CN102713618B - 蛋白激酶复合物和抑制剂 - Google Patents
蛋白激酶复合物和抑制剂 Download PDFInfo
- Publication number
- CN102713618B CN102713618B CN201080050753.3A CN201080050753A CN102713618B CN 102713618 B CN102713618 B CN 102713618B CN 201080050753 A CN201080050753 A CN 201080050753A CN 102713618 B CN102713618 B CN 102713618B
- Authority
- CN
- China
- Prior art keywords
- group
- protein kinase
- prot
- seq
- ring
- 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.)
- Expired - Fee Related
Links
- 0 CC1(CSCCC(C(NC*)=O)C#N)CC1 Chemical compound CC1(CSCCC(C(NC*)=O)C#N)CC1 0.000 description 18
- XUYPGCLHHYIAOJ-IBZGOXDYSA-N C/C(/NC=O)=C\C(\F)=C(/C=C)\Oc1ccnc(NC(CC2)CCN2C=O)c1 Chemical compound C/C(/NC=O)=C\C(\F)=C(/C=C)\Oc1ccnc(NC(CC2)CCN2C=O)c1 XUYPGCLHHYIAOJ-IBZGOXDYSA-N 0.000 description 1
- BCTIWZZEENAJGL-QBFSEMIESA-N C=C/C(/C(CC1)Cc2c1c(C#N)c(NC(C1=CC=CCC1F)=O)[s]2)=C/OCc1n[o]c(F)n1 Chemical compound C=C/C(/C(CC1)Cc2c1c(C#N)c(NC(C1=CC=CCC1F)=O)[s]2)=C/OCc1n[o]c(F)n1 BCTIWZZEENAJGL-QBFSEMIESA-N 0.000 description 1
- RHHNOUUVSDJFCS-FPLPWBNLSA-N C=C/C(/OC1=CCNCC1)=C/F Chemical compound C=C/C(/OC1=CCNCC1)=C/F RHHNOUUVSDJFCS-FPLPWBNLSA-N 0.000 description 1
- PIZWKSPQMNWMAP-ICWBMWKASA-N C=C/C=C/C=C\ON Chemical compound C=C/C=C/C=C\ON PIZWKSPQMNWMAP-ICWBMWKASA-N 0.000 description 1
- KXTDKJNHLXISOJ-UHFFFAOYSA-N CC(C)(C)OC(NCCNc1nc(Nc(ccc(C(NC2CCN(C)CC2)=O)c2)c2OC)ncc1C(F)(F)F)=O Chemical compound CC(C)(C)OC(NCCNc1nc(Nc(ccc(C(NC2CCN(C)CC2)=O)c2)c2OC)ncc1C(F)(F)F)=O KXTDKJNHLXISOJ-UHFFFAOYSA-N 0.000 description 1
- MZQVWIWUZVRLIR-SNAWJCMRSA-N CC(C)(CNc1cc(Oc(cc2)ccc2NC(NC(CC(CC2)=CC=C2F)=O)=O)ccn1)OC(/C=C/C)=O Chemical compound CC(C)(CNc1cc(Oc(cc2)ccc2NC(NC(CC(CC2)=CC=C2F)=O)=O)ccn1)OC(/C=C/C)=O MZQVWIWUZVRLIR-SNAWJCMRSA-N 0.000 description 1
- WXXGIUQWWHWEHL-UHFFFAOYSA-N CC(CC1)Cc2c1c(C#N)c(NC(c1ccccc1)=O)[s]2 Chemical compound CC(CC1)Cc2c1c(C#N)c(NC(c1ccccc1)=O)[s]2 WXXGIUQWWHWEHL-UHFFFAOYSA-N 0.000 description 1
- VSAYUYVESSTPCR-PEZBUJJGSA-N CCC(C/C(/F)=C/OC(C1)=CC=NC1NC(CCC1)CN1C(C=C)=O)NC(NC(C)=O)=O Chemical compound CCC(C/C(/F)=C/OC(C1)=CC=NC1NC(CCC1)CN1C(C=C)=O)NC(NC(C)=O)=O VSAYUYVESSTPCR-PEZBUJJGSA-N 0.000 description 1
- NBBWMNRXJBKEJV-UHFFFAOYSA-O CCCSC([NH2+]C=C)=CSN Chemical compound CCCSC([NH2+]C=C)=CSN NBBWMNRXJBKEJV-UHFFFAOYSA-O 0.000 description 1
- SUBQJEVAXOXKNF-UHFFFAOYSA-N CNC(Cc(cc1)ccc1F)O Chemical compound CNC(Cc(cc1)ccc1F)O SUBQJEVAXOXKNF-UHFFFAOYSA-N 0.000 description 1
- VZAWNHGYRZSUCY-NBGKIGBDSA-N C[C@H](CC(SC1NC(/C=C/C=C\C)=O)=CC1C#N)Oc1cc(C(C=C(C)C)=O)ccc1 Chemical compound C[C@H](CC(SC1NC(/C=C/C=C\C)=O)=CC1C#N)Oc1cc(C(C=C(C)C)=O)ccc1 VZAWNHGYRZSUCY-NBGKIGBDSA-N 0.000 description 1
- JJSZIEZZOAJYPG-VAWYXSNFSA-N Cc1c(/C=C/C([IH]F)=O)c(C(CC2)Cc3c2c(C#N)c(NC(c(cccc2)c2F)=O)[s]3)ccc1 Chemical compound Cc1c(/C=C/C([IH]F)=O)c(C(CC2)Cc3c2c(C#N)c(NC(c(cccc2)c2F)=O)[s]3)ccc1 JJSZIEZZOAJYPG-VAWYXSNFSA-N 0.000 description 1
- QPNNSLZSFVUBLU-UHFFFAOYSA-N Cs1(C)ccccc1 Chemical compound Cs1(C)ccccc1 QPNNSLZSFVUBLU-UHFFFAOYSA-N 0.000 description 1
- SPOAMLFCRBFURV-UHFFFAOYSA-N FC1CC=CCC1 Chemical compound FC1CC=CCC1 SPOAMLFCRBFURV-UHFFFAOYSA-N 0.000 description 1
- MGFLCNPHQWBPBI-QSAPEBAKSA-N N#C[C@@H](C(NCCCNc1cc(Oc(c(F)c2)ccc2NC(NC(Cc(cc2)ccc2F)O)=O)ccn1)=C1)SN=C1O Chemical compound N#C[C@@H](C(NCCCNc1cc(Oc(c(F)c2)ccc2NC(NC(Cc(cc2)ccc2F)O)=O)ccn1)=C1)SN=C1O MGFLCNPHQWBPBI-QSAPEBAKSA-N 0.000 description 1
- VXEBFVAFZCOXEA-UHFFFAOYSA-N N#Cc1c(NC(C2=CC=[I]C=C2F)=O)[s]c(C2)c1CCC2c1cccc(C2)c1CN2C(C1SSCCC1)=O Chemical compound N#Cc1c(NC(C2=CC=[I]C=C2F)=O)[s]c(C2)c1CCC2c1cccc(C2)c1CN2C(C1SSCCC1)=O VXEBFVAFZCOXEA-UHFFFAOYSA-N 0.000 description 1
- YBTJCLCGOKJKTE-UHFFFAOYSA-N N#Cc1c(NC(c2cccc3c2CCC=C3)=O)[s]c(C2)c1CCN2C(CCN1CC(CNC(C2=CC=CCC=C2F)=O)CCC1)=O Chemical compound N#Cc1c(NC(c2cccc3c2CCC=C3)=O)[s]c(C2)c1CCN2C(CCN1CC(CNC(C2=CC=CCC=C2F)=O)CCC1)=O YBTJCLCGOKJKTE-UHFFFAOYSA-N 0.000 description 1
- CEMTWYOWRIQZPU-UHFFFAOYSA-N O=CNC(CC(CC1)=CC=C1F)=O Chemical compound O=CNC(CC(CC1)=CC=C1F)=O CEMTWYOWRIQZPU-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
- C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
-
- 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
- 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
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510330338.8A CN105063001A (zh) | 2009-09-16 | 2010-09-15 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24298809P | 2009-09-16 | 2009-09-16 | |
| US61/242,988 | 2009-09-16 | ||
| PCT/US2010/048916 WO2011034907A2 (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510330338.8A Division CN105063001A (zh) | 2009-09-16 | 2010-09-15 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102713618A CN102713618A (zh) | 2012-10-03 |
| CN102713618B true CN102713618B (zh) | 2015-07-15 |
Family
ID=43759252
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080050753.3A Expired - Fee Related CN102713618B (zh) | 2009-09-16 | 2010-09-15 | 蛋白激酶复合物和抑制剂 |
| CN201510330338.8A Pending CN105063001A (zh) | 2009-09-16 | 2010-09-15 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510330338.8A Pending CN105063001A (zh) | 2009-09-16 | 2010-09-15 | 蛋白激酶复合物和含有该复合物的药物组合物以及它们的用途 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9556426B2 (enExample) |
| EP (1) | EP2478361A4 (enExample) |
| JP (4) | JP5806670B2 (enExample) |
| KR (1) | KR20120093220A (enExample) |
| CN (2) | CN102713618B (enExample) |
| AU (2) | AU2010295690B2 (enExample) |
| BR (1) | BR112012005962A8 (enExample) |
| CA (1) | CA2773985A1 (enExample) |
| IL (1) | IL218678A0 (enExample) |
| IN (1) | IN2012DN02534A (enExample) |
| MX (1) | MX339811B (enExample) |
| NZ (2) | NZ620174A (enExample) |
| RU (1) | RU2012114902A (enExample) |
| SG (1) | SG179172A1 (enExample) |
| WO (1) | WO2011034907A2 (enExample) |
Families Citing this family (92)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2529621B1 (en) | 2006-09-22 | 2016-10-05 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| JP2011523646A (ja) | 2008-05-21 | 2011-08-18 | 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 | キナーゼ阻害剤としてのリン誘導体 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
| JP2012501654A (ja) * | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス, インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
| CN102713618B (zh) | 2009-09-16 | 2015-07-15 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和抑制剂 |
| US8946197B2 (en) | 2009-11-16 | 2015-02-03 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| WO2011082285A1 (en) | 2009-12-30 | 2011-07-07 | Avila Therapeutics, Inc. | Ligand-directed covalent modification of protein |
| MX380504B (es) | 2010-06-03 | 2025-03-12 | Pharmacyclics Llc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| AU2011260323A1 (en) | 2010-06-04 | 2012-11-15 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as LRRK2 modulators |
| KR101566091B1 (ko) | 2010-11-10 | 2015-11-04 | 에프. 호프만-라 로슈 아게 | Lrrk2 조절제로서 피라졸 아미노피리미딘 유도체 |
| AU2012250517B2 (en) | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US8889716B2 (en) | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| WO2013009812A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc | Methods of treatment |
| WO2013009827A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009810A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009830A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| DK3686193T3 (da) | 2011-07-27 | 2022-05-30 | Astrazeneca Ab | 2-(2,4,5-substitueret anilino)pyrimidinforbindelser |
| JP6106685B2 (ja) | 2011-11-17 | 2017-04-05 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | C−jun−n−末端キナーゼ(jnk)の阻害剤 |
| AR089182A1 (es) * | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| WO2013157540A1 (ja) * | 2012-04-17 | 2013-10-24 | 富士フイルム株式会社 | 含窒素複素環化合物またはその塩 |
| 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 |
| MA37711A1 (fr) | 2012-06-04 | 2017-05-31 | Pharmacyclics Inc | Formes cristallines d'un inhibiteur de tyrosine kinase de bruton |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| HK1206073A1 (en) | 2012-07-24 | 2015-12-31 | 药品循环有限责任公司 | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| KR20150084923A (ko) | 2012-11-15 | 2015-07-22 | 파마시클릭스, 인코포레이티드 | 키나제 억제제로서의 피롤로피리미딘 화합물 |
| PT2970205T (pt) | 2013-03-14 | 2019-08-26 | Tolero Pharmaceuticals Inc | Inibidores da jak2 e da alk2 e métodos para a sua utilização |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| JP6800750B2 (ja) | 2013-08-02 | 2020-12-16 | ファーマサイクリックス エルエルシー | 固形腫瘍の処置方法 |
| CA2920534A1 (en) | 2013-08-12 | 2015-02-19 | Pharmacyclics Llc | Methods for the treatment of her2 amplified cancer |
| CA2922398C (en) | 2013-09-12 | 2023-08-29 | Dana-Farber Cancer Institute, Inc. | Methods for evaluating and treating waldenstrom's macroglobulinemia |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| US9885086B2 (en) | 2014-03-20 | 2018-02-06 | Pharmacyclics Llc | Phospholipase C gamma 2 and resistance associated mutations |
| MX358346B (es) * | 2014-04-04 | 2018-08-15 | Syros Pharmaceuticals Inc | Inhibidores de la quinasa dependiente de ciclina 7 (cdk7). |
| CA2959602A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| US9545407B2 (en) | 2014-08-07 | 2017-01-17 | Pharmacyclics Llc | Formulations of a bruton's tyrosine kinase inhibitor |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of proton tyrosine kinase inhibitor |
| EP3912979B1 (en) | 2015-06-03 | 2026-03-25 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| DK3386500T3 (da) | 2015-12-09 | 2022-12-12 | Univ Illinois | Benzothiophen-baserede selektive østrogenreceptor ned-regulatorer |
| CN121974842A (zh) | 2016-05-10 | 2026-05-05 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| US11285218B2 (en) | 2016-06-23 | 2022-03-29 | Dana-Farber Cancer Institute, Inc. | Degradation of bromodomain-containing protein 9 (BRD9) by conjugation of BRD9 inhibitors with E3 ligase ligand and methods of use |
| CN109789143A (zh) | 2016-07-01 | 2019-05-21 | G1治疗公司 | 基于嘧啶的抗增殖剂 |
| CN110022900A (zh) | 2016-09-08 | 2019-07-16 | 蓝图药品公司 | 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合 |
| WO2018187294A1 (en) * | 2017-04-03 | 2018-10-11 | Asana Biosciences, Llc | Pyrimido-pyridazinone compound combinations, methods, kits and formulations thereof |
| EP4717317A3 (en) | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| EP3645001B1 (en) | 2017-06-29 | 2024-07-03 | G1 Therapeutics, Inc. | Morphic forms of git38 and methods of manufacture thereof |
| EP3663285B1 (en) * | 2017-08-04 | 2024-01-24 | Abbisko Therapeutics Co., Ltd. | Formylpyridine derivative having fgfr4 inhibitory activity, preparation method therefor and use thereof |
| WO2019136451A1 (en) | 2018-01-08 | 2019-07-11 | G1 Therapeutics, Inc. | G1t38 superior dosage regimes |
| CN111902141A (zh) | 2018-03-26 | 2020-11-06 | C4医药公司 | 用于ikaros降解的羟脑苷脂结合剂 |
| IL259810A (en) * | 2018-06-04 | 2018-07-31 | Yeda Res & Dev | Mitogen-activated protein kinase kinase 7 inhibitors |
| KR20210038906A (ko) | 2018-07-26 | 2021-04-08 | 스미토모 다이니폰 파마 온콜로지, 인크. | 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제 |
| WO2020045941A1 (ko) * | 2018-08-27 | 2020-03-05 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| WO2020097396A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| US12509455B2 (en) | 2018-11-07 | 2025-12-30 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as Janus kinase 2 inhibitors and uses thereof |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| EP3902805A4 (en) | 2018-12-28 | 2023-03-01 | SPV Therapeutics Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| JP2022526159A (ja) | 2019-03-29 | 2022-05-23 | アストラゼネカ・アクチエボラーグ | 非小細胞肺がんの治療に使用するためのオシメルチニブ |
| KR102947433B1 (ko) | 2019-04-12 | 2026-04-06 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스 및 아이올로스의 트리시클릭 분해제 |
| CA3147741A1 (en) * | 2019-07-19 | 2021-01-28 | Bridgene Biosciences, Inc. | Inhibitors of tyrosine kinase |
| CA3156828A1 (en) | 2019-10-03 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Tricyclic kinase inhibitors and uses thereof |
| EP4681715A3 (en) | 2019-12-20 | 2026-01-28 | C4 Therapeutics, Inc. | Isoindolinone and indazole compounds for the degradation of egfr |
| CN119823124A (zh) | 2020-03-05 | 2025-04-15 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| TW202204350A (zh) | 2020-05-06 | 2022-02-01 | 美商雅捷可斯治療公司 | 作為jak2抑制劑之6-雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| JP7853532B2 (ja) | 2020-05-19 | 2026-04-30 | ファーマコスモス ホールディング エー/エス | 医学的障害を治療するためのサイクリン依存性キナーゼ阻害化合物 |
| EP4164653A4 (en) | 2020-06-15 | 2024-06-19 | G1 Therapeutics, Inc. | MORPHIC FORMS OF TRILACICLIB AND METHODS OF PREPARING THE SAME |
| CN116490186B (zh) | 2020-08-05 | 2025-10-31 | C4医药公司 | 用于ret的靶向降解的化合物 |
| CA3193488A1 (en) | 2020-09-23 | 2022-03-31 | Jason Allan Wiles | Pharmaceutical compounds for the treatment of complement mediated disorders |
| EP4267574B1 (en) | 2020-12-23 | 2025-04-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| BR112023024507A2 (pt) | 2021-05-26 | 2024-02-15 | C4 Therapeutics Inc | Método para tratar um câncer mediado por receptor do fator de crescimento epidérmico mutante que sofreu metástase para o cérebro ou sistema nervoso central |
| AU2022290851A1 (en) | 2021-06-08 | 2023-11-23 | C4 Therapeutics, Inc. | Therapeutics for the degradation of mutant braf |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ck12抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| TW202345806A (zh) | 2022-03-31 | 2023-12-01 | 美商艾伯維有限公司 | 噻唑并〔5,4-b〕吡啶malt-1抑制劑 |
| KR20250055538A (ko) | 2022-08-03 | 2025-04-24 | 브리스톨-마이어스 스큅 컴퍼니 | Ret 단백질을 조정하기 위한 화합물 |
| KR20250117789A (ko) | 2022-11-04 | 2025-08-05 | 브리스톨-마이어스 스큅 컴퍼니 | Ret-ldd 단백질 분해제 |
| JP2025540906A (ja) | 2022-11-04 | 2025-12-17 | ブリストル-マイヤーズ スクイブ カンパニー | Ret-lddタンパク質阻害剤 |
| CN122206684A (zh) | 2023-06-30 | 2026-06-12 | 默克专利有限公司 | 用于kras蛋白降解的异双功能化合物 |
| CN118766549A (zh) * | 2024-06-24 | 2024-10-15 | 重庆医科大学附属第一医院 | 脊柱转移性肿瘤微创切吸治疗系统 |
| GB202416727D0 (en) * | 2024-11-13 | 2024-12-25 | Imperial College Innovations Ltd | RAB27 inhibitors |
| WO2026139448A1 (en) | 2024-12-23 | 2026-07-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101054380A (zh) * | 2006-04-13 | 2007-10-17 | 沈阳药科大学 | 用作细胞周期依赖性蛋白激酶抑制剂的吡唑并嘧啶类衍生物 |
| US7407939B2 (en) * | 2001-07-26 | 2008-08-05 | Curegenics Ltd. | Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics |
| US20090137588A1 (en) * | 2007-10-19 | 2009-05-28 | Avila Therapeutics, Inc. | Heteroaryl compounds and uses thereof |
Family Cites Families (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
| US5650270A (en) | 1982-02-01 | 1997-07-22 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| US4709016A (en) | 1982-02-01 | 1987-11-24 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| US5756466A (en) * | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5856116A (en) * | 1994-06-17 | 1999-01-05 | Vertex Pharmaceuticals, Incorporated | Crystal structure and mutants of interleukin-1 beta converting enzyme |
| US5760041A (en) * | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| CN100503580C (zh) | 1996-04-12 | 2009-06-24 | 沃尼尔·朗伯公司 | 酪氨酸激酶的不可逆抑制剂 |
| CA2261974A1 (en) * | 1996-07-25 | 1998-02-05 | Biogen, Inc. | Molecular model for vla-4 inhibitors |
| US6686350B1 (en) * | 1996-07-25 | 2004-02-03 | Biogen, Inc. | Cell adhesion inhibitors |
| JP4274584B2 (ja) | 1996-12-06 | 2009-06-10 | バーテックス ファーマシューティカルズ インコーポレイテッド | インターロイキン−1β変換酵素のインヒビター |
| US6002008A (en) * | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| ZA986732B (en) | 1997-07-29 | 1999-02-02 | Warner Lambert Co | Irreversible inhibitiors of tyrosine kinases |
| US6251912B1 (en) | 1997-08-01 | 2001-06-26 | American Cyanamid Company | Substituted quinazoline derivatives |
| US6162613A (en) * | 1998-02-18 | 2000-12-19 | Vertex Pharmaceuticals, Inc. | Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases |
| US7383135B1 (en) * | 1998-05-04 | 2008-06-03 | Vertex Pharmaceuticals Incorporated | Methods of designing inhibitors for JNK kinases |
| US6919178B2 (en) | 2000-11-21 | 2005-07-19 | Sunesis Pharmaceuticals, Inc. | Extended tethering approach for rapid identification of ligands |
| US6335155B1 (en) * | 1998-06-26 | 2002-01-01 | Sunesis Pharmaceuticals, Inc. | Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules |
| WO2000018895A1 (en) * | 1998-09-25 | 2000-04-06 | The Children's Medical Center Corporation | Short peptides which selectively modulate the activity of protein kinases |
| US6288082B1 (en) | 1998-09-29 | 2001-09-11 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| CN1160338C (zh) | 1998-11-19 | 2004-08-04 | 沃尼尔·朗伯公司 | N-[4-(3-氯-4-氟-苯基氨基)-7-(3-吗啉-4-基-丙氧基)-喹唑啉-6-基]-丙烯酰胺,不可逆的酪氨酸激酶抑制剂 |
| CA2375229A1 (en) * | 1999-06-17 | 2000-12-28 | Source Precision Medicine, Inc. | Method and compounds for inhibiting activity of serine elastases |
| US6420364B1 (en) * | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
| EP1207864A2 (en) * | 2000-02-05 | 2002-05-29 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of erk |
| US6384051B1 (en) | 2000-03-13 | 2002-05-07 | American Cyanamid Company | Method of treating or inhibiting colonic polyps |
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| CA2417500C (en) * | 2000-07-28 | 2008-11-18 | Georgetown University Medical Center | Erbb-2 selective small molecule kinase inhibitors |
| MXPA03001256A (es) | 2000-08-11 | 2004-12-06 | Vertex Pharma | Inhibidores de p38. |
| BR0116493A (pt) * | 2000-12-21 | 2003-09-30 | Vertex Pharma | Compostos de pirazol úteis como inibidores de proteìna cinase |
| US7235576B1 (en) * | 2001-01-12 | 2007-06-26 | Bayer Pharmaceuticals Corporation | Omega-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| WO2003046200A2 (en) | 2001-11-21 | 2003-06-05 | Sunesis Pharmaceuticals, Inc. | Methods for ligand discovery |
| JP2006516170A (ja) | 2001-12-07 | 2006-06-22 | リサーチ・インベストメント・ネットワーク・インコーポレーテッド | フォトニクス回折メモリを読むための固体マイクロ光エレクトロメカニカル・システム(moems) |
| US7109230B2 (en) | 2002-01-07 | 2006-09-19 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| WO2003081210A2 (en) | 2002-03-21 | 2003-10-02 | Sunesis Pharmaceuticals, Inc. | Identification of kinase inhibitors |
| GB0213186D0 (en) | 2002-06-08 | 2002-07-17 | Univ Dundee | Methods |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| EP1375517A1 (en) | 2002-06-21 | 2004-01-02 | Smithkline Beecham Corporation | Structure of a glucocorticoid receptor ligand binding domain comprising an expanded binding pocket and methods employing same |
| GB0221169D0 (en) | 2002-09-12 | 2002-10-23 | Univ Bath | Crystal |
| WO2004048343A1 (en) | 2002-11-28 | 2004-06-10 | Schering Aktiengesellschaft | Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents |
| PE20040945A1 (es) | 2003-02-05 | 2004-12-14 | Warner Lambert Co | Preparacion de quinazolinas substituidas |
| AU2004210972A1 (en) * | 2003-02-11 | 2004-08-26 | Immusol Incorporated | siRNA libraries optimized for predetermined protein families |
| EP1603879A2 (en) | 2003-02-28 | 2005-12-14 | Bayer Pharmaceuticals Corporation | Substituted pyridine derivatives useful in the treatment of cancer and other disorders |
| UY28213A1 (es) * | 2003-02-28 | 2004-09-30 | Bayer Pharmaceuticals Corp | Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos. |
| JP4594925B2 (ja) | 2003-02-28 | 2010-12-08 | ニッポネックス インコーポレイテッド | 増殖亢進性、血管新生性及び炎症性疾患の治療に有用な2−オキソ−1,3,5−パーヒドロトリアザピン誘導体 |
| WO2004087059A2 (en) * | 2003-03-26 | 2004-10-14 | The University Of Texas | Covalent attachment of ligands to nucleophilic proteins guided by non-covalent binding |
| WO2005000197A2 (en) | 2003-04-11 | 2005-01-06 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
| US8748601B2 (en) | 2003-04-11 | 2014-06-10 | The Regents Of The University Of California | Selective serine/threonine kinase inhibitors |
| EP1636585B2 (en) * | 2003-05-20 | 2012-06-13 | Bayer HealthCare LLC | Diaryl ureas with kinase inhibiting activity |
| KR20060054412A (ko) * | 2003-08-01 | 2006-05-22 | 와이어쓰 홀딩스 코포레이션 | 암 치료 및 억제용 표피 성장인자 수용체 키나제 억제제와세포독성제의 배합물 용도 |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| EP1670422A4 (en) * | 2003-09-17 | 2007-08-01 | Sunesis Pharmaceuticals Inc | IDENTIFYING KINASE INHIBITORS |
| WO2005043118A2 (en) * | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| BRPI0506883A (pt) | 2004-01-16 | 2007-05-29 | Univ Michigan | miméticos de smac conformacionalmente comprimidos e seus usos |
| RU2006131045A (ru) * | 2004-01-30 | 2008-03-10 | Мерк Патент ГмбХ (DE) | Производные бисарилмочевины |
| US20080268460A1 (en) | 2004-05-20 | 2008-10-30 | Wyeth | Assays to Identify Irreversibly Binding Inhibitors of Receptor Tyrosine Kinases |
| WO2005115145A2 (en) * | 2004-05-20 | 2005-12-08 | Wyeth | Quinone substituted quinazoline and quinoline kinase inhibitors |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| US20060079494A1 (en) * | 2004-09-27 | 2006-04-13 | Santi Daniel V | Specific kinase inhibitors |
| MX2007004248A (es) | 2004-10-13 | 2007-06-12 | Merck Patent Gmbh | Derivados heterociclicos de bisarilurea sustituidos como inhibidores de cinasa. |
| NZ556673A (en) | 2005-02-03 | 2010-03-26 | Gen Hospital Corp | Method for treating gefitinib and/or erlotinib resistant cancer with an EGFR inhibitor |
| AU2006236940A1 (en) * | 2005-04-14 | 2006-10-26 | Wyeth | Use of an epidermal growth factor receptor kinase inhibitor (EGFR) in gefitinib resistant patients |
| TW200716132A (en) | 2005-05-03 | 2007-05-01 | Smithkline Beecham Corp | Novel chemical compounds |
| MX2007013257A (es) | 2005-05-05 | 2008-01-21 | Chroma Therapeutics Ltd | Conjugados de ester de alfa-aminoacido-farmaco hidrolizables por carboxilesterasa. |
| GB0509224D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Inhibitors of intracellular enzymatic activity |
| JP2008545670A (ja) | 2005-05-27 | 2008-12-18 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | 疾患を処置するためのジアリールウレア類を含む組合せ治療 |
| WO2007053452A1 (en) | 2005-11-01 | 2007-05-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| JP5249770B2 (ja) * | 2005-11-03 | 2013-07-31 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼインヒビターとして有用なアミノピリジン |
| WO2007062459A1 (en) | 2005-11-29 | 2007-06-07 | Cytopia Research Pty Ltd | Selective kinase inhibitors based on pyridine scaffold |
| JP2009520038A (ja) | 2005-12-19 | 2009-05-21 | ジェネンテック・インコーポレーテッド | ピリミジンキナーゼインヒビター |
| TW200736232A (en) | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| EP2007801A4 (en) | 2006-04-07 | 2010-08-04 | Modpro Ab | BINDER FOR C-REACTIVE PROTEIN |
| US7601852B2 (en) | 2006-05-11 | 2009-10-13 | Kosan Biosciences Incorporated | Macrocyclic kinase inhibitors |
| US8604031B2 (en) * | 2006-05-18 | 2013-12-10 | Mannkind Corporation | Intracellular kinase inhibitors |
| US8217177B2 (en) * | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US8198448B2 (en) * | 2006-07-14 | 2012-06-12 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| PE20121506A1 (es) * | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| EP2529621B1 (en) * | 2006-09-22 | 2016-10-05 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| DK2089369T3 (da) | 2006-10-19 | 2011-05-09 | Rigel Pharmaceuticals Inc | 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme |
| JP5208123B2 (ja) | 2006-12-08 | 2013-06-12 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
| CA2670645A1 (en) | 2006-12-19 | 2008-07-03 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| CA2702647C (en) | 2007-01-31 | 2016-03-22 | Ym Biosciences Australia Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| US8242271B2 (en) | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| WO2009030890A1 (en) | 2007-09-03 | 2009-03-12 | University Court Of The University Of Dundee | Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| US8309685B2 (en) | 2007-12-21 | 2012-11-13 | Celgene Avilomics Research, Inc. | HCV protease inhibitors and uses thereof |
| CN104557880A (zh) | 2007-12-21 | 2015-04-29 | 阿维拉制药公司 | Hcv蛋白酶抑制剂和其用途 |
| US8293705B2 (en) | 2007-12-21 | 2012-10-23 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
| WO2009082697A1 (en) | 2007-12-21 | 2009-07-02 | Avila Therapeutics, Inc. | Hcv protease inhibitors and uses thereof |
| CA2713388C (en) | 2008-01-14 | 2016-03-29 | William Scott | Sulfone substituted 2,3-dihydroimidazo [1,2-c] quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AU2009262068C1 (en) | 2008-06-27 | 2015-07-02 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| US8188137B2 (en) | 2008-08-15 | 2012-05-29 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
| JP2012501654A (ja) | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス, インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
| US8603737B2 (en) | 2008-09-19 | 2013-12-10 | Celgene Avilomics Research, Inc. | Methods for identifying HCV protease inhibitors |
| KR20120063515A (ko) | 2009-09-09 | 2012-06-15 | 아빌라 테라퓨틱스, 인크. | Pi3 키나제 억제제 및 이들의 용도 |
| CN102713618B (zh) | 2009-09-16 | 2015-07-15 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和抑制剂 |
| WO2011082285A1 (en) | 2009-12-30 | 2011-07-07 | Avila Therapeutics, Inc. | Ligand-directed covalent modification of protein |
| PH12013500246A1 (en) | 2010-08-10 | 2019-10-11 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
-
2010
- 2010-09-15 CN CN201080050753.3A patent/CN102713618B/zh not_active Expired - Fee Related
- 2010-09-15 MX MX2012003332A patent/MX339811B/es active IP Right Grant
- 2010-09-15 IN IN2534DEN2012 patent/IN2012DN02534A/en unknown
- 2010-09-15 CN CN201510330338.8A patent/CN105063001A/zh active Pending
- 2010-09-15 WO PCT/US2010/048916 patent/WO2011034907A2/en not_active Ceased
- 2010-09-15 CA CA2773985A patent/CA2773985A1/en not_active Abandoned
- 2010-09-15 JP JP2012529871A patent/JP5806670B2/ja active Active
- 2010-09-15 BR BR112012005962A patent/BR112012005962A8/pt not_active IP Right Cessation
- 2010-09-15 EP EP10817748.6A patent/EP2478361A4/en not_active Withdrawn
- 2010-09-15 KR KR1020127009760A patent/KR20120093220A/ko not_active Ceased
- 2010-09-15 RU RU2012114902/04A patent/RU2012114902A/ru not_active Application Discontinuation
- 2010-09-15 NZ NZ620174A patent/NZ620174A/en not_active IP Right Cessation
- 2010-09-15 NZ NZ598705A patent/NZ598705A/en not_active IP Right Cessation
- 2010-09-15 SG SG2012018545A patent/SG179172A1/en unknown
- 2010-09-15 AU AU2010295690A patent/AU2010295690B2/en not_active Ceased
- 2010-09-15 US US12/882,484 patent/US9556426B2/en active Active
-
2012
- 2012-03-15 IL IL218678A patent/IL218678A0/en unknown
-
2015
- 2015-09-04 JP JP2015174949A patent/JP6397389B2/ja not_active Ceased
-
2016
- 2016-07-18 US US15/213,319 patent/US10662195B2/en active Active
- 2016-10-24 AU AU2016250339A patent/AU2016250339A1/en not_active Abandoned
-
2018
- 2018-08-31 JP JP2018163436A patent/JP6889689B2/ja not_active Expired - Fee Related
-
2021
- 2021-05-21 JP JP2021086337A patent/JP2021121219A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407939B2 (en) * | 2001-07-26 | 2008-08-05 | Curegenics Ltd. | Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics |
| CN101054380A (zh) * | 2006-04-13 | 2007-10-17 | 沈阳药科大学 | 用作细胞周期依赖性蛋白激酶抑制剂的吡唑并嘧啶类衍生物 |
| US20090137588A1 (en) * | 2007-10-19 | 2009-05-28 | Avila Therapeutics, Inc. | Heteroaryl compounds and uses thereof |
Non-Patent Citations (3)
| Title |
|---|
| Cysteine 116 participates in intermolecular bonding of the human VEGF121 homodimer;Nicholas J et al;《Archives of Biochemistry and Biophysics》;20021231;第404卷;126-135 * |
| Design of novel synthetic MTS conjugates of bile acids for site-directed sulfhydryl labeling of cysteine residues in bile acid binding and transporting proteins;Abhijit Ray et al;《Bioorganic & Medicinal Chemistry Letters》;20061231;第16卷;1473-1476 * |
| In Situ Preparation of Protein-"Smart" Polymer Conjugates with Retention of Bioactivity;Karina L. Heredia et al;《J. AM. CHEM. SOC》;20051231;第127卷;16955-16960 * |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6889689B2 (ja) | プロテインキナーゼコンジュゲート及びインヒビター | |
| RU2536584C2 (ru) | Гетероарильные соединения и их применение | |
| AU2010343055B2 (en) | Heteroaryl compounds and uses thereof | |
| RU2427578C2 (ru) | Аминопиримидины в качестве ингибиторов киназ | |
| ES2566339T3 (es) | Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas | |
| CN101902911B (zh) | 杂芳基化合物和其用途 | |
| US8557830B2 (en) | RAF kinase modulators and methods of use | |
| CN110603256B (zh) | 可用作wee-1激酶抑制剂的嘧啶并嘧啶酮 | |
| CN102448462A (zh) | 杂芳基化合物和其用途 | |
| CA2907243A1 (en) | Substituted dihydropyrimidopyrimidinone compounds and pharmaceutical compositions thereof use fgfr4 inhibitor | |
| AU2014250836A1 (en) | Quinazolines and azaquinazolines as dual inhibitors of RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways | |
| AU2015274285B2 (en) | Pyrimidine compounds and methods using the same | |
| CN104837835A (zh) | Vegfr3抑制剂 | |
| CN105153190B (zh) | 含联芳基酰胺结构的杂环并嘧啶类化合物及其制备方法和应用 | |
| CN107793417A (zh) | 吡咯并[2,3‑d]嘧啶类化合物及其盐,及制备方法和药用用途 | |
| CN101287727A (zh) | 新的高亲和力喹啉基激酶配体 | |
| CN104086562B (zh) | 含芳腙结构的杂环并嘧啶类化合物的制备及应用 | |
| WO2022028556A1 (zh) | Cdk9抑制剂及其用途 | |
| AU2016253570B2 (en) | Heteroaryl compounds and uses thereof | |
| AU2013202496B2 (en) | Heteroaryl compounds 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 | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: Massachusetts, USA Applicant after: Xinji Aveiro Meeks Research Inc. Address before: Massachusetts, USA Applicant before: Avila Therapeutics Inc. |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: AVILA THERAPEUTICS INC. TO: XINJI AVEIRO MEEKS RESEARCH INC. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150715 Termination date: 20170915 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |