TWI758300B - 免疫調節劑化合物 - Google Patents

免疫調節劑化合物 Download PDF

Info

Publication number
TWI758300B
TWI758300B TW106121437A TW106121437A TWI758300B TW I758300 B TWI758300 B TW I758300B TW 106121437 A TW106121437 A TW 106121437A TW 106121437 A TW106121437 A TW 106121437A TW I758300 B TWI758300 B TW I758300B
Authority
TW
Taiwan
Prior art keywords
alkyl
group
independently selected
haloalkyl
conr
Prior art date
Application number
TW106121437A
Other languages
English (en)
Chinese (zh)
Other versions
TW201803844A (zh
Inventor
克里斯多夫 蘭格
維克漢姆 馬拉菘爾
達倫 J 麥克默特里
辛尼瓦斯 普納
羅瑾德 斯穎
菊 楊
朋烈 張
Original Assignee
美商卡默森屈有限公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 美商卡默森屈有限公司 filed Critical 美商卡默森屈有限公司
Publication of TW201803844A publication Critical patent/TW201803844A/zh
Application granted granted Critical
Publication of TWI758300B publication Critical patent/TWI758300B/zh

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/075—Ethers or acetals
    • A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • 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
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • 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
    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • 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
    • A61K31/02—Halogenated hydrocarbons
    • A61K31/025—Halogenated hydrocarbons carbocyclic
    • A61K31/03—Halogenated hydrocarbons carbocyclic aromatic
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/12—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to hydrocarbon groups substituted by hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/22—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated the carbon skeleton being further substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/59—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C317/22—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/03—Ethers having all ether-oxygen atoms bound to acyclic carbon atoms
    • C07C43/14—Unsaturated ethers
    • C07C43/164—Unsaturated ethers containing six-membered aromatic rings
    • C07C43/168—Unsaturated ethers containing six-membered aromatic rings containing six-membered aromatic rings and other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen 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
    • C07D213/61—Halogen atoms or nitro 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
    • C07D213/79—Acids; Esters
    • C07D213/80—Acids; Esters in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
    • C07D239/30—Halogen atoms or nitro radicals
    • 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
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/58—Pyridine rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW106121437A 2016-06-27 2017-06-27 免疫調節劑化合物 TWI758300B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662355119P 2016-06-27 2016-06-27
US62/355,119 2016-06-27
US201662440100P 2016-12-29 2016-12-29
US62/440,100 2016-12-29

Publications (2)

Publication Number Publication Date
TW201803844A TW201803844A (zh) 2018-02-01
TWI758300B true TWI758300B (zh) 2022-03-21

Family

ID=60786614

Family Applications (1)

Application Number Title Priority Date Filing Date
TW106121437A TWI758300B (zh) 2016-06-27 2017-06-27 免疫調節劑化合物

Country Status (11)

Country Link
US (3) US10639284B2 (enExample)
EP (1) EP3474845B1 (enExample)
JP (1) JP7185532B2 (enExample)
KR (1) KR102401963B1 (enExample)
CN (1) CN109803651B (enExample)
AU (1) AU2017289038B2 (enExample)
CA (1) CA3029256A1 (enExample)
ES (1) ES2979332T3 (enExample)
IL (1) IL263752B (enExample)
TW (1) TWI758300B (enExample)
WO (1) WO2018005374A1 (enExample)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2652664T3 (es) 2011-12-01 2018-02-05 Chemocentryx, Inc. Anilinas sustituidas como antagonistas de CCR(4)
KR102622891B1 (ko) 2015-05-21 2024-01-08 케모센트릭스, 인크. Ccr2 조절제
KR102401963B1 (ko) * 2016-06-27 2022-05-25 케모센트릭스, 인크. 면역조절제 화합물
WO2018124766A2 (ko) 2016-12-28 2018-07-05 주식회사 녹십자랩셀 키메라 항원 수용체 및 이를 발현하는 자연 살해 세포
US11130740B2 (en) 2017-04-25 2021-09-28 Arbutus Biopharma Corporation Substituted 2,3-dihydro-1H-indene analogs and methods using same
CN111225896B (zh) * 2017-07-28 2024-03-26 凯莫森特里克斯股份有限公司 免疫调节剂化合物
KR102670486B1 (ko) 2017-08-08 2024-05-28 케모센트릭스, 인크. 마크로사이클릭 면역조절제
KR102677442B1 (ko) * 2017-09-25 2024-06-20 케모센트릭스, 인크. 케모카인 수용체 2(ccr2) 길항제 및 pd-1/pd-l1 억제제를 사용하는 병용 요법
CA3082328A1 (en) 2017-11-14 2019-05-23 Green Cross Lab Cell Corporation Anti-her2 antibody or antigen-binding fragment thereof, and chimeric antigen receptor comprising same
US11649294B2 (en) 2017-11-14 2023-05-16 GC Cell Corporation Anti-HER2 antibody or antigen-binding fragment thereof, and chimeric antigen receptor comprising same
US20190269664A1 (en) 2018-01-08 2019-09-05 Chemocentryx, Inc. Methods of treating solid tumors with ccr2 antagonists
ES2991280T3 (es) 2018-01-08 2024-12-03 Chemocentryx Inc Antagonistas de CCR2 para el tratamiento del linfoma cutáneo de linfocitos T
CN110092745B (zh) * 2018-01-29 2022-12-30 广州丹康医药生物有限公司 一种含芳环的化合物及其应用
SI3752501T1 (sl) 2018-02-13 2023-08-31 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
EP3755311A4 (en) * 2018-02-22 2021-11-10 ChemoCentryx, Inc. INDANAMINE AS PD-L1 ANTAGONISTS
US11578054B2 (en) 2018-03-01 2023-02-14 Bristol-Myers Squibb Company Compounds useful as immunomodulators
US12083118B2 (en) 2018-03-29 2024-09-10 Arbutus Biopharma Corporation Substituted 1,1′-biphenyl compounds, analogues thereof, and methods using same
CA3093130C (en) 2018-04-19 2023-10-17 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
EP3810109B1 (en) 2018-05-31 2024-08-07 Peloton Therapeutics, Inc. Compounds and compositions for inhibiting cd73
SI3820572T1 (sl) * 2018-07-13 2023-12-29 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
US11446289B2 (en) * 2018-08-29 2022-09-20 Chemocentryx, Inc. Combination therapy using C-C chemokine receptor 4 (CCR4) antagonists and one or more immune checkpoint inhibitors
MA53506A (fr) * 2018-08-29 2021-07-07 Chemocentryx Inc Méthodes de traitement du cancer avec des inhibiteurs de pd-l1 à petites molécules
JP7158577B2 (ja) * 2018-10-24 2022-10-21 ギリアード サイエンシーズ， インコーポレイテッド Ｐｄ－１／ｐｄ－ｌ１阻害剤
US20220168268A1 (en) 2019-03-22 2022-06-02 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Small-molecule inhibitor of pd-1/pd-l1, pharmaceutical composition thereof with pd-l1 antibody, and application of same
CN114340633A (zh) 2019-05-15 2022-04-12 凯莫森特里克斯股份有限公司 用于治疗pd-l1疾病的三芳基化合物
CN110128415B (zh) * 2019-05-31 2022-03-25 沈阳药科大学 用作免疫调节剂的吲哚啉类化合物及其制备方法
CA3138494A1 (en) * 2019-06-07 2020-12-10 David Craig Mc Gowan Heterocyclic immunomodulators as pdl1 checkpoint inhibitor
AU2020294781B2 (en) * 2019-06-20 2025-10-09 Chemocentryx, Inc. Compounds for treatment of PD-L1 diseases
EP3996711A4 (en) * 2019-07-10 2023-08-16 ChemoCentryx, Inc. Indanes as pd-l1 inhibitors
CN112457305B (zh) * 2019-09-09 2025-01-10 上海长森药业有限公司 含三环结构的芳香杂环化合物，及其制备方法和应用
US11866429B2 (en) 2019-10-16 2024-01-09 Chemocentryx, Inc. Heteroaryl-biphenyl amines for the treatment of PD-L1 diseases
KR20220084119A (ko) * 2019-10-16 2022-06-21 케모센트릭스, 인크. Pd-l1 질환의 치료를 위한 헤테로아릴-바이페닐 아미드
JP7720099B2 (ja) 2020-05-11 2025-08-07 シャンハイ ロングウッド バイオファルマシューティカルズ カンパニー リミテッド 免疫調節剤としてのビアリール環結合芳香族複素環誘導体の調製およびその適用
US11833209B2 (en) 2020-09-11 2023-12-05 Nammi Therapeutics, Inc. Formulated and/or co-formulated liposome compositions containing PD-1 antagonist prodrugs useful in the treatment of cancer and methods thereof
CN114437051A (zh) * 2021-09-18 2022-05-06 药康众拓(江苏)医药科技有限公司 一类联苯类化合物、其制备方法和用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200909393A (en) * 2007-08-03 2009-03-01 Boehringer Ingelheim Int Viral polymerase inhibitors
US20100292227A1 (en) * 2009-05-15 2010-11-18 Boehringer Ingleheim International Gmbh Inhibitors of human immunodeficiency virus replication
TW201329025A (zh) * 2011-11-01 2013-07-16 Astex Therapeutics Ltd 醫藥化合物
WO2015160641A2 (en) * 2014-04-14 2015-10-22 Bristol-Myers Squibb Company Compounds useful as immunomodulators

Family Cites Families (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1268002A (en) 1917-09-12 1918-05-28 William M Goodwin Measuring instrument.
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
IL120266A (en) 1996-02-28 2005-05-17 Pfizer Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions
CN101415683B (zh) 2006-03-31 2013-07-17 诺瓦提斯公司 新化合物
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
WO2008089307A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of pain, inflammation and cancer
EP2368876A1 (en) * 2010-03-01 2011-09-28 Sanofi Derivatives of aminoindanes, their preparation and their application in therapeutics
US9308236B2 (en) 2013-03-15 2016-04-12 Bristol-Myers Squibb Company Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
US20160145247A1 (en) * 2013-07-18 2016-05-26 Novartis Ag Aminomethyl-Biaryl Derivatives Complement Factor D inhibitors and uses thereof
EA029901B1 (ru) * 2013-09-04 2018-05-31 Бристол-Майерс Сквибб Компани Соединения для применения в качестве иммуномодуляторов
CN105849092A (zh) 2013-09-06 2016-08-10 奥瑞基尼探索技术有限公司 作为免疫调节剂的1，3，4-*二唑和1，3，4-噻二唑衍生物
BR112016004889B1 (pt) 2013-09-06 2023-10-03 Aurigene Discovery Technologies Limited Derivados de 1,2,4-oxadiazol como imunomoduladores
WO2016088082A1 (en) 2014-12-05 2016-06-09 Novartis Ag Amidomethyl-biaryl derivatives complement factor d inhibitors and uses thereof
US10745382B2 (en) 2015-10-15 2020-08-18 Bristol-Myers Squibb Company Compounds useful as immunomodulators
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
PT3377488T (pt) 2015-11-19 2022-11-21 Incyte Corp Compostos heterocíclicos como imunomoduladores
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
SI3394033T1 (sl) 2015-12-22 2021-03-31 Incyte Corporation Heterociklične spojine kot imunomodulatorji
EP3190103A1 (en) 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
RU2745195C2 (ru) 2016-04-07 2021-03-22 Кемосентрикс, Инк. Уменьшение массы опухоли путем введения ccr1 антагонистов в комбинации с pd-1 ингибиторами или pd-l1 ингибиторами
WO2017192961A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017202277A1 (zh) 2016-05-23 2017-11-30 中国医学科学院药物研究所 2-羟基-4-(2，3-双取代苄氧基)-5-取代苯甲醛衍生物的制备方法
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
PL3472167T3 (pl) 2016-06-20 2022-12-19 Incyte Corporation Związki heterocykliczne jako immunomodulatory
KR102401963B1 (ko) * 2016-06-27 2022-05-25 케모센트릭스, 인크. 면역조절제 화합물
WO2018006795A1 (zh) 2016-07-05 2018-01-11 广州再极医药科技有限公司 芳香乙炔或芳香乙烯类化合物、其中间体、制备方法、药物组合物及应用
EP3481815B1 (en) 2016-07-08 2021-09-29 Bristol-Myers Squibb Company 1,3-dihydroxy-phenyl derivatives useful as immunomodulators
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
US10144706B2 (en) 2016-09-01 2018-12-04 Bristol-Myers Squibb Company Compounds useful as immunomodulators
US20180065917A1 (en) 2016-09-02 2018-03-08 Polaris Pharmaceuticals, Inc. Immune checkpoint inhibitors, compositions and methods thereof
KR102599339B1 (ko) 2016-12-20 2023-11-08 브리스톨-마이어스 스큅 컴퍼니 면역조정제로서 유용한 화합물
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US20180179201A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
KR102696516B1 (ko) 2016-12-22 2024-08-22 인사이트 코포레이션 면역조절제로서의 벤조옥사졸 유도체
MY197501A (en) 2016-12-22 2023-06-19 Incyte Corp Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
EP3558973B1 (en) 2016-12-22 2021-09-15 Incyte Corporation Pyridine derivatives as immunomodulators
US20180177784A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
CN108250159B (zh) 2016-12-29 2023-07-11 深圳微芯生物科技股份有限公司 脲类化合物、其制备方法及其应用
CN108395443B (zh) 2017-02-04 2021-05-04 广州丹康医药生物有限公司 抑制程序性死亡受体配体1的环状化合物及其用途
KR20190133714A (ko) 2017-03-27 2019-12-03 브리스톨-마이어스 스큅 컴퍼니 면역조정제로서 유용한 치환된 이소퀴놀린 유도체
JOP20180040A1 (ar) * 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
TW201841896A (zh) 2017-04-26 2018-12-01 大陸商南京聖和藥業股份有限公司 作為pd—l1抑制劑的雜環類化合物
CN108863963B (zh) 2017-05-08 2022-05-27 南京圣和药物研发有限公司 作为pd-l1抑制剂的杂环类化合物
CN111225896B (zh) * 2017-07-28 2024-03-26 凯莫森特里克斯股份有限公司 免疫调节剂化合物
KR102670486B1 (ko) 2017-08-08 2024-05-28 케모센트릭스, 인크. 마크로사이클릭 면역조절제
EP3669872A4 (en) 2017-08-18 2021-05-05 Shanghai Ennovabio Pharmaceuticals Co., Ltd. FORMYL PYRIDINE DERIVATIVE WITH PD-L1 INHIBITORING EFFECT, MANUFACTURING METHOD FOR IT AND USE THEREOF
CN111051332B (zh) 2017-10-03 2024-09-06 百时美施贵宝公司 免疫调节剂
CN109665968B (zh) 2017-10-16 2022-02-22 四川科伦博泰生物医药股份有限公司 并环化合物及其制备方法和用途
CN109678796B (zh) 2017-10-19 2023-01-10 上海长森药业有限公司 Pd-1/pd-l1小分子抑制剂及其制备方法和用途
CN109721527B (zh) 2017-10-27 2024-03-12 广州丹康医药生物有限公司 一种新型抗pd-l1化合物、其应用及含其的组合物
AU2018362046B2 (en) 2017-11-06 2023-04-13 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
CN109956898B (zh) 2017-12-22 2021-03-26 上海海雁医药科技有限公司 免疫调节剂及其制法与医药上的用途
AU2018398887B2 (en) 2017-12-29 2024-03-14 Guangzhou Maxinovel Pharmaceuticals Co., Ltd Aromatic vinyl or aromatic ethyl derivative, preparation method therefor, intermediate, pharmaceutical composition, and application
JP7214752B2 (ja) 2018-01-23 2023-01-30 ブリストル－マイヤーズ スクイブ カンパニー 免疫調節剤として有用な２，８－ジアシル－２，８－ジアザスピロ［５．５］ウンデカン化合物
CN110092745B (zh) * 2018-01-29 2022-12-30 广州丹康医药生物有限公司 一种含芳环的化合物及其应用
EP3750887B1 (en) 2018-02-05 2025-05-28 Abbisko Therapeutics Co., Ltd. Biaryl derivatives and their pharmaceutical application for the treatment of pd-1/pd-l1 signal pathway-mediated diseases
SI3752501T1 (sl) 2018-02-13 2023-08-31 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
EP3755311A4 (en) 2018-02-22 2021-11-10 ChemoCentryx, Inc. INDANAMINE AS PD-L1 ANTAGONISTS
US11578054B2 (en) * 2018-03-01 2023-02-14 Bristol-Myers Squibb Company Compounds useful as immunomodulators
CN111788193B (zh) 2018-03-13 2023-04-04 广东东阳光药业有限公司 Pd-1/pd-l1类小分子抑制剂及其在药物中的应用
EP3765453A1 (en) 2018-03-13 2021-01-20 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
EP4212529B1 (en) 2018-03-30 2025-01-29 Incyte Corporation Heterocyclic compounds as immunomodulators
JP2021520342A (ja) 2018-04-03 2021-08-19 ベータ ファーマシューティカルズ カンパニー リミテッド 免疫調節物質、組成物及びそれらの方法
CA3093130C (en) 2018-04-19 2023-10-17 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
FI4219492T3 (fi) 2018-05-11 2025-02-17 Incyte Corp Heterosyklisiä yhdisteitä immunomodulaattoreina
CN111886219B (zh) 2018-07-11 2023-04-25 上海和誉生物医药科技有限公司 免疫抑制剂及其制备方法和在药学上的应用
WO2020011243A1 (en) 2018-07-12 2020-01-16 Betta Pharmaceuticals Co., Ltd Immunomodulators, compositions and methods thereof
SI3820572T1 (sl) * 2018-07-13 2023-12-29 Gilead Sciences, Inc. Inhibitorji pd-1/pd-l1
CN112424194B (zh) 2018-07-19 2024-02-06 贝达药业股份有限公司 免疫调节剂及其组合物和制备方法
CN112566900B (zh) 2018-07-19 2024-04-26 贝达药业股份有限公司 免疫调节剂及其组合物和制备方法
WO2020025030A1 (zh) 2018-08-01 2020-02-06 上海轶诺药业有限公司 一类具有免疫调节功能的芳香化合物的制备和应用
MA53506A (fr) 2018-08-29 2021-07-07 Chemocentryx Inc Méthodes de traitement du cancer avec des inhibiteurs de pd-l1 à petites molécules
CN109336857A (zh) 2018-11-13 2019-02-15 南方医科大学 一种含取代联苯的黄酮及其应用
CN109438263A (zh) 2018-11-28 2019-03-08 南方医科大学 一种含取代联苯的萘及其应用
CN109503546A (zh) 2019-01-10 2019-03-22 南方医科大学 一种间苯二酚二苯甲醚及其应用
CN109776377B (zh) 2019-02-01 2021-08-24 沈阳药科大学 吲哚啉类化合物及其制备方法和应用
CN109776445B (zh) 2019-03-28 2022-12-06 中国药科大学 苯并噁二唑类化合物及其制备方法和医药用途
CN114340633A (zh) 2019-05-15 2022-04-12 凯莫森特里克斯股份有限公司 用于治疗pd-l1疾病的三芳基化合物
CN110200959A (zh) 2019-05-30 2019-09-06 天津科技大学 一种黄酮类化合物的应用
CN110128415B (zh) 2019-05-31 2022-03-25 沈阳药科大学 用作免疫调节剂的吲哚啉类化合物及其制备方法
EP3996711A4 (en) 2019-07-10 2023-08-16 ChemoCentryx, Inc. Indanes as pd-l1 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200909393A (en) * 2007-08-03 2009-03-01 Boehringer Ingelheim Int Viral polymerase inhibitors
US20100292227A1 (en) * 2009-05-15 2010-11-18 Boehringer Ingleheim International Gmbh Inhibitors of human immunodeficiency virus replication
TW201329025A (zh) * 2011-11-01 2013-07-16 Astex Therapeutics Ltd 醫藥化合物
WO2015160641A2 (en) * 2014-04-14 2015-10-22 Bristol-Myers Squibb Company Compounds useful as immunomodulators

Also Published As

Publication number Publication date
TW201803844A (zh) 2018-02-01
US11426364B2 (en) 2022-08-30
IL263752A (en) 2019-01-31
US20210052514A1 (en) 2021-02-25
CN109803651B (zh) 2022-05-31
US20230117425A1 (en) 2023-04-20
EP3474845A1 (en) 2019-05-01
ES2979332T3 (es) 2024-09-25
AU2017289038A1 (en) 2019-02-07
EP3474845A4 (en) 2020-02-26
JP2019527202A (ja) 2019-09-26
US20180008554A1 (en) 2018-01-11
WO2018005374A1 (en) 2018-01-04
JP7185532B2 (ja) 2022-12-07
IL263752B (en) 2022-04-01
EP3474845B1 (en) 2024-03-20
KR102401963B1 (ko) 2022-05-25
US10639284B2 (en) 2020-05-05
AU2017289038B2 (en) 2021-07-22
CN109803651A (zh) 2019-05-24
KR20190053836A (ko) 2019-05-20
CA3029256A1 (en) 2018-01-04
US11793771B2 (en) 2023-10-24

Similar Documents

Publication Publication Date Title
TWI758300B (zh) 免疫調節劑化合物
CN111225896B (zh) 免疫调节剂化合物
US11266643B2 (en) Triaryl compounds for treatment of PD-L1 diseases
CN111225665B (zh) 大环免疫调节剂
JP7736678B2 (ja) Ｐｄ－ｌ１疾患の処置のためのヘテロアリール－ビフェニルアミド
JP7387616B2 (ja) Ｐｄ－ｌ１アンタゴニストとしてのインダン－アミン
TWI902711B (zh) 用於治療ｐｄ-ｌ１疾病之雜芳基-聯苯基醯胺
RU2848051C1 (ru) Гетероарилбифенил амиды для лечения pd-l1 заболеваний
HK40007517B (en) Immunomodulator compounds
HK40007517A (en) Immunomodulator compounds