HRP20230306T1 - Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori - Google Patents

Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori Download PDF

Info

Publication number
HRP20230306T1
HRP20230306T1 HRP20230306TT HRP20230306T HRP20230306T1 HR P20230306 T1 HRP20230306 T1 HR P20230306T1 HR P20230306T T HRP20230306T T HR P20230306TT HR P20230306 T HRP20230306 T HR P20230306T HR P20230306 T1 HRP20230306 T1 HR P20230306T1
Authority
HR
Croatia
Prior art keywords
methyl
tetrahydro
imidazo
cancer
membered
Prior art date
Application number
HRP20230306TT
Other languages
English (en)
Inventor
Liangxing Wu
Kaijiong Xiao
Wenqing Yao
Original Assignee
Incyte Corporation
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=66625434&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20230306(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corporation filed Critical Incyte Corporation
Publication of HRP20230306T1 publication Critical patent/HRP20230306T1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants

Claims (21)

1. Spoj, naznačen time, da je predstavljen Formulom I: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, pri čemu: R1 je metil, CN, F, Cl, ili Br; R2 je metil, CN, F, Cl, ili Br; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil ili 4-člani do 6-člani heterocikloalkil-C1-2 alkil-, gdje svaki 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil i 4-člani do 6-člani heterocikloalkil-C1-2 alkil-, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil i 4-člani do 6-člani heterocikloalkil-C1-2 alkil- od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, OH, CON(CH3)2, CH3, F, Cl, Br, CN, etila, i propila.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da ima Formulu I: [image] ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, pri čemu: R1 je metil, CN, F, Cl, ili Br; R2 je metil, CN, F, Cl, ili Br; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil ili 4-člani do 6-člani heterocikloalkil-C1-2 alkil-, gdje svaki 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil i 4-člani do 6-člani heterocikloalkil-C1-2 alkil-, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril, 5-člani do 6-člani heteroaril-C1-2 alkil, 4-člani do 6-člani heterocikloalkil i 4-člani do 6-člani heterocikloalkil-C1-2 alkil- od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, i OH.
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R1 je metil, F, Cl, ili Br; ili (b) R1 je metil; ili (c) R1 je F, Cl, ili Br; ili (d) R1 je Cl.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R2 je metil; ili (b) R2 je CN; ili (c) R2 je F, Cl, ili Br; ili (d) R2 je Cl.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R1 je Cl i R2 je Cl; ili (b) R1 je Cl i R2 je metil; ili (c) R1 je metil i R2 je Cl; ili (d) R1 je Cl i R2 je CN; ili (e) R1 je metil i R2 je metil.
6. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, OH, CON(CH3)2, i CH3; ili (b) R3 je C1-4 alkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH, OH, i CON(CH3)2; ili (c) R3 je C3-8 cikloalkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH, OH, i CH3; ili (d) R3 je ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, 4-karboksifenetil, (4-karboksicikloheksil)etil, ili 4-karboksi-4-metilcikloheksil; ili (e) R3 je H, metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, 2-karboksi-2-metilpropil, ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, 4-karboksifenetil, (1H-pirazol-3-il)metil, tetrahidro-2H-piran-4-il, 1-karbamoilpiperidin-4-il, 1-sulfamoilpiperidin-4-il, (3-karboksi-1H-pirazol-5-il)metil, 4-karboksibutil, (4-karboksicikloheksil)etil, ili 4-karboksi-4-metilcikloheksil.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, i OH; ili (b) R3je H; ili (c) R3 je C1-4 alkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH i OH; ili (d) R3 je metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, 2-karboksi-2-metilpropil, ili 4-karboksibutil; ili (e) R3 je metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, ili 2-karboksi-2-metilpropil; ili (f) R3 je C3-8cikloalkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH i OH; ili (g) R3 je C3-8 cikloalkil-C1-2 alkil-, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH i OH; ili (h) R3 je C6-10 aril-C1-2 alkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od COOH i OH; ili (i) R3 je ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, ili 4-karboksifenetil; ili (j) R3 je 5-člani do 6-člani heteroaril-C1-2 alkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2 i COOH; ili (k) R3 je 4-člani do 6-člani heterocikloalkil, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2 i COOH; ili (l) R3 je (1H-pirazol-3-il)metil, tetrahidro-2H-piran-4-il, 1-karbamoilpiperidin-4-il, 1-sulfamoilpiperidin-4-il, ili (3-karboksi-1H-pirazol-5-il)metil; ili (m) R3 je H, metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, 2-karboksi-2-metilpropil, ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, 4-karboksifenetil, (1H-pirazol-3-il)metil, tetrahidro-2H-piran-4-il, 1-karbamoilpiperidin-4-il, 1-sulfamoilpiperidin-4-il, ili (3-karboksi-1H-pirazol-5-il)metil.
8. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, naznačen time, da: (a) R1 je metil, CN, F, Cl, ili Br; R2 je metil, CN, F, Cl, ili Br; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, OH, CON(CH3)2, i CH3; ili (b) R1 je metil, CN, F, Cl, ili Br; R2 je metil, CN, F, Cl, ili Br; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, i OH; ili (c) R1 je metil, ili Cl; R2 je metil, CN, ili Cl; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, OH, CON(CH3)2, i CH3; ili (d) R1 je metil, ili Cl; R2 je metil, CN, ili Cl; i R3 je H, C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, ili 4-člani do 6-člani heterocikloalkil, gdje svaki 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil, ima jedan ili dva heteroatoma kao članove u prstenu, odabrane od O, N i S, i pri čemu je svaki C1-4 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-2 alkil-, C6-10 aril-C1-2 alkil, 5-člani do 6-člani heteroaril-C1-2 alkil, i 4-člani do 6-člani heterocikloalkil od R3, opcionalno supstituiran s jednim ili dva supstituenta neovisno odabrana od CONH2, SO2NH2, COOH, i OH; ili (e) R1 je metil, ili Cl; R2 je metil, CN, ili Cl; i R3 je H, metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, 2-karboksi-2-metilpropil, ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, 4-karboksifenetil, (1H-pirazol-3-il)metil, tetrahidro-2H-piran-4-il, 1-karbamoilpiperidin-4-il, 1-sulfamoilpiperidin-4-il, (3-karboksi-1H-pirazol-5-il)metil, 4-karboksibutil, (4-karboksicikloheksil)etil, ili 4-karboksi-4-metilcikloheksil; ili (f) R1 je metil, ili Cl; R2 je metil, CN, ili Cl; i R3 je H, metil, etil, izopropil, 1,3-dihidroksipropan-2-il, 2,3-dihidroksipropil, 2-hidroksipropil, 2-hidroksietil, 3-hidroksipropil, karboksimetil, 3-karboksipropil, 2-karboksi-2-metilpropil, ciklobutil, 4-hidroksicikloheksil, (1-karboksiciklopropil)metil, (4-karboksibiciklo[2.2.1]heptan-1-il)etil, (4-karboksibiciklo[2.2.1]heptan-1-il)metil, (4-karboksibiciklo[2.2.2]oktan-1-il)metil, (3-karboksibiciklo[1.1.1]pentan-1-il)metil, 4-karboksifenetil, (1H-pirazol-3-il)metil, tetrahidro-2H-piran-4-il, 1-karbamoilpiperidin-4-il, 1-sulfamoilpiperidin-4-il, ili (3-karboksi-1H-pirazol-5-il)metil.
9. Spoj prema patentnom zahtjevu 1, naznačen time, da se spoj bira od sljedećih: (a) 4-(2-(2-((2,2'-dikloro-3'-(1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(1-metil-5-(tetrahidro-2H-piran-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(1,5-dimetil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-etil-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-izopropil-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-ciklobutil-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(1-karbamoilpiperidin-4-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(1-metil-5-(1-sulfamoilpiperidin-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-((1H-pirazol-3-il)metil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-(1,3-dihidroksipropan-2-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((2,2'-dikloro-3'-(5-(2,3-dihidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (S)-4-(2-(2-((2,2'-dikloro-3'-(5-(2,3-dihidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((2,2'-dikloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (S)-4-(2-(2-((2,2'-dikloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-(3-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4,4'-(((((2,2'-dikloro-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina); 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(karboksimetil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(3-karboksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(karboksi-2-metilpropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-((1-karboksiciklopropil)metil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.2]oktan-1-karboksilna kiselina; 3-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[1.1.1]pentan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(4-karboksifenetil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 5-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo-1H-pirazol-3-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-metil-3'-(1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-metil-3'-(1-metil-5-(tetrahidro-2H-piran-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-metil-3'-(1,5-dimetil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(1-karbamoilpiperidin-4-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-kloro-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((2-kloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (S)-4-(2-(2-((2-kloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-3'-(5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4,4'-(((((2-kloro-2'-metil-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina); 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-kloro-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(4-karboksifenetil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-kloro-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2'-kloro-2-metil-3'-(1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2'-kloro-2-metil-3'-(1-metil-5-(tetrahidro-2H-piran-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2'-kloro-3'-(1,5-dimetil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(1-karbamoilpiperidin-4-il)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-kloro-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((2'-kloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (S)-4-(2-(2-((2'-kloro-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2'-kloro-3'-(5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2-kloro-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(4-karboksifenetil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-kloro-2-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-cijano-3'-(1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-cijano-3'-(1-metil-5-(tetrahidro-2H-piran-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-cijano-3'-(1,5-dimetil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((2-kloro-2'-cijano-3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2-kloro-2'-cijano-3'-(5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4,4'-(((((2-kloro-2'-cijano-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina); 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-kloro-2-cijano-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dimetil-3'-(1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4,4'-(((((2,2'-dimetil-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina); 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dimetil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dimetil-3'-(1-metil-5-(tetrahidro-2H-piran-4-il)-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (R)-4-(2-(2-((3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dimetil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; (S)-4-(2-(2-((3'-(5-(2-hidroksipropil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dimetil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(2-hidroksietil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dimetil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-(4-hidroksicikloheksil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; i 4-(2-(2-((2-kloro-3'-(5-(4-hidroksicikloheksil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2'-metil-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; ili njihova farmaceutski prihvatljiva sol; ili (b) 4-(2-(2-((3'-(5-(2-(trans-4-karboksicikloheksil)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(4-karboksibutil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((2,2'-dikloro-3'-(5-(5-(dimetilamino)-5-oksopentil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; 4-(2-(2-((3'-(5-(cis-4-karboksi-4-metilcikloheksil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; i 4-(2-(2-((3'-(5-(trans-4-karboksi-4-metilcikloheksil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)etil)biciklo[2.2.1]heptan-1-karboksilna kiselina; ili njihova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1, naznačen time, da je 4,4'-(((((2-kloro-2'-metil-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina), ili njezina farmaceutski prihvatljiva sol.
11. Spoj prema patentnom zahtjevu 1, naznačen time, da je 4,4'-(((((2,2'-dikloro-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina), ili njezina farmaceutski prihvatljiva sol.
12. Spoj prema patentnom zahtjevu 1, naznačen time, da je 4-((2-((3'-(5-(2-(4-karboksibiciklo[2.2.1]heptan-1-il)etil)-1-metil-4,5,6,7-tetrahidro-1H-imidazo[4,5-c]piridin-2-karboksamido)-2,2'-dikloro-[1,1'-bifenil]-3-il)karbamoil)-1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-5-il)metil)biciklo[2.2.1]heptan-1-karboksilna kiselina, ili njezina farmaceutski prihvatljiva sol.
13. Spoj prema patentnom zahtjevu 1, naznačen time, da je 4,4'-(((((2-kloro-2'-cijano-[1,1'-bifenil]-3,3'-diil)bis(azandiil))bis(karbonil))bis(1-metil-1,4,6,7-tetrahidro-5H-imidazo[4,5-c]piridin-2,5-diil))bis(etan-2,1-diil))bis(biciklo[2.2.1]heptan-1-karboksilna kiselina), ili njezina farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol ili njegov stereoizomer, ili spoj prema bilo kojem od patentnih zahtjeva 9 do 13, ili njegovu farmaceutski prihvatljivu sol, te farmaceutski prihvatljivo pomoćno sredstvo ili nosač.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, ili spoj prema bilo kojem od patentnih zahtjeva 9 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u inhibiranju interakcije PD-1/PD-L1.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, ili spoj prema bilo kojem od patentnih zahtjeva 9 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u liječenju bolesti ili poremećaja koji su povezani s inhibiranjem interakcije PD-1/PD-L1.
17. Spoj, sol, ili stereoizomer za uporabu prema patentnom zahtjevu 16, naznačen time, da se kod bolesti ili poremećaja radi o zaraznoj bolesti, upali, autoimunoj bolesti, raku, ili neurodegenerativnom poremećaju.
18. Spoj, sol, ili stereoizomer za uporabu prema patentnom zahtjevu 16, naznačen time, da se kod bolesti ili poremećaja radi o raku.
19. Spoj, sol ili stereoizomer za uporabu prema patentnom zahtjevu 18, naznačen time, da: (a) rak se bira od sljedećih: rak kostiju, rak gušterače, rak kože, rak glave i vrata, kožni maligni melanom, očni maligni melanom, rak maternice, rak jajnika, rak rektuma, rak analne regije, rak abdomena, rak testisa, karcinom falopijevih cijevi, rak endometrija, karcinom cerviksa, karcinom vagine, karcinom vulve, ne-Hodgkinov limfom, rak jednjaka, rak malog crijeva, rak endokrinog sustava, rak tiroidne žlijezde, rak paratiroidne žlijezde, rak adrenalne žlijezde, sarkom mekog tkiva, rak uretre, rak penisa, kronične ili akutne leukemije, solidni tumori u djetinjstvu, limfom limfocita, rak mokraćnog mjehura, rak bubrega, karcinom bubrežne zdjelice, neoplazma središnjeg živčanog sustava (CNS), primarni limfom središnjeg živčanog sustava (CNS), tumorska angiogeneza, tumor kralježnice, gliom moždanog debla, pituitarni adenom, Kaposijev sarkom, epidermoidni rak, rak rožnatih stanica, limfom T stanica, vrste raka koje su inducirane okolišem uključujući one koje su inducirane azbestom, melanom, metastatski maligni melanom, rak bubrega, karcinom svijetlih bubrežnih stanica, rak prostate, adenokarcinom prostate koji je hormonski otporan, rak dojke, rak debelog crijeva, rak pluća, rak rožnatih stanica glave i vrata, urotelni rak, vrste raka s velikom mikrosatelitskom nestabilnošću (MSIhigh), solidni tumori, solidni tumori raka prostate, solidni tumori raka debelog crijeva, solidni tumori raka jednjaka, solidni tumori raka endometrija, solidni tumori raka bubrega, solidni tumori raka jetre, solidni tumori raka gušterače, solidni tunori raka želuca, solidni tumori raka dojke, solidni tumori raka pluća, solidni tumori raka glave i vrata, solidni tumori tiroidnog raka, solidni tumori glioblastoma, solidni tumori sarkoma, solidni tumori raka mokraćnog mjehura, povratni ne-Hodgkinov limfom, uporni ne-Hodgkinov limfom, periodični folikularni ne-Hodgkinov limfom, Hodgkinov limfom, holangiokarcinom, rak žučnih vodova, rabdomiosarkom, leiomiosarkom, hepatocelularni karcinom, Ewingov sarkom, rak mozga, tumor mozga, astrocitom, neuroblastom, karcinom bazalnih stanica, hondrosarkom, epitelni sarkom, rak oka, gastrointestinalni rak, gastrointestinalni stromalni tumori, leukemija kosmatih stanica, intestinalni rak, rak otočićkih stanica, oralni rak, rak usta, rak grla, rak grkljana, rak usne, mezoteliom, rak vrata, rak nosne šupljine, okularni rak, okularni melanom, rak karlice, karcinom renalnih stanica, rak žlijezde slinovnice, rak sinusa, rak kičme, rak jezika, tubularni karcinom, rak mokraćnih kanala, vrste raka genitourinarnog trakta, vrste raka živčanog sustava, hematološke vrste raka, hematološki limfomi, hematološke leukemije, akutna limfoblastična leukemija (ALL), akutna mijeloična leukemija (AML), akutna promijelocitna leukemija (APL), kronična limfocitna leukemija (CLL), kronična mijeloična leukemija (CML), difuzni limfom velikih B stanica (DLBCL), limfom plaštenih stanica, mijeloproliferativne bolesti, primarna mijelofibroza (PMF), policitemija vera (PV), esencijalna trombocitoza (ET), sindrom mijelodisplazije (MDS), akutni limfoblastični limfom T stanica (T-ALL), multipli mijelom (MM), sarkomi, osteosarkomi, angiosarkomi, fibrosarkomi, liposarkomi, miksomi, rabdomiom, rabdosarkom, fibrom, lipom, harmatom, teratom, rak ne-malih stanica pluća (NSCLC), rak malih stanica pluća, bronhogeni karcinom, bronhogeni sarkom rožnatih stanica, bronhogeni karcinom nediferenciranih malih stanica, bronhogeni karcinom nediferenciranih velikih stanica, bronhogeni adenokarcinom, alveolni (bronhijalni) karcinom, bronhijalni adenom, hondromatozni hamartom, karcinom rožnatih stanica jednjaka, adenokarcinom jednjaka, leiomiosarkom jednjaka, limfom jednjaka, karcinom abdomena, limfom abdomena, leiomiosarkom abdomena, duktalni adenokarcinom, inzulinom, glukagonom, gastrinom, karcinoidni tumori gušterače, vipom, vrste raka malog crijeva, adenokarcinom malog crijeva, limfom malog crijeva, karcionidni tumori malog crijeva, leiomiom malog crijeva, hemangiom malog crijeva, lipom malog crijeva, neurofibrom malog crijeva, fibrom malog crijeva, vrste raka velikog crijeva, adenokarcinom velikog crijeva, tubularni adenom velikog crijeva, vilozni adenom velikog crijeva, hamartom velikog crijeva, leiomiom velikog crijeva, kolorektalni rak, adenokarcinom bubrega, Wilmov tumor (nefroblastom), karcinom rožnatih stanica mokraćnog mjehura, karcinom prijelaznih stanica mokraćnog mjehura, adenokarcinom mokraćnog mjehura, karcinom rožnatih stanica uretre, karcinom prijelaznih stanica uretre, adenokarcinom uretre, adenokarcinom prostate, sarkom prostate, vrste raka testisa, seminom testisa, teratom testisa, embrionalni karcinom testisa, teratokarcinom testisa, horiokarcinom testisa, sarkom testisa, karcinom intersticijskih stanica testisa, fibrom testisa, fibroadenom testisa, adenomatoidni tumori testisa, lipom testisa, vrste raka jetre, hepatom, hepatoblastom, hepatocelularni adenom, hemangiom, maligni fibrozni histiocitom, maligni limfom (sarkom retikularnih stanica), maligni tumorski hordom divovskih stanica, osteohronfrom (osteokartilagne ekstoze), benigni hondrom, hondroblastom, hondromiksofibrom, osteoidni osteom, tumori divovskih stanica, vrste raka lubanje, osteom, granulom, ksantom, osteitis deformans, meningne vrste raka, meningiom, meningiosarkom, gliomatoza, moždani astrocitom, moždani meduloblastom, moždani gliom, moždani ependimom, moždani germinom (pinealom), moždani glioblastom, multiformni moždani glioblastom, moždani oligodendrogliom, švanom mozga, moždani retinoblastom, kongenitalni tumori mozga, vrste raka kralježnice, neurofibrom kralježnice, meningiom kralježnice, gliom kralježnice, sarkom kralježnice, bolest Lhermitte-Duclos, ginekološke vrste raka, vrste raka maternice, endometrijski karcinom, predtumorna cervikalna displazija, karcinom jajnika, serozni cistadenokarcinom, mucinozni cistadenokarcinom, neklasificirani karcinom, tumori granulozno-tekalnih stanica, tumori Sertoli-Leydig stanica, disgerminom, maligni teratom, karcinom rožnatih stanica vulve, karcinom intraepitelija vulve, adenokarcinom vulve, fibrosarkom vulve, melanom vulve, karcinom svijetlih stanica vagine, karcinom rožnatih stanica vagine, botrioidni sarkom, embrionalni rabdomiosarkom, karcinom rožnatih stanica, atipičan madež displastični nevus, lipom kože, angiom, dermatofibrom, keloidi, trostruko negativni rak dojke (TNBC), i urotelni karcinom; ili (b) rak je metastatski rak koji eksprimira PD-L1; ili (c) rak je rak pluća; ili (d) rak je rak malih stanica pluća; ili (e) rak je rak ne-malih stanica pluća (NSCLC); ili (f) rak je karcinom rožnatih stanica; ili (g) rak je hepatski rak; ili (h) rak je hepatocelularni karcinom; ili (i) rak je melanom; ili (j) rak je rak mokraćnog mjehura; ili (k) rak je rak uretre; ili (l) rak je renalni rak; ili (m) rak je karcinom svijetlih bubrežnih stanica.
20. Spoj, sol ili stereoizomer za uporabu prema patentnom zahtjevu 18, naznačen time, da: (a) rak se bira od sljedećih: kožni melanom, invazivni karcinom dojke, karcinom rožnatih stanica glave i vrata, nemišićni invazivni rak mokraćnog mjehura (NMIBC), rak žučnog trakta, rak rožnatih stanica ne-malih stanica pluća (NSCLC), karcinom jednjaka, adenokarcinom abdomena, kolorektalni adenokarcinom, urološke vrste raka, papilarni karcinom bubrega, rak zametnih stanica testisa, karcinom hromofobnih bubrežnih stanica, serozni adenokarcinom, i karcinom kožnih rožnatih stanica; ili (b) rak je karcinom kožnih rožnatih stanica.
21. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol ili njegov stereoizomer, ili spoj prema bilo kojem od patentnih zahtjeva 9 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u poboljšavanju, pospješivanju i/ili povećavanju imunosnog odgovora kod pacijenta.
HRP20230306TT 2018-05-11 2019-05-10 Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori HRP20230306T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862670249P 2018-05-11 2018-05-11
US201862688164P 2018-06-21 2018-06-21
EP19725627.4A EP3790877B1 (en) 2018-05-11 2019-05-10 Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators
PCT/US2019/031728 WO2019217821A1 (en) 2018-05-11 2019-05-10 Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators

Publications (1)

Publication Number Publication Date
HRP20230306T1 true HRP20230306T1 (hr) 2023-05-12

Family

ID=66625434

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20230306TT HRP20230306T1 (hr) 2018-05-11 2019-05-10 Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori

Country Status (30)

Country Link
US (4) US10618916B2 (hr)
EP (2) EP3790877B1 (hr)
JP (2) JP7328995B2 (hr)
KR (1) KR20210018282A (hr)
CN (1) CN112752756A (hr)
AU (2) AU2019267824B2 (hr)
BR (1) BR112020022936A2 (hr)
CA (1) CA3099994A1 (hr)
CL (2) CL2020002922A1 (hr)
CO (1) CO2020015437A2 (hr)
CR (1) CR20200614A (hr)
DK (1) DK3790877T3 (hr)
EC (1) ECSP20079887A (hr)
ES (1) ES2943028T3 (hr)
FI (1) FI3790877T3 (hr)
HR (1) HRP20230306T1 (hr)
HU (1) HUE061503T2 (hr)
JO (1) JOP20200288A1 (hr)
LT (1) LT3790877T (hr)
MD (1) MD3790877T2 (hr)
MX (1) MX2020012045A (hr)
PE (1) PE20211918A1 (hr)
PH (1) PH12020551927A1 (hr)
PL (1) PL3790877T3 (hr)
PT (1) PT3790877T (hr)
RS (1) RS64188B1 (hr)
SG (1) SG11202011165TA (hr)
SI (1) SI3790877T1 (hr)
TW (1) TWI821288B (hr)
WO (1) WO2019217821A1 (hr)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
WO2016134320A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
JP7148401B2 (ja) 2015-11-19 2022-10-05 インサイト・コーポレイション 免疫調節剤としての複素環化合物
SI3394033T1 (sl) 2015-12-22 2021-03-31 Incyte Corporation Heterociklične spojine kot imunomodulatorji
US20170320875A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
MX2018016273A (es) 2016-06-20 2019-07-04 Incyte Corp Compuestos heterociclicos como inmunomoduladores.
KR102401963B1 (ko) 2016-06-27 2022-05-25 케모센트릭스, 인크. 면역조절제 화합물
WO2018013789A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
BR112019012993A2 (pt) 2016-12-22 2019-12-03 Incyte Corp derivados de benzo-oxazol como imunomoduladores
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
HUE060233T2 (hu) 2016-12-22 2023-02-28 Incyte Corp Tetrahidro imidazo[4,5-c]piridin-származékok mint a PD-L1 internalizációját indukáló szerek
US11130740B2 (en) 2017-04-25 2021-09-28 Arbutus Biopharma Corporation Substituted 2,3-dihydro-1H-indene analogs and methods using same
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
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
MA49859A (fr) 2017-08-08 2021-04-07 Chemocentryx Inc Immunomodulateurs macrocycliques
TWI707849B (zh) 2018-02-13 2020-10-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
MA51232A (fr) 2018-02-22 2020-10-07 Chemocentryx Inc Indane-amines utiles en tant qu'antagonistes de pd-l1
CR20200441A (es) 2018-02-27 2021-03-15 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
SI3774791T1 (sl) 2018-03-30 2023-04-28 Incyte Corporation Heterociklične spojine kot imunomodulatorji
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
MA52494A (fr) 2018-05-04 2021-03-10 Incyte Corp Formes solides d'un inhibiteur de fgfr et leurs procédés de préparation
EP3788046A1 (en) 2018-05-04 2021-03-10 Incyte Corporation Salts of an fgfr inhibitor
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
CA3100731A1 (en) 2018-05-18 2019-11-21 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2020014643A1 (en) 2018-07-13 2020-01-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN112955435A (zh) 2018-10-24 2021-06-11 吉利德科学公司 Pd-1/pd-l1抑制剂
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020168178A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Cyclin-dependent kinase 2 biomarkers and uses thereof
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
BR112021022659A2 (pt) 2019-05-15 2022-03-29 Chemocentryx Inc Compostos triarílicos para o tratamento de doenças pd-l1
MA55325A (fr) 2019-06-20 2022-04-27 Chemocentryx Inc Composés pour le traitement de maladies pd-l1
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220034829A (ko) 2019-07-10 2022-03-18 케모센트릭스, 인크. Pd-l1 억제제로서의 인단
JP2022544189A (ja) 2019-08-09 2022-10-17 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
US11427567B2 (en) 2019-08-14 2022-08-30 Incyte Corporation Imidazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2021067217A1 (en) 2019-09-30 2021-04-08 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
KR20220099970A (ko) 2019-10-11 2022-07-14 인사이트 코포레이션 Cdk2 억제제로서의 이환식 아민
EP4045151A1 (en) 2019-10-14 2022-08-24 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX2022004450A (es) 2019-10-16 2022-05-03 Chemocentryx Inc Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1.
AU2020368393A1 (en) 2019-10-16 2022-04-21 Chemocentryx, Inc. Heteroaryl-biphenyl amides for the treatment of PD-L1 diseases
BR112022009031A2 (pt) * 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CA3162010A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
KR20220125278A (ko) * 2020-01-03 2022-09-14 상하이 한서 바이오메디컬 컴퍼니 리미티드 비페닐 유도체 억제제, 이의 제조 방법 및 용도
JP2023509456A (ja) 2020-01-03 2023-03-08 インサイト・コーポレイション Ａ２ａ／ａ２ｂ及びｐｄ－１／ｐｄ－ｌ１阻害剤を含む併用療法
US20230014651A1 (en) 2020-01-07 2023-01-19 Abbisko Therapeutics Co., Ltd. Biphenyl fluorine double bond derivative, preparation method therefor, and pharmaceutical application thereof
WO2021178779A1 (en) 2020-03-06 2021-09-10 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
IL297165A (en) 2020-04-16 2022-12-01 Incyte Corp Soysag tricyclic CRS inhibitors
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
CN115605475A (zh) * 2020-06-17 2023-01-13 上海和誉生物医药科技有限公司（Cn） 一种免疫抑制剂、其制备方法和应用
US20220064188A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
AU2021369898A1 (en) 2020-10-29 2023-05-18 Shenzhen Chipscreen Biosciences Co., Ltd. Biphenyl compound as immunomodulator, preparation method therefor and application thereof
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
AR124001A1 (es) 2020-11-06 2023-02-01 Incyte Corp Proceso para fabricar un inhibidor pd-1 / pd-l1 y sales y formas cristalinas del mismo
TW202241441A (zh) 2020-12-29 2022-11-01 美商英塞特公司 包含ａ２ａ／ａ２ｂ抑制劑、ｐｄ－１／ｐｄ－ｌ１抑制劑及抗ｃｄ７３抗體之組合療法
CN116710460A (zh) * 2021-01-18 2023-09-05 上海齐鲁制药研究中心有限公司 联苯衍生物及其应用
EP4286383A1 (en) 2021-02-01 2023-12-06 Shenzhen Chipscreen Biosciences Co., Ltd. Biphenyl compound as immunomodulator, preparation method therefor and use thereof
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
US20230002384A1 (en) 2021-06-09 2023-01-05 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US20230056631A1 (en) 2021-07-07 2023-02-23 Incyte Corporation Tricyclic compounds as inhibitors of kras
CA3224841A1 (en) 2021-07-14 2023-01-19 Zhenwu Li Tricyclic compounds as inhibitors of kras
WO2023034290A1 (en) 2021-08-31 2023-03-09 Incyte Corporation Naphthyridine compounds as inhibitors of kras
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
US20230149409A1 (en) * 2021-09-24 2023-05-18 Incyte Corporation Treatment of human papillomavirus-associated cancers by pd-l1 inhibitors
US20230143938A1 (en) 2021-10-01 2023-05-11 Incyte Corporation Pyrazoloquinoline kras inhibitors
US11939328B2 (en) 2021-10-14 2024-03-26 Incyte Corporation Quinoline compounds as inhibitors of KRAS
TW202320792A (zh) 2021-11-22 2023-06-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｋｒａｓ抑制劑之組合療法
WO2023122134A1 (en) 2021-12-22 2023-06-29 Incyte Corporation Salts and solid forms of an fgfr inhibitor and processes of preparing thereof
WO2023207933A1 (zh) * 2022-04-26 2023-11-02 深圳微芯生物科技股份有限公司 一种作为免疫调节剂的联苯类化合物的晶型及其制备方法
TW202346308A (zh) * 2022-04-26 2023-12-01 大陸商深圳微芯生物科技股份有限公司 作為免疫調節劑的聯苯類化合物的鹽型、晶型及其製備方法
TW202402279A (zh) 2022-06-08 2024-01-16 美商英塞特公司 作為ｄｇｋ抑制劑之三環三唑并化合物
US20240101557A1 (en) 2022-07-11 2024-03-28 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants

Family Cites Families (333)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3272781A (en) 1963-08-07 1966-09-13 American Potash & Chem Corp Boroureas of phosphinoborine polymers
FR1425700A (fr) 1965-02-22 1966-01-24 Basf Ag Composés formant des complexes métalliques et procédé pour les préparer et les utiliser
US4208328A (en) 1978-04-27 1980-06-17 General Electric Company Alkyl 3,5-dihydroxy-4-(2-benzothiazolyl)benzoates
US4789711A (en) 1986-12-02 1988-12-06 Ciba-Geigy Corporation Multifunctional epoxide resins
JPH0611031Y2 (ja) 1988-02-27 1994-03-23 タマパック株式会社 ゴルフ用パッティンググリーン
DE3828535A1 (de) 1988-08-23 1990-03-08 Basf Ag Benzimidazol-2-carbonsaeureanilide, ihre verwendung als lichtschutzmittel fuer organisches material und mit diesen aniliden stabilisiertes organisches material
US5077164A (en) 1989-06-21 1991-12-31 Minolta Camera Kabushiki Kaisha Photosensitive member containing an azo dye
EP0644460B1 (en) 1993-09-20 1999-12-08 Fuji Photo Film Co., Ltd. Positive working photoresist composition
JP3461397B2 (ja) 1995-01-11 2003-10-27 富士写真フイルム株式会社 ポジ型フオトレジスト組成物
WO1998027108A2 (en) 1996-12-16 1998-06-25 Fujisawa Pharmaceutical Co., Ltd. New amide compounds and their use as nitric oxide synthase inhibitors
JPH10316853A (ja) 1997-05-15 1998-12-02 Sumitomo Bakelite Co Ltd 半導体多層配線用層間絶縁膜樹脂組成物及び該絶縁膜の製造方法
EP1019391A1 (en) 1997-10-02 2000-07-19 Merck & Co. Inc. Inhibitors of prenyl-protein transferase
WO1999044992A1 (fr) 1998-03-05 1999-09-10 Nissan Chemical Industries, Ltd. Composes d'anilide et herbicide
JP2000128984A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及び樹脂
JP2000128986A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及びポリベンゾオキサゾール
JP2000128987A (ja) 1998-10-28 2000-05-09 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール前駆体及びポリベンゾオキサゾール
US6297351B1 (en) 1998-12-17 2001-10-02 Sumitomo Bakelite Company Limited Polybenzoxazole resin and precursor thereof
UA70976C2 (uk) 1998-12-18 2004-11-15 Аксіз Фармасьютікелз, Інк. (гетеро)арилбіциклічні гетероарильні похідні, їх одержання та використання як інгібіторів протеаз
JP2000212281A (ja) 1999-01-27 2000-08-02 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾ―ル前駆体及びポリベンゾオキサゾ―ル樹脂
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
JP2001114893A (ja) 1999-10-15 2001-04-24 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂およびその前駆体
US6372907B1 (en) 1999-11-03 2002-04-16 Apptera Corporation Water-soluble rhodamine dye peptide conjugates
JP2001163975A (ja) 1999-12-03 2001-06-19 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂及びその前駆体
RU2223761C2 (ru) 1999-12-27 2004-02-20 Джапан Тобакко Инк. Соединения с конденсированным кольцом и их использование в качестве лекарственных средств
EP1257551B1 (de) 2000-02-01 2007-09-05 Abbott GmbH & Co. KG Heterozyklische verbindungen und deren anwendung als parp-inhibitoren
US6521618B2 (en) 2000-03-28 2003-02-18 Wyeth 3-cyanoquinolines, 3-cyano-1,6-naphthyridines, and 3-cyano-1,7-naphthyridines as protein kinase inhibitors
ES2286114T3 (es) 2000-03-31 2007-12-01 Ortho-Mcneil Pharmaceutical, Inc. Imidazopiridina fenil-substituidos.
JP2003531194A (ja) 2000-04-24 2003-10-21 メルク フロスト カナダ アンド カンパニー プロスタグランジンｅ阻害薬としてフェニルおよびビアリール誘導体を用いる治療方法および該方法に有用な化合物
PL202623B1 (pl) 2000-06-28 2009-07-31 Smithkline Beecham Plc Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna
AU2001294515A1 (en) 2000-08-11 2002-02-25 The Regents Of The University Of California Use of stat-6 inhibitors as therapeutic agents
AU2002224927A1 (en) 2000-12-13 2002-06-24 Basf Aktiengesellschaft Use of substituted imidazoazines, novel imidazoazines, methods for the production thereof, and agents containing these compounds
ES2245380T3 (es) 2000-12-15 2006-01-01 Glaxo Group Limited Pirazolopiridinas.
SE0100567D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
ES2244772T3 (es) 2001-03-14 2005-12-16 Eli Lilly And Company Moduladores de receptores de retinoides x.
WO2002078700A1 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Pyralopyridines, process for their preparation and use as therapteutic compounds
DE60212949T2 (de) 2001-04-10 2007-01-04 Smithkline Beecham Corp. Antivirale pyrazolopyridin verbindungen
JP2002316966A (ja) 2001-04-19 2002-10-31 Ueno Seiyaku Oyo Kenkyusho:Kk ビナフトール誘導体およびその製法
WO2002088124A2 (en) 2001-04-27 2002-11-07 Smithkline Beecham Corporation Pyrazolo'1,5-a!pyridine derivatives
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
US20040214834A1 (en) 2001-09-07 2004-10-28 Kristjan Gudmunsson Pyrazolo-pyridines for the treatment of herpes infections
TWI331526B (en) 2001-09-21 2010-10-11 Bristol Myers Squibb Pharma Co Lactam-containing compounds and derivatives thereof as factor xa inhibitors
BR0213208A (pt) 2001-10-09 2004-08-31 Upjohn Co Compostos de tetraidro- e hexaidro-carbazóis de arilsulfonila substituìda, suas composições e usos
US20030143199A1 (en) 2001-10-09 2003-07-31 Carson Dennis A. Use of STAT-6 inhibitors as therapeutic agents
JP4024579B2 (ja) 2002-01-22 2007-12-19 住友ベークライト株式会社 プラスチック光導波路用材料及び光導波路
EP2468744A2 (en) 2002-04-11 2012-06-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
CN100343255C (zh) 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US20060004010A1 (en) 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
JP2004059761A (ja) 2002-07-30 2004-02-26 Sumitomo Bakelite Co Ltd ポリベンゾオキサゾール樹脂、その前駆体及びこれらを用いた光導波路材料並びに光導波路
JP2004091369A (ja) 2002-08-30 2004-03-25 Sumitomo Pharmaceut Co Ltd 新規ビフェニル化合物
JPWO2004035522A1 (ja) 2002-08-30 2006-02-16 株式会社 ビーエフ研究所 プリオン蛋白蓄積性疾患の診断プローブおよび治療薬ならびにプリオン蛋白の染色剤
EP1546148A1 (en) 2002-10-03 2005-06-29 SmithKline Beecham Corporation Therapeutic compounds based on pyrazolopyridine derivatives
EP1551842A1 (en) 2002-10-15 2005-07-13 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
KR100624406B1 (ko) 2002-12-30 2006-09-18 삼성에스디아이 주식회사 비페닐 유도체 및 이를 채용한 유기 전계 발광 소자
US7320989B2 (en) 2003-02-28 2008-01-22 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
JP4595288B2 (ja) 2003-03-25 2010-12-08 住友ベークライト株式会社 ポリベンゾオキサゾール樹脂、その前駆体及びこれらを用いた光導波路材料並びに光導波路
EA010634B1 (ru) 2003-04-11 2008-10-30 Гленмарк Фармасьютикалс С.А. Новые гетероциклические соединения, применяемые для лечения нарушений аллергической или воспалительной природы: способы синтеза и содержащие их фармацевтические составы
MXPA05012461A (es) 2003-05-19 2006-02-22 Irm Llc Compuestos y composiciones inmunosupresores.
JP2005002330A (ja) 2003-05-19 2005-01-06 Sumitomo Electric Ind Ltd 光学樹脂材料、光学素子、光モジュール、フッ素化ポリマー前駆体及びフッ素化ポリマー
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US20060183746A1 (en) 2003-06-04 2006-08-17 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
US20050014786A1 (en) 2003-07-11 2005-01-20 Chongqing Sun Tetrahydroquinoline derivatives as cannabinoid receptor modulators
US7691870B2 (en) 2003-07-11 2010-04-06 Merck Patent Gmbh Benzimidazole carboxamides as raf kinase inhibitors
JPWO2005012221A1 (ja) 2003-08-04 2006-09-14 小野薬品工業株式会社 ジフェニルエーテル化合物、その製造方法および用途
WO2005014543A1 (ja) 2003-08-06 2005-02-17 Japan Tobacco Inc. 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
US20070099938A1 (en) 2003-10-24 2007-05-03 Ono Pharmaceutical Co., Ltd. Antistress drug and medical use thereof
WO2005047290A2 (en) 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
WO2005063710A1 (de) 2003-12-23 2005-07-14 Basf Aktiengesellschaft 3-trifluormethylpicolinsäureanilide und ihre verwendung als fungizide
JP2007524682A (ja) 2004-02-12 2007-08-30 メルク　エンド　カムパニー　インコーポレーテッド 代謝調節型グルタミン酸受容体−５の調節物質としてのビピリジルアミド
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
GB0403864D0 (en) 2004-02-20 2004-03-24 Ucl Ventures Modulator
JP2005248082A (ja) 2004-03-05 2005-09-15 Sumitomo Electric Ind Ltd ポリベンゾオキサゾール樹脂前駆体の製造方法およびポリベンゾオキサゾール樹脂の製造方法
WO2005086904A2 (en) 2004-03-08 2005-09-22 Amgen Inc. Therapeutic modulation of ppar (gamma) activity
EP1745045A4 (en) 2004-03-08 2009-07-22 Univ North Carolina NEW DIKATIONIC IMIDAZO [1,2-A] PYRIDINES AND 5,6,7,8-TETRAHYDROIMIDAZO [1,2-A] PYRIDINES AS AGENTS AGAINST PROTOZOES
EP1761496A2 (en) 2004-03-31 2007-03-14 Janssen Pharmaceutica N.V. Non-imidazole heterocyclic compounds as histamine h3-receptor ligands
JP2005290301A (ja) 2004-04-02 2005-10-20 Sumitomo Electric Ind Ltd ポリベンゾオキサゾール樹脂前駆体の製造方法およびポリベンゾオキサゾール樹脂の製造方法
US7331997B2 (en) 2004-04-06 2008-02-19 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
AU2005236055B2 (en) 2004-04-20 2011-10-06 Transtech Pharma, Llc Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
DE102004021716A1 (de) 2004-04-30 2005-12-01 Grünenthal GmbH Substituierte Imidazo[1,2-a]pyridin-Verbindungen und Arzneimittel enthaltend substituierte Imidazo[1,2-a]pyridin-Verbindungen
EP1745036A2 (en) 2004-05-03 2007-01-24 Boehringer Ingelheim Pharmaceuticals Inc. Cytokine inhibitors
TW200626142A (en) 2004-09-21 2006-08-01 Glaxo Group Ltd Chemical compounds
CN101035528A (zh) 2004-09-23 2007-09-12 惠氏公司 治疗丙型肝炎病毒感染的咔唑和环戊二烯并吲哚衍生物
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
EP1812442A2 (en) 2004-11-10 2007-08-01 CGI Pharmaceuticals, Inc. Imidazo[1,2-a]pyrazin-8-ylamines useful as modulators of kinase activity
DE102004054665A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte bi- und tricyclische Pyrazol-Derivate Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
CA2599987A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
KR101357524B1 (ko) 2005-03-10 2014-02-03 질레드 코네티컷 인코포레이티드 특정 치환된 아미드, 그의 제조 방법, 및 사용 방법
JP2006290883A (ja) 2005-03-17 2006-10-26 Nippon Nohyaku Co Ltd 置換ヘテロ環カルボン酸アニリド誘導体、その中間体及び農園芸用薬剤並びにその使用方法
WO2006125101A2 (en) 2005-05-20 2006-11-23 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
US20080220968A1 (en) 2005-07-05 2008-09-11 Ge Healthcare Bio-Sciences Ab [1, 2, 4] Triazolo [1, 5-A] Pyrimidine Derivatives as Chromatographic Adsorbent for the Selective Adsorption of Igg
WO2007034282A2 (en) 2005-09-19 2007-03-29 Pfizer Products Inc. Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US7723336B2 (en) 2005-09-22 2010-05-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
BRPI0617852A2 (pt) 2005-10-25 2011-08-09 Shionogi & Co compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos
EP1954290B1 (en) 2005-11-22 2012-07-25 Merck Sharp & Dohme Corp. Tricyclic compounds useful as inhibitors of kinases
WO2007067711A2 (en) 2005-12-08 2007-06-14 Amphora Discovery Corporation Certain chemical entities, compositions, and methods for modulating trpv1
WO2007069565A1 (ja) 2005-12-12 2007-06-21 Ono Pharmaceutical Co., Ltd. 二環式複素環化合物
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
CA2645018A1 (en) 2006-03-08 2007-09-13 Takeda Pharmaceutical Company Limited Pharmaceutical combination
WO2007113226A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
WO2008118122A2 (en) 2006-05-08 2008-10-02 Molecular Neuroimaging, Llc Compounds and amyloid probes thereof for therapeutic and imaging uses
EP2035005A4 (en) 2006-06-09 2011-07-06 Kemia Inc THERAPY BASED ON CYTOKINE INHIBITORS
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
US20080021026A1 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
DE102006035018B4 (de) 2006-07-28 2009-07-23 Novaled Ag Oxazol-Triplett-Emitter für OLED-Anwendungen
WO2008021745A2 (en) 2006-08-16 2008-02-21 Itherx Pharmaceuticals, Inc. Hepatitis c virus entry inhibitors
TWI389895B (zh) 2006-08-21 2013-03-21 Infinity Discovery Inc 抑制ｂｃｌ蛋白質與結合夥伴間之交互作用的化合物及方法
US7563797B2 (en) 2006-08-28 2009-07-21 Forest Laboratories Holding Limited Substituted imidazo(1,2-A)pyrimidines and imidazo(1,2-A) pyridines as cannabinoid receptor ligands
US20100160292A1 (en) 2006-09-11 2010-06-24 Cgi Pharmaceuticals, Inc Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
PE20080839A1 (es) 2006-09-11 2008-08-23 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
BRPI0716804A2 (pt) 2006-09-11 2013-11-05 Matrix Lab Ltd Derivados de dibenzofuranco como inibidores de pde-4 e pde-10
AR063707A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmacéuticas que las comprenden.
FR2906250B1 (fr) 2006-09-22 2008-10-31 Sanofi Aventis Sa Derives de 2-aryl-6phenyl-imidazo(1,2-a) pyridines, leur preparation et leur application en therapeutique
JP2010507674A (ja) 2006-10-27 2010-03-11 ワイス エルエルシー マトリクスメタロプロテアーゼ阻害剤としての三環式化合物
CL2007003226A1 (es) 2006-11-08 2008-02-08 Bristol Myers Squibb Co Compuestos derivados de piridinona; composicion farmaceutica; y uso para tratar el cancer.
GB0623209D0 (en) 2006-11-21 2007-01-03 F2G Ltd Antifungal agents
WO2008064317A1 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Lipophilic opioid receptor active compounds
WO2008064318A2 (en) 2006-11-22 2008-05-29 University Of Medicine And Dentistry Of New Jersey Peripheral opioid receptor active compounds
WO2008071944A1 (en) 2006-12-14 2008-06-19 Boehringer Ingelheim International Gmbh Benzoxazoles useful in the treatment of inflammation
JP5492565B2 (ja) 2006-12-22 2014-05-14 インサイト・コーポレイション Ｊａｎｕｓキナーゼ阻害剤としての置換複素環
WO2008104077A1 (en) 2007-02-28 2008-09-04 Methylgene Inc. Small molecule inhibitors of protein arginine methyltransferases (prmts)
EP1964840A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]pyridines and their use as pharmaceuticals
EP1964841A1 (en) 2007-02-28 2008-09-03 sanofi-aventis Imidazo[1,2-a]azine and their use as pharmaceuticals
JP2008218327A (ja) 2007-03-07 2008-09-18 Hitachi Ltd 電解質、電解質膜、それを用いた膜電極接合体、燃料電池電源及び燃料電池電源システム
JP2010120852A (ja) 2007-03-09 2010-06-03 Daiichi Sankyo Co Ltd 新規なジアミド誘導体
MX2009010059A (es) 2007-03-22 2009-10-12 Astrazeneca Ab Derivados de quinolina para el tratamiento de enfermedades inflamatorias.
ES2476605T3 (es) 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
WO2008134553A1 (en) 2007-04-26 2008-11-06 Xenon Pharmaceuticals Inc. Methods of using bicyclic compounds in treating sodium channel-mediated diseases
US20110206607A1 (en) 2007-05-10 2011-08-25 Roger Olsson Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors
WO2009027733A1 (en) 2007-08-24 2009-03-05 Astrazeneca Ab (2-pyridin-3-ylimidazo[1,2-b]pyridazin-6-yl) urea derivatives as antibacterial agents
CL2008002793A1 (es) * 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
DE602008006209D1 (de) 2007-09-20 2011-05-26 Amgen Inc 1-(4-(4-benzylbenzamid)-benzyl)-azetidin-3-carboxylsäurederivate und entsprechende verbindungen als s1p-rezeptor-modulatoren zur behandlung von immunerkrankungen
DE102007048716A1 (de) 2007-10-11 2009-04-23 Merck Patent Gmbh Imidazo[1,2-a]pyrimidinderivate
TW200932219A (en) 2007-10-24 2009-08-01 Astellas Pharma Inc Oxadiazolidinedione compound
AU2008315746A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
US7868001B2 (en) 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
WO2009062059A2 (en) 2007-11-08 2009-05-14 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
CA2707491A1 (en) 2007-12-13 2009-06-18 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
RU2364597C1 (ru) 2007-12-14 2009-08-20 Андрей Александрович Иващенко ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ Hh-СИГНАЛЬНОГО КАСКАДА, ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АББЕРАНТНОЙ АКТИВНОСТЬЮ Hh СИГНАЛЬНОЙ СИСТЕМЫ
NZ585883A (en) 2007-12-19 2011-11-25 Syngenta Participations Ag Oxazoline derivatives as insecticidal compounds
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
CA2710016A1 (en) 2007-12-21 2009-07-02 The University Of Sydney Translocator protein ligands
ES2548774T3 (es) 2008-01-18 2015-10-20 Eisai R&D Management Co., Ltd. Derivado de aminodihidrotiazina condensado
WO2009096202A1 (ja) 2008-01-31 2009-08-06 Konica Minolta Holdings, Inc. ハロ多環芳香族化合物及びその製造方法
CN101959889A (zh) 2008-02-26 2011-01-26 诺瓦提斯公司 作为cxcr2抑制剂的杂环化合物
EP2095818A1 (en) 2008-02-29 2009-09-02 AEterna Zentaris GmbH Use of LHRH antagonists at non-castrating doses
FR2928924B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 6-heteroaryle-imidazo°1,2-a! pyridines, leur preparation et leur application en therapeutique
FR2928922B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives de 2-aryl-6-phenyl-imidazo°1,2-a!pyridines polysubstitues, leur preparation et leur application en therapeutique
FR2928921B1 (fr) 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 2-aryl-6-phenyl-imidazo°1,2-a!pyridines, leur preparation et leur application en therapeutique
EP2271646A1 (en) 2008-03-31 2011-01-12 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
KR101034351B1 (ko) 2008-05-14 2011-05-16 한국화학연구원 신규 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의약학적으로 허용가능한 염, 이의 제조방법 및 이를유효성분으로 함유하는 이상세포 성장 질환의 예방 및치료용 약학적 조성물
JP5774982B2 (ja) 2008-05-19 2015-09-09 サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． イミダゾ［１，２−ａ］ピリジン化合物
JP2011521960A (ja) 2008-05-29 2011-07-28 サートリス ファーマシューティカルズ， インコーポレイテッド サーチュイン調節薬としてのイミダゾピリジンおよび関連する類似体
JP2011529073A (ja) 2008-07-24 2011-12-01 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ調節因子として有用な縮合ヘテロ環化合物
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
JP2011231017A (ja) 2008-09-09 2011-11-17 Nissan Chem Ind Ltd 光学活性エポキシ化合物及び光学活性スルホキシド化合物の製造方法、並びに該方法に用いる配位子、錯体及び該錯体の製造方法
US8598174B2 (en) 2008-11-12 2013-12-03 Genetech, Inc. Pyridazinones, method of making, and method of use thereof
US20120010188A1 (en) 2008-12-04 2012-01-12 Promimagen Ltd. Imidazopyridine Compounds
EP2376491B1 (en) 2008-12-19 2015-03-04 Cephalon, Inc. Pyrrolotriazines as alk and jak2 inhibitors
KR20110098827A (ko) 2008-12-19 2011-09-01 브리스톨-마이어스 스큅 컴퍼니 키나제 억제제로서 유용한 카르바졸 카르복스아미드 화합물
EP2370407B1 (en) 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
JP5624275B2 (ja) 2008-12-22 2014-11-12 ユー・ディー・シー アイルランド リミテッド 有機電界発光素子
ES2567047T3 (es) 2008-12-23 2016-04-19 Abbvie Inc. Derivados de pirimidina anti-virales
JP5578490B2 (ja) 2008-12-26 2014-08-27 味の素株式会社 ピラゾロピリミジン化合物
JP2010202530A (ja) 2009-02-27 2010-09-16 Tokyo Institute Of Technology 含ヘテロ芳香族化合物および光学材料
WO2010104307A2 (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
AU2010233917B2 (en) 2009-04-02 2015-07-02 Merck Serono S.A. Dihydroorotate dehydrogenase inhibitors
MX2011010915A (es) 2009-04-16 2012-01-27 Ct Nac Investigaciones Oncologicas Cnio Imidazopirazinas para usarse como inhibidores decinasa.
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
CA2763194A1 (en) 2009-06-30 2011-01-06 Siga Technologies, Inc. Treatment and prevention of dengue virus infections
US8993604B2 (en) 2009-06-30 2015-03-31 Siga Technologies, Inc. Treatment and prevention of dengue virus infections
TWI625121B (zh) 2009-07-13 2018-06-01 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
JP2011057661A (ja) 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US9095596B2 (en) 2009-10-15 2015-08-04 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
CN102712647B (zh) 2009-10-16 2018-04-24 梅琳塔治疗公司 抗微生物化合物和其制备和使用方法
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
JPWO2011078221A1 (ja) 2009-12-24 2013-05-09 味の素株式会社 イミダゾピリダジン化合物
US20130022629A1 (en) 2010-01-04 2013-01-24 Sharpe Arlene H Modulators of Immunoinhibitory Receptor PD-1, and Methods of Use Thereof
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
TW201136919A (en) 2010-03-02 2011-11-01 Merck Sharp & Amp Dohme Corp Inhibitors of hepatitis C virus NS5B polymerase
EP2542076B1 (en) 2010-03-04 2021-01-13 Merck Sharp & Dohme Corp. Inhibitors of catechol o-methyl transferase and their use in the treatment of psychotic disorders
BR112012023576B1 (pt) 2010-03-18 2022-08-23 Institut Pasteur Korea Compostos anti-infecciosos e composições compreendendo os mesmos
US8410117B2 (en) 2010-03-26 2013-04-02 Hoffmann-La Roche Inc. Imidazopyrimidine derivatives
WO2011159857A1 (en) 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
CN102295642B (zh) 2010-06-25 2016-04-06 中国人民解放军军事医学科学院毒物药物研究所 2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物、其制备方法及用途
EP2402345A1 (en) 2010-06-29 2012-01-04 Basf Se Pyrazole fused bicyclic compounds
CN101891895B (zh) 2010-07-28 2011-11-30 南京航空航天大学 基于桥联双水杨醛结构的苯并噻唑类金属配位聚合物及其制法及应用
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
US8633200B2 (en) 2010-09-08 2014-01-21 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
CN101993415B (zh) 2010-09-15 2013-08-14 北京韩美药品有限公司 作为Hedgehog通路抑制剂的化合物以及包含该化合物的药物组合物及其应用
CN103889428A (zh) 2010-10-04 2014-06-25 肝炎与病毒研究所 乙型肝炎病毒抗原分泌的新型抑制剂
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
CN103282034A (zh) 2010-11-18 2013-09-04 利亘制药公司 造血生长因子模拟物的用途
CN103261188A (zh) 2010-12-17 2013-08-21 先正达参股股份有限公司 杀虫化合物
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
CN103402996B (zh) 2011-01-04 2015-02-11 诺瓦提斯公司 可用于治疗年龄相关性黄斑变性(amd)的吲哚化合物或其类似物
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
US8921368B2 (en) 2011-03-17 2014-12-30 Bristol-Myers Squibb Company Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
CA2832473A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions, and their use
CN102796103A (zh) 2011-05-23 2012-11-28 南京英派药业有限公司 6-（芳基甲酰）咪唑并[1,2-a]嘧啶和6-（芳基甲酰）[1,2,4]三唑并[4,3-a]嘧啶作为Hedgehog抑制剂及其应用
WO2012166951A1 (en) 2011-05-31 2012-12-06 Receptos, Inc. Novel glp-1 receptor stabilizers and modulators
GB201109763D0 (en) 2011-06-10 2011-07-27 Ucl Business Plc Compounds
WO2012175991A1 (en) 2011-06-24 2012-12-27 Pharminox Limited Fused pentacyclic anti - proliferative compounds
JP6145451B2 (ja) 2011-07-08 2017-06-14 ノバルティス アーゲー 新規なピロロピリミジン誘導体
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
WO2013033901A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
WO2013040528A1 (en) 2011-09-16 2013-03-21 Microbiotix, Inc. Antimicrobial compounds
US9351973B2 (en) 2011-09-22 2016-05-31 Merck Sharp & Dohme Corp. Pyrazolopyridyl compounds as aldosterone synthase inhibitors
JP6040677B2 (ja) 2011-09-29 2016-12-07 東洋インキＳｃホールディングス株式会社 太陽電池封止材用樹脂組成物
MX2014004479A (es) 2011-10-13 2014-08-01 Novartis Ag Derivados de oxazina novedosos y su uso en el tratamiento de enfermedades.
WO2013059594A1 (en) 2011-10-20 2013-04-25 Sirtris Pharmaceuticals, Inc. Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
EP2768832A1 (en) 2011-10-21 2014-08-27 Torrent Pharmaceuticals Limited Novel substituted imidazopyrimidines as gpbar1 receptor modulators
WO2013120040A1 (en) 2012-02-10 2013-08-15 Children's Medical Center Corporation Targeted pathway inhibition to improve muscle structure, function and activity in muscular dystrophy
US9034882B2 (en) 2012-03-05 2015-05-19 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
IN2014MN01897A (hr) 2012-03-09 2015-07-10 Carna Biosciences Inc
EP3070081B1 (en) 2012-04-20 2018-02-28 Gilead Sciences, Inc. Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
WO2013163404A1 (en) 2012-04-27 2013-10-31 The Uab Research Foundation TREATING VIRAL INFECTIONS HAVING VIRAL RNAs TRANSLATED BY A NON-IRES MEDIATED MECHANISM
CN104379567A (zh) 2012-06-18 2015-02-25 住友化学株式会社 稠合杂环化合物
US9630976B2 (en) 2012-07-03 2017-04-25 Ono Pharmaceutical Co., Ltd. Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes
ES2689429T3 (es) 2012-07-13 2018-11-14 Ucb Biopharma Sprl Derivados de imidazopiridina como moduladores de actividad de TNF
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
JP2015178457A (ja) 2012-07-25 2015-10-08 杏林製薬株式会社 ピラゾロピリジン誘導体、またはその薬理学的に許容される塩
EP2892899B1 (en) 2012-09-06 2018-03-21 Bristol-Myers Squibb Company Imidazopyridazine jak3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
US9328106B2 (en) 2012-09-26 2016-05-03 Genentech, Inc. Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
WO2014061693A1 (ja) 2012-10-17 2014-04-24 塩野義製薬株式会社 新規非芳香族炭素環又は非芳香族複素環誘導体
WO2014081878A2 (en) 2012-11-21 2014-05-30 Stategics, Inc. Substituted triazolo-pyrimidine compounds for modulating cell proliferation, differentiation and survival
JP6037804B2 (ja) 2012-12-03 2016-12-07 富士フイルム株式会社 ガス分離膜
EP2945939B1 (en) 2013-01-15 2020-03-04 Incyte Holdings Corporation Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
RU2015132181A (ru) 2013-01-22 2017-03-02 Ф. Хоффманн-Ля Рош Аг Фтор-[1,3]-оксазины в качестве ингибиторов васе1
CN103933036B (zh) 2013-01-23 2017-10-13 中国人民解放军军事医学科学院毒物药物研究所 2‑芳基咪唑并[1,2‑α]吡啶‑3‑乙酰胺衍生物在制备防治PTSD的药物中的用途
WO2014121085A1 (en) 2013-01-31 2014-08-07 Thomas Jefferson University Pd-l1 and pd-l2-based fusion proteins and uses thereof
CN106957317B (zh) 2013-02-27 2019-12-31 持田制药株式会社 新型吡唑衍生物
SG11201507196WA (en) 2013-03-08 2015-10-29 Amgen Inc Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN104045552B (zh) 2013-03-13 2019-06-11 江苏先声药业有限公司 作为神经保护剂的药用化合物
US20160050895A1 (en) 2013-03-13 2016-02-25 Australian Nuclear Science And Technology Organization Transgenic non-human organisms with non-functional tspo genes
ES2705247T3 (es) 2013-03-14 2019-03-22 Univ Columbia 4-fenilpiperidinas, su preparación y uso
EP2968265A4 (en) 2013-03-14 2016-12-28 Celtaxsys Inc INHIBITORS OF THE LEUKOTRIEN A4 HYDROLASE
JP2016512558A (ja) 2013-03-14 2016-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヒト免疫不全ウイルス複製の阻害剤
KR102189529B1 (ko) 2013-03-14 2020-12-11 큐라데브 파마 프라이버트 리미티드 키누레닌 경로의 억제제
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
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
SG10201802444XA (en) 2013-06-26 2018-05-30 Abbvie Inc Primary carboxamides as btk inhibitors
JP6677637B2 (ja) 2013-07-02 2020-04-08 シンジェンタ パーティシペーションズ アーゲー 有害生物防除的に活性な、硫黄含有置換基を有する二環式または三環式複素環
EP4219477A1 (en) 2013-07-17 2023-08-02 Otsuka Pharmaceutical Co., Ltd. Cyanotriazole compounds
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
EP2835375A1 (en) 2013-08-09 2015-02-11 Fundació Institut Català d'Investigació Química Bis-salphen compounds and carbonaceous material composites comprising them
KR101715090B1 (ko) 2013-08-28 2017-03-13 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
AU2014315457B2 (en) 2013-09-04 2018-05-10 Bristol-Myers Squibb Company Compounds useful as immunomodulators
TR201809838T4 (tr) 2013-09-06 2018-07-23 Aurigene Discovery Tech Ltd İmmünomodülatörler olarak 1,2,4-oksadiazol türevleri.
HUE039014T2 (hu) 2013-09-06 2018-12-28 Aurigene Discovery Tech Ltd 1,3,4-Oxadiazol és 1,3,4-tiadiazol származékok, mint immunomodulátorok
WO2015036927A1 (en) 2013-09-10 2015-03-19 Aurigene Discovery Technologies Limited Immunomodulating peptidomimetic derivatives
JP6336870B2 (ja) 2013-09-30 2018-06-06 日本ポリプロ株式会社 ビフェノール化合物及びそれを用いるオレフィン重合用触媒並びにオレフィン重合体の製造方法
FR3012140B1 (fr) 2013-10-18 2016-08-26 Arkema France Unite et procede pour la purification de methacrylate de methyle brut
GB201321733D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321736D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321746D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
WO2015095337A2 (en) 2013-12-18 2015-06-25 The Rockefeller University PYRAZOLO[1,5-a]PYRIMIDINECARBOXAMIDE DERIVATIVES FOR TREATING COGNITIVE IMPAIRMENT
CA2935646A1 (en) 2014-01-03 2015-07-09 Bayer Animal Health Gmbh Novel pyrazolyl-heteroarylamides as pesticides
US20160356794A1 (en) 2014-02-10 2016-12-08 Merck Sharp & Dohme Corp. Antibodies that bind to human tau and assay for quantifying human tau using the antibodies
US9796741B2 (en) 2014-02-25 2017-10-24 Achillion Pharmaceuticals, Inc. Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated disorders
JP6490464B2 (ja) 2014-03-26 2019-03-27 三井化学株式会社 遷移金属化合物、オレフィン重合用触媒およびオレフィン系重合体の製造方法
UA121386C2 (uk) 2014-04-04 2020-05-25 Айомет Фарма Лтд Похідні індолу, фармацевтична композиція, яка їх містить, та способи їх застосування
US9850225B2 (en) 2014-04-14 2017-12-26 Bristol-Myers Squibb Company Compounds useful as immunomodulators
CN106065009B (zh) 2014-06-28 2019-03-01 广东东阳光药业有限公司 作为丙型肝炎抑制剂的化合物及其在药物中的应用
CN104211726B (zh) 2014-08-11 2017-06-16 中南民族大学 非茂类三齿双核钛配合物、制备方法及用途
WO2016044604A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
EP3194368B1 (en) 2014-09-19 2020-12-23 MacKay Medical Foundation the Presbyterian Church in Taiwan MacKay Memorial Hospital Benzo-heterocyclic compounds and their applications
US10253023B2 (en) 2014-10-06 2019-04-09 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
US10017520B2 (en) 2014-12-10 2018-07-10 Massachusetts Institute Of Technology Myc modulators and uses thereof
JP6853619B2 (ja) 2015-01-16 2021-03-31 大塚製薬株式会社 シアノトリアゾール化合物の医薬用途
WO2016116525A1 (de) 2015-01-20 2016-07-28 Cynora Gmbh Organische moleküle, insbesondere zur verwendung in optoelektronischen bauelementen
WO2016118404A1 (en) 2015-01-20 2016-07-28 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use
WO2016156282A1 (en) 2015-04-02 2016-10-06 Bayer Cropscience Aktiengesellschaft Novel triazole compounds for controlling phytopathogenic harmful fungi
WO2017035405A1 (en) 2015-08-26 2017-03-02 Achillion Pharmaceuticals, Inc. Amino compounds for treatment of immune and inflammatory disorders
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
US10633370B2 (en) 2015-10-21 2020-04-28 University of Pittsburgh—of the Commonwealth System of Higher Education Phenyl indole allosteric inhibitors of p97 ATPase
KR101717601B1 (ko) 2015-11-10 2017-03-20 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
JP7148401B2 (ja) 2015-11-19 2022-10-05 インサイト・コーポレイション 免疫調節剤としての複素環化合物
TW201726623A (zh) 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
EP3393457A1 (en) 2015-12-22 2018-10-31 Synthon B.V. Pharmaceutical composition comprising amorphous lenalidomide and an antioxidant
SG10202111399YA (en) 2015-12-22 2021-11-29 Immatics Biotechnologies Gmbh Peptides and combination of peptides for use in immunotherapy against breast cancer and other cancers
US10750742B2 (en) 2015-12-22 2020-08-25 Syngenta Participations Ag Pesticidally active pyrazole derivatives
SI3394033T1 (sl) 2015-12-22 2021-03-31 Incyte Corporation Heterociklične spojine kot imunomodulatorji
KR101653560B1 (ko) 2016-02-02 2016-09-12 한국화학연구원 신규한 화합물 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 인플루엔자 바이러스 감염으로 인한 질환의 예방 또는 치료용 약학적 조성물
US20170320875A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3028683A1 (en) 2016-06-20 2017-12-28 Ambrx, Inc. Pegylated porcine interferon and methods of use thereof
MX2018016273A (es) 2016-06-20 2019-07-04 Incyte Corp Compuestos heterociclicos como inmunomoduladores.
US11091489B2 (en) 2016-06-20 2021-08-17 Novartis Ag Crystalline forms of a triazolopyrimidine compound
CN116554168A (zh) 2016-06-21 2023-08-08 X4 制药有限公司 Cxcr4抑制剂及其用途
WO2018013789A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
JP2019530732A (ja) 2016-08-03 2019-10-24 アライジング・インターナショナル・インコーポレイテッドＡｒｉｓｉｎｇ Ｉｎｔｅｒｎａｔｉｏｎａｌ， Ｉｎｃ． 免疫モジュレータとして有用な対称または半対称化合物
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
KR102558540B1 (ko) 2016-08-30 2023-07-21 테트라페이즈 파마슈티컬스, 인코포레이티드 테트라사이클린 화합물 및 치료 방법
TWI795381B (zh) 2016-12-21 2023-03-11 比利時商健生藥品公司 作為ｍａｌｔ１抑制劑之吡唑衍生物
ES2856248T3 (es) 2016-12-21 2021-09-27 Acerta Pharma Bv Inhibidores de imidazopirazina de la tirosina quinasa de Bruton
HUE060233T2 (hu) * 2016-12-22 2023-02-28 Incyte Corp Tetrahidro imidazo[4,5-c]piridin-származékok mint a PD-L1 internalizációját indukáló szerek
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers
ES2881395T3 (es) 2016-12-22 2021-11-29 Calithera Biosciences Inc Composiciones y métodos para inhibir la actividad de la arginasa
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
BR112019012993A2 (pt) 2016-12-22 2019-12-03 Incyte Corp derivados de benzo-oxazol como imunomoduladores
CA3047991A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
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
MA49859A (fr) 2017-08-08 2021-04-07 Chemocentryx Inc Immunomodulateurs macrocycliques
WO2019034172A1 (zh) 2017-08-18 2019-02-21 上海轶诺药业有限公司 一种具有pd-l1抑制活性的化合物、其制备方法及用途
SI3774791T1 (sl) 2018-03-30 2023-04-28 Incyte Corporation Heterociklične spojine kot imunomodulatorji
WO2019192506A1 (en) 2018-04-03 2019-10-10 Betta Pharmaceuticals Co., Ltd Immunomodulators, compositions and methods thereof
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
CN112955435A (zh) 2018-10-24 2021-06-11 吉利德科学公司 Pd-1/pd-l1抑制剂
KR20210089195A (ko) 2018-11-02 2021-07-15 상하이 맥시노벨 파마수티컬스 씨오., 엘티디. 비페닐계 화합물, 이의 중간체, 제조 방법, 약학 조성물 및 용도
CA3128426A1 (en) 2019-01-31 2020-08-06 Betta Pharmaceuticals Co., Ltd. Immunomodulators, compositions and methods thereof
JP2022544189A (ja) 2019-08-09 2022-10-17 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
WO2021067217A1 (en) 2019-09-30 2021-04-08 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1

Also Published As

Publication number Publication date
JP2021524842A (ja) 2021-09-16
PH12020551927A1 (en) 2021-06-14
AU2019267824A1 (en) 2021-01-07
WO2019217821A1 (en) 2019-11-14
AU2019267824B2 (en) 2023-10-05
ES2943028T3 (es) 2023-06-08
EP3790877A1 (en) 2021-03-17
CA3099994A1 (en) 2019-11-04
US10618916B2 (en) 2020-04-14
CR20200614A (es) 2021-04-27
CN112752756A (zh) 2021-05-04
JP7328995B2 (ja) 2023-08-17
EP4219492A1 (en) 2023-08-02
ECSP20079887A (es) 2021-03-31
US20190345170A1 (en) 2019-11-14
TW201946626A (zh) 2019-12-16
US20210115068A1 (en) 2021-04-22
TWI821288B (zh) 2023-11-11
PL3790877T3 (pl) 2023-06-12
JP2023162216A (ja) 2023-11-08
CL2021002995A1 (es) 2022-06-24
MX2020012045A (es) 2021-03-29
EP3790877B1 (en) 2023-03-01
KR20210018282A (ko) 2021-02-17
SI3790877T1 (sl) 2023-06-30
MD3790877T2 (ro) 2023-08-31
RS64188B1 (sr) 2023-06-30
SG11202011165TA (en) 2020-12-30
HUE061503T2 (hu) 2023-07-28
US20220348594A1 (en) 2022-11-03
PT3790877T (pt) 2023-05-10
CL2020002922A1 (es) 2021-04-16
PE20211918A1 (es) 2021-09-28
CO2020015437A2 (es) 2021-01-18
BR112020022936A2 (pt) 2021-02-02
LT3790877T (lt) 2023-05-10
DK3790877T3 (da) 2023-04-24
FI3790877T3 (fi) 2023-05-09
AU2023227554A1 (en) 2023-09-28
US10906920B2 (en) 2021-02-02
US11414433B2 (en) 2022-08-16
US20200277309A1 (en) 2020-09-03
JOP20200288A1 (ar) 2020-11-11

Similar Documents

Publication Publication Date Title
HRP20230306T1 (hr) Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori
HRP20221216T1 (hr) Derivati tetrahidro imidazo[4,5-c]piridina kao induktori internalizacije pd-l1
US10221139B2 (en) Inhibitors of histone demethylases
CN107304191B (zh) 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
CA2472372C (en) Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
HRP20170802T1 (hr) Supstituirani triciklički benzimidazoli kao inhibitori kinaze
JPWO2021067217A5 (hr)
WO2019193541A1 (en) Bicyclic aromatic ring derivatives of formula (i) as atf4 inhibitors
ES2432070T3 (es) Diazaheteroarilos broncodilatadores novedosos
ES2614034T3 (es) Derivados de amidina tricíclica como inhibidores de la unión del VIH
RU2011101898A (ru) Триазолпиридиновые соединения, ингибирующие jak, и способы
CA2807498A1 (en) 2-substituted-8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitriles and uses thereof
MXPA04001887A (es) Derivados de indeno[1,2,-c]isoquinolina sustituida y metodos de uso de los mismos.
ES2616432T3 (es) Derivados de alquenos tricíclicos como inhibidores de la unión del VIH
RU2656209C2 (ru) Терапевтически активные производные оксазолина
EP3414251A1 (en) Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors
WO2016095089A1 (en) Erk inhibitors
RU2019112863A (ru) Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
CA3019026A1 (en) Fused pentacyclic imidazole derivatives as modulators of tnf activity
WO2017181849A1 (zh) 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
RU2013109416A (ru) Композиция, включающая ретинол, его предшественник или продукт его реакции и экстракт из по меньшей мере одного растения chamomilla, для лечения рака
US11358967B2 (en) Substituted pyrazino[2,3-b]pyrazines and pyrazino[2,3-c]pyridazines as modulators of ROR gamma
ES2914526T3 (es) Composiciones de biarilo y métodos para modular una cascada de cinasa
ES2529865A1 (es) USO DE COMPUESTOS DERIVADOS DE SALES DE PIRIDAZINO[1',6':1,2]PIRIDO[3,4-b]INDOLINIO COMO AGENTES ANTIINFLAMATORIOS
AU2018200876B2 (en) Inhibitors of histone demethylases