[go: up one dir, main page]

AR048927A1 - Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa - Google Patents

Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa

Info

Publication number
AR048927A1
AR048927A1 ARP050101365A ARP050101365A AR048927A1 AR 048927 A1 AR048927 A1 AR 048927A1 AR P050101365 A ARP050101365 A AR P050101365A AR P050101365 A ARP050101365 A AR P050101365A AR 048927 A1 AR048927 A1 AR 048927A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
aryl
het
substituted
Prior art date
Application number
ARP050101365A
Other languages
English (en)
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34962601&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR048927(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR048927A1 publication Critical patent/AR048927A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos que inhiben el enlace de la proteína S mac al inhibidor de Proteínas de Apoptosis (IAP) de la formula (1) y utilizables en el tratamiento de enfermedades proliferativas incluyendo cáncer. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en donde: R1 es H, alquilo C1-4; alquenilo C1-4; alquinilo C1-4, o cicloalquilo C3-10, los cuales están insustituidos o sustituidos; R2 es H, alquilo C1-4, alquenilo C1-4, alquinilo C1-4, o cicloalquilo C3-10, los cuales están insustituidos o sustituidos; R3 es H; -CF3; -C2F5; alquilo C1-4; alquenilo C1-4; alquinilo C1-4; -CH2-Z; o R2 y R3, junto con el N, forman un anillo het; Z es H; -OH; F; Cl; -CH3; -CH2Cl; -CH2F, o -CH2OH; R4 es alquilo recto o ramificado C1-16, alquenilo C1-16; alquinilo C1-16; o cicloalquilo C3-10; -(CH2)1-6-Z1; -(CH2)0-6-arilo; y -(CH2)0-6-het; en donde alquilo, cicloalquilo, y fenilo están insustituidos o sustituidos; Z1 es -N(R8)-C(O)-alquilo C1-10, -N(R8)-C(O)-(CH2)1-6-cicloalquilo C3- 7; -N(R8)-C(O)-(CH2)0-6-fenilo; -N(R8)-C(O)-(CH2)1-6-het; -C(O)-N(R9)(R10); -C(O)-O-alquilo C1-10; -C(O)-O-(CH2)1-6-cicloalquilo C3-7; -C(O)-O-(CH2)0-6-fenilo; -C(O)-O-(CH2)1-6-het; -O-C(O)-alquilo C1-10; -O-C(O)-(CH2)1-6-cicloalquilo C3-7; -O-C(O)- (CH2)0-6-fenilo; -O-C(O)-(CH2)1-6-het; en donde alquilo, cicloalquilo, y fenilo están insustituidos o sustituidos; het es un anillo heterocíclico de 5 a 7 miembros que contiene de 1 a 4 heteroátomos seleccionados a partir de N, O, y S, o un sistema de anillo fusionado de 8 a 12 miembros, incluyendo cuando menos un anillo heterocíclico de 5 a 7 miembros que contiene 1, 2, o 3 heteroátomos seleccionados a partir de N, O y S, cuyo anillo heterocíclico o sistema de anillo fusionado está insustituido o sustituido sobre un átomo de C o N; R8 es H; -CH3; -CF3; -CH2OH, o -CH2Cl; R9 y R10 son cada uno independientemente H; alquilo C1-4, cicloalquilo C3-7, -(CH2)1-6-cicloalquilo C3-7; -(CH2)0-6-fenilo; en donde alquilo, cicloalquilo, y fenilo están insustituidos o sustituidos, o R9 y R10, junto con el N, forman het; R5 es H; alquilo C1-10; arilo; fenilo; cicloalquilo C3-7, -(CH2)0-6-fenilo; -(CH2)0-4-CH-((CH2)1-4-fenilo)2; -(CH2)0-6-CH (fenilo)2; -indanilo; -C(O)-alquilo C1-10; - C(O)-(CH2)1-6-cicloalquilo C3-7; -C(O)-(CH2)0-6-fenilo; -(CH2)0-6-C(O)-fenilo; -(CH2)0-6-het; -C(O)-(CH2)1-6-het; o R5 es un residuo de un aminoácido, en donde los sustituyentes de alquilo, cicloalquilo, fenilo, y arilo están insustituidos o sustituidos; U es como se muestra en la estructura (2) en donde: n = 0 a 5; X es -CH o N; Ra y Rb son independientemente un átomo de O, S, o N, o alquilo C0-8, en donde uno o más de los átomos de C en la cadena de alquilo puede ser reemplazado por un heteroátomo seleccionado a partir de O, S, o N, y en donde el alquilo puede estar insustituido o sustituido; Rd se selecciona a partir de: (a) -Re-Q-(Rf)p(Rg)q; o (b) Ar1-D-Ar2; Rc es H, o Rc y Rd pueden formar juntos un cicloalquilo o het; en donde, si Rd y Rc forman un cicloalquilo o het, R5 se une al anillo formado en un átomo de C o N; p y q son independientemente 0 o 1; Re es alquilo C1-8 o alquilideno, y Re puede estar insustituido o sustituido; Q es N, O, S, S(O), o S(O)2; Ar1 y Ar2 son arilo sustituido o insustituido, o het; Rf y Rg son cada uno independientemente H; alquilo C1-10; alquilo C1-10-arilo; -OH; -O-alquilo C1-10; -(CH2)0-6-cicloalquilo C3-7; -O-(CH2)0-6-arilo; fenilo; arilo; fenil-fenilo; -(CH2)1-6-het; -O- (CH2)1-6-het; -OR11; -C(O)-R11; -C(O)-N(R11)(R12); -N(R11)(R12); -S-R11; -S(O)-R11; -S(O)2R11; -S(O)2-NR11R12; -NR11-S(O)2-R12; S-alquilo C1-10; aril-alquilo C1-4, het-alquilo C1-4, en donde alquilo, cicloalquilo, het, y arilo están insustituidos o sustituidos; -SO2-alquilo C1-2; -SO2-alquilo C1-2-fenilo; -O-alquilo C1-4; o Rg y Rf forman un anillo seleccionado a partir de het o arilo; D es -CO-; -C(O)-alquileno C1-7 o arileno; -CF2-; -O-; -S(O)r, en donde r es de 0 a 2; 1,3-dioxolano; o alquilo C1-7-OH; en donde alquilo, alquileno, o arileno pueden estar insustituidos o sustituidos con uno o más halogenos, OH, -O-alquilo C1-6, -S-alquilo C1-6, o -CF3; o D es -N(Rh), en donde Rh es H; alquilo C1-7 (insustituido o sustituido); arilo; -O-(cicloalquilo C1-7) (insustituido o sustituido); C(O)-alquilo C1-10; C(O)-alquilo C0-10-arilo; C-O-alquilo C1-10; C-O-alquilo C0-10-arilo, o SO2-alquilo C1-10; SO2-(alquilo C0-10-arilo); R6, R7, R'6 y R'7 son cada uno independientemente H; - alquilo C1-10; -alcoxilo C1-10; aril-alcoxilo C1-10; -OH; -O-alquilo C1-10; -(CH2)0-6-cicloalquilo C3-7, -O-(CH2)0-6-arilo; fenilo; -(CH2)1-6-het; -O-(CH2)1-6-het; -OR11; -C(O)R11; -C(O)-N(R11)(R12); -N(R11)(R12); -S-R11; -S(O)-R11; -S(O)2-R11; - S(O)2-NR11R12; -NR11-S(O)2-R12; en donde alquilo, cicloalquilo, y arilo están insustituidos o sustituidos; y R6, R7, R'6, y R'7 se pueden unir para formar un sistema de anillo; R11 y R12 son independientemente H; alquilo C1-10; -(CH2)0-6- cicloalquilo C3-7; -(CH2)0-6-(CH0-1(arilo)1-2; -C(O)-alquilo C1-10; -C(O)-(CH2)1-6-cicloalquilo C3-7; -C(O)-O-(CH2)0-6-arilo; -C(O)-(CH2)0-6-O-fluorenilo; -C(O)-NH-(CH2)0-6-arilo; -C(O)-(CH2)0-6-arilo; -C(O)-(CH2)1-6-het; -C(S)-alquilo C1-10; -C(S)- (CH2)1-6-cicloalquilo C3-7; -C(S)-O-(CH2)0-6-arilo; -C(S)-(CH2)0-6-O-fluorenilo; -C(S)-NH-(CH2)0-6-arilo; -C(S)-(CH2)0-6-arilo; -C(S)-(CH2)1-6-het; en donde alquilo, cicloalquilo, y arilo están insustituidos o sustituidos; o R11 y R12 son un sustituyente que facilita el transporte de la molécula a través de una membrana celular; o R11 y R12, junto con el átomo de N, forman het; en donde los sustituyentes de alquilo de R11 y R12 pueden estar insustituidos o sustituidos por uno o más sustituyentes seleccionados a partir de alquilo C1-10, halogeno, OH, -O-alquilo C1-6, -S-alquilo C1-6, o -CF3; los sustituyentes de cicloalquilo sustituido de R11 y R12 están sustituidos por uno o más sustituyentes seleccionados a partir de alqueno C1-10; alquilo C1-6; halogeno; OH; -O-alquilo C1-6; -S-alquilo C1-6, o -CF3; y fenilo o arilo sustituidos de R11 y R12 están sustituidos por uno o más sustituyentes seleccionados a partir de halogeno; hidroxilo; alquilo C1-4; alcoxilo C1-4; nitro; - CN; -O-C(O)-alquilo C1-4, y -C(O)-O-arilo C1-4; o sales farmacéuticamente aceptables del mismo.
ARP050101365A 2004-04-07 2005-04-06 Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa AR048927A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US56018604P 2004-04-07 2004-04-07

Publications (1)

Publication Number Publication Date
AR048927A1 true AR048927A1 (es) 2006-06-14

Family

ID=34962601

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101365A AR048927A1 (es) 2004-04-07 2005-04-06 Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa

Country Status (31)

Country Link
US (4) US20080242658A1 (es)
EP (3) EP2065368A1 (es)
JP (3) JP4691549B2 (es)
KR (2) KR100892185B1 (es)
CN (1) CN1964970B (es)
AR (1) AR048927A1 (es)
AU (1) AU2005231956B2 (es)
BR (1) BRPI0509721A (es)
CA (1) CA2560162C (es)
CY (1) CY1113511T1 (es)
DK (1) DK2253614T3 (es)
EC (1) ECSP066893A (es)
ES (2) ES2394441T3 (es)
HR (1) HRP20121023T1 (es)
IL (1) IL178104A (es)
MA (1) MA28630B1 (es)
ME (1) ME02125B (es)
MY (1) MY165401A (es)
NO (1) NO20065114L (es)
NZ (1) NZ549925A (es)
PE (2) PE20060166A1 (es)
PL (1) PL2253614T3 (es)
PT (1) PT2253614E (es)
RS (1) RS52545B (es)
RU (1) RU2425838C2 (es)
SG (1) SG152225A1 (es)
SI (1) SI2253614T1 (es)
TN (1) TNSN06323A1 (es)
TW (1) TWI417092B (es)
WO (1) WO2005097791A1 (es)
ZA (1) ZA200607696B (es)

Families Citing this family (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5122275B2 (ja) 2004-03-23 2013-01-16 ジェネンテック， インコーポレイテッド Ｉａｐのアザビシクロ−オクタンインヒビター
BRPI0509721A (pt) 2004-04-07 2007-09-25 Novartis Ag inibidores de iap
NZ588799A (en) 2004-07-02 2012-06-29 Genentech Inc Inhibitors of iap
WO2006020060A2 (en) * 2004-07-15 2006-02-23 Tetralogic Pharmaceuticals Corporation Iap binding compounds
DE602005022936D1 (de) 2004-12-20 2010-09-23 Genentech Inc Pyrrolidine als inhibitoren von iap
CA2598838A1 (en) * 2005-02-23 2006-08-31 Prexa Pharmaceuticals, Inc. Multimediator 5-ht6 receptor antagonists, and uses related thereto
WO2006091972A2 (en) 2005-02-25 2006-08-31 Tetralogic Pharmaceuticals Dimeric iap inhibitors
WO2006107964A2 (en) * 2005-04-06 2006-10-12 Novartis Ag Processes to prepare 6-phenethyl-octahydro-pyrrolo [2 , 3-c] pyridine and related compounds
CA2607940C (en) 2005-05-18 2009-12-15 Aegera Therapeutics Inc. Bir domain binding compounds
US20100256046A1 (en) * 2009-04-03 2010-10-07 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
AU2006279929A1 (en) * 2005-08-09 2007-02-22 Tetralogic Pharmaceuticals Corporation Treatment of proliferative disorders
AU2006308453B9 (en) 2005-10-25 2011-12-01 Pharmascience Inc. IAP BIR domain binding compounds
EP1973899A4 (en) * 2005-12-19 2010-10-20 Genentech Inc HEMMER OF IAP
EP1965865B1 (en) 2005-12-20 2018-05-16 Novartis AG Combination of an iap-inhibitor and a taxane
TWI543988B (zh) 2006-03-16 2016-08-01 科學製藥股份有限公司 結合於細胞凋亡抑制蛋白（ｉａｐ）之桿狀病毒ｉａｐ重複序列（ｂｉｒ）區域之化合物
AU2007234382B2 (en) * 2006-04-05 2011-06-09 Novartis Ag Combinations comprising BCR-ABL/C-KIT/PDGF-R TK inhibitors for treating cancer
US20090099103A1 (en) * 2006-04-05 2009-04-16 Novartis Ag. Combinations of therapeutic agents for treating cancer
US8168383B2 (en) 2006-04-14 2012-05-01 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
EP2450437B1 (en) 2006-04-14 2017-05-17 Cell Signaling Technology, Inc. Gene defects and mutant ALK kinase in human solid tumors
AU2007250443B2 (en) * 2006-05-16 2013-06-13 Pharmascience Inc. IAP BIR domain binding compounds
MX2008014502A (es) * 2006-05-16 2008-11-27 Aegera Therapeutics Inc Compuestos de union a dominio de repeticion de proteinas inhibidoras de apoptosis baculovirales de las proteinas inhibidoras de apoptosis.
US20100144650A1 (en) * 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
US20100113326A1 (en) * 2006-07-24 2010-05-06 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
AR063943A1 (es) 2006-07-24 2009-03-04 Tetralogic Pharmaceuticals Cor Dipeptidos antagonistas de iap, una composicion farmaceutica que los comprende y el uso de los mismos para el tratamiento del cancer.
WO2008014236A1 (en) * 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
WO2008014252A2 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Iap inhibitors
PE20110218A1 (es) * 2006-08-02 2011-04-01 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS
CN101595121A (zh) * 2006-10-12 2009-12-02 诺瓦提斯公司 作为iap抑制剂的吡咯烷衍生物
US20100316573A1 (en) * 2006-10-19 2010-12-16 Larry Alexander Gaither Organic Compounds
AU2007325280B2 (en) * 2006-11-28 2011-03-10 Dana-Farber Cancer Institute, Inc. Combination of IAP inhibitors and FLT3 inhibitors
EP2089027A1 (en) * 2006-11-28 2009-08-19 Novartis AG Use of iap inhibitors for the treatment of acute myeloid leukemia
CA2671607A1 (en) * 2006-12-19 2008-07-03 Genentech, Inc. Imidazopyridine inhibitors of iap
WO2008109057A1 (en) * 2007-03-02 2008-09-12 Dana-Farber Cancer Institute, Inc. Organic compounds and their uses
CA2684169C (en) 2007-04-12 2012-06-19 Joyant Pharmaceuticals, Inc. Smac mimetic dimers and trimers useful as anti-cancer agents
AR066348A1 (es) * 2007-04-30 2009-08-12 Genentech Inc Inhibidores de las iap
US20110008802A1 (en) * 2007-05-07 2011-01-13 Tetralogic Pharmaceuticals Corp. TNFalpha GENE EXPRESSION AS A BIOMARKER OF SENSITIVITY TO ANTAGONISTS OF INHIBITOR OF APOPTOSIS PROTEINS
US20100203012A1 (en) * 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
EP2240506B1 (en) * 2008-01-11 2012-12-26 Genentech, Inc. Inhibitors of iap
KR20100119768A (ko) * 2008-01-24 2010-11-10 테트랄로직 파마슈티칼스 코포레이션 아이에이피 억제제
US20110117081A1 (en) * 2008-05-05 2011-05-19 Aegera Therapeutics, Inc. Functionalized pyrrolidines and use thereof as iap inhibitors
ES2882855T3 (es) * 2008-05-16 2021-12-02 Dana Farber Cancer Inst Inc Inmunomodulación por inhibidores de IAP
EP2310402A1 (en) * 2008-06-27 2011-04-20 Aegera Therapeutics Inc. Bridged secondary amines and use thereof as iap bir domain binding compounds
CN102171209A (zh) 2008-08-02 2011-08-31 健泰科生物技术公司 Iap抑制剂
AU2009282978A1 (en) * 2008-08-16 2010-02-25 Genentech, Inc. Azaindole inhibitors of IAP
WO2010033531A1 (en) * 2008-09-17 2010-03-25 Tetralogic Pharmaceuticals Corp. Iap inhibitors
US8841067B2 (en) 2009-01-09 2014-09-23 Dana-Farber Cancer Institute, Inc. NOL3 is a predictor of patient outcome
EA201171415A1 (ru) * 2009-05-28 2013-01-30 Тетралоджик Фармасьютикалз Корп. Ингибиторы белков семейства iap
AU2010254209A1 (en) * 2009-05-28 2011-12-15 Tetralogic Pharmaceuticals Corp. IAP inhibitors
CN101928326B (zh) * 2009-06-24 2015-07-08 中国人民解放军军事医学科学院毒物药物研究所 取代的氨酰基五元杂环烷类化合物及其用途
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
US20110034469A1 (en) * 2009-08-04 2011-02-10 Takeda Pharmaceutical Company Limited Heterocyclic Compound
CN105646471A (zh) * 2009-08-12 2016-06-08 诺华股份有限公司 细胞凋亡蛋白抑制剂的固体口服制剂和晶形
EP2478358A1 (en) 2009-09-18 2012-07-25 Novartis AG Biomarkers for iap inhibitor compounds
CN102958928B (zh) 2009-10-28 2015-05-13 焦阳特制药股份有限公司 二聚体smac模拟物
EP2534170B1 (en) 2010-02-12 2017-04-19 Pharmascience Inc. Iap bir domain binding compounds
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
EP2560659A4 (en) * 2010-04-19 2013-05-01 Stanford Res Inst Int COMPOSITIONS AND METHODS FOR TREATING MULTIPLE MYELOMA
WO2012052758A1 (en) 2010-10-22 2012-04-26 Astrazeneca Ab Response biomarkers for iap antagonists in human cancers
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
WO2013049350A1 (en) 2011-09-30 2013-04-04 Tetralogic Pharmaceuticals Corporation Smac mimetic (birinapant) for use in the treatment of proliferative diseases (cancer)
GB201121124D0 (en) 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes
GB201121132D0 (en) * 2011-12-08 2012-01-18 Dow Corning Modifying polymeric materials by amines
GB201121133D0 (en) * 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes
GB201121122D0 (en) 2011-12-08 2012-01-18 Dow Corning Hydrolysable silanes and elastomer compositions containing them
GB201121128D0 (en) 2011-12-08 2012-01-18 Dow Corning Treatment of filler with silane
US20130196927A1 (en) * 2012-01-27 2013-08-01 Christopher BENETATOS Smac Mimetic Therapy
AU2013256182A1 (en) 2012-05-04 2014-11-13 Novartis Ag Biomarkers for IAP inhibitor therapy
KR20140011773A (ko) * 2012-07-19 2014-01-29 한미약품 주식회사 이중 저해 활성을 갖는 헤테로고리 유도체
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
AU2014235474B2 (en) 2013-03-15 2017-05-25 Novartis Ag Antibody drug conjugates
US20140303090A1 (en) * 2013-04-08 2014-10-09 Tetralogic Pharmaceuticals Corporation Smac Mimetic Therapy
JP6785653B2 (ja) 2013-06-25 2020-11-18 ザ・ウォルター・アンド・エリザ・ホール・インスティテュート・オブ・メディカル・リサーチ 細胞内感染の処置方法
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US9249151B2 (en) * 2013-08-23 2016-02-02 Boehringer Ingelheim International Gmbh Bis-amido pyridines
US9278978B2 (en) * 2013-08-23 2016-03-08 Boehringer Ingelheim International Gmbh 6-Alkynyl Pyridine
DK3083616T3 (da) 2013-12-20 2021-08-30 Astex Therapeutics Ltd Bicykliske heterocykliske forbindelser og disses anvendelser i terapi
US10441654B2 (en) 2014-01-24 2019-10-15 Children's Hospital Of Eastern Ontario Research Institute Inc. SMC combination therapy for the treatment of cancer
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3151920B1 (en) 2014-06-04 2025-08-06 Sanford-Burnham Medical Research Institute Use of inhibitor of apoptosis protein (iap) antagonists in hiv therapy
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
WO2016024195A1 (en) 2014-08-12 2016-02-18 Novartis Ag Anti-cdh6 antibody drug conjugates
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
BR112017015497A2 (pt) 2015-01-20 2018-01-30 Arvinas, Inc. composto, e, composição
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN104592214A (zh) * 2015-02-13 2015-05-06 佛山市赛维斯医药科技有限公司 含葡萄糖酰胺吡啶和烷氧吡嗪结构的化合物及用途
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US20190194315A1 (en) 2015-06-17 2019-06-27 Novartis Ag Antibody drug conjugates
BR112017028269A2 (pt) * 2015-07-13 2018-09-04 Arvinas Inc composto, composição farmacêutica, uso de uma quantidade efetiva de um composto, estado ou condição de doença, e, método para identificar um composto.
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
CN105566447B (zh) * 2016-01-20 2019-09-20 广东工业大学 一种凋亡抑制蛋白的类肽拮抗剂及其合成方法与应用
CN105585583B (zh) * 2016-01-20 2018-04-13 广东工业大学 一种非肽类凋亡抑制蛋白拮抗剂及其合成方法与应用
CN106188098B (zh) * 2016-07-06 2017-11-03 广东工业大学 一种杂化抗癌药物及其制备方法与应用
AU2017319135B2 (en) * 2016-08-29 2021-03-18 The Regents Of The University Of Michigan Aminopyrimidines as ALK inhibitors
JP6899993B2 (ja) * 2016-10-04 2021-07-07 国立医薬品食品衛生研究所長 複素環化合物
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
PL3689868T3 (pl) 2016-12-01 2024-03-11 Arvinas Operations, Inc. Pochodne tetrahydronaftalenu i tetrahydroizochinoliny jako degradery receptorów estrogenowych
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
AU2017382436C1 (en) 2016-12-23 2021-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of Rapidly Accelerated Fibrosarcoma polypeptides
BR112019012682A2 (pt) 2016-12-23 2019-12-17 Arvinas Operations Inc moléculas quiméricas visando a proteólise de egfr e métodos associados de uso
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
BR112019015312A2 (pt) 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
WO2018163051A1 (en) 2017-03-06 2018-09-13 Novartis Ag Methods of treatment of cancer with reduced ubb expression
WO2018185618A1 (en) 2017-04-03 2018-10-11 Novartis Ag Anti-cdh6 antibody drug conjugates and anti-gitr antibody combinations and methods of treatment
AR111651A1 (es) 2017-04-28 2019-08-07 Novartis Ag Conjugados de anticuerpos que comprenden agonistas del receptor de tipo toll y terapias de combinación
JP2020520671A (ja) 2017-05-24 2020-07-16 ノバルティス アーゲー 抗体−サイトカイングラフト化タンパク質及び使用方法
WO2018215937A1 (en) 2017-05-24 2018-11-29 Novartis Ag Interleukin-7 antibody cytokine engrafted proteins and methods of use in the treatment of cancer
AU2018274216A1 (en) 2017-05-24 2019-12-12 Novartis Ag Antibody-cytokine engrafted proteins and methods of use in the treatment of cancer
CN114685602A (zh) * 2017-11-13 2022-07-01 正大天晴药业集团股份有限公司 用作iap抑制剂的smac模拟物及其用途
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
US11028088B2 (en) 2018-03-10 2021-06-08 Yale University Modulators of BTK proteolysis and methods of use
US11161841B2 (en) 2018-04-04 2021-11-02 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
HRP20231295T1 (hr) 2018-07-10 2024-02-02 Novartis Ag Derivati 3-(5-hidroksi-1-oksoizoindolin-2-il)piperidin-2,6-diona i njihova upotreba u liječenju bolesti ovisnih o cinkovom prstu 2 (ikzf2) obitelji ikaros
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
US20200038513A1 (en) 2018-07-26 2020-02-06 Arvinas Operations, Inc. Modulators of fak proteolysis and associated methods of use
WO2020041331A1 (en) 2018-08-20 2020-02-27 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
KR20240028539A (ko) 2018-09-07 2024-03-05 아비나스 오퍼레이션스, 인코포레이티드 급속 진행형 섬유육종 폴리펩티드의 표적화 분해를 위한 다중 고리 화합물 및 방법
WO2020089811A1 (en) 2018-10-31 2020-05-07 Novartis Ag Dc-sign antibody drug conjugates
CA3123511A1 (en) 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CA3234463A1 (en) 2018-12-21 2019-12-18 Novartis Ag Antibodies to pmel17 and conjugates thereof
ES3032659T3 (en) 2019-02-15 2025-07-23 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
MX2021009764A (es) 2019-02-15 2021-09-08 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona sustituidos y usos de los mismos.
DK3967702T3 (da) * 2019-05-10 2024-04-15 Chia Tai Tianqing Pharmaceutical Group Co Ltd Krystallisering af smac-mimic anvendt som iap-inhibitor og fremgangsmåde til fremstilling deraf
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
CN114514032A (zh) 2019-08-02 2022-05-17 兰提欧派普有限公司 用于治疗癌症的血管紧张素2型(at2)受体激动剂
IL320609A (en) 2019-08-26 2025-07-01 Arvinas Operations Inc Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents
CN115175937A (zh) 2019-12-20 2022-10-11 诺华股份有限公司 用于治疗骨髓纤维化和骨髓增生异常综合征的抗TIM-3抗体MBG453和抗TGF-β抗体NIS793与或不与地西他滨或抗PD-1抗体斯巴达珠单抗的组合
KR20220130190A (ko) 2020-01-20 2022-09-26 아스트라제네카 아베 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제
WO2021220178A1 (en) 2020-04-29 2021-11-04 Cominnex Zrt. Iap antagonists and their therapeutic applications
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
CA3185455A1 (en) 2020-06-11 2021-12-16 Novartis Ag Zbtb32 inhibitors and uses thereof
WO2021260528A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
JP2023536164A (ja) 2020-08-03 2023-08-23 ノバルティス アーゲー ヘテロアリール置換３－（１－オキソイソインドリン－２－イル）ピペリジン－２，６－ジオン誘導体及びその使用
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
PE20231555A1 (es) 2020-09-14 2023-10-03 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradacion dirigida del receptor de estrogenos
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
EP4323526A1 (en) 2021-04-16 2024-02-21 Novartis AG Antibody drug conjugates and methods for making thereof
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
WO2023214325A1 (en) 2022-05-05 2023-11-09 Novartis Ag Pyrazolopyrimidine derivatives and uses thereof as tet2 inhibitors
EP4562010A1 (en) 2022-07-26 2025-06-04 Novartis AG Crystalline forms of an akr1c3 dependent kars inhibitor
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
AU2024212035A1 (en) 2023-01-26 2025-08-14 Arvinas Operations, Inc. Cereblon-based kras degrading protacs ans uses related thereto

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
DE2714880A1 (de) * 1977-04-02 1978-10-26 Hoechst Ag Cephemderivate und verfahren zu ihrer herstellung
DE3372965D1 (en) 1982-07-23 1987-09-17 Ici Plc Amide derivatives
JPS59141547A (ja) 1983-02-01 1984-08-14 Eisai Co Ltd 鎮痛作用を有する新規ペプタイドおよび製法
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
FR2575753B1 (fr) * 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
DK167813B1 (da) * 1989-12-07 1993-12-20 Carlbiotech Ltd As Pentapeptidderivat, farmaceutisk acceptable salte heraf, fremgangsmaade til fremstilling deraf og farmaceutisk praeparat indeholdende et saadant derivat
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5559209A (en) * 1993-02-18 1996-09-24 The General Hospital Corporation Regulator regions of G proteins
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
ES2332984T3 (es) 1995-03-30 2010-02-16 Pfizer Products Inc. Derivados de quinazolinas.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
ES2172670T3 (es) 1995-07-06 2002-10-01 Novartis Ag Pirrolpirimidinas y procedimientos para su preparacion.
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
NZ332119A (en) 1996-04-12 2001-08-31 Warner Lambert Co Quinazoline compounds which are irreversible inhibitors of tyrosine kinases
BR9709959A (pt) 1996-06-24 2000-05-09 Pfizer Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas
JP2001500851A (ja) 1996-08-30 2001-01-23 ノバルティス アクチエンゲゼルシャフト エポシロンの製造法および製造過程中に得られる中間生産物
AU4141697A (en) 1996-09-06 1998-03-26 Obducat Ab Method for anisotropic etching of structures in conducting materials
WO1998010767A2 (en) 1996-09-13 1998-03-19 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
WO1998022461A1 (de) 1996-11-18 1998-05-28 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Epothilone c, d, e und f, deren herstellung und deren verwendung als cytostatische mittel bzw. als pflanzenschutzmittel
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
EP1058679B1 (en) 1998-02-25 2005-10-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues therof
US6472172B1 (en) * 1998-07-31 2002-10-29 Schering Aktiengesellschaft DNA encoding a novel human inhibitor-of-apoptosis protein
CA2339961C (en) 1998-08-11 2009-01-20 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
CN100381566C (zh) 1998-11-20 2008-04-16 科森生物科学公司 产生环氧噻酮及其衍生物的重组方法和材料
AP2002002407A0 (en) * 2000-05-23 2002-03-31 Vertex Pharma Caspase inhibitors and uses thereof.
US6608026B1 (en) * 2000-08-23 2003-08-19 Board Of Regents, The University Of Texas System Apoptotic compounds
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US20020160975A1 (en) * 2001-02-08 2002-10-31 Thomas Jefferson University Conserved XIAP-interaction motif in caspase-9 and Smac/DIABLO for mediating apoptosis
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
US20030157522A1 (en) * 2001-11-09 2003-08-21 Alain Boudreault Methods and reagents for peptide-BIR interaction screens
WO2004005248A1 (en) * 2002-07-02 2004-01-15 Novartis Ag Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
ES2318167T3 (es) * 2002-07-15 2009-05-01 The Trustees Of Princeton University Compuestos de union a iap.
US20040171554A1 (en) * 2003-02-07 2004-09-02 Genentech, Inc. Compositions and methods for enhancing apoptosis
AU2004291936A1 (en) * 2003-11-13 2005-06-02 Burnham Institute Compositions and methods for screening pro-apoptotic compounds
CA2553871A1 (en) 2004-01-16 2005-08-04 The Regents Of The University Of Michigan Smac peptidomimetics and the uses thereof
AU2005218555B2 (en) * 2004-03-01 2008-01-03 Board Of Regents, The University Of Texas System Dimeric small molecule potentiators of apoptosis
BRPI0509721A (pt) * 2004-04-07 2007-09-25 Novartis Ag inibidores de iap
NZ588799A (en) 2004-07-02 2012-06-29 Genentech Inc Inhibitors of iap
DE602005022936D1 (de) 2004-12-20 2010-09-23 Genentech Inc Pyrrolidine als inhibitoren von iap
PE20110218A1 (es) 2006-08-02 2011-04-01 Novartis Ag DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS

Also Published As

Publication number Publication date
NZ549925A (en) 2010-08-27
NO20065114L (no) 2007-01-08
EP1735307A1 (en) 2006-12-27
CA2560162A1 (en) 2005-10-20
AU2005231956A1 (en) 2005-10-20
IL178104A (en) 2015-08-31
ES2396195T3 (es) 2013-02-19
ME02125B (me) 2013-04-30
RS52545B (sr) 2013-04-30
AU2005231956B2 (en) 2009-11-05
KR20060134200A (ko) 2006-12-27
CN1964970A (zh) 2007-05-16
US8207183B2 (en) 2012-06-26
TWI417092B (zh) 2013-12-01
US20050234042A1 (en) 2005-10-20
PE20060166A1 (es) 2006-04-25
US8338440B2 (en) 2012-12-25
DK2253614T3 (da) 2013-01-07
HRP20121023T1 (hr) 2013-01-31
EP2253614A1 (en) 2010-11-24
CN1964970B (zh) 2011-08-03
RU2425838C2 (ru) 2011-08-10
KR20080083220A (ko) 2008-09-16
ZA200607696B (en) 2008-03-26
HK1100930A1 (en) 2007-10-05
KR100892185B1 (ko) 2009-04-07
EP1735307B1 (en) 2012-08-29
JP2013049733A (ja) 2013-03-14
US20080242658A1 (en) 2008-10-02
US20110281875A1 (en) 2011-11-17
SG152225A1 (en) 2009-05-29
JP4691549B2 (ja) 2011-06-01
CY1113511T1 (el) 2016-06-22
US7419975B2 (en) 2008-09-02
SI2253614T1 (sl) 2013-01-31
EP2253614B1 (en) 2012-09-19
WO2005097791A1 (en) 2005-10-20
PT2253614E (pt) 2013-01-09
JP2007532504A (ja) 2007-11-15
MA28630B1 (fr) 2007-06-01
ECSP066893A (es) 2006-11-24
TW200602029A (en) 2006-01-16
US20120207769A1 (en) 2012-08-16
ES2394441T3 (es) 2013-01-31
EP2065368A1 (en) 2009-06-03
MY165401A (en) 2018-03-21
IL178104A0 (en) 2006-12-31
PE20110102A1 (es) 2011-02-07
TNSN06323A1 (en) 2008-02-22
RU2006139010A (ru) 2008-05-20
JP2010215635A (ja) 2010-09-30
BRPI0509721A (pt) 2007-09-25
PL2253614T3 (pl) 2013-03-29
CA2560162C (en) 2013-05-21

Similar Documents

Publication Publication Date Title
AR048927A1 (es) Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa
AR061840A1 (es) Compuestos fosfinatos antivirales
AR062159A1 (es) Compuestos que inhiben el enlace de la proteina smac al inhibidor de proteinas de apoptosis (iap)
AR069494A1 (es) Derivados de acidos fosfonicos
AR054837A1 (es) Compuestos inhibidores del virus de la hepatitis c
CL2012000999A1 (es) Compuestos derivados de pirazoloespirocetona sustituida, inhibidores de acetil-coa carboxilasa; composicion farmaceutica que los comprende; uso para tratar o retrasar la progresion o el inicio de diabetes tipo 2, higado graso no alcoholico (hgna) o la resistencia hepatica a la insulina.
AR054838A1 (es) Compuestos inhibidores del virus de la hepatitis c
AR071314A1 (es) Antagonistas de receptor de cgrp
AR062050A1 (es) Derivados de amina utiles como agentes anti-cancerigenos
ES2570127T3 (es) Compuestos y composiciones como inhibidores de la proteína quinasa
AR037731A1 (es) Uso de ureas de benzotiazoles
AR078163A1 (es) Utilizacion de aminodihidrotiazinas para el tratamiento o prevencion de la diabetes
CA2525547A1 (en) Compounds and uses thereof in modulating amyloid beta
AR069326A1 (es) Derivados bis-(sulfonilamino), proceso de preparacion, composiciones farmaceuticas que los contienen y su uso en terapia.
ECSP034865A (es) Resolución óptica de (1-benzilo-4-metilopiperidina-3-il)-metilamina y su uso para la preparación de derivados de pirrolo 2,3-pirimidina como inhibidores de proteina quinasas
AR044116A1 (es) Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos.
AR074109A1 (es) Pirrolidinas heterociclicas agonistas de receptores de la melanocortina, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de la obesidad, diabetes y disfuncion erectil.
AR069813A1 (es) Derivados de 2- amino-pirimidina, una composicion farmaceutica, un metodo de preparacion del compuesto y uso del mismo para preparar un medicamento
AR058198A1 (es) Derivados de morfolina y composiciones farmaceuticas
AR061057A1 (es) Derivados de pirazolo(3,4-d)pirimidina utiles para desordenes respiratorios
AR077516A1 (es) Composiciones farmaceuticas de uso oftalmico de antagonistas del receptor dp2. uso. compuesto.
AR059184A1 (es) Derivados de sulfonamidas, su preparacion y su aplicacion en tarapeutica
AR083081A1 (es) Isoxazolin oximas como agentes antiparasitarios
AR043111A1 (es) Derivados monoacilados de o-fenilendiaminas
AR056980A1 (es) Derivados de dihidrobenzofurano, composiciones farmaceuticas, y uso de los mismos

Legal Events

Date Code Title Description
FC Refusal