere Pharmaceutical R & D Co., Ltd. | Dérivés de 3-pyrrolo-cyclohexylène-2-dihydro-indolinone et utilisations de ceux-ci |
| US20090099157A1 (en) | 2007-02-15 | 2009-04-16 | Ameriks Michael K | Tetrahydro-pyrazolo-pyridine thioether modulators of cathepsin s |
| US8338437B2 (en) | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| EP2143714B1 (en) * | 2007-04-04 | 2013-06-05 | Kowa Company, Ltd. | Tetrahydroisoquinoline compound |
| DE102007020492A1 (de) | 2007-04-30 | 2008-11-06 | Grünenthal GmbH | Substituierte Sulfonamid-Derivate |
| WO2008145398A1 (en) | 2007-06-01 | 2008-12-04 | Pfizer Italia S.R.L. | 4-arylpyrrole substituted 2-indoline derivatives active as protein kinase inhibitors |
| WO2008148159A1 (en) | 2007-06-07 | 2008-12-11 | Simons Haplomics Limited | Epigenetic methods |
| AU2008261951A1 (en) | 2007-06-08 | 2008-12-18 | Asuragen, Inc. | miR-34 regulated genes and pathways as targets for therapeutic intervention |
| EP2014651A1 (en) | 2007-07-12 | 2009-01-14 | Exonhit Therapeutics SA | Compounds and methods for modulating Rho GTPases |
| RU2345996C1 (ru) * | 2007-07-17 | 2009-02-10 | Андрей Александрович Иващенко | Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения |
| NZ562237A (en) | 2007-10-05 | 2011-02-25 | Pacific Edge Biotechnology Ltd | Proliferation signature and prognosis for gastrointestinal cancer |
| US20090093493A1 (en) | 2007-10-09 | 2009-04-09 | Francesco Berardi | 1-phenylalcoxy-2-beta-phenylethyl derivatives as p-glycoprotein (p-gp) inhibitors useful in drug resistance events |
| MX2010004718A (es) | 2007-11-01 | 2010-07-28 | Acucela Inc | Compuestos derivados de amina para tratar enfermedades y trastornos oftalmicos. |
| US8722851B2 (en) | 2007-11-02 | 2014-05-13 | Pain Therapeutics, Inc. | Analgesia with minimal tolerance and dependence by a mu opioid receptor agonist that also binds filamin A |
| JP2011507910A (ja) | 2007-12-21 | 2011-03-10 | ユニバーシティー オブ ロチェスター | 真核生物の寿命を変更するための方法 |
| RU2371444C1 (ru) * | 2008-01-24 | 2009-10-27 | Андрей Александрович Иващенко | ФУРО- И ТИЕНО[2,3-b]-ХИНОЛИН-2-КАРБОКСАМИДЫ, СПОСОБ ПОЛУЧЕНИЯ И ПРОТИВОТУБЕРКУЛЕЗНАЯ АКТИВНОСТЬ |
| WO2009126782A1 (en) | 2008-04-11 | 2009-10-15 | High Point Pharmaceuticals, Llc | Histamine h3 receptor ligands |
| EP2307345A4 (en) | 2008-07-01 | 2012-05-02 | Purdue Research Foundation | NON-PEPTIDINHIBITORS OF HIV-1 PROTEASE |
| NZ592057A (en) | 2008-09-05 | 2013-01-25 | Acucela Inc | Sulfur-linked compounds for treating opthalmic diseases and disorders |
| BRPI0919920A2 (pt) | 2008-10-22 | 2016-02-16 | Acucela Inc | compostos para tratamento de doenças e desordens oftálmicas |
| WO2010057101A2 (en) | 2008-11-17 | 2010-05-20 | Schering Corporation | Compounds useful as hiv blockers |
| NZ595723A (en) | 2009-03-17 | 2012-10-26 | Daiichi Sankyo Co Ltd | Amide derivative |
| US8309547B2 (en) | 2009-04-28 | 2012-11-13 | Apotex Pharmachem Inc. | Processes for the preparation of rivaroxaban and intermediates thereof |
| KR20120018224A (ko) | 2009-06-09 | 2012-02-29 | 아브락시스 바이오사이언스, 엘엘씨 | 헷지호그 신호전달 억제제로서의 이소퀴놀린, 퀴놀린 및 퀴나졸린 유도체 |
| WO2011008260A2 (en) | 2009-07-13 | 2011-01-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| GB0922332D0 (en) | 2009-12-22 | 2010-02-03 | Isis Innovation | Method of treatment and screening method |
| US20110177105A1 (en) * | 2010-01-15 | 2011-07-21 | Roman Lopez | Novel Selective Inhibitors of Ubiquitin Specific Protease 7, the Pharmaceutical Compositions Thereof and Their Therapeutic Applications |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| TWI513694B (zh) | 2010-05-11 | 2015-12-21 | Amgen Inc | 抑制間變性淋巴瘤激酶的嘧啶化合物 |
| JOP20190250A1 (ar) | 2010-07-14 | 2017-06-16 | Regeneron Pharma | صيغ مستقرة تحتوي على الأجسام المضادة لمضاد عامل نمو الأعصاب |
| EP2630143B1 (en) | 2010-10-18 | 2017-11-29 | Apotex Pharmachem Inc. | Processes for the preparation of rivaroxaban and intermediates thereof |
| WO2012054896A1 (en) | 2010-10-22 | 2012-04-26 | Biotime Inc. | Methods of modifying transcriptional regulatory networks in stem cells |
| BR112013013668A2 (pt) | 2010-12-03 | 2016-09-06 | Epizyme Inc | moduladores 7-deazapurina de histona metiltransferase, e métodos de uso dos mesmos |
| US9029343B2 (en) | 2010-12-03 | 2015-05-12 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| CA2826238A1 (en) | 2011-03-25 | 2012-10-04 | Almac Sciences (Scotland) Limited | Enzyme assays |
| WO2012149493A2 (en) | 2011-04-28 | 2012-11-01 | Sloan-Kettering Institute For Cancer Research | Hsp90 combination therapy |
| KR102025142B1 (ko) | 2011-07-08 | 2019-09-26 | 슬로안-케테링인스티튜트퍼캔서리서치 | 표지된 hsp90 억제제의 용도 |
| WO2013038378A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine amide derivatives |
| WO2013038381A1 (en) | 2011-09-16 | 2013-03-21 | Novartis Ag | Pyridine/pyrazine amide derivatives |
| WO2013052505A2 (en) | 2011-10-03 | 2013-04-11 | Celmatix, Inc. | Methods and devices for assessing risk to a putative offspring of developing a condition |
| TWI577671B (zh) | 2011-11-14 | 2017-04-11 | Sunshine Lake Pharma Co Ltd | Aminoquinazoline derivatives and salts thereof and methods of use thereof |
| US10214476B2 (en) | 2011-12-30 | 2019-02-26 | Ecole Nationale Superieure De Chimie De Clermont Ferrand | Pain relief compounds |
| EP3470073A1 (en) | 2012-04-03 | 2019-04-17 | Reneuron Limited | Stem cell microparticles |
| EP2872899B1 (en) | 2012-07-13 | 2018-07-11 | Pain Therapeutics, Inc. | Alzheimer's disease assay in a living patient |
| AU2013291761B2 (en) | 2012-07-19 | 2018-03-15 | Reneuron Limited | Stem cell microparticles |
| US9585891B2 (en) | 2012-09-25 | 2017-03-07 | Merck Patent Gmbh | Alpha hydroxy amides |
| CN110898067A (zh) | 2012-10-15 | 2020-03-24 | Epizyme股份有限公司 | 癌症治疗方法 |
| EP2925301A4 (en) | 2012-11-29 | 2016-06-01 | Penn State Res Found | THERAPEUTIC PRODUCT AND ANTI-CANCER IMMUNOMODULATOR DHS1P PHOTODYNAMIC |
| US8906900B2 (en) | 2012-12-21 | 2014-12-09 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| CA2894230A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Methods of inhibiting prmt5 |
| CA2894157A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP2935243B1 (en) | 2012-12-21 | 2018-03-14 | Epizyme, Inc. | Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
| CA2899363A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| SI2935222T1 (sl) | 2012-12-21 | 2019-02-28 | Epizyme Inc. | Inhibitorji PRMT5 in njihove uporabe |
| BR112015022785A2 (pt) | 2013-03-14 | 2017-07-18 | Epizyme Inc | composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt |
| WO2014153090A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives asprmt1 inhibitors and uses thereof |
| WO2014153100A2 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014178954A1 (en) | 2013-03-14 | 2014-11-06 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153172A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9765035B2 (en) | 2013-03-14 | 2017-09-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9133189B2 (en) | 2013-03-14 | 2015-09-15 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9738651B2 (en) | 2013-03-15 | 2017-08-22 | Epizyme, Inc. | CARM1 inhibitors and uses thereof |
| US9346802B2 (en) | 2013-03-15 | 2016-05-24 | Epizyme, Inc. | CARM1 inhibitors and uses thereof |
| WO2014144455A1 (en) | 2013-03-15 | 2014-09-18 | Epizyme, Inc. | 1 -phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof |
| JP6113354B2 (ja) | 2013-05-03 | 2017-04-12 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 神経新生刺激イソキノリン誘導体 |
| EP3160477A4 (en) | 2014-06-25 | 2018-07-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| SMT202100260T1 (it) | 2014-06-25 | 2021-07-12 | Glaxosmithkline Ip Dev Ltd | Sali cristallini di (s)-6-((1-acetilpiperidin-4-il)ammino)-n-(3-(3,4-diidroisochinolin-2(1h)-il)-2-idrossipropil) pirimidin-4-carbossammide. |
| WO2015200677A2 (en) | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP3177288A4 (en) | 2014-08-04 | 2018-04-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| WO2016044604A1 (en) | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
| US20170283400A1 (en) | 2014-09-17 | 2017-10-05 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2016044576A1 (en) | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Salts, co-crystals, amorphous forms, and crystalline forms of an arginine methyltransferase inhibitor |
| JP2017527594A (ja) | 2014-09-17 | 2017-09-21 | エピザイム,インコーポレイティド | コアクチベーター関連アルギニンメチルトランスフェラーゼ1(carm1)阻害剤の塩、共結晶、非晶質形態、および結晶形態 |
| US20170280720A1 (en) | 2014-09-17 | 2017-10-05 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US20170291905A1 (en) | 2014-09-17 | 2017-10-12 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US20170283440A1 (en) | 2014-09-17 | 2017-10-05 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
| WO2016044641A2 (en) | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
| JP2018505207A (ja) | 2015-02-11 | 2018-02-22 | バジリア・ファルマスーチカ・インターナショナル・アーゲーBasilea Pharmaceutica International Ag | 置換モノおよびポリアザナフタレン誘導体およびその使用 |
| WO2017136699A1 (en) | 2016-02-05 | 2017-08-10 | Epizyme, Inc | Arginine methyltransferase inhibitors and uses thereof |
| AR108326A1 (es) | 2016-04-27 | 2018-08-08 | Samumed Llc | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas |
| GB201704476D0 (en) | 2017-03-21 | 2017-05-03 | Antabio Sas | Chemical compounds |
-
2013
- 2013-12-20 SI SI201331283T patent/SI2935222T1/sl unknown
- 2013-12-20 RS RS20181485A patent/RS58040B1/sr unknown
- 2013-12-20 PT PT13821599T patent/PT2935222T/pt unknown
- 2013-12-20 PE PE2015001047A patent/PE20151501A1/es unknown
- 2013-12-20 EP EP23156656.3A patent/EP4219465A3/en active Pending
- 2013-12-20 MY MYPI2015001447A patent/MY199894A/en unknown
- 2013-12-20 PL PL13821599T patent/PL2935222T3/pl unknown
- 2013-12-20 EP EP13821599.1A patent/EP2935222B1/en active Active
- 2013-12-20 EP EP18192271.7A patent/EP3498701B1/en active Active
- 2013-12-20 KR KR1020157019530A patent/KR102024417B1/ko active Active
- 2013-12-20 US US14/136,569 patent/US8993555B2/en active Active
- 2013-12-20 CN CN201380070441.2A patent/CN105452226B/zh active Active
- 2013-12-20 CA CA2894228A patent/CA2894228C/en active Active
- 2013-12-20 WO PCT/US2013/077235 patent/WO2014100719A2/en not_active Ceased
- 2013-12-20 HR HRP20182037TT patent/HRP20182037T1/hr unknown
- 2013-12-20 EA EA201590975A patent/EA027908B1/ru unknown
- 2013-12-20 JP JP2015549821A patent/JP6678455B2/ja active Active
- 2013-12-20 MX MX2015008052A patent/MX375184B/es active IP Right Grant
- 2013-12-20 KR KR1020197027023A patent/KR102173874B1/ko active Active
- 2013-12-20 ES ES13821599T patent/ES2701069T3/es active Active
- 2013-12-20 BR BR112015014590-6A patent/BR112015014590B1/pt active IP Right Grant
- 2013-12-20 US US14/654,253 patent/US9604930B2/en active Active
- 2013-12-20 SM SM20180669T patent/SMT201800669T1/it unknown
- 2013-12-20 UA UAA201505700A patent/UA118548C2/uk unknown
- 2013-12-20 LT LTEP13821599.1T patent/LT2935222T/lt unknown
- 2013-12-20 DK DK13821599.1T patent/DK2935222T3/en active
- 2013-12-20 HU HUE13821599A patent/HUE040323T2/hu unknown
-
2015
- 2015-02-11 US US14/619,371 patent/US9365519B2/en active Active
- 2015-06-09 IL IL239296A patent/IL239296B/en active IP Right Grant
- 2015-06-15 PH PH12015501351A patent/PH12015501351A1/en unknown
- 2015-06-19 CL CL2015001790A patent/CL2015001790A1/es unknown
- 2015-06-19 DO DO2015000158A patent/DOP2015000158A/es unknown
- 2015-07-13 CR CR20150371A patent/CR20150371A/es unknown
- 2015-07-20 ZA ZA2015/05212A patent/ZA201505212B/en unknown
-
2016
- 2016-02-26 US US15/054,193 patent/US9675614B2/en active Active
-
2017
- 2017-01-30 US US15/419,260 patent/US10307413B2/en active Active
- 2017-05-04 US US15/586,775 patent/US20180098987A1/en not_active Abandoned
- 2017-12-15 US US15/844,097 patent/US10391089B2/en active Active
-
2018
- 2018-03-26 AU AU2018202150A patent/AU2018202150B2/en active Active
- 2018-07-30 IL IL260876A patent/IL260876B/en active IP Right Grant
- 2018-12-05 CY CY20181101294T patent/CY1121625T1/el unknown
-
2019
- 2019-01-23 PH PH12019500163A patent/PH12019500163A1/en unknown
- 2019-04-26 US US16/395,844 patent/US20190343826A1/en not_active Abandoned
- 2019-06-16 IL IL267364A patent/IL267364A/en unknown
- 2019-07-08 US US16/504,910 patent/US10980794B2/en active Active
-
2021
- 2021-03-02 US US17/189,989 patent/US20210308121A1/en not_active Abandoned
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1370170A (zh) * | 1999-05-25 | 2002-09-18 | 宾夕法尼亚州研究基金会 | Dna甲基转移酶抑制剂 |
| CN101157929A (zh) * | 2007-02-02 | 2008-04-09 | 中国科学院上海有机化学研究所 | 番红霉素的生物合成基因簇 |
| CN102099338A (zh) * | 2008-07-18 | 2011-06-15 | 国家科学研究中心 | 用于治疗神经退行性疾病的杂环衍生物 |
| WO2011079236A1 (en) * | 2009-12-22 | 2011-06-30 | The Ohio State University Research Foundation | Compositions and methods for cancer detection and treatment |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN105452226B (zh) | 四氢‑和二氢‑异喹啉prmt5抑制剂及其用途 | |
| EP2935243B1 (en) | Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof | |
| EP2935247B1 (en) | Prmt5 inhibitors and uses thereof | |
| CN110546133A (zh) | 抗纤维化化合物 | |
| HK1212690B (en) | Prmt5 inhibitors and uses thereof | |
| AU2013364163A1 (en) | Teatrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof | |
| AU2013364037A1 (en) | PRMT5 inhibitors and uses thereof | |
| AU2013364033A1 (en) | PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |