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 PDFInfo
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- 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
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- imidazo
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- BTMWJZPJQDYRFI-UHFFFAOYSA-N 2,3,3a,4-tetrahydro-1h-imidazo[4,5-c]pyridine Chemical class C1N=CC=C2NCNC21 BTMWJZPJQDYRFI-UHFFFAOYSA-N 0.000 title 1
- 239000002955 immunomodulating agent Substances 0.000 title 1
- 229940121354 immunomodulator Drugs 0.000 title 1
- -1 4-hydroxycyclohexyl Chemical group 0.000 claims 115
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 60
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 54
- 206010028980 Neoplasm Diseases 0.000 claims 51
- LKXGYGYFPTZHLC-UHFFFAOYSA-N bicyclo[2.2.1]heptane-4-carboxylic acid Chemical compound C1CC2CCC1(C(=O)O)C2 LKXGYGYFPTZHLC-UHFFFAOYSA-N 0.000 claims 50
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 46
- 125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims 44
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 39
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- 150000001875 compounds Chemical class 0.000 claims 26
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- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 25
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- 125000001424 substituent group Chemical group 0.000 claims 16
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Classifications
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- 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
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- 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
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- 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
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
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- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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- Plural Heterocyclic Compounds (AREA)
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.
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Families Citing this family (99)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
JP6449244B2 (ja) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Fgfr抑制剤としての二環式複素環 |
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 |
EP3365340B1 (en) | 2015-10-19 | 2022-08-10 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
HRP20221035T1 (hr) | 2015-11-19 | 2022-11-11 | Incyte Corporation | Heterociklički spojevi kao imunomodulatori |
PE20230731A1 (es) | 2015-12-22 | 2023-05-03 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores |
AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
EP3464279B1 (en) | 2016-05-26 | 2021-11-24 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
TWI771305B (zh) | 2016-06-20 | 2022-07-21 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
EP3474845B1 (en) | 2016-06-27 | 2024-03-20 | ChemoCentryx, Inc. | Immunomodulator compounds |
WO2018013789A1 (en) | 2016-07-14 | 2018-01-18 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
US20180057486A1 (en) | 2016-08-29 | 2018-03-01 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
WO2018119221A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Pyridine derivatives as immunomodulators |
ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
PE20200005A1 (es) | 2016-12-22 | 2020-01-06 | Incyte Corp | Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1 |
WO2018119266A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
WO2018200571A1 (en) | 2017-04-25 | 2018-11-01 | 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 |
IL272258B (en) | 2017-07-28 | 2022-08-01 | Chemocentryx Inc | Immunomodulator compounds |
US10392405B2 (en) | 2017-08-08 | 2019-08-27 | Chemocentryx, Inc. | Macrocyclic immunomodulators |
AU2019222644B2 (en) | 2018-02-13 | 2021-04-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
US10568874B2 (en) | 2018-02-22 | 2020-02-25 | Chemocentryx, Inc. | Indane-amines as PD-L1 antagonists |
IL303087B1 (en) | 2018-02-27 | 2024-08-01 | Incyte Corp | Midazopyrimidines and triazolopyrimidines as A2A /A2B inhibitors |
US12083118B2 (en) | 2018-03-29 | 2024-09-10 | Arbutus Biopharma Corporation | Substituted 1,1′-biphenyl compounds, analogues thereof, and methods using same |
FI3774791T3 (fi) | 2018-03-30 | 2023-03-21 | Incyte Corp | Heterosyklisiä yhdisteitä immunomodulaattoreina |
CN112041311B (zh) | 2018-04-19 | 2023-10-03 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
DK3788047T3 (da) | 2018-05-04 | 2024-09-16 | Incyte Corp | Faste former af en FGFR-inhibitor og fremgangsmåder til fremstilling deraf |
SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
BR112020022936A2 (pt) | 2018-05-11 | 2021-02-02 | Incyte Corporation | derivados de tetra-hidro-imidazo[4,5-c]piridina como imunomoduladores de pd-l1 |
US11168089B2 (en) | 2018-05-18 | 2021-11-09 | Incyte Corporation | Fused pyrimidine derivatives as A2A / A2B inhibitors |
CN113166153A (zh) | 2018-07-05 | 2021-07-23 | 因赛特公司 | 作为a2a/a2b抑制剂的稠合吡嗪衍生物 |
EP4234030A3 (en) | 2018-07-13 | 2023-10-18 | 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 |
WO2020086556A1 (en) | 2018-10-24 | 2020-04-30 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
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 |
EP3923949A1 (en) | 2019-02-15 | 2021-12-22 | 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 |
WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
US11447494B2 (en) | 2019-05-01 | 2022-09-20 | 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 |
AU2020276277A1 (en) | 2019-05-15 | 2021-12-09 | Chemocentryx, Inc. | Triaryl compounds for treatment of PD-L1 diseases |
KR20220024701A (ko) | 2019-06-20 | 2022-03-03 | 케모센트릭스, 인크. | Pd-l1 질환의 치료를 위한 화합물 |
WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
BR112021025888A2 (pt) | 2019-07-10 | 2022-04-26 | Chemocentryx Inc | Indanos como inibidores de pd-l1 |
WO2021030162A1 (en) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
WO2021030537A1 (en) | 2019-08-14 | 2021-02-18 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
JP7559059B2 (ja) | 2019-09-30 | 2024-10-01 | インサイト・コーポレイション | 免疫調節剤としてのピリド[3,2-d]ピリミジン化合物 |
PE20221905A1 (es) | 2019-10-11 | 2022-12-23 | Incyte Corp | Aminas biciclicas como inhibidoras de la cdk2 |
MX2022004513A (es) | 2019-10-14 | 2022-07-19 | Incyte Corp | Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr). |
MX2022004450A (es) | 2019-10-16 | 2022-05-03 | Chemocentryx Inc | Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1. |
WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
US11713307B2 (en) | 2019-10-16 | 2023-08-01 | Chemocentryx, Inc. | Heteroaryl-biphenyl amides for the treatment of PD-L1 diseases |
MX2022005651A (es) * | 2019-11-11 | 2022-07-27 | Incyte Corp | Sales y formas cristalinas de un inhibidor de la proteina de muerte celular programada 1 (pd-1)/ligando de muerte celular programada 1 (pd-l1). |
BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
CN115279766A (zh) | 2020-01-03 | 2022-11-01 | 因赛特公司 | 包含a2a/a2b和pd-1/pd-l1抑制剂的组合疗法 |
JP2023509155A (ja) * | 2020-01-03 | 2023-03-07 | 上▲海▼翰森生物医▲薬▼科技有限公司 | ビフェニル系誘導体阻害剤、その調製方法及び使用 |
WO2021139647A1 (zh) * | 2020-01-07 | 2021-07-15 | 上海和誉生物医药科技有限公司 | 一种联苯基氟代双键衍生物及其制备方法和在药学上的应用 |
US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
EP4135844A1 (en) | 2020-04-16 | 2023-02-22 | Incyte Corporation | Fused tricyclic kras inhibitors |
WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
WO2021254005A1 (zh) * | 2020-06-17 | 2021-12-23 | 上海和誉生物医药科技有限公司 | 一种免疫抑制剂、其制备方法和应用 |
US11999752B2 (en) | 2020-08-28 | 2024-06-04 | 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 |
CN114698376B (zh) | 2020-10-29 | 2022-10-18 | 深圳微芯生物科技股份有限公司 | 作为免疫调节剂的联苯类化合物及其制备方法和应用 |
KR20230117573A (ko) | 2020-11-06 | 2023-08-08 | 인사이트 코포레이션 | Pd-1 및 pd-l1 억제제, 및 이의 염 및 결정형의 제조 방법 |
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 |
JP2024502005A (ja) | 2020-12-29 | 2024-01-17 | インサイト・コーポレイション | A2a/a2b阻害剤、pd-1/pd-l1阻害剤、及び抗cd73抗体を含む併用療法 |
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 |
KR20230141812A (ko) * | 2021-02-01 | 2023-10-10 | 쉔젠 칩스크린 바이오사이언스 씨오., 엘티디. | 면역 조절제로서의 바이페닐 화합물, 이의 제조방법 및 용도 |
EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
TW202317565A (zh) | 2021-07-07 | 2023-05-01 | 美商英塞特公司 | 作為kras抑制劑的三環化合物 |
JP2024529347A (ja) | 2021-07-14 | 2024-08-06 | インサイト・コーポレイション | Krasの阻害剤としての三環式化合物 |
EP4396187A1 (en) | 2021-08-31 | 2024-07-10 | Incyte Corporation | Naphthyridine compounds as inhibitors of kras |
US12030883B2 (en) | 2021-09-21 | 2024-07-09 | 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 |
JP2024537824A (ja) | 2021-10-01 | 2024-10-16 | インサイト・コーポレイション | ピラゾロキノリンkras阻害剤 |
IL312114A (en) | 2021-10-14 | 2024-06-01 | Incyte Corp | Quinoline compounds as Kras inhibitors |
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 |
CN114209815B (zh) * | 2021-11-22 | 2024-04-26 | 山东大学 | 一种药物组合物及其制备方法和应用 |
US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
AR128043A1 (es) | 2021-12-22 | 2024-03-20 | Incyte Corp | Sales y formas sólidas de un inhibidor de fgfr y procesos para su preparación |
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 |
US20230399342A1 (en) | 2022-06-08 | 2023-12-14 | Incyte Corporation | Tricyclic triazolo compounds as dgk inhibitors |
US20240101557A1 (en) | 2022-07-11 | 2024-03-28 | Incyte Corporation | Fused tricyclic compounds as inhibitors of kras g12v mutants |
TW202428272A (zh) | 2022-11-18 | 2024-07-16 | 美商英塞特公司 | 作為dgk抑制劑之雜芳基氟烯烴 |
TW202428575A (zh) | 2023-01-12 | 2024-07-16 | 美商英塞特公司 | 作為dgk抑制劑之雜芳基氟代烯烴 |
WO2024196989A1 (en) * | 2023-03-20 | 2024-09-26 | University Of Central Florida Research Foundation, Inc. | Anti-malarial therapy |
Family Cites Families (333)
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 |
DE69421982T2 (de) | 1993-09-20 | 2000-03-30 | Fuji Photo Film Co., Ltd. | Positiv arbeitende Photoresistzusammensetzung |
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 |
JP2001505585A (ja) | 1996-12-16 | 2001-04-24 | 藤沢薬品工業株式会社 | 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途 |
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 |
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 |
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 |
US6297351B1 (en) | 1998-12-17 | 2001-10-02 | Sumitomo Bakelite Company Limited | Polybenzoxazole resin and precursor thereof |
EA200100675A1 (ru) | 1998-12-18 | 2001-12-24 | Аксис Фармасьютикалз, Инк. | Ингибиторы протеазы |
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 |
CN1623984A (zh) | 1999-12-27 | 2005-06-08 | 日本烟草产业株式会社 | 稠环化合物及其药物用途 |
DE50112961D1 (de) | 2000-02-01 | 2007-10-18 | 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 |
ATE361297T1 (de) | 2000-03-31 | 2007-05-15 | Ortho Mcneil Pharm Inc | Phenyl-substituierte imidazopyridine |
EP1278734A2 (en) | 2000-04-24 | 2003-01-29 | Merck Frosst Canada & Co. | Method of treatment using phenyl and biaryl derivatives as prostaglandin e inhibitors and compounds useful therefore |
CZ303572B6 (cs) | 2000-06-28 | 2012-12-12 | Smithkline Beecham P. L. C. | Jemne rozmelnený prostredek a zpusob jeho prípravy |
WO2002014321A1 (en) | 2000-08-11 | 2002-02-21 | 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 |
US6919352B2 (en) | 2000-12-15 | 2005-07-19 | Smithkline Beecham Corporation | Pyrazolopyridinyl pyridine and pyrimidine therapeutic compounds |
SE0100567D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
AU2002258550B2 (en) | 2001-03-14 | 2006-04-27 | Eli Lilly And Company | Retinoid X receptor modulators |
WO2002078700A1 (en) | 2001-03-30 | 2002-10-10 | Smithkline Beecham Corporation | Pyralopyridines, process for their preparation and use as therapteutic compounds |
WO2002083672A1 (en) | 2001-04-10 | 2002-10-24 | Smithkline Beecham Corporation | Antiviral pyrazolopyridine compounds |
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 |
EP1423389B1 (en) | 2001-09-07 | 2007-06-06 | SmithKline Beecham Corporation | 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 |
WO2003031587A2 (en) | 2001-10-09 | 2003-04-17 | The Regents Of The University Of California | Use of stat-6 inhibitors as therapeutic agents |
MXPA04003419A (es) | 2001-10-09 | 2004-07-08 | Upjohn Co | Tetrahidro y hexahidro-carbazoles sustituidos con arilsulfonilo como ligandos del receptor 5-ht-6. |
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 |
PL373399A1 (en) | 2002-04-11 | 2005-08-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
WO2003091256A1 (fr) | 2002-04-23 | 2003-11-06 | Shionogi & Co., Ltd. | Derive de pyrazolo[1,5-a]pyrimidine et inhibiteur de la nad(p)h oxydase contenant ledit derive |
US20060004010A1 (en) | 2002-07-10 | 2006-01-05 | Hiromu Habashita | Ccr4 antagonist and medical use thereof |
WO2004006906A2 (en) | 2002-07-15 | 2004-01-22 | 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 |
US20050260126A1 (en) | 2002-08-30 | 2005-11-24 | Yukitsuka Kudo | Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein |
JP2004091369A (ja) | 2002-08-30 | 2004-03-25 | Sumitomo Pharmaceut Co Ltd | 新規ビフェニル化合物 |
AU2003275266A1 (en) | 2002-10-03 | 2004-05-04 | Smithkline Beecham Corporation | Therapeutic compounds based on pyrazolopyridine derivatives |
JP2006504755A (ja) | 2002-10-15 | 2006-02-09 | スミスクライン ビーチャム コーポレーション | Gsk−3阻害薬としてのピリダジン化合物 |
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 |
BRPI0409747A (pt) | 2003-04-11 | 2006-05-09 | Glenmark Pharmaceuticals Sa | novos compostos heterocìclicos úteis para tratamento de distúrbios inflamatórios e alérgicos, processo para sua preparação e composições farmacêuticas contendo estes |
PE20050158A1 (es) | 2003-05-19 | 2005-05-12 | Irm Llc | Compuestos inmunosupresores y composiciones |
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 |
EP1644335A4 (en) | 2003-07-11 | 2008-06-04 | Bristol Myers Squibb Co | TETRAHYDROQUINOLINE DERIVATIVES COMPRISING MODULATORS OF CANNABINOID RECEPTORS |
US7691870B2 (en) | 2003-07-11 | 2010-04-06 | Merck Patent Gmbh | Benzimidazole carboxamides as raf kinase inhibitors |
EP1661879A4 (en) | 2003-08-04 | 2006-11-29 | Ono Pharmaceutical Co | A DIPHENYL ETHER COMPOUND, PROCESS FOR THE PRODUCTION AND USE THEREOF |
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 |
SG146624A1 (en) | 2003-09-11 | 2008-10-30 | Kemia Inc | Cytokine inhibitors |
JP4758349B2 (ja) | 2003-10-08 | 2011-08-24 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼ阻害剤としての化合物および組成物 |
EP1679309A4 (en) | 2003-10-24 | 2007-03-28 | Ono Pharmaceutical Co | ANTISTRESS MEDICAMENT AND ITS MEDICAL USE |
WO2005047290A2 (en) | 2003-11-11 | 2005-05-26 | Cellular Genomics Inc. | Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors |
EP1699763A1 (de) | 2003-12-23 | 2006-09-13 | Basf Aktiengesellschaft | 3-trifluormethylpicolins ureanilide und ihre verwendung als fungizide |
EP1715867A4 (en) | 2004-02-12 | 2009-04-15 | Merck & Co Inc | BIPYRIDYL AMIDES AS MODULATORS OF GLUTAMATE METABOTROPIC REPEATER-5 |
JPWO2005077948A1 (ja) | 2004-02-16 | 2008-01-10 | 第一製薬株式会社 | 抗真菌作用複素環化合物 |
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 |
AU2005220882A1 (en) | 2004-03-08 | 2005-09-22 | Georgia State University Research Foundation, Inc | Novel dicationic imidazo(1,2-a)pyridines and 5,6,7,8-tetrahydro-imidazo(1,2a)pyridines as antiprotozoal agents |
US7423147B2 (en) | 2004-03-31 | 2008-09-09 | Janssen Pharmaceutical, N.V. | Pyridine compounds as histamine H3 modulators |
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 |
WO2005099656A2 (en) | 2004-04-06 | 2005-10-27 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
CN1946703A (zh) | 2004-04-20 | 2007-04-11 | 特兰斯泰克制药公司 | 取代的噻唑和嘧啶衍生物作为黑素细胞皮质激素受体调节剂 |
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 |
PE20060748A1 (es) | 2004-09-21 | 2006-10-01 | Smithkline Beecham Corp | Derivados de indolcarboxamida como inhibidores de quinasa ikk2 |
JP2008514611A (ja) | 2004-09-23 | 2008-05-08 | ワイス | C型肝炎ウイルスによる感染を処置するためのカルバゾールおよびシクロペンタインドールの誘導体 |
US7713973B2 (en) | 2004-10-15 | 2010-05-11 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
WO2006053121A2 (en) | 2004-11-10 | 2006-05-18 | 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 |
WO2006094235A1 (en) | 2005-03-03 | 2006-09-08 | Sirtris Pharmaceuticals, Inc. | Fused heterocyclic compounds and their use as sirtuin modulators |
TW200716551A (en) | 2005-03-10 | 2007-05-01 | Cgi Pharmaceuticals Inc | Certain substituted amides, method of making, and method of use thereof |
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 |
EP1902056A2 (en) | 2005-05-20 | 2008-03-26 | 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 |
US7723336B2 (en) | 2005-09-22 | 2010-05-25 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
ES2572263T3 (es) | 2005-10-25 | 2016-05-31 | Shionogi & Co | Derivados de dihidrooxazina y tetrahidropirimidina como inhibidores de BACE 1 |
AU2006316322B2 (en) | 2005-11-22 | 2011-08-25 | Merck Canada Inc. | 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 |
US20090281120A1 (en) | 2005-12-12 | 2009-11-12 | Ono Pharmaceutical Co., Ltd | Bicyclic heterocyclic compound |
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 |
US20090304821A1 (en) | 2006-03-08 | 2009-12-10 | Takeda Pharmaceutical Company Limited | Pharmaceutical Combination |
MX2008012617A (es) | 2006-03-31 | 2008-10-10 | Novartis Ag | Compuestos organicos. |
EP2023919A4 (en) | 2006-05-08 | 2010-12-22 | Molecular Neuroimaging Llc | COMPOUNDS AND AMYLOID PROBES FOR THERAPY AND IMAGING USES |
AU2007257959A1 (en) | 2006-06-09 | 2007-12-21 | Kemia, Inc. | Therapy using cytokine inhibitors |
US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
EP2044061A2 (en) | 2006-07-20 | 2009-04-08 | 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 |
WO2008027812A2 (en) | 2006-08-28 | 2008-03-06 | Forest Laboratories Holdings Limited | Imidazopyridine and imidazopyrimidine derivatives |
CA2663178C (en) | 2006-09-11 | 2016-01-12 | Matrix Laboratories Ltd. | Dibenzofuran derivatives as inhibitors of pde-4 and pde-10 |
AR063706A1 (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 farmaceuticas que las comprenden. |
JP2010502751A (ja) | 2006-09-11 | 2010-01-28 | シージーアイ ファーマシューティカルズ,インコーポレイティド | キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法 |
US7838523B2 (en) | 2006-09-11 | 2010-11-23 | Cgi Pharmaceuticals, Inc. | Certain substituted amides, method of making, and method of use thereof |
PE20081370A1 (es) | 2006-09-11 | 2008-11-28 | Cgi Pharmaceuticals Inc | Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas |
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 |
MX2009004289A (es) | 2006-10-27 | 2009-05-05 | Wyeth Corp | Compuestos triciclicos como inhibidores de metaloproteinasas matriciales. |
EP2089364B1 (en) | 2006-11-08 | 2013-06-12 | Bristol-Myers Squibb Company | Pyridinone compounds |
GB0623209D0 (en) | 2006-11-21 | 2007-01-03 | F2G Ltd | Antifungal agents |
WO2008064318A2 (en) | 2006-11-22 | 2008-05-29 | University Of Medicine And Dentistry Of New Jersey | Peripheral opioid receptor active compounds |
WO2008064317A1 (en) | 2006-11-22 | 2008-05-29 | University Of Medicine And Dentistry Of New Jersey | Lipophilic opioid receptor active compounds |
WO2008071944A1 (en) | 2006-12-14 | 2008-06-19 | Boehringer Ingelheim International Gmbh | Benzoxazoles useful in the treatment of inflammation |
US8513270B2 (en) | 2006-12-22 | 2013-08-20 | Incyte Corporation | Substituted heterocycles as Janus kinase inhibitors |
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 |
US8338437B2 (en) | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
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 |
ES2388454T3 (es) | 2007-03-22 | 2012-10-15 | Astrazeneca Ab | Derivados de quinolina para el tratamiento de enfermedades inflamatorias |
EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
WO2008134553A1 (en) | 2007-04-26 | 2008-11-06 | Xenon Pharmaceuticals Inc. | Methods of using bicyclic compounds in treating sodium channel-mediated diseases |
ES2395583T3 (es) | 2007-05-10 | 2013-02-13 | Ge Healthcare Limited | IMIDAZOL (1,2-A)PIRIDINAS y compuestos relacionados con actividad frente a los receptores cannabinoides CB2 |
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 |
ATE505454T1 (de) | 2007-09-20 | 2011-04-15 | 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 |
AU2008337876A1 (en) | 2007-12-19 | 2009-06-25 | Syngenta Participations Ag | Insecticidal compounds |
WO2009079683A1 (en) | 2007-12-21 | 2009-07-02 | The University Of Sydney | Translocator protein ligands |
WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
ES2548774T3 (es) | 2008-01-18 | 2015-10-20 | Eisai R&D Management Co., Ltd. | Derivado de aminodihidrotiazina condensado |
JP5381718B2 (ja) | 2008-01-31 | 2014-01-08 | コニカミノルタ株式会社 | ハロ多環芳香族化合物及びその製造方法 |
AU2009218515A1 (en) | 2008-02-26 | 2009-09-03 | Novartis Ag | Heterocyclic compounds as inhibitors of CXCR2 |
EP2095818A1 (en) | 2008-02-29 | 2009-09-02 | AEterna Zentaris GmbH | Use of LHRH antagonists at non-castrating doses |
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 |
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 |
JP5432982B2 (ja) | 2008-03-31 | 2014-03-05 | 武田薬品工業株式会社 | アポトーシスシグナル調節キナーゼ1阻害剤 |
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 |
US20110077248A1 (en) | 2008-05-29 | 2011-03-31 | Sirtris Pharmaceuticals, Inc. | Imidazopyridine and related analogs as sirtuin modulators |
EP2323665B1 (en) | 2008-07-24 | 2013-06-19 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
US9643922B2 (en) | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
US9540322B2 (en) | 2008-08-18 | 2017-01-10 | 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 |
EP2365970B1 (en) | 2008-11-12 | 2018-03-21 | Gilead Connecticut, Inc. | Pyridazinones and their use as btk inhibitors |
EP2376490B1 (en) | 2008-12-04 | 2013-01-23 | Proximagen Limited | Imidazopyridine compounds |
JP5557849B2 (ja) | 2008-12-19 | 2014-07-23 | ブリストル−マイヤーズ スクイブ カンパニー | カルバゾールおよびカルボリンキナーゼ阻害剤 |
CN102325753B (zh) | 2008-12-19 | 2014-09-10 | 百时美施贵宝公司 | 用作激酶抑制剂的咔唑甲酰胺化合物 |
AR074830A1 (es) | 2008-12-19 | 2011-02-16 | Cephalon Inc | Pirrolotriazinas como inhibidores de alk y jak2 |
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 |
WO2010075376A2 (en) | 2008-12-23 | 2010-07-01 | Abbott Laboratories | Anti-viral compounds |
WO2010074284A1 (ja) | 2008-12-26 | 2010-07-01 | 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 |
KR20100101054A (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 |
SG10201401169QA (en) | 2009-04-02 | 2014-05-29 | Merck Serono Sa | Dihydroorotate dehydrogenase inhibitors |
ES2475091T3 (es) | 2009-04-16 | 2014-07-10 | Centro Nacional De Investigaciones Oncol�Gicas (Cnio) | Imidazopirazinas como inhibidores de proteína cinasas |
US8338441B2 (en) | 2009-05-15 | 2012-12-25 | Gilead Sciences, Inc. | Inhibitors of human immunodeficiency virus replication |
KR20120049852A (ko) | 2009-06-30 | 2012-05-17 | 시가 테크놀로지스, 인크. | 뎅기 바이러스 감염의 치료 및 예방 |
US8993604B2 (en) | 2009-06-30 | 2015-03-31 | Siga Technologies, Inc. | Treatment and prevention of dengue virus infections |
TWI598347B (zh) | 2009-07-13 | 2017-09-11 | 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 |
MX2012004340A (es) | 2009-10-16 | 2012-11-23 | Rib X Pharmaceuticals Inc | Compuestos antimicrobianos y metodos para fabricar y utilizar los mismos. |
WO2011050245A1 (en) | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
EP2518072A4 (en) | 2009-12-24 | 2014-06-04 | Ajinomoto Kk | IMIDAZOPYRIDAZINE COMPOUNDS |
WO2011082400A2 (en) | 2010-01-04 | 2011-07-07 | President And Fellows Of Harvard College | 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 |
AR080433A1 (es) | 2010-03-02 | 2012-04-11 | Merck Sharp & Dohme | Derivados de benzofurancarboxamidas utiles para tratar o prevenir infecciones por vhc y composiciones farmaceuticas que los contienen. |
KR101720824B1 (ko) | 2010-03-04 | 2017-03-28 | 머크 샤프 앤드 돔 코포레이션 | 카테콜 o-메틸 트랜스퍼라제의 억제제 및 정신병적 장애의 치료에서의 그의 용도 |
EP2547678B1 (en) | 2010-03-18 | 2016-03-16 | Institut Pasteur Korea | Anti-infective compounds |
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 |
WO2012047856A2 (en) | 2010-10-04 | 2012-04-12 | Institute For Hepatitis And Virus Research | Novel inhibitors of secretion of hepatitis b virus antigens |
WO2012052745A1 (en) | 2010-10-21 | 2012-04-26 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Combinations of pi3k inhibitors with a second anti -tumor agent |
EP2444084A1 (en) | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
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 |
WO2012080376A1 (en) | 2010-12-17 | 2012-06-21 | Syngenta Participations Ag | Insecticidal compounds |
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 |
KR20140027090A (ko) | 2011-01-04 | 2014-03-06 | 노파르티스 아게 | 연령-관련 황반 변성 (amd)의 치료에 유용한 인돌 화합물 또는 그의 유사체 |
CA2825098C (en) | 2011-01-27 | 2020-03-10 | Universite De Montreal | 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 |
US9464065B2 (en) | 2011-03-24 | 2016-10-11 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
WO2012139425A1 (en) | 2011-04-13 | 2012-10-18 | Schering Corporation | 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 |
US9278910B2 (en) | 2011-05-31 | 2016-03-08 | Receptos, Inc. | 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 |
AU2012282229B2 (en) | 2011-07-08 | 2015-05-07 | Novartis Ag | Novel pyrrolo pyrimidine derivatives |
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 |
EP2757884B1 (en) | 2011-09-22 | 2022-07-27 | Merck Sharp & Dohme LLC | 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 |
CA2851445A1 (en) | 2011-10-13 | 2013-04-18 | Novartis Ag | Novel oxazine derivatives and their use in the treatment of disease |
RU2014120180A (ru) | 2011-10-20 | 2015-11-27 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Замещенные бициклические аза-гетероциклы и аналоги в качестве модуляторов сиртуина |
CA2852615A1 (en) | 2011-10-21 | 2013-04-25 | 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 |
US20150011751A1 (en) | 2012-03-09 | 2015-01-08 | Carna Biosciences, Inc. | Novel triazine derivative |
WO2013157021A1 (en) | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
ES2571479T3 (es) | 2012-04-20 | 2016-05-25 | Gilead Sciences Inc | Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH |
US20150105433A1 (en) | 2012-04-27 | 2015-04-16 | The Uab Research Foundation | TREATING VIRAL INFECTIONS HAVING VIRAL RNAs TRANSLATED BY A NON-IRES MEDIATED MECHANISM |
WO2013191113A1 (ja) | 2012-06-18 | 2013-12-27 | 住友化学株式会社 | 縮合複素環化合物 |
EP2871179A4 (en) | 2012-07-03 | 2016-03-16 | Ono Pharmaceutical Co | CONNECTION WITH AGONISTIC EFFECT ON THE SOMATOSTATIN RECEPTOR AND ITS USE FOR MEDICAL PURPOSES |
EA028722B1 (ru) | 2012-07-13 | 2017-12-29 | Юсб Байофарма Спрл | Производные имидазопиридина в качестве модуляторов активности 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 |
US9428511B2 (en) | 2012-09-06 | 2016-08-30 | Bristol-Myers Squibb Company | Imidazopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases |
WO2014048939A1 (en) | 2012-09-26 | 2014-04-03 | F. Hoffmann-La Roche Ag | 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 |
US9163027B2 (en) | 2012-11-21 | 2015-10-20 | 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 |
ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
JP2016505055A (ja) | 2013-01-22 | 2016-02-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害剤としてのフルオロ−[1,3]オキサジン |
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 |
EP2950814A4 (en) | 2013-01-31 | 2016-06-08 | Univ Jefferson | PD-L1 AND PD-L2 BASED FUSION PROTEINS AND USES THEREOF |
EP2963037B1 (en) | 2013-02-27 | 2019-03-27 | Mochida Pharmaceutical Co., Ltd. | Novel pyrazole derivative |
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 |
JP2016516399A (ja) | 2013-03-13 | 2016-06-09 | オーストラリアン ニュークリア サイエンス アンド テクノロジー オーガニゼーション | 非機能性tspo遺伝子を有するトランスジェニック非ヒト生物 |
US9527842B2 (en) | 2013-03-14 | 2016-12-27 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
CA2902594C (en) | 2013-03-14 | 2023-01-10 | Curadev Pharma Private Ltd. | Inhibitors of the kynurenine pathway |
DK2968304T3 (en) | 2013-03-14 | 2019-01-28 | Univ Columbia | 4-PHENYLPIPERIDINES, THEIR PREPARATION AND USE. |
EP2968265A4 (en) | 2013-03-14 | 2016-12-28 | Celtaxsys Inc | INHIBITORS OF THE LEUKOTRIEN A4 HYDROLASE |
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 |
NZ754039A (en) | 2013-06-26 | 2021-06-25 | Abbvie Inc | Primary carboxamides as btk inhibitors |
MX2015017821A (es) | 2013-07-02 | 2016-04-15 | Syngenta Participations Ag | Heterociclos bi-o triciclicos activos como plaguicidas con sustituyentes que contienen azufre. |
TWI641595B (zh) | 2013-07-17 | 2018-11-21 | 日商大塚製藥股份有限公司 | 氰基三唑化合物類 |
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 |
BR112016004194A8 (pt) | 2013-09-04 | 2020-02-11 | Bristol Myers Squibb Co | compostos úteis como imunomoduladores |
HUE038169T2 (hu) | 2013-09-06 | 2018-09-28 | Aurigene Discovery Tech Ltd | 1,2,4-Oxadiazol származékok mint immunomodulátorok |
KR20160081898A (ko) | 2013-09-06 | 2016-07-08 | 오리진 디스커버리 테크놀로지스 리미티드 | 면역조절제로서 1,3,4-옥사디아졸 및 1,3,4-티아디아졸 유도체 |
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 |
GB201321736D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
GB201321733D0 (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 |
RU2016131792A (ru) | 2014-01-03 | 2018-02-06 | Байер Энимэл Хельс ГмбХ | Новые пиразолил-гетероариламиды в качестве средств для борьбы с вредителями |
CA2938152A1 (en) | 2014-02-10 | 2015-08-13 | Merck Sharp & Dohme Corp. | Antibodies that bind to human tau and assay for quantifying human tau using the antibodies |
PT3110418T (pt) | 2014-02-25 | 2020-01-22 | Achillion Pharmaceuticals Inc | Compostos de arilo, heteroarilo e heterocíclicos para tratamento de distúrbios mediados por complemento |
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 |
WO2015150097A1 (en) | 2014-04-04 | 2015-10-08 | Iomet Pharma Ltd | Indole derivatives for use in medicine |
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 |
US20170305922A1 (en) | 2014-09-17 | 2017-10-26 | 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 |
AU2015328285B2 (en) | 2014-10-06 | 2019-07-18 | Merck Patent Gmbh | Heteroaryl compounds as BTK inhibitors and uses thereof |
AU2015360416A1 (en) | 2014-12-10 | 2017-06-08 | Massachusetts Institute Of Technology | Fused 1,3-azole derivatives useful for the treatment of proliferative diseases |
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 |
DE112016000383A5 (de) | 2015-01-20 | 2017-10-05 | 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 |
EP3365340B1 (en) | 2015-10-19 | 2022-08-10 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
WO2017070320A1 (en) | 2015-10-21 | 2017-04-27 | 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 |
HRP20221035T1 (hr) | 2015-11-19 | 2022-11-11 | Incyte Corporation | Heterociklički spojevi kao imunomodulatori |
US20170174671A1 (en) | 2015-12-17 | 2017-06-22 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
CN108463109B (zh) | 2015-12-22 | 2022-04-29 | 先正达参股股份有限公司 | 杀有害生物活性吡唑衍生物 |
WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
PE20230731A1 (es) | 2015-12-22 | 2023-05-03 | Incyte Corp | Compuestos heterociclicos como inmunomoduladores |
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 |
AU2016378482A1 (en) | 2015-12-22 | 2018-07-12 | Synthon B.V. | Pharmaceutical composition comprising amorphous lenalidomide and an antioxidant |
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 |
AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
EP3464279B1 (en) | 2016-05-26 | 2021-11-24 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
TWI771305B (zh) | 2016-06-20 | 2022-07-21 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
MX2018016331A (es) | 2016-06-20 | 2019-05-20 | Novartis Ag | Formas cristalinas de compuesto de triazolopirimidina. |
MX2018016295A (es) | 2016-06-20 | 2019-09-16 | Elanco Us Inc | Interferon porcino pegilado y metodos de utilizacion del mismo. |
ES2870920T3 (es) | 2016-06-21 | 2021-10-28 | X4 Pharmaceuticals Inc | Inhibidores de CXCR4 y usos de los mismos |
WO2018013789A1 (en) | 2016-07-14 | 2018-01-18 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
EP3493804A1 (en) * | 2016-08-03 | 2019-06-12 | Arising International, Inc. | Symmetric or semi-symmetric compounds useful as immunomodulators |
US20180057486A1 (en) | 2016-08-29 | 2018-03-01 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
CN110167560B (zh) | 2016-08-30 | 2023-08-18 | 四相制药公司 | 四环素化合物和治疗方法 |
KR102559851B1 (ko) | 2016-12-21 | 2023-07-25 | 아세르타 파마. 비.브이. | 브루톤 티로신 키나제의 이미다조피라진 저해제 |
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 |
PE20200005A1 (es) * | 2016-12-22 | 2020-01-06 | Incyte Corp | Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de internalizacion pd-l1 |
WO2018119266A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
WO2018119263A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds derivatives as pd-l1 internalization inducers |
WO2018119286A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
WO2018119221A1 (en) * | 2016-12-22 | 2018-06-28 | Incyte Corporation | Pyridine derivatives as immunomodulators |
ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
SI3559009T1 (sl) | 2016-12-22 | 2021-08-31 | Calithera Biosciences, Inc. | Sestavki in postopki za zaviranje arginazne dejavnosti |
JOP20180040A1 (ar) | 2017-04-20 | 2019-01-30 | Gilead Sciences Inc | مثبطات pd-1/pd-l1 |
IL272258B (en) | 2017-07-28 | 2022-08-01 | Chemocentryx Inc | Immunomodulator compounds |
US10392405B2 (en) | 2017-08-08 | 2019-08-27 | Chemocentryx, Inc. | Macrocyclic immunomodulators |
CN109400522B (zh) | 2017-08-18 | 2023-04-28 | 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 |
FI3774791T3 (fi) | 2018-03-30 | 2023-03-21 | Incyte Corp | Heterosyklisiä yhdisteitä immunomodulaattoreina |
WO2019192506A1 (en) | 2018-04-03 | 2019-10-10 | Betta Pharmaceuticals Co., Ltd | Immunomodulators, compositions and methods thereof |
CN112041311B (zh) | 2018-04-19 | 2023-10-03 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
BR112020022936A2 (pt) | 2018-05-11 | 2021-02-02 | Incyte Corporation | derivados de tetra-hidro-imidazo[4,5-c]piridina como imunomoduladores de pd-l1 |
WO2020086556A1 (en) | 2018-10-24 | 2020-04-30 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
KR20210089195A (ko) | 2018-11-02 | 2021-07-15 | 상하이 맥시노벨 파마수티컬스 씨오., 엘티디. | 비페닐계 화합물, 이의 중간체, 제조 방법, 약학 조성물 및 용도 |
WO2020156323A1 (en) | 2019-01-31 | 2020-08-06 | Betta Pharmaceuticals Co., Ltd | Immunomodulators, compositions and methods thereof |
WO2021030162A1 (en) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
JP7559059B2 (ja) | 2019-09-30 | 2024-10-01 | インサイト・コーポレイション | 免疫調節剤としてのピリド[3,2-d]ピリミジン化合物 |
MX2022005651A (es) | 2019-11-11 | 2022-07-27 | Incyte Corp | Sales y formas cristalinas de un inhibidor de la proteina de muerte celular programada 1 (pd-1)/ligando de muerte celular programada 1 (pd-l1). |
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