AR108186A1 - Péptidos macrocíclicos que inhiben las interacciones proteína / proteína, proteína de muerte programada 1 (pd-1) / ligando de pd-1 (pd-l1) y pd-l1 / cd80 - Google Patents
Péptidos macrocíclicos que inhiben las interacciones proteína / proteína, proteína de muerte programada 1 (pd-1) / ligando de pd-1 (pd-l1) y pd-l1 / cd80Info
- Publication number
- AR108186A1 AR108186A1 ARP170100881A ARP170100881A AR108186A1 AR 108186 A1 AR108186 A1 AR 108186A1 AR P170100881 A ARP170100881 A AR P170100881A AR P170100881 A ARP170100881 A AR P170100881A AR 108186 A1 AR108186 A1 AR 108186A1
- Authority
- AR
- Argentina
- Prior art keywords
- 3alkyl
- 2nhc
- independently selected
- optionally substituted
- halo
- Prior art date
Links
- 102000008096 B7-H1 Antigen Human genes 0.000 title abstract 4
- 108010074708 B7-H1 Antigen Proteins 0.000 title abstract 4
- 101000914484 Homo sapiens T-lymphocyte activation antigen CD80 Proteins 0.000 title abstract 2
- 102100027222 T-lymphocyte activation antigen CD80 Human genes 0.000 title abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 title abstract 2
- 102000004169 proteins and genes Human genes 0.000 title 3
- 108090000623 proteins and genes Proteins 0.000 title 3
- 230000003993 interaction Effects 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 39
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 18
- 239000001257 hydrogen Substances 0.000 abstract 16
- 229910052739 hydrogen Inorganic materials 0.000 abstract 16
- -1 amino, hydroxy Chemical group 0.000 abstract 15
- 125000005843 halogen group Chemical group 0.000 abstract 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 10
- 125000004429 atom Chemical group 0.000 abstract 9
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 8
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 125000003275 alpha amino acid group Chemical group 0.000 abstract 5
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 abstract 5
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 4
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 4
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004122 cyclic group Chemical group 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001041 indolyl group Chemical group 0.000 abstract 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 abstract 2
- 229960002685 biotin Drugs 0.000 abstract 2
- 235000020958 biotin Nutrition 0.000 abstract 2
- 239000011616 biotin Substances 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229940046009 vitamin E Drugs 0.000 abstract 2
- 239000011709 vitamin E Substances 0.000 abstract 2
- 101100240521 Caenorhabditis elegans nhr-16 gene Proteins 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 230000006916 protein interaction Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Virology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Péptidos macrocíclicos que inhiben las interacciones proteína / proteína PD-1 / PD-L1 y PD-L1 / CD80, y por ende, son útiles para la mejora de distintas enfermedades, que incluyen el cáncer y las enfermedades infecciosas. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde: A se selecciona de un enlace, o un compuesto del grupo de fórmulas (2); en donde: la línea ondulada * indica el punto de unión al grupo carbonilo y la línea ondulada indica el punto de unión al átomo de nitrógeno; z es 0, 1 ó 2; w es 1 ó 2; n es 0 ó 1; m es 1 ó 2; m es 0 ó 1; p es 0, 1 ó 2; Rˣ se selecciona de hidrógeno, amino, hidroxi y metilo; R¹⁴ y R¹⁵ se seleccionan independientemente de hidrógeno y metilo; y Rᶻ se selecciona de hidrógeno y -C(O)NHR¹⁶; en donde R¹⁶ se selecciona de hidrógeno, -CHR¹⁷C(O)NH₂, -CHR¹⁷C(O)NHCHR¹⁸C(O)NH₂ y -CHR¹⁷C(O)NHCHR¹⁸C(O)NHCH₂C(O)NH₂; en donde R¹⁷ se selecciona de hidrógeno y -CH₂OH, y en donde R¹⁸ se selecciona de hidrógeno y metilo; Rᵛ es hidrógeno o una cadena lateral de aminoácidos naturales; la línea ondulada * indica el punto de unión al grupo carbonilo y la línea ondulada indica el punto de unión al átomo de nitrógeno; Rᶜ, Rᶠ, Rʰ, Rⁱ, Rᵐ y Rⁿ son hidrógeno; Rᵃ, Rᵉ, Rʲ y Rᵏ se seleccionan cada uno independientemente de hidrógeno y metilo; R¹⁰ es indolilC₁₋₃alquilo, en donde la parte de indolilo se sustituye opcionalmente con un grupo seleccionado de C₁₋₆alcoxi, C₁₋₆alcoxicarbonilo, C₁₋₆alcoxicarbonilC₁₋₃alquilo, (C₁₋₆alquil)S(O)₂NHC(O)C₁₋₃alquilo, arilS(O)₂NHC(O)C₁₋₃alquilo, arilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, heteroarilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, -NRᵖRq, (NRᵖRq)C₁₋₃alquilo y tetrazolilC₁₋₃alquilo, o con dos grupos seleccionados de C₁₋₆alcoxi, C₁₋₆alcoxicarbonilo, C₁₋₆alcoxicarbonilC₁₋₃alquilo, C₁₋₃alquilo, (C₁₋₆alquil)S(O)₂NHC(O)C₁₋₃alquilo, arilS(O)₂NHC(O)C₁₋₃alquilo, arilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, carboxi, carboxiC₁₋₃alquilo, ciano, C₃₋₆cicloalquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, halo, haloC₁₋₃alcoxi, haloC₁₋₃alquilo, heteroarilS(O)₂NHC(O)C₁₋₃alquilo, heteroarilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, hidroxi, -NRᵖRq, (NRᵖRq)C₁₋₃alquilo, tetrazolilo, tetrazolilC₁₋₃alquilo y fenilo, en donde el fenilo también se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados independientemente de C₁₋₃alcoxi, C₁₋₃alquilo y halo; o R¹⁰ es azaindolilC₁₋₃alquilo, en donde la parte de azaindolilo de azaindolilC₁₋₃alquilo se sustituye con 1 ó 2 grupos diferentes seleccionados independientemente de C₁₋₆alcoxi, C₁₋₆alcoxicarbonilo, C₁₋₆alcoxicarbonilC₁₋₃alquilo, C₁₋₃alquilo, (C₁₋₆alquil)S(O)₂NHC(O)C₁₋₃alquilo, arilS(O)₂NHC(O)C₁₋₃alquilo, arilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, carboxi, carboxiC₁₋₃alquilo, ciano, C₃₋₆cicloalquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, halo, haloC₁₋₃alcoxi, haloC₁₋₃alquilo, heteroarilS(O)₂NHC(O)C₁₋₃alquilo, heteroarilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, hidroxi, -NRᵖRq, (NRᵖRq)C₁₋₃alquilo, tetrazolilo, tetrazolilC₁₋₃alquilo y fenilo, en donde el fenilo también se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados independientemente de C₁₋₃alcoxi, C₁₋₃alquilo y halo; o R¹⁰ es -(CH₂)ₙQ es un sistema de anillos 5,6 fusionados saturados o insaturados que contiene 1, 2, 3 ó 4 átomos de nitrógeno, en donde el sistema de anillos se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados de C₁₋₆alcoxi, C₁₋₆alcoxicarbonilo, C₁₋₆alcoxicarbonilC₁₋₃alquilo, C₁₋₃alquilo, (C₁₋₆alquil)S(O)₂NHC(O)C₁₋₃alquilo, arilS(O)₂NHC(O)C₁₋₃alquilo, arilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, carboxi, carboxiC₁₋₃alquilo, ciano, C₃₋₆cicloalquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, halo, haloC₁₋₃alcoxi, haloC₁₋₃alquilo, heteroarilS(O)₂NHC(O)C₁₋₃alquilo, heteroarilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, hidroxi, -NRᵖRq, (NRᵖRq)C₁₋₃alquilo, tetrazolilo, tetrazolilC₁₋₃alquilo y fenilo, en donde el fenilo también se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados independientemente de C₁₋₃alcoxi, C₁₋₃alquilo y halo; siempre que Q no sea azaindolilo o indolilo; o R¹⁰ es -(CH₂)ₙZ, en donde n es 1 - 3 y Z es un sistema de anillos 6,6 fusionados saturados o insaturados que contiene 1, 2, 3 ó 4 átomos de nitrógeno, en donde el sistema de anillos se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados de C₁₋₆alcoxi, C₁₋₆alcoxicarbonilo, C₁₋₆alcoxicarbonilC₁₋₃alquilo, C₁₋₃alquilo, (C₁₋₆alquil)S(O)₂NHC(O)C₁₋₃alquilo, arilS(O)₂NHC(O)C₁₋₃alquilo, arilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, carboxi, carboxiC₁₋₃alquilo, ciano, C₃₋₆cicloalquilS(O)₂NHC(O)C₁₋₃alquilo, C₃₋₆cicloalquilC₁₋₃alquilS(O)NHC(O)C₁₋₃alquilo, halo, haloC₁₋₃alcoxi, haloC₁₋₃alquilo, heteroarilS(O)₂NHC(O)C₁₋₃alquilo, heteroarilC₁₋₃alquilS(O)₂NHC(O)C₁₋₃alquilo, hidroxi, -NRᵖRq, (NRᵖRq)C₁₋₃alquilo, tetrazolilo, tetrazolilC₁₋₃alquilo y fenilo, en donde el fenilo también se sustituye opcionalmente con 1, 2 ó 3 grupos seleccionados independientemente de C₁₋₃alcoxi, C₁₋₃alquilo y halo; Rᵖ y Rq se seleccionan independientemente de hidrógeno y C₁₋₆ alquilo; R¹³ se selecciona de una cadena lateral de aminoácidos naturales, una cadena lateral de aminoácidos no naturales y -(C(R¹⁷ᵃ)₂)₂-X-R³⁰; -C(R¹⁷ᵃ)₂C(O)N(R¹⁶ᵃ)C(R¹⁷ᵃ)₂-X-R³¹; -C(R¹⁷ᵃ)₂[C(O)N(R¹⁶ᵃ)C(R¹⁷ᵃ)₂]ʷ-X-R³¹; -(C(R¹⁷ᵃ)(R¹⁷)C(O)NR¹⁶ᵃ)ₙ-H; y -(C(R¹⁷ᵃ)(R¹⁷)C(O)NR¹⁶ᵃ)ₘ-C(R¹⁷ᵃ)(R¹⁷)-CO₂H; w es 2 ó 3; n es 1 - 6; m es 0 - 5; X es una cadena de 1 a 172 átomos, en donde los átomos se seleccionan de carbono y oxígeno, y en donde la cadena puede contener 1, 2, 3 ó 4 grupos seleccionados de -NHC(O)NH- y -C(O)NH- incrustados; y en donde la cadena se sustituye opcionalmente con 1 a 6 grupos seleccionados independientemente de -CO₂H, -C(O)NH₂, -CH₂C(O)NH₂ y -(CH₂)CO₂H; X es una cadena de 1 a 172 átomos, en donde los átomos se seleccionan de carbono y oxígeno, y en donde la cadena puede contener 1, 2, 3 ó 4 grupos seleccionados de -NHC(O)NH- y -C(O)NH- incrustados; y en donde la cadena se sustituye opcionalmente con 1 a 6 grupos seleccionados independientemente de -CO₂H, -C(O)NH₂ y -CH₂CO₂H, siempre que X no sea PEG no sustituido; R³⁰ se selecciona de -CO₂H, -C(O)NRʷRˣ y -CH₃, en donde Rʷ y Rˣ se seleccionan independientemente de hidrógeno y C₁₋₆alquilo, siempre que cuando X es carbono, R³⁰ no sea -CH₃; R³¹ es -CO₂H, -C(O)NRʷRˣ, -CH₃, alexa-5-SDP y biotina; cada R¹⁷ᵃ se selecciona independientemente de hidrógeno, C₁₋₆alquilo, -CH₂OH, -CH₂CO₂H, -(CH₂)₂CO₂H; cada R¹⁷ se selecciona independientemente de hidrógeno, -CH₃, (CH₂)ᶻN₃, -(CH₂)ᶻNH₂, -X-R³¹, -(CH₂)ᶻCO₂H, -CH₂OH, CH₂CCºCCH y -(CH₂)ᶻ-triazolil-X-R³⁵, en donde z es 1 - 6, y R³⁵ se selecciona de -CO₂H, -C(O)NRʷRˣ, CH₃, biotina, -2-fluoropiridina, -C(O)-(CH₂)₂-C(O)O-vitamina E, -C(O)O-vitamina E; y el compuesto de fórmula (3) siempre que al menos un R¹⁷ no sea hidrógeno, -CH₃ o -CH₂OH; R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹¹ y R¹² se seleccionan independientemente de una cadena lateral de aminoácidos naturales y una cadena lateral aminoácidos no naturales, o forman un anillo con el grupo R próximo correspondiente, como se describe a continuación; Rᵉ y Rᵏ pueden formar, cada uno, un anillo con el grupo R próximo correspondiente y los átomos a los que están unidos, seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi; Rᵇ es metilo, o Rᵇ y R², junto con los átomos a los que están unidos, forman un anillo seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con 1 a 4 grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi; Rᵈ es hidrógeno o metilo, o Rᵈ y R⁴, junto con los átomos a los que están unidos, pueden formar un anillo seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con 1 a 4 grupos seleccionados independientemente de amino, ciano, metilo, halo, hidroxi y fenilo; Rᵍ es hidrógeno o metilo, o Rᵍ y R⁷, junto con los átomos a los que están unidos, pueden formar un anillo seleccionado de azetidina, pirrolidina, morfolina, piperidina, piperazina y tetrahidrotiazol; en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, bencilo opcionalmente sustituido con un grupo halo, benciloxi, ciano, ciclohexilo, metilo, halo, hidroxi, isoquinoliniloxi opcionalmente sustituido con un grupo metoxi, quinoliniloxi opcionalmente sustituido con un grupo halo, y tetrazolilo; y en donde los anillos de pirrolidina y piperidina están opcionalmente fusionados con un grupo ciclohexilo, fenilo o indol; y RL es metilo, o RL y R¹², junto con los átomos a los que están unidos, forman un anillo seleccionado de azetidina y pirrolidina, en donde cada anillo se sustituye opcionalmente con uno a cuatro grupos seleccionados independientemente de amino, ciano, metilo, halo e hidroxi.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662318417P | 2016-04-05 | 2016-04-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR108186A1 true AR108186A1 (es) | 2018-07-25 |
Family
ID=59960204
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170100881A AR108186A1 (es) | 2016-04-05 | 2017-04-05 | Péptidos macrocíclicos que inhiben las interacciones proteína / proteína, proteína de muerte programada 1 (pd-1) / ligando de pd-1 (pd-l1) y pd-l1 / cd80 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US10358463B2 (es) |
| EP (1) | EP3440097B1 (es) |
| JP (1) | JP7122255B2 (es) |
| KR (1) | KR102548798B1 (es) |
| CN (1) | CN109311943A (es) |
| AR (1) | AR108186A1 (es) |
| AU (1) | AU2017246216A1 (es) |
| BR (1) | BR112018070377A2 (es) |
| CA (1) | CA3020300A1 (es) |
| EA (1) | EA201892243A1 (es) |
| ES (1) | ES2998042T3 (es) |
| IL (1) | IL262126A (es) |
| MA (1) | MA43774A (es) |
| MX (1) | MX2018012039A (es) |
| SG (1) | SG11201808678QA (es) |
| TW (1) | TW201738260A (es) |
| UY (1) | UY37194A (es) |
| WO (1) | WO2017176608A1 (es) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9856292B2 (en) | 2014-11-14 | 2018-01-02 | Bristol-Myers Squibb Company | Immunomodulators |
| US9861680B2 (en) * | 2014-12-18 | 2018-01-09 | Bristol-Myers Squibb Company | Immunomodulators |
| US9944678B2 (en) * | 2014-12-19 | 2018-04-17 | Bristol-Myers Squibb Company | Immunomodulators |
| US10143746B2 (en) | 2016-03-04 | 2018-12-04 | Bristol-Myers Squibb Company | Immunomodulators |
| MX2018014028A (es) | 2016-05-19 | 2019-04-04 | Squibb Bristol Myers Co | Inmunomoduladores de produccion de imagenes de tomografia por emision de positrones (pet). |
| FI3526323T3 (fi) | 2016-10-14 | 2023-06-06 | Prec Biosciences Inc | Hepatiitti B -viruksen genomissa oleville tunnistussekvensseille spesifisiä muokattuja meganukleaaseja |
| WO2018085750A2 (en) * | 2016-11-07 | 2018-05-11 | Bristol-Myers Squibb Company | Immunomodulators |
| US20190336533A1 (en) | 2016-12-28 | 2019-11-07 | Green Cross Lab Cell Corporation | Chimeric antigen receptor and natural killer cells expressing same |
| CN110997698B (zh) * | 2017-06-23 | 2023-12-26 | 百时美施贵宝公司 | 充当pd-1拮抗剂的免疫调节剂 |
| EP3692053A1 (en) | 2017-10-03 | 2020-08-12 | Bristol-Myers Squibb Company | Immunomodulators |
| JP7386796B2 (ja) | 2017-11-14 | 2023-11-27 | グリーン クロス ラボ セル コーポレーション | 抗－ｈｅｒ２抗体又はその抗原結合フラグメント、及びこれを含むキメラ抗原受容体 |
| US11649294B2 (en) | 2017-11-14 | 2023-05-16 | GC Cell Corporation | Anti-HER2 antibody or antigen-binding fragment thereof, and chimeric antigen receptor comprising same |
| WO2019123340A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| AU2018392212B9 (en) | 2017-12-20 | 2021-03-18 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
| US11801244B2 (en) * | 2018-02-02 | 2023-10-31 | Eustralis Pharmaceuticals Limited | Parenteral formulations and uses thereof |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| CA3091142C (en) | 2018-02-26 | 2023-04-11 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| WO2019195181A1 (en) | 2018-04-05 | 2019-10-10 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| US11142750B2 (en) | 2018-04-12 | 2021-10-12 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome |
| EP3781556B1 (en) | 2018-04-19 | 2025-06-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| WO2019211799A1 (en) | 2018-05-03 | 2019-11-07 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide |
| WO2019230919A1 (ja) | 2018-05-31 | 2019-12-05 | 小野薬品工業株式会社 | 免疫チェックポイント阻害薬の有効性判定バイオマーカー |
| EP3810109B1 (en) | 2018-05-31 | 2024-08-07 | Peloton Therapeutics, Inc. | Compounds and compositions for inhibiting cd73 |
| PL3820572T3 (pl) | 2018-07-13 | 2024-02-26 | Gilead Sciences, Inc. | Inhibitory pd-1/pd-l1 |
| WO2020028097A1 (en) | 2018-08-01 | 2020-02-06 | Gilead Sciences, Inc. | Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid |
| TWI855000B (zh) | 2018-10-11 | 2024-09-11 | 日商小野藥品工業股份有限公司 | Ｓｔｉｎｇ促效化合物 |
| CA3117199C (en) | 2018-10-24 | 2024-03-19 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| CN117105933A (zh) | 2018-10-31 | 2023-11-24 | 吉利德科学公司 | 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物 |
| CR20210215A (es) | 2018-10-31 | 2021-06-17 | Gilead Sciences Inc | Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1 |
| KR102808642B1 (ko) | 2019-03-07 | 2025-05-14 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | 3'3'-사이클릭 다이뉴클레오티드 및 이의 프로드럭 |
| CA3129022C (en) | 2019-03-07 | 2023-08-01 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| CN113891748A (zh) | 2019-03-28 | 2022-01-04 | 百时美施贵宝公司 | 治疗肿瘤的方法 |
| KR20210146348A (ko) | 2019-03-28 | 2021-12-03 | 브리스톨-마이어스 스큅 컴퍼니 | 종양을 치료하는 방법 |
| TWI751516B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| US20220251141A1 (en) * | 2019-05-21 | 2022-08-11 | Bristol-Myers Squibb Company | Immunomodulators |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| KR20220016155A (ko) | 2019-05-30 | 2022-02-08 | 브리스톨-마이어스 스큅 컴퍼니 | 면역-종양학 (i-o) 요법에 적합한 대상체를 확인하는 방법 |
| US20220233691A1 (en) | 2019-05-30 | 2022-07-28 | Bristol-Myers Squibb Company | Cell localization signature and combination therapy |
| WO2020243563A1 (en) | 2019-05-30 | 2020-12-03 | Bristol-Myers Squibb Company | Multi-tumor gene signatures for suitability to immuno-oncology therapy |
| PH12022550244A1 (en) | 2019-08-05 | 2022-12-12 | Nat Cancer Ct | Biomarkers for determining the efficacy of immune checkpoint inhibitors |
| EP4017476A1 (en) | 2019-08-19 | 2022-06-29 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| CA3153777A1 (en) | 2019-09-22 | 2021-03-25 | Bristol-Myers Squibb Company | Quantitative spatial profiling for lag-3 antagonist therapy |
| SI4037708T1 (sl) | 2019-09-30 | 2025-01-31 | Gilead Sciences, Inc. | Cepiva proti hbv in postopki zdravljenja hbv |
| BR112022008191A2 (pt) | 2019-11-08 | 2022-07-12 | Bristol Myers Squibb Co | Terapia com antagonista de lag-3 para melanoma |
| US20230022400A1 (en) * | 2019-11-19 | 2023-01-26 | Bristol-Myers Squibb Company | Immunomodulators |
| DK4069729T3 (da) | 2019-12-06 | 2025-04-07 | Prec Biosciences Inc | Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet |
| JP7550864B2 (ja) * | 2020-01-06 | 2024-09-13 | ブリストル－マイヤーズ スクイブ カンパニー | 癌および感染症を治療するためのｐｄ－ｌ１阻害剤および免疫調節剤としての大環状ペプチド |
| KR20220122752A (ko) | 2020-01-06 | 2022-09-02 | 브리스톨-마이어스 스큅 컴퍼니 | 면역조정제 |
| EP4121437A1 (en) | 2020-03-20 | 2023-01-25 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
| KR20220161407A (ko) | 2020-03-30 | 2022-12-06 | 브리스톨-마이어스 스큅 컴퍼니 | 면역조정제 |
| JPWO2021206158A1 (es) | 2020-04-10 | 2021-10-14 | ||
| EP4134134A4 (en) | 2020-04-10 | 2023-12-27 | ONO Pharmaceutical Co., Ltd. | STING AGONISTIC COMPOUND |
| CN113754736A (zh) * | 2020-06-02 | 2021-12-07 | 南京礼威生物医药有限公司 | 含酰肼结构的pd-l1环肽抑制剂 |
| CN111961117B (zh) * | 2020-08-19 | 2022-03-11 | 中山大学 | 一种环肽化合物及其应用 |
| KR20230058442A (ko) | 2020-08-28 | 2023-05-03 | 브리스톨-마이어스 스큅 컴퍼니 | 간세포성 암종에 대한 lag-3 길항제 요법 |
| EP4204453A1 (en) | 2020-08-31 | 2023-07-05 | Bristol-Myers Squibb Company | Cell localization signature and immunotherapy |
| IL301907A (en) | 2020-10-23 | 2023-06-01 | Bristol Myers Squibb Co | Lag-3 antagonist therapy for lung cancer |
| WO2022120179A1 (en) | 2020-12-03 | 2022-06-09 | Bristol-Myers Squibb Company | Multi-tumor gene signatures and uses thereof |
| EP4313127A1 (en) | 2021-03-29 | 2024-02-07 | Juno Therapeutics, Inc. | Methods for dosing and treatment with a combination of a checkpoint inhibitor therapy and a car t cell therapy |
| US20240269142A1 (en) | 2021-05-13 | 2024-08-15 | Gilead Sciences, Inc. | COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS |
| EP4352077A1 (en) * | 2021-06-09 | 2024-04-17 | Bristol-Myers Squibb Company | Cyclic peptide immunomodulators |
| CA3222269A1 (en) | 2021-06-11 | 2022-12-15 | Gilead Sciences, Inc. | Combination mcl-1 inhibitors with anti-cancer agents |
| KR20240019330A (ko) | 2021-06-11 | 2024-02-14 | 길리애드 사이언시즈, 인코포레이티드 | Mcl-1 저해제와 항체 약물 접합체의 조합 |
| EP4359411A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| JP7686086B2 (ja) | 2021-06-23 | 2025-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリエルコール（ｄｉａｃｙｌｇｌｙｅｒｃｏｌ）キナーゼ調節化合物 |
| CN117396478A (zh) | 2021-06-23 | 2024-01-12 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| WO2022271684A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| IL309227A (en) | 2021-10-29 | 2024-02-01 | Bristol Myers Squibb Co | LAG-3 antagonist therapy for hematological cancer |
| US20250215076A1 (en) | 2022-01-26 | 2025-07-03 | Bristol-Myers Squibb Company | Combination therapy for hepatocellular carcinoma |
| CN119731651A (zh) | 2022-04-08 | 2025-03-28 | 百时美施贵宝公司 | 三级淋巴结构的机器学习标识、分类和量化 |
| EP4578876A1 (en) | 2022-08-23 | 2025-07-02 | ONO Pharmaceutical Co., Ltd. | Bispecific antibody |
| KR20250123912A (ko) | 2022-12-21 | 2025-08-18 | 브리스톨-마이어스 스큅 컴퍼니 | 폐암에 대한 병용 요법 |
| CN121194985A (zh) * | 2023-02-03 | 2025-12-23 | 默沙东有限责任公司 | 用于抑制tnf受体1活性的环肽 |
| WO2024196952A1 (en) | 2023-03-20 | 2024-09-26 | Bristol-Myers Squibb Company | Tumor subtype assessment for cancer therapy |
| WO2025061971A1 (en) | 2023-09-20 | 2025-03-27 | Trimt Gmbh | Functionalized peptides for in-vivo addressing of pd-l1 expression |
| WO2025166198A1 (en) * | 2024-02-01 | 2025-08-07 | Merck Sharp & Dohme Llc | Methods of using cyclic peptides that bind to tnfr1 |
| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240243A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with bulevirtide and an inhibitory nucleic acid targeting hepatitis b virus |
| WO2025240244A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025245489A1 (en) | 2024-05-24 | 2025-11-27 | Bristol-Myers Squibb Company | Treatment of tumors in subjects having fgl-1 positive samples |
Family Cites Families (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4475196A (en) | 1981-03-06 | 1984-10-02 | Zor Clair G | Instrument for locating faults in aircraft passenger reading light and attendant call control system |
| US4447233A (en) | 1981-04-10 | 1984-05-08 | Parker-Hannifin Corporation | Medication infusion pump |
| US4439196A (en) | 1982-03-18 | 1984-03-27 | Merck & Co., Inc. | Osmotic drug delivery system |
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US4447224A (en) | 1982-09-20 | 1984-05-08 | Infusaid Corporation | Variable flow implantable infusion apparatus |
| US4487603A (en) | 1982-11-26 | 1984-12-11 | Cordis Corporation | Implantable microinfusion pump system |
| US4486194A (en) | 1983-06-08 | 1984-12-04 | James Ferrara | Therapeutic device for administering medicaments through the skin |
| US4596556A (en) | 1985-03-25 | 1986-06-24 | Bioject, Inc. | Hypodermic injection apparatus |
| US5374548A (en) | 1986-05-02 | 1994-12-20 | Genentech, Inc. | Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor |
| MX9203291A (es) | 1985-06-26 | 1992-08-01 | Liposome Co Inc | Metodo para acoplamiento de liposomas. |
| US4790824A (en) | 1987-06-19 | 1988-12-13 | Bioject, Inc. | Non-invasive hypodermic injection device |
| US4941880A (en) | 1987-06-19 | 1990-07-17 | Bioject, Inc. | Pre-filled ampule and non-invasive hypodermic injection device assembly |
| US5108921A (en) | 1989-04-03 | 1992-04-28 | Purdue Research Foundation | Method for enhanced transmembrane transport of exogenous molecules |
| US5064413A (en) | 1989-11-09 | 1991-11-12 | Bioject, Inc. | Needleless hypodermic injection device |
| US5312335A (en) | 1989-11-09 | 1994-05-17 | Bioject Inc. | Needleless hypodermic injection device |
| US5383851A (en) | 1992-07-24 | 1995-01-24 | Bioject Inc. | Needleless hypodermic injection device |
| US6410690B1 (en) | 1995-06-07 | 2002-06-25 | Medarex, Inc. | Therapeutic compounds comprised of anti-Fc receptor antibodies |
| US5869451A (en) | 1995-06-07 | 1999-02-09 | Glaxo Group Limited | Peptides and compounds that bind to a receptor |
| US5811097A (en) | 1995-07-25 | 1998-09-22 | The Regents Of The University Of California | Blockade of T lymphocyte down-regulation associated with CTLA-4 signaling |
| US5922845A (en) | 1996-07-11 | 1999-07-13 | Medarex, Inc. | Therapeutic multispecific compounds comprised of anti-Fcα receptor antibodies |
| US6277818B1 (en) | 1998-10-29 | 2001-08-21 | Angstrom Pharmaceuticals, Inc. | Cyclic peptide ligands that target urokinase plasminogen activator receptor |
| CN1423655A (zh) * | 1999-12-15 | 2003-06-11 | 卡比斯特制药公司 | 作为抗菌剂的新颖的脂肽 |
| JP4511943B2 (ja) | 2002-12-23 | 2010-07-28 | ワイス エルエルシー | Ｐｄ−１に対する抗体およびその使用 |
| EP2439273B1 (en) | 2005-05-09 | 2019-02-27 | Ono Pharmaceutical Co., Ltd. | Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics |
| HRP20151102T1 (xx) | 2005-07-01 | 2015-11-20 | E. R. Squibb & Sons, L.L.C. | Humana monoklonska antitijela za ligand programirane smrti 1 (pd-l1) |
| EP3012265B1 (en) | 2007-03-26 | 2017-06-28 | The University of Tokyo | Process for synthesizing cyclic peptide compound |
| US8168757B2 (en) | 2008-03-12 | 2012-05-01 | Merck Sharp & Dohme Corp. | PD-1 binding proteins |
| EA201170375A1 (ru) | 2008-08-25 | 2012-03-30 | Эмплиммьюн, Инк. | Антагонисты pd-1 и способы их применения |
| US8907053B2 (en) | 2010-06-25 | 2014-12-09 | Aurigene Discovery Technologies Limited | Immunosuppression modulating compounds |
| JP5818237B2 (ja) | 2010-09-09 | 2015-11-18 | 国立大学法人 東京大学 | Ｎ−メチルアミノ酸およびその他の特殊アミノ酸を含む特殊ペプチド化合物ライブラリーの翻訳構築と活性種探索法 |
| US10195578B2 (en) | 2010-12-03 | 2019-02-05 | The University Of Tokyo | Peptide library production method, peptide library, and screening method |
| CN103732238A (zh) | 2011-06-08 | 2014-04-16 | 奥瑞基尼探索技术有限公司 | 用于免疫调节的治疗性化合物 |
| US9422339B2 (en) | 2012-03-29 | 2016-08-23 | Aurigene Discovery Technologies Limited | Immunomodulating cyclic compounds |
| CN104603145B (zh) | 2012-06-06 | 2018-05-18 | 波利弗尔股份公司 | β-发夹肽模拟物 |
| JP2013253842A (ja) | 2012-06-06 | 2013-12-19 | Univ Of Tokyo | ｐＨ依存的に標的分子に結合するペプチドのスクリーニング方法 |
| 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 |
| KR20230070054A (ko) | 2013-03-15 | 2023-05-19 | 제넨테크, 인크. | Pd-1 및 pd-l1 관련 상태를 치료하기 위한 바이오마커 및 방법 |
| EA201891818A3 (ru) | 2013-09-06 | 2019-03-29 | Ауриген Дискавери Текнолоджиз Лимитед | Способ получения соединений, используемых при получении циклических пептидомиметических соединений |
| WO2015044900A1 (en) | 2013-09-27 | 2015-04-02 | Aurigene Discovery Technologies Limited | Therapeutic immunomodulating compounds |
| WO2015131100A1 (en) | 2014-02-28 | 2015-09-03 | The Scripps Research Institute | Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids |
| EA034496B1 (ru) * | 2014-09-11 | 2020-02-13 | Бристол-Майерс Сквибб Компани | Макроциклические ингибиторы белок/белковых взаимодействий pd-1/pd-l1 и cd80(b7-1)/pd-l1 |
| US9732119B2 (en) * | 2014-10-10 | 2017-08-15 | Bristol-Myers Squibb Company | Immunomodulators |
| US9856292B2 (en) | 2014-11-14 | 2018-01-02 | Bristol-Myers Squibb Company | Immunomodulators |
| US9861680B2 (en) | 2014-12-18 | 2018-01-09 | Bristol-Myers Squibb Company | Immunomodulators |
| US9944678B2 (en) * | 2014-12-19 | 2018-04-17 | Bristol-Myers Squibb Company | Immunomodulators |
| US20160222060A1 (en) | 2015-02-04 | 2016-08-04 | Bristol-Myers Squibb Company | Immunomodulators |
| US9809625B2 (en) | 2015-03-18 | 2017-11-07 | Bristol-Myers Squibb Company | Immunomodulators |
| US10143746B2 (en) | 2016-03-04 | 2018-12-04 | Bristol-Myers Squibb Company | Immunomodulators |
| MX2018014028A (es) | 2016-05-19 | 2019-04-04 | Squibb Bristol Myers Co | Inmunomoduladores de produccion de imagenes de tomografia por emision de positrones (pet). |
-
2017
- 2017-03-31 US US15/475,227 patent/US10358463B2/en active Active
- 2017-04-03 AU AU2017246216A patent/AU2017246216A1/en not_active Abandoned
- 2017-04-03 SG SG11201808678QA patent/SG11201808678QA/en unknown
- 2017-04-03 JP JP2018552242A patent/JP7122255B2/ja active Active
- 2017-04-03 MX MX2018012039A patent/MX2018012039A/es unknown
- 2017-04-03 WO PCT/US2017/025677 patent/WO2017176608A1/en not_active Ceased
- 2017-04-03 MA MA043774A patent/MA43774A/fr unknown
- 2017-04-03 KR KR1020187031601A patent/KR102548798B1/ko active Active
- 2017-04-03 EA EA201892243A patent/EA201892243A1/ru unknown
- 2017-04-03 EP EP17718218.5A patent/EP3440097B1/en active Active
- 2017-04-03 CN CN201780033784.XA patent/CN109311943A/zh active Pending
- 2017-04-03 BR BR112018070377A patent/BR112018070377A2/pt not_active Application Discontinuation
- 2017-04-03 CA CA3020300A patent/CA3020300A1/en not_active Abandoned
- 2017-04-03 ES ES17718218T patent/ES2998042T3/es active Active
- 2017-04-05 UY UY0001037194A patent/UY37194A/es unknown
- 2017-04-05 AR ARP170100881A patent/AR108186A1/es unknown
- 2017-04-05 TW TW106111442A patent/TW201738260A/zh unknown
-
2018
- 2018-10-04 IL IL262126A patent/IL262126A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017176608A1 (en) | 2017-10-12 |
| EP3440097B1 (en) | 2024-10-23 |
| IL262126A (en) | 2018-11-29 |
| US10358463B2 (en) | 2019-07-23 |
| UY37194A (es) | 2017-10-31 |
| JP7122255B2 (ja) | 2022-08-19 |
| TW201738260A (zh) | 2017-11-01 |
| MA43774A (fr) | 2018-11-28 |
| EA201892243A1 (ru) | 2019-03-29 |
| EP3440097A1 (en) | 2019-02-13 |
| KR102548798B1 (ko) | 2023-06-27 |
| SG11201808678QA (en) | 2018-11-29 |
| ES2998042T3 (en) | 2025-02-18 |
| CN109311943A (zh) | 2019-02-05 |
| JP2019513734A (ja) | 2019-05-30 |
| KR20180132775A (ko) | 2018-12-12 |
| MX2018012039A (es) | 2019-01-14 |
| US20170283463A1 (en) | 2017-10-05 |
| BR112018070377A2 (pt) | 2019-02-05 |
| CA3020300A1 (en) | 2017-10-12 |
| AU2017246216A1 (en) | 2018-11-22 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR108186A1 (es) | Péptidos macrocíclicos que inhiben las interacciones proteína / proteína, proteína de muerte programada 1 (pd-1) / ligando de pd-1 (pd-l1) y pd-l1 / cd80 | |
| AR107802A1 (es) | Inmunomoduladores | |
| AR103182A1 (es) | Inmunomoduladores | |
| AR113299A1 (es) | Compuestos de isoindolina | |
| AR103969A1 (es) | Inmunomoduladores | |
| AR096461A1 (es) | Anticuerpos conjugados de fármacos | |
| AR116666A1 (es) | Compuestos heterocíclicos | |
| AR110139A1 (es) | COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV | |
| NI201100197A (es) | Espironucleósidos uracílicos oxetánicos | |
| AR115871A1 (es) | MÉTODO PARA CONTROLAR EL HONGO DE LA ROYA DE LA SOJA QUE TIENE RESISTENCIA AL INHIBIDOR DE SITIO Qₒ | |
| AR079164A1 (es) | Derivados heterociclicos de indol, composiciones farmaceuticas que los comprenden y uso de los mismos para la profilaxis o tratamiento de enfermedades alergicas, inflamatorias y/o autoinmunes. | |
| MX385158B (es) | Derivados indol para uso en medicina. | |
| AR087841A1 (es) | Derivados de tetrahidrotriazolopirimidina | |
| AR110498A1 (es) | DERIVADOS DE ISOXAZOLIL ÉTER COMO MODULADORES ALOSTÉRICOS POSITIVOS (PAM) DE RECEPTORES DE GABAA a5 | |
| AR100418A1 (es) | Compuestos y composiciones para inducir condrogénesis | |
| AR116114A1 (es) | Amidas heterocíclicas de entre 5 y 7 miembros como inhibidores de jak | |
| AR119910A1 (es) | DERIVADOS DE 4,4a,5,7,8,8a-HEXAHIDROPIRIDO[4,3-b][1,4]OXAZIN-3-ONA COMO INHIBIDORES DE MAGL | |
| AR099914A1 (es) | Derivados de indol y de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen | |
| AR111271A1 (es) | Inhibidores dobles de magl y faah | |
| AR127404A1 (es) | Inhibidores de la metionina adenosiltransferasa 2a (mat2a) y usos de los mismos | |
| AR088246A1 (es) | Derivados de etinilo | |
| AR041883A1 (es) | Compuestos de piridopirimidinona, procedimiento para su preparacion y composiciones farmaceuticas que los contienen | |
| AR109487A1 (es) | Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas bet | |
| AR096041A1 (es) | Derivados de ácido carboxílico alquilo sustituidos como agonistas rpg | |
| AR116400A1 (es) | Compuesto de imidazopiridinona |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |