CA2773848A1 - Pi3 kinase inhibitors and uses thereof - Google Patents
Pi3 kinase inhibitors and uses thereof Download PDFInfo
- Publication number
- CA2773848A1 CA2773848A1 CA2773848A CA2773848A CA2773848A1 CA 2773848 A1 CA2773848 A1 CA 2773848A1 CA 2773848 A CA2773848 A CA 2773848A CA 2773848 A CA2773848 A CA 2773848A CA 2773848 A1 CA2773848 A1 CA 2773848A1
- Authority
- CA
- Canada
- Prior art keywords
- ring
- nitrogen
- oxygen
- sulfur
- independently selected
- 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
- YJOFXSCEMRWZOX-UHFFFAOYSA-N CC(C)=CC(CCCC(NCC#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O Chemical compound CC(C)=CC(CCCC(NCC#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O YJOFXSCEMRWZOX-UHFFFAOYSA-N 0.000 description 2
- CYEZBBVQQVTBFJ-UHFFFAOYSA-N CC(C)=CC(CCc(cc1)ccc1C#Cc1cc(N2CCOCC2)nc(-c2c(cn[nH]3)c3ccc2)c1)=O Chemical compound CC(C)=CC(CCc(cc1)ccc1C#Cc1cc(N2CCOCC2)nc(-c2c(cn[nH]3)c3ccc2)c1)=O CYEZBBVQQVTBFJ-UHFFFAOYSA-N 0.000 description 2
- YWQHCFQXVKZVGY-UHFFFAOYSA-N CC(C)CC(CCc(cc1)ccc1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2C)c1)=O Chemical compound CC(C)CC(CCc(cc1)ccc1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2C)c1)=O YWQHCFQXVKZVGY-UHFFFAOYSA-N 0.000 description 2
- QDYWKFVJZQYBTD-UHFFFAOYSA-N Cc(nc(N)nc1)c1-c1nc(N2CCOCC2)cc(C(NCc(cc2)ccc2NC(C=C)=O)=O)c1 Chemical compound Cc(nc(N)nc1)c1-c1nc(N2CCOCC2)cc(C(NCc(cc2)ccc2NC(C=C)=O)=O)c1 QDYWKFVJZQYBTD-UHFFFAOYSA-N 0.000 description 2
- HJOSLZGXDBPWRH-ODCIPOBUSA-N C/C(/C(CCC(N1CCN(Cc2cc3nc(-c4c(cn[nH]5)c5ccc4)nc(N4CCOCC4)c3[s]2)CC1)=O)=O)=C\COC Chemical compound C/C(/C(CCC(N1CCN(Cc2cc3nc(-c4c(cn[nH]5)c5ccc4)nc(N4CCOCC4)c3[s]2)CC1)=O)=O)=C\COC HJOSLZGXDBPWRH-ODCIPOBUSA-N 0.000 description 1
- UYPWEJTZSBYEFO-BIMFAAKUSA-N C/C=C(\C)/C(CCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O Chemical compound C/C=C(\C)/C(CCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O UYPWEJTZSBYEFO-BIMFAAKUSA-N 0.000 description 1
- CPAFFGGNKKQMSS-DUXPYHPUSA-N C/C=C/C(CCC(N(CC1)CCC1(CCc1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)O)=O)=O Chemical compound C/C=C/C(CCC(N(CC1)CCC1(CCc1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)O)=O)=O CPAFFGGNKKQMSS-DUXPYHPUSA-N 0.000 description 1
- BLHFNSJUVSBBKQ-DUXPYHPUSA-N C/C=C/C(CCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O Chemical compound C/C=C/C(CCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O BLHFNSJUVSBBKQ-DUXPYHPUSA-N 0.000 description 1
- DNJQXVQDWPLYES-UHFFFAOYSA-N C=CC(N(CC1)CCC1(CC1)CCN1C(c1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)=O)=O Chemical compound C=CC(N(CC1)CCC1(CC1)CCN1C(c1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)=O)=O DNJQXVQDWPLYES-UHFFFAOYSA-N 0.000 description 1
- VGPRFBSTFWGPCJ-UHFFFAOYSA-N C=CC(N(CC1)CCC1N(CC1)CCN1C(c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O Chemical compound C=CC(N(CC1)CCC1N(CC1)CCN1C(c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O VGPRFBSTFWGPCJ-UHFFFAOYSA-N 0.000 description 1
- ZBEIOECWCODXII-UHFFFAOYSA-N C=CC(N(CC1)CCN1C(C1CCN(Cc2cc3nc(-c4cc(O)ccc4)nc(N4CCOCC4)c3[s]2)CC1)=O)=O Chemical compound C=CC(N(CC1)CCN1C(C1CCN(Cc2cc3nc(-c4cc(O)ccc4)nc(N4CCOCC4)c3[s]2)CC1)=O)=O ZBEIOECWCODXII-UHFFFAOYSA-N 0.000 description 1
- ACUFWIDQZSMZER-UHFFFAOYSA-N C=CC(N(CC1)CCN1C(CC1)CCC1(c1cc(nc(-c2cccc3c2cn[nH]3)nc2N3CCOCC3)c2[s]1)O)=O Chemical compound C=CC(N(CC1)CCN1C(CC1)CCC1(c1cc(nc(-c2cccc3c2cn[nH]3)nc2N3CCOCC3)c2[s]1)O)=O ACUFWIDQZSMZER-UHFFFAOYSA-N 0.000 description 1
- LGXKISSMIGDJRC-UHFFFAOYSA-N C=CC(NCC(N(CCC1)c2c1cccc2-c1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)=O)=O Chemical compound C=CC(NCC(N(CCC1)c2c1cccc2-c1cc(nc(-c2cccc(O)c2)nc2N3CCOCC3)c2[s]1)=O)=O LGXKISSMIGDJRC-UHFFFAOYSA-N 0.000 description 1
- AJGDDGZSHTUZQA-UHFFFAOYSA-N C=CC(NCC(N(CCc1c2)Cc1ccc2-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O Chemical compound C=CC(NCC(N(CCc1c2)Cc1ccc2-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O AJGDDGZSHTUZQA-UHFFFAOYSA-N 0.000 description 1
- XZWJLXZKOHSYDS-UHFFFAOYSA-N C=CC(Nc(cc1)ccc1C(N(CC1)CC=C1c1cc(nc(-c2cnc(N)nc2)nc2C3=CCOCC3)c2[s]1)=O)=O Chemical compound C=CC(Nc(cc1)ccc1C(N(CC1)CC=C1c1cc(nc(-c2cnc(N)nc2)nc2C3=CCOCC3)c2[s]1)=O)=O XZWJLXZKOHSYDS-UHFFFAOYSA-N 0.000 description 1
- ANHRRUPOZYHHDO-UHFFFAOYSA-N C=CC(Nc(cc1)ccc1OCc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O Chemical compound C=CC(Nc(cc1)ccc1OCc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O ANHRRUPOZYHHDO-UHFFFAOYSA-N 0.000 description 1
- BCXIDVLTCGSAPF-UHFFFAOYSA-N C=CC(Nc1ccc(CCNC(c2cc3nc(Cl)nc(N4CCOCC4)c3[s]2)=O)cc1)=O Chemical compound C=CC(Nc1ccc(CCNC(c2cc3nc(Cl)nc(N4CCOCC4)c3[s]2)=O)cc1)=O BCXIDVLTCGSAPF-UHFFFAOYSA-N 0.000 description 1
- BVNQYLHBTRKYEY-UHFFFAOYSA-N CC(C(CCC(NCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O)=O)=C Chemical compound CC(C(CCC(NCC(N1CCN(Cc2cc(nc(-c3cccc4c3cn[nH]4)nc3N4CCOCC4)c3[s]2)CC1)=O)=O)=O)=C BVNQYLHBTRKYEY-UHFFFAOYSA-N 0.000 description 1
- WNMYJECCBSIWSE-UHFFFAOYSA-N CC(C)=CC(C(N(CC1)CCN1C(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O)=O Chemical compound CC(C)=CC(C(N(CC1)CCN1C(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O)=O WNMYJECCBSIWSE-UHFFFAOYSA-N 0.000 description 1
- LFTFVABLKOGPGN-UHFFFAOYSA-N CC(C)=CC(C1(CC1)C(N(CC1)CC=C1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O Chemical compound CC(C)=CC(C1(CC1)C(N(CC1)CC=C1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O LFTFVABLKOGPGN-UHFFFAOYSA-N 0.000 description 1
- VUAPLIRXKFGYBA-UHFFFAOYSA-N CC(C)=CC(C1(CC1)C(N(CC1)CCC1(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O)=O Chemical compound CC(C)=CC(C1(CC1)C(N(CC1)CCC1(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O)=O VUAPLIRXKFGYBA-UHFFFAOYSA-N 0.000 description 1
- GWJFHFHYKFEFBU-UHFFFAOYSA-N CC(C)=CC(C1(CC1)C(N(CC1)CCC1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O Chemical compound CC(C)=CC(C1(CC1)C(N(CC1)CCC1C#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O)=O GWJFHFHYKFEFBU-UHFFFAOYSA-N 0.000 description 1
- ZRRUFHNORFGAEA-UHFFFAOYSA-N CC(C)=CC(CCC(NCc(cc1)ccc1-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O Chemical compound CC(C)=CC(CCC(NCc(cc1)ccc1-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O)=O ZRRUFHNORFGAEA-UHFFFAOYSA-N 0.000 description 1
- NSLRPIWQYUXUEA-UHFFFAOYSA-N CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c(c(C(F)(F)F)c2)cnc2N)c1)=O Chemical compound CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c(c(C(F)(F)F)c2)cnc2N)c1)=O NSLRPIWQYUXUEA-UHFFFAOYSA-N 0.000 description 1
- GMESVEOKCNUMKI-UHFFFAOYSA-N CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c2c(cn[nH]3)c3ccc2)c1)=O Chemical compound CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c2c(cn[nH]3)c3ccc2)c1)=O GMESVEOKCNUMKI-UHFFFAOYSA-N 0.000 description 1
- KTDVWQABRBXING-UHFFFAOYSA-N CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O Chemical compound CC(C)=CC(CCCCC#Cc1cc(N2CCOCC2)nc(-c2cnc(N)nc2)c1)=O KTDVWQABRBXING-UHFFFAOYSA-N 0.000 description 1
- QNDFPTGIHJMMPV-UHFFFAOYSA-N CC(C)=CC(CN(CC1)CCN1C(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O Chemical compound CC(C)=CC(CN(CC1)CCN1C(CC1)CCN1c1cc(-c2cnc(N)nc2)nc(N2CCOCC2)c1)=O QNDFPTGIHJMMPV-UHFFFAOYSA-N 0.000 description 1
- OSYKHUOOCVNKKI-UHFFFAOYSA-N CC(C)=CC(c1ccc(CCNC(c2cc(-c3c(C(F)(F)F)cc(N)nc3)nc(N3CCOCC3)c2)=O)cc1)=O Chemical compound CC(C)=CC(c1ccc(CCNC(c2cc(-c3c(C(F)(F)F)cc(N)nc3)nc(N3CCOCC3)c2)=O)cc1)=O OSYKHUOOCVNKKI-UHFFFAOYSA-N 0.000 description 1
- ILOHHBANDPCPHD-UHFFFAOYSA-N CC(C)=CC(c1ccc(CCNC(c2cc(-c3cnc(N)nc3)nc(N3CCOCC3)c2)=O)cc1)=O Chemical compound CC(C)=CC(c1ccc(CCNC(c2cc(-c3cnc(N)nc3)nc(N3CCOCC3)c2)=O)cc1)=O ILOHHBANDPCPHD-UHFFFAOYSA-N 0.000 description 1
- LYMNEWLGMQZYGW-QPJJXVBHSA-N CN(C)C/C=C/C(NC(CC1)CCN1c(cc1)ccc1-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O Chemical compound CN(C)C/C=C/C(NC(CC1)CCN1c(cc1)ccc1-c1cc(nc(-c2cc(O)ccc2)nc2N3CCOCC3)c2[s]1)=O LYMNEWLGMQZYGW-QPJJXVBHSA-N 0.000 description 1
- RBPOZJDRLNQAKJ-UHFFFAOYSA-N CN(Cc1cc2nc(-c3cc(O)ccc3)nc(N3CCOCC3)c2[s]1)C(C(CC1)CCC1NC(C=C)=O)=O Chemical compound CN(Cc1cc2nc(-c3cc(O)ccc3)nc(N3CCOCC3)c2[s]1)C(C(CC1)CCC1NC(C=C)=O)=O RBPOZJDRLNQAKJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Wood Science & Technology (AREA)
- Molecular Biology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Biotechnology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Microbiology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Communicable Diseases (AREA)
- Heart & Thoracic Surgery (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24094709P | 2009-09-09 | 2009-09-09 | |
| US61/240,947 | 2009-09-09 | ||
| US37139610P | 2010-08-06 | 2010-08-06 | |
| US61/371,396 | 2010-08-06 | ||
| PCT/US2010/048317 WO2011031896A2 (en) | 2009-09-09 | 2010-09-09 | Pi3 kinase inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2773848A1 true CA2773848A1 (en) | 2011-03-17 |
Family
ID=43733099
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2773848A Abandoned CA2773848A1 (en) | 2009-09-09 | 2010-09-09 | Pi3 kinase inhibitors and uses thereof |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20110230476A1 (enExample) |
| EP (1) | EP2475375A4 (enExample) |
| JP (1) | JP2013504325A (enExample) |
| KR (1) | KR20120063515A (enExample) |
| CN (1) | CN102625708A (enExample) |
| AU (1) | AU2010292198A1 (enExample) |
| BR (1) | BR112012008385A2 (enExample) |
| CA (1) | CA2773848A1 (enExample) |
| IL (1) | IL218555A0 (enExample) |
| MX (1) | MX339584B (enExample) |
| NZ (2) | NZ598808A (enExample) |
| PH (1) | PH12012500491A1 (enExample) |
| RU (1) | RU2595718C2 (enExample) |
| SG (2) | SG10201405598QA (enExample) |
| TW (2) | TW201609747A (enExample) |
| WO (1) | WO2011031896A2 (enExample) |
Families Citing this family (136)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101402474B1 (ko) * | 2006-04-26 | 2014-06-19 | 제넨테크, 인크. | 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
| EP2478361A4 (en) | 2009-09-16 | 2014-05-21 | Celgene Avilomics Res Inc | CONJUGATES AND INHIBITORS OF PROTEIN KINASE |
| WO2011060321A1 (en) | 2009-11-16 | 2011-05-19 | Chdi, Inc. | Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| CN102812167A (zh) | 2009-12-30 | 2012-12-05 | 阿维拉制药公司 | 蛋白的配体-介导的共价修饰 |
| JP6130305B2 (ja) | 2011-02-23 | 2017-05-17 | インテリカイン, エルエルシー | キナーゼ阻害剤の組み合わせおよびそれらの使用 |
| US20120258967A1 (en) * | 2011-03-09 | 2012-10-11 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| WO2012154608A1 (en) * | 2011-05-06 | 2012-11-15 | Intellikine, Llc | Reactive mtor and pi3 kinase inhibitors and uses thereof |
| WO2012154610A1 (en) * | 2011-05-06 | 2012-11-15 | Intellikine, Llc | Reactive pi3k kinase inhibitors and uses thereof |
| US8889716B2 (en) | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| AU2012283775A1 (en) | 2011-07-13 | 2014-01-23 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| MX342326B (es) | 2011-09-27 | 2016-09-26 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| WO2013144180A1 (en) * | 2012-03-28 | 2013-10-03 | Intervet International B.V. | Heteroaryl compounds with cyclic bridging unit for use in the treatment helminth infection |
| US20150087628A1 (en) | 2012-04-10 | 2015-03-26 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| US9879003B2 (en) | 2012-04-11 | 2018-01-30 | Dana-Farber Cancer Institute, Inc. | Host targeted inhibitors of dengue virus and other viruses |
| AU2013251475B2 (en) | 2012-04-26 | 2018-01-04 | The General Hospital Corporation | Agents and methods for treating and preventing seborrheic keratosis |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
| US20150204846A1 (en) * | 2012-05-15 | 2015-07-23 | New York University | Phosphatidylinositol-3-kinase c2 beta modulators and methods of use thereof |
| WO2014012093A1 (en) * | 2012-07-13 | 2014-01-16 | Wake Forest University Health Sciences | Prostate cancer targeted prodrugs and methods of use thereof |
| US9572811B2 (en) | 2012-08-03 | 2017-02-21 | Principia Biopharma Inc. | Treatment of dry eye |
| US11458199B2 (en) | 2012-08-21 | 2022-10-04 | Opko Pharmaceuticals, Llc | Liposome formulations |
| HUE058912T2 (hu) | 2012-08-21 | 2022-09-28 | Opko Pharmaceuticals Llc | Liposzóma készítmények |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| NZ708870A (en) | 2012-12-21 | 2016-09-30 | Gilead Calistoga Llc | Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors |
| JP6125663B2 (ja) | 2012-12-21 | 2017-05-10 | ギリアード カリストガ エルエルシー | ホスファチジルイノシトール3−キナーゼ阻害剤としての置換ピリミジンアミノアルキル−キナゾロン |
| WO2014130612A1 (en) * | 2013-02-20 | 2014-08-28 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| PE20151939A1 (es) | 2013-03-14 | 2016-01-08 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante |
| US10202356B2 (en) | 2013-03-14 | 2019-02-12 | Tolero Pharmaceuticals, Inc. | JAK2 and ALK2 inhibitors and methods for their use |
| TW201524952A (zh) * | 2013-03-15 | 2015-07-01 | Araxes Pharma Llc | Kras g12c之共價抑制劑 |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| CN105246482A (zh) * | 2013-03-15 | 2016-01-13 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| JP6378918B2 (ja) * | 2013-04-03 | 2018-08-22 | 株式会社ヤクルト本社 | チアゾリジン誘導体又はその塩を有効成分とするPim阻害剤 |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| MA42164B1 (fr) * | 2013-05-01 | 2019-12-31 | Hoffmann La Roche | Composes biheteroaryle et leurs utilisations |
| US10508309B2 (en) * | 2013-05-17 | 2019-12-17 | The General Hospital Corporation | Methods for detecting and treating variants of seborrheic keratoses |
| NZ714710A (en) | 2013-06-14 | 2016-11-25 | Gilead Sciences Inc | Phosphatidylinositol 3-kinase inhibitors |
| UY35675A (es) | 2013-07-24 | 2015-02-27 | Novartis Ag | Derivados sustituidos de quinazolin-4-ona |
| US9624224B2 (en) | 2013-09-30 | 2017-04-18 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| WO2015057655A1 (en) | 2013-10-14 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
| MD4635C1 (ro) | 2013-10-14 | 2020-01-31 | Eisai R&D Management Co., Ltd. | Compuşi de chinolină substituiţi selectiv |
| ES2676734T3 (es) * | 2013-10-18 | 2018-07-24 | Syros Pharmaceuticals, Inc. | Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas |
| AU2014352463B2 (en) * | 2013-11-20 | 2017-05-11 | Beijing Forelandpharma Co. Ltd. | Ketone derivatives of imidazoles, pharmaceutical combinations and uses thereof |
| KR102331833B1 (ko) | 2013-12-02 | 2021-11-25 | 케모센트릭스, 인크. | Ccr6 화합물 |
| KR20220027271A (ko) | 2014-02-21 | 2022-03-07 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| RU2704826C2 (ru) * | 2014-12-24 | 2019-10-31 | Китер Бьотек С.Р.Л. | НОВЫЙ ПЕПТИД-ИНГИБИТОР PI3Kγ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ОРГАНОВ ДЫХАНИЯ |
| EP3280708B1 (en) | 2015-04-10 | 2021-09-01 | Araxes Pharma LLC | Substituted quinazoline compounds and methods of use thereof |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| WO2016172952A1 (zh) | 2015-04-30 | 2016-11-03 | 江苏挪贝肽医药科技有限公司 | PI4KIIIα蛋白及相关的膜蛋白复合体在治疗阿尔茨海默病中的应用 |
| EP3297629A1 (en) | 2015-05-20 | 2018-03-28 | Novartis AG | Pharmaceutical combination of everolimus with dactolisib |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058792A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3364977A4 (en) | 2015-10-19 | 2019-09-04 | Araxes Pharma LLC | PROCESS FOR SCREENING INHIBITORS OF RAS |
| EA038635B9 (ru) | 2015-11-16 | 2021-10-26 | Араксис Фарма Ллк | 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| RU2617694C1 (ru) * | 2015-12-24 | 2017-04-26 | Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) | Амиды акриловой и метакриловой кислот с олигопиперидинами и способ их получения |
| RU2617409C1 (ru) * | 2015-12-24 | 2017-04-25 | Федеральное государственное бюджетное учреждение науки Институт элементоорганических соединений им. А.Н. Несмеянова Российской академии наук (ИНЭОС РАН) | Амиды акриловой и метакриловой кислот с n-алкилпиперазино-пиперидинами и способ их получения |
| GB201602527D0 (en) * | 2016-02-12 | 2016-03-30 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| US10822312B2 (en) | 2016-03-30 | 2020-11-03 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| EP3464275B1 (en) | 2016-05-26 | 2024-05-08 | Recurium IP Holdings, LLC | Egfr inhibitor compounds |
| WO2018005849A1 (en) | 2016-06-29 | 2018-01-04 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| WO2018002958A1 (en) | 2016-06-30 | 2018-01-04 | Sun Pharma Advanced Research Company Limited | Novel hydrazide containing compounds as btk inhibitors |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| US10280172B2 (en) | 2016-09-29 | 2019-05-07 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| JP2019534260A (ja) | 2016-10-07 | 2019-11-28 | アラクセス ファーマ エルエルシー | Rasの阻害剤としての複素環式化合物およびその使用方法 |
| BR112019010470A2 (pt) | 2016-11-23 | 2019-09-10 | Novartis Ag | métodos de realce de resposta imune com everolimo, dactolisib ou ambos |
| CN106755343A (zh) * | 2016-12-01 | 2017-05-31 | 北京致成生物医学科技有限公司 | 胰腺癌预后诊断分子标记物 |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| WO2018140600A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused hetero-hetero bicyclic compounds and methods of use thereof |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140514A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| WO2018195649A1 (en) * | 2017-04-26 | 2018-11-01 | Alberta Research Chemicals Inc. | Substituted tetrahydropyridine derivatives as ido-1 inhibitors and uses thereof |
| CN110869357A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | 化合物及其用于治疗癌症的使用方法 |
| US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
| AU2018271990A1 (en) | 2017-05-25 | 2019-12-12 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| US10596165B2 (en) | 2018-02-12 | 2020-03-24 | resTORbio, Inc. | Combination therapies |
| CA3096984A1 (en) | 2018-04-05 | 2019-10-10 | Sumitomo Dainippon Pharma Oncology, Inc. | Axl kinase inhibitors and use of the same |
| ES3032793T3 (en) | 2018-04-10 | 2025-07-24 | Neuropore Therapies Inc | Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways |
| ES2929292T3 (es) | 2018-04-10 | 2022-11-28 | Neuropore Therapies Inc | Derivados de morfolina como inhibidores de Vps34 |
| MX2021000977A (es) | 2018-07-26 | 2021-04-12 | Sumitomo Pharma Oncology Inc | Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos. |
| US12134620B2 (en) * | 2018-08-01 | 2024-11-05 | Araxes Pharma Llc | Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| EP3849545A1 (en) * | 2018-09-10 | 2021-07-21 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of neurofibromatosis |
| WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| CN120789282A (zh) * | 2019-09-19 | 2025-10-17 | 托特斯医药公司 | 治疗性缀合物 |
| TWI877239B (zh) | 2019-10-14 | 2025-03-21 | 美商普林斯匹亞生物製藥公司 | 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法 |
| EP4045485A1 (en) | 2019-10-18 | 2022-08-24 | The Regents Of The University Of California | 3-phenylsulphonyl-quinoline derivatives as agents for treating pathogenic blood vessels disorders |
| WO2021142252A1 (en) * | 2020-01-10 | 2021-07-15 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| US11530218B2 (en) | 2020-01-20 | 2022-12-20 | Incyte Corporation | Spiro compounds as inhibitors of KRAS |
| BR112022014149A2 (pt) | 2020-01-22 | 2022-09-27 | Principia Biopharma Inc | Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenóxi-fenil)-1h-pirazolo[3,4-d]pirimidina-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrila |
| TWI874791B (zh) | 2020-02-18 | 2025-03-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| AR121356A1 (es) | 2020-02-18 | 2022-05-11 | Gilead Sciences Inc | Compuestos antivirales |
| TWI883391B (zh) | 2020-02-18 | 2025-05-11 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| WO2021242859A1 (en) * | 2020-05-27 | 2021-12-02 | Duke University | Compositions and methods for sensitizing acute myeloid leukemias to chemotherapy |
| WO2022047093A1 (en) | 2020-08-28 | 2022-03-03 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of kras |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| CN113045582B (zh) * | 2021-02-05 | 2022-12-23 | 中国药科大学 | Parp-1/pi3k双靶点抑制剂或其药学上可接受的盐及其制备方法与用途 |
| EP4308121A4 (en) * | 2021-03-18 | 2025-02-19 | Totus Medicines Inc. | THERAPEUTIC CONJUGATES |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| CN117396470A (zh) * | 2021-04-09 | 2024-01-12 | 巴塞尔大学 | 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物 |
| JP2024516361A (ja) * | 2021-04-09 | 2024-04-15 | ウニヴェアズィテート バーゼル | Pi3kの可逆的および不可逆的共有結合性阻害剤としてのトリアジン誘導体 |
| EP4323362B1 (en) | 2021-04-16 | 2025-05-07 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
| WO2023283213A1 (en) | 2021-07-07 | 2023-01-12 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| TW202321191A (zh) * | 2021-07-29 | 2023-06-01 | 美商賽迪拉治療股份有限公司 | Tead抑制劑及其用途 |
| CA3228162A1 (en) | 2021-08-18 | 2023-02-23 | Gilead Sciences, Inc. | Phospholipid compounds and methods of making and using the same |
| CA3229855A1 (en) | 2021-08-31 | 2023-03-09 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| CN113754680B (zh) * | 2021-09-28 | 2022-07-22 | 云白药征武科技(上海)有限公司 | 一种α氟代酰基哌嗪衍生物及其制备和应用 |
| WO2023056421A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| MX2024004444A (es) | 2021-10-14 | 2024-05-08 | Incyte Corp | Compuestos de quinolina como inhibidores de la proteina del virus de sarcoma de rata kirsten (kras). |
| WO2024182447A1 (en) * | 2023-02-28 | 2024-09-06 | Vividion Therapeutics, Inc. | Compounds and methods for modulating ras-pi3k |
| WO2025188658A1 (en) * | 2024-03-06 | 2025-09-12 | Alterome Therapeutics, Inc. | Akt1 modulators |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) * | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| HRP20131159B1 (hr) * | 2002-09-30 | 2019-11-01 | Bayer Ip Gmbh | Taljeni azol-pirimidin derivati |
| AR046845A1 (es) * | 2003-11-21 | 2005-12-28 | Novartis Ag | Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas |
| RS55546B1 (sr) * | 2004-05-13 | 2017-05-31 | Icos Corp | Hinazolinoni kao inhibitori humane fosfatidilonozitol 3-delta kinaze |
| AU2006214190A1 (en) * | 2005-02-17 | 2006-08-24 | Icos Corporation | Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| EP2041139B1 (en) * | 2006-04-26 | 2011-11-09 | F. Hoffmann-La Roche AG | Pharmaceutical compounds |
| KR101402474B1 (ko) * | 2006-04-26 | 2014-06-19 | 제넨테크, 인크. | 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물 |
| GB0611152D0 (en) * | 2006-06-06 | 2006-07-19 | Ucb Sa | Therapeutic agents |
| DK2050749T3 (en) * | 2006-08-08 | 2018-01-08 | Chugai Pharmaceutical Co Ltd | PYRIMIDINE DERIVATIVES AS PI3K INHIBITOR AND USE THEREOF |
| US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| PE20090717A1 (es) * | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| CA2689989A1 (en) * | 2007-06-04 | 2008-12-11 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| CA2699202C (en) * | 2007-09-12 | 2016-09-27 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| US8354528B2 (en) * | 2007-10-25 | 2013-01-15 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| GB0805818D0 (en) * | 2008-03-31 | 2008-04-30 | Ucb Pharma Sa | Therapeutic agents |
| EA024252B1 (ru) * | 2009-01-08 | 2016-08-31 | Кьюрис, Инк. | Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой |
-
2010
- 2010-09-09 JP JP2012528906A patent/JP2013504325A/ja active Pending
- 2010-09-09 SG SG10201405598QA patent/SG10201405598QA/en unknown
- 2010-09-09 TW TW104118050A patent/TW201609747A/zh unknown
- 2010-09-09 PH PH1/2012/500491A patent/PH12012500491A1/en unknown
- 2010-09-09 NZ NZ598808A patent/NZ598808A/en not_active IP Right Cessation
- 2010-09-09 KR KR1020127009074A patent/KR20120063515A/ko not_active Ceased
- 2010-09-09 NZ NZ626650A patent/NZ626650A/en not_active IP Right Cessation
- 2010-09-09 US US12/878,965 patent/US20110230476A1/en not_active Abandoned
- 2010-09-09 BR BR112012008385A patent/BR112012008385A2/pt not_active IP Right Cessation
- 2010-09-09 EP EP10816104A patent/EP2475375A4/en not_active Ceased
- 2010-09-09 TW TW099130780A patent/TWI499592B/zh not_active IP Right Cessation
- 2010-09-09 WO PCT/US2010/048317 patent/WO2011031896A2/en not_active Ceased
- 2010-09-09 RU RU2012110024/04A patent/RU2595718C2/ru not_active IP Right Cessation
- 2010-09-09 CA CA2773848A patent/CA2773848A1/en not_active Abandoned
- 2010-09-09 AU AU2010292198A patent/AU2010292198A1/en not_active Abandoned
- 2010-09-09 MX MX2012002972A patent/MX339584B/es active IP Right Grant
- 2010-09-09 CN CN201080048947XA patent/CN102625708A/zh active Pending
- 2010-09-09 SG SG2012016960A patent/SG179085A1/en unknown
-
2012
- 2012-03-08 IL IL218555A patent/IL218555A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102625708A (zh) | 2012-08-01 |
| SG179085A1 (en) | 2012-04-27 |
| RU2012110024A (ru) | 2013-11-10 |
| RU2595718C2 (ru) | 2016-08-27 |
| JP2013504325A (ja) | 2013-02-07 |
| MX2012002972A (es) | 2012-06-25 |
| TWI499592B (zh) | 2015-09-11 |
| NZ598808A (en) | 2014-07-25 |
| TW201120047A (en) | 2011-06-16 |
| EP2475375A2 (en) | 2012-07-18 |
| SG10201405598QA (en) | 2014-11-27 |
| US20110230476A1 (en) | 2011-09-22 |
| NZ626650A (en) | 2015-12-24 |
| TW201609747A (zh) | 2016-03-16 |
| KR20120063515A (ko) | 2012-06-15 |
| AU2010292198A1 (en) | 2012-04-05 |
| EP2475375A4 (en) | 2013-02-20 |
| IL218555A0 (en) | 2012-05-31 |
| PH12012500491A1 (en) | 2018-03-21 |
| WO2011031896A3 (en) | 2011-05-12 |
| MX339584B (es) | 2016-06-01 |
| WO2011031896A2 (en) | 2011-03-17 |
| BR112012008385A2 (pt) | 2019-09-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2773848A1 (en) | Pi3 kinase inhibitors and uses thereof | |
| AU2012225382B2 (en) | PI3 kinase inhibitors and uses thereof | |
| US12358915B2 (en) | METTL3 inhibitory compounds | |
| US10968236B2 (en) | TYK2 inhibitors and uses thereof | |
| JP7530360B2 (ja) | Tyk2阻害剤およびその使用 | |
| JP5808826B2 (ja) | 複素環化合物およびその使用 | |
| US12338242B2 (en) | TYK2 inhibitors and uses thereof | |
| TW200911810A (en) | Substituted imidazopyridazines and pyrrolopyrimidines as lipid kinase inhibitors | |
| KR20130031234A (ko) | 헤테로사이클릭 화합물 및 이의 용도 | |
| CA2878040A1 (en) | Irak inhibitors and uses thereof | |
| AU2012310168B2 (en) | 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase | |
| EP4194450A1 (en) | Cdk9 inhibitor and use thereof | |
| CN113493471A (zh) | 杂芳环类激酶抑制剂 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20150901 |
|
| FZDE | Discontinued |
Effective date: 20180717 |