ES2644286T3 - Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas - Google Patents

Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas Download PDF

Info

Publication number
ES2644286T3
ES2644286T3 ES10771608.6T ES10771608T ES2644286T3 ES 2644286 T3 ES2644286 T3 ES 2644286T3 ES 10771608 T ES10771608 T ES 10771608T ES 2644286 T3 ES2644286 T3 ES 2644286T3
Authority
ES
Spain
Prior art keywords
substituted
nr9r10
heteroalkyl
compound
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES10771608.6T
Other languages
English (en)
Inventor
Randall L. Halcomb
Paul A. Roethle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Application granted granted Critical
Publication of ES2644286T3 publication Critical patent/ES2644286T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Description

5
10
15
20
25
30
35
40
45
50
55
DESCRIPCION
Derivados de purina o deazapurina utiles para el tratamiento de (entre otros) infecciones vlricas Campo de la invencion
Esta solicitud se refiere en general a derivados de biaril purina y 3-deazapurina, y a composiciones farmaceuticas que modulan de forma selectiva los receptores de tipo toll (tales como TLR-7) y al uso de tales compuestos.
Antecedentes de la invencion
El sistema inmunitario innato provee al cuerpo de una primera llnea de defensa frente a los patogenos invasores. En una respuesta inmunitaria innata, un receptor codificado en la estirpe germinal reconoce un patogeno invasor, cuya activacion inicia una cascada de senalizacion que conduce a la induccion de la expresion de citocinas. Los receptores del sistema inmunitario innato tienen una amplia especificidad, reconociendo estructuras moleculares que estan altamente conservadas entre distintos patogenos. Una familia de estos receptores se conoce como los receptores de tipo Toll (los TLR), debido a su homologla con los receptores identificados en primer lugar y nombrados en Drosophila, y estan presentes en celulas tales como macrofagos, celulas dendrlticas y celulas epiteliales.
En mamlferos existen al menos diez TLR distintos. Para algunos de estos receptores se han identificado los ligandos y las correspondientes cascadas de senalizacion. Por ejemplo, TLR-2 es activado por la lipoprotelna de bacterias (por ejemplo, E. coli.), el TLR-3 se activa por ARN bicatenario, el TLR-4 se activa por lipopolisacarido (es decir, LPS o endotoxina) o bacterias gramnegativas (por ejemplo, Salmonella y E. coli O157:H7), el TLR-5 se activa por la flagelina de las bacterias moviles (por ejemplo, Listeria), el TLR-7 reconoce y responde a imiquimod (y ARNmc) y el TLR-9 se activa por secuencias CpG no metiladas de ADN patogeno. La estimulacion de cada uno de estos receptores conduce a la activacion del factor de transcripcion NF-kB y otras moleculas de senalizacion que estan implicadas en la regulacion de la expresion de los genes de citocinas, incluyendo los que codifican el factor de necrosis tumoral alfa (TNF-a), la interleucina-1 (IL-1) y determinadas citocinas. Los agonistas del TLR-7 son inmunoestimulantes e inducen la produccion de interferon-a endogeno in vivo.
Existen varias enfermedades, trastornos y afecciones vinculadas a los TLR, de forma que se cree que las terapias que utilizan un agonista del TLR son prometedoras, incluyendo, pero sin limitacion, melanoma, el carcinoma de pulmon no microcltico, el carcinoma hepatocelular, el carcinoma de celulas basales, el carcinoma de celulas renales, el mieloma, la rinitis alergica, el asma, la EPOC, la colitis ulcerosa, fibrosis hepatica e infecciones vlricas tales como el VHB, el VHC, el VPH, el VRS, el SRAG, el VIH o la gripe.
Sumario de la invencion
De acuerdo con lo anterior, en un aspecto la presente invencion proporciona compuestos de Formula I:
imagen1
L1 es -O-;
R1 es H, alquilo, alquilo sustituido, heteroalquilo, heteroalquilo sustituido, carbociclilo, carbociclilo sustituido, heterociclilo, heterociclilo sustituido, carbociclilalquilo, carbociclilalquilo sustituido, heterociclilalquilo o heterocicilalquilo sustituido;
X1 es alquileno;
D1 es arilo o heteroarilo;
D2 es arilo o heteroarilo; n es 0, 1 o 2;
cada R3 y R4 es independientemente alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, halogeno, haloalquilo, haloalcoxi, heteroalquilo, heteroalquilo sustituido, =O, -OR8, -SR8, -NR9R10, =NR8, =NOR8, =NNR8R9, -CN, -OCN, -SCN, -N=C=O, -NCS, -NO, -NO2, =N2, -N3, -NR8C(=O)R9, -NR8C(=O)OR9,
5
10
15
20
25
30
35
-NR8C(=O)NR9R10, -C(=O)NR9R10, S(=O)2R8, -OS(=O)2OR8
-C(=O)OR8, -OC(=O)NR9R10, -OC(=O)OR8, -C(=O)R8, -S(=O)2OR8, - -S(=O)2NR9R10, -S(=O)R8, -NR8S(=O)2R9, -NR8S(=O)2NR9R10, -NR8S(=O)2OR9, - OS(O)2NR9R10, -OP(=O)(OR8)2, -P(=O)(OR8)2, -P(O](OR8)(R9)l -P(O)R9R10, -OP(=))R9R10, -C(=S)R8, -C(=S)OR8, -C(=O)SR8, -C(=S)SR8, -C(=S)NR9R10, -C(=NR8)NR9R10 o -NR8C(=NR8)NR9R10; m es 1 o 2;
L2 es alquileno;
X2 es N o C-R5;
R5 es H, halogeno, alquilo, alquilo sustituido, haloalquilo, heteroalquilo, heteroalquilo sustituido, ciano, azido, - C(O)H, -C(O)R8, -S(O)R8, -S(O)2R8, -S(O)2NR8R9, -C(O)OR8 o -C(O)NR9R10;
R2 es -NR6R7;
R6 y R7 junto con el nitrogeno al que estan unidos forman un heterociclilo de 3 a 8 miembros, sustituido o sin sustituir, que puede contener uno o mas heteroatomos adicionales seleccionados entre N, O, S o P; y R8, R9 y R10 son cada uno independientemente H, alquilo, alquilo sustituido, haloalquilo, heteroalquilo, heteroalquilo sustituido, carbociclilo, carbociclilo sustituido, carbociclilalquilo, carbociclilalquilo sustituido, heterociclilo, heterociclilo sustituido, heterociclilalquilo, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilalquilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, carbociclilalquenilo, carbociclilalquenilo sustituido, carbociclilalquinilo, carbociclilalquinilo sustituido,
heterociclilalquenilo, heterociclilalquenilo sustituido, heterociclilalquinilo, heterociclilalquinilo sustituido,
arilalquenilo, arilalquenilo sustituido, arilalquinilo, arilalquinilo sustituido, heteroarilalquenilo, heteroarilalquenilo sustituido, heteroarilalquinilo, heteroarilalquinilo sustituido, carbociclilheteroalquilo, carbociclilheteroalquilo sustituido, heterociclilheteroalquilo, heterociclilheteroalquilo sustituido, arilheteroalquilo, arilheteroalquilo sustituido, heteroarilheteroalquilo o heteroarilheteroalquilo sustituido.
En una realizacion, X2 es N.
En otra realizacion, X2 es C-R5.
En otra realizacion, D1 es arilo. En otra realizacion, D1 es fenilo. En otra realizacion, D2 es arilo.
En otra realizacion, el compuesto se selecciona entre el grupo que consiste en:
imagen2

Claims (12)

  1. 5
    10
    15
    20
    25
    30
    35
    40
    45
    50
    1. Un compuesto de Formula I:
    imagen1
    o una sal farmaceuticamente aceptable del mismo, en donde:
    L1 es -O-;
    R1 es H, alquilo, alquilo sustituido, heteroalquilo, heteroalquilo sustituido, carbocililo, carbociclilo sustituido, heterociclilo, heterociclilo sustituido, carbociclilalquilo, carbociclilalquilo sustituido, heterociclilalquilo o heterocicilalquilo sustituido;
    X1 es alquileno;
    D1 es arilo o heteroarilo;
    D2 es arilo o heteroarilo; n es 0, 1 o 2;
    cada R3 y R4 es independientemente alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, halogeno, haloalquilo, haloalcoxi, heteroalquilo, heteroalquilo sustituido, =O, -OR8, -SR8, -NR9R10, =NR8, =NOR8, =NNR8R9, -CN, -OCN, -SCN, -N=C=O, -NCS, -NO, -NO2, =N2, -N3, -NR8C(=O)R9, -NR8C(=O)OR9, -NR8C(=O)NR9R10, -C(=O)NR9R10, -C(=O)OR8, -OC(=O)NR9R10, -OC(=O)OR8, -C(=O)R8, -S(=O)2OR8, - S(=O)2R8, -OS(=O)2OR8, -S(=O)2NR9R10, -S(=O)R8, -NR8S(=O)2R9, -NR8S(=O)2NR9R10, -NR8S(=O)2OR9, - OS(O)2NR9R10, -OP(=O)(OR8)2, -P(=O)(OR8)2, -P(O)(OR8)(R9), -P(O)R9R10, -OP(=))R9R10, -C(=S)R8, -C(=S)OR8, -C(=O)SR8, -C(=S)SR8, -C(=S)NR9R10, -C(=NR8)NR9R10 o -NR8C(=NR8)NR9R10; m es 1 o 2;
    L2 es alquileno;
    X2 es N o C-R5;
    R5 es H, halogeno, alquilo, alquilo sustituido, haloalquilo, heteroalquilo, heteroalquilo sustituido, ciano, azido, - C(O)H, -C(O)R8, -S(O)R8, -S(O)2R8, -S(O)2NR8R9, -C(O)OR8 o -C(O)NR9R10;
    R2 es -NR6R7;
    R6 y R7 junto con el nitrogeno al que estan unidos forman un heterociclilo de 3 a 8 miembros, sustituido o sin sustituir, que puede contener uno o mas heteroatomos adicionales seleccionados entre N, O, S o P; y R8, R9 y R10 son cada uno independientemente H, alquilo, alquilo sustituido, haloalquilo, heteroalquilo, heteroalquilo sustituido, carbociclilo, carbociclilo sustituido, carbociclilalquilo, carbociclilalquilo sustituido, heterociclilo, heterociclilo sustituido, heterociclilalquilo, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilalquilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, carbociclilalquenilo, carbociclilalquenilo sustituido, carbociclilalquinilo, carbociclilalquinilo sustituido,
    heterociclilalquenilo, heterociclilalquenilo sustituido, heterociclilalquinilo, heterociclilalquinilo sustituido,
    arilalquenilo, arilalquenilo sustituido, arilalquinilo, arilalquinilo sustituido, heteroarilalquenilo, heteroarilalquenilo sustituido, heteroarilalquinilo, heteroarilalquinilo sustituido, carbociclilheteroalquilo, carbociclilheteroalquilo sustituido, heterociclilheteroalquilo, heterociclilheteroalquilo sustituido, arilheteroalquilo, arilheteroalquilo sustituido, heteroarilheteroalquilo o heteroarilheteroalquilo sustituido.
  2. 2. El compuesto de la reivindicacion 1, en donde X2 es N.
  3. 3. El compuesto de la reivindicacion 1 o de la reivindicacion 2, en donde X2 es C-R5.
  4. 4. El compuesto de una cualquiera de las reivindicaciones 1 - 3, en donde D1 es arilo.
  5. 5. El compuesto de la reivindicacion 4, en donde D1 es fenilo.
  6. 6. El compuesto de una cualquiera de las reivindicaciones 1 - 5, en donde D2 es arilo.
  7. 7. Un compuesto de acuerdo con la reivindicacion 1 seleccionado entre el grupo que consiste en:
    imagen2
    imagen3
    00
    h-
    imagen4
    imagen5
    CT>
    N-
    imagen6
    imagen7
    a
    0 o
    Q
    1V)
    Q
    (i A \ ^zJ
    fl (S jT>, \ jJ
    «AZJ
    iza/
    iH z=< o <
    x~H zHRZ O < „ V_7 \*=/
    > o \
    ) 0 \ o> \
    imagen8
    imagen9
    imagen10
    imagen11
    imagen12
    *sf
    00
    imagen13
    imagen14
    imagen15
    CD
    00
    y
    imagen16
    5 o una sal farmaceuticamente aceptable del mismo.
  8. 8. Un compuesto de acuerdo con la reivindicacion 1, que tiene la formula:
    imagen17
    o una sal farmaceuticamente aceptable del mismo.
    5 9. Una composicion farmaceutica que comprende un compuesto de acuerdo con las reivindicaciones 1 - 8, y uno o
    mas vehlculos o excipientes farmaceuticamente aceptables.
  9. 10. La composicion farmaceutica de la reivindicacion 9, que comprende adicionalmente uno o mas agentes terapeuticos adicionales.
    10
  10. 11. Un compuesto de acuerdo con una cualquiera de las reivindicaciones 1 - 8, para su uso en un metodo para el tratamiento de una infeccion vlrica.
  11. 12. El compuesto para su uso de acuerdo con la reivindicacion 11, en donde el tratamiento da como resultado uno o 15 mas de una reduccion de la carga vlrica o la eliminacion de ARN vlrico.
  12. 13. Un compuesto de acuerdo con una cualquiera de las reivindicaciones 1 - 8, para su uso en un metodo para el tratamiento o la prevencion de melanoma, carcinoma de pulmon no microcltico, carcinoma hepatocelular, carcinoma de celulas basales, carcinoma de celulas renales, mieloma, rinitis alergica, asma, EPOC, colitis ulcerosa, fibrosis
    20 hepatica, VHB, VHC, VPH, VRS, SRAG, VIH o gripe.
ES10771608.6T 2009-10-22 2010-10-15 Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas Active ES2644286T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25410309P 2009-10-22 2009-10-22
US254103P 2009-10-22
US36679010P 2010-07-22 2010-07-22
US366790P 2010-07-22
PCT/US2010/052802 WO2011049825A1 (en) 2009-10-22 2010-10-15 Derivatives of purine or deazapurine useful for the treatment of (inter alia) viral infections

Publications (1)

Publication Number Publication Date
ES2644286T3 true ES2644286T3 (es) 2017-11-28

Family

ID=43502860

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10771608.6T Active ES2644286T3 (es) 2009-10-22 2010-10-15 Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas

Country Status (27)

Country Link
US (3) US8507507B2 (es)
EP (1) EP2491035B1 (es)
JP (1) JP5694345B2 (es)
KR (1) KR101793300B1 (es)
CN (1) CN102666541B (es)
AP (1) AP3103A (es)
AU (1) AU2010310813B2 (es)
BR (1) BR112012009329A2 (es)
CA (1) CA2777824C (es)
CL (1) CL2012000988A1 (es)
CO (1) CO6531469A2 (es)
CR (1) CR20120255A (es)
EA (1) EA020488B1 (es)
EC (1) ECSP12011915A (es)
ES (1) ES2644286T3 (es)
IL (1) IL218747A (es)
IN (1) IN2012DN02984A (es)
MX (1) MX2012004706A (es)
NO (1) NO2491035T3 (es)
NZ (1) NZ598933A (es)
PE (1) PE20121091A1 (es)
PL (1) PL2491035T3 (es)
PT (1) PT2491035T (es)
SG (1) SG10201406813RA (es)
SI (1) SI2491035T1 (es)
WO (1) WO2011049825A1 (es)
ZA (1) ZA201202858B (es)

Families Citing this family (238)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2620182A1 (en) 2005-08-22 2007-03-01 Dennis A. Carson Tlr agonists
WO2007142755A2 (en) * 2006-05-31 2007-12-13 The Regents Of The University Of California Purine analogs
ES2552471T3 (es) 2007-02-07 2015-11-30 The Regents Of The University Of California Conjugados de agonistas de TLR sintéticos y usos de los mismos
EP2259788A4 (en) * 2008-02-07 2011-03-16 Univ California TREATMENT OF BLADDER DISEASES WITH A TLR7 ACTIVATOR
WO2010077613A1 (en) 2008-12-09 2010-07-08 Gilead Sciences, Inc. Modulators of toll-like receptors
SG173617A1 (en) * 2009-02-11 2011-09-29 Univ California Toll-like receptor modulators and treatment of diseases
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
CN102666541B (zh) 2009-10-22 2015-11-25 吉里德科学公司 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
AR079529A1 (es) * 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
KR101946499B1 (ko) 2011-04-08 2019-02-11 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염 치료를 위한 피리미딘 유도체
AU2016201747B2 (en) * 2011-05-16 2017-06-01 Romark Laboratories, L.C. Use of thiazolide compounds for the prevention and treatment of viral diseases, cancer and diseases caused by intracellular infections
KR102037162B1 (ko) * 2011-05-16 2019-10-29 로마크 레버러토리즈, 엘.씨. 바이러스병, 암 및 세포내 감염으로 인한 질병의 예방 및 치료를 위한 티아졸리드 화합물의 용도
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
EP2776439B1 (en) 2011-11-09 2018-07-04 Janssen Sciences Ireland UC Purine derivatives for the treatment of viral infections
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
CA2874800C (en) 2012-07-13 2021-04-06 Janssen R&D Ireland Macrocyclic purines for the treatment of viral infections
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
NZ705589A (en) 2012-10-10 2019-05-31 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
AU2013346793B2 (en) 2012-11-16 2018-03-08 Janssen Sciences Ireland Uc Heterocyclic substituted 2-amino-quinazoline derivatives for the treatment of viral infections
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
KR102225233B1 (ko) 2013-02-21 2021-03-09 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염의 치료를 위한 2-아미노피리미딘 유도체
MX366481B (es) 2013-03-29 2019-07-09 Janssen Sciences Ireland Uc Deaza-purinonas macrociclicas para el tratamiento de infecciones virales.
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
MY188071A (en) 2013-05-24 2021-11-16 Janssen Sciences Ireland Uc Pyridone derivatives for the treatment of viral infections and further diseases
CN109369643B (zh) 2013-06-27 2021-05-18 爱尔兰詹森科学公司 用于治疗病毒感染和其他疾病的吡咯并[3,2-d]嘧啶衍生物
EP3027624B1 (en) 2013-07-30 2018-09-12 Janssen Sciences Ireland UC Thieno[3,2-d]pyrimidines derivatives for the treatment of viral infections
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
EP4140485A1 (en) * 2014-07-11 2023-03-01 Gilead Sciences, Inc. Modulators of toll-like receptors for the treatment of hiv
EA201790369A1 (ru) 2014-09-16 2017-10-31 Джилид Сайэнс, Инк. Твердые формы модулятора толл-подобного рецептора
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG10202105371YA (en) 2014-12-26 2021-07-29 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
PL3097102T3 (pl) 2015-03-04 2018-04-30 Gilead Sciences Inc Związki 4,6-diamino-pirydo[3,2-d]pirymidyny modulujące działanie receptora toll-podobnego
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US20210292327A1 (en) 2015-08-26 2021-09-23 Gilead Sciences, Inc. Deuterated toll-like receptor modulators
MA44077A (fr) 2015-12-15 2021-05-05 Gilead Sciences Inc Anticorps neutralisants le virus de l'immunodéficience humaine
CU20180059A7 (es) 2015-12-17 2018-10-04 Gilead Sciences Inc Compuestos inhibidores de la quinasa de unión a tank
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
ES2989988T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros heterorocíclicos para la degradación de proteínas diana
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
US11697851B2 (en) 2016-05-24 2023-07-11 The Regents Of The University Of California Early ovarian cancer detection diagnostic test based on mRNA isoforms
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
ES2969239T3 (es) 2016-05-27 2024-05-17 Gilead Sciences Inc Combinación de ledipasvir y sofosbuvir para su uso en el tratamiento de infecciones por el virus de la hepatitis B en humanos
WO2018002319A1 (en) 2016-07-01 2018-01-04 Janssen Sciences Ireland Uc Dihydropyranopyrimidines for the treatment of viral infections
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
KR102459155B1 (ko) * 2016-08-29 2022-10-28 에프. 호프만-라 로슈 아게 바이러스 감염의 치료 및 예방을 위한 7-치환된 설폰이미도일푸린온 화합물
ES2826748T3 (es) 2016-09-02 2021-05-19 Gilead Sciences Inc Derivados de 4,6-diamino-pirido[3,2-d]pirimidina como moduladores de receptores de tipo Toll
KR102268448B1 (ko) 2016-09-02 2021-06-22 길리애드 사이언시즈, 인코포레이티드 톨 유사 수용체 조정제 화합물
CN115215886B (zh) * 2016-09-09 2024-10-11 诺华股份有限公司 作为内体Toll样受体抑制剂的化合物及组合物
WO2018060317A1 (en) 2016-09-29 2018-04-05 Janssen Sciences Ireland Uc Pyrimidine prodrugs for the treatment of viral infections and further diseases
MA46535A (fr) 2016-10-14 2019-08-21 Prec Biosciences Inc Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b
ES2886973T3 (es) * 2016-11-28 2021-12-21 Jiangsu Hengrui Medicine Co Derivado pirazolo-heteroarilo, método de preparación y uso médico del mismo
TWI868958B (zh) 2017-01-31 2025-01-01 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
US10487084B2 (en) * 2017-08-16 2019-11-26 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a heterobiaryl moiety, conjugates thereof, and methods and uses therefor
US10472361B2 (en) 2017-08-16 2019-11-12 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor
US10457681B2 (en) 2017-08-16 2019-10-29 Bristol_Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor
US10508115B2 (en) 2017-08-16 2019-12-17 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
US10494370B2 (en) 2017-08-16 2019-12-03 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a pyridine or pyrazine moiety, conjugates thereof, and methods and uses therefor
JP6934562B2 (ja) 2017-08-22 2021-09-15 ギリアード サイエンシーズ， インコーポレイテッド 治療用複素環式化合物
WO2019084060A1 (en) 2017-10-24 2019-05-02 Silverback Therapeutics, Inc. CONJUGATES AND METHODS OF USE FOR THE SELECTIVE DELIVERY OF IMMUNOMODULATORY AGENTS
JP2021035910A (ja) * 2017-11-01 2021-03-04 大日本住友製薬株式会社 置換プリン化合物
CN111936136B (zh) 2017-11-14 2024-07-05 儿童医学中心公司 新咪唑并嘧啶化合物及其用途
US11730810B2 (en) 2017-11-14 2023-08-22 Children's Medical Center Corporation Composition comprising an antigen and a substituted imidazo[1,2-a]pyrimidine for enhancing human immune response
FI3706762T3 (fi) 2017-12-07 2024-12-13 Univ Emory N4-hydroksisytidiini ja johdannaisia sekä niihin liittyviä virusten vastaisia käyttötapoja
KR20200100113A (ko) 2017-12-15 2020-08-25 실버백 테라퓨틱스, 인크. 간염 치료용 항체 구조물-약물 접합체
EP3728283B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CN111511754B (zh) 2017-12-20 2023-09-12 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸
EP3752505B1 (en) 2018-02-12 2023-01-11 F. Hoffmann-La Roche AG Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection
WO2019160882A1 (en) 2018-02-13 2019-08-22 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
MX2020008746A (es) * 2018-02-28 2020-09-28 Hoffmann La Roche Compuestos de sulfonimidoilpurinona 7-sustituidos y sus derivados para el tratamiento y prevencion del cancer de higado.
TW202415645A (zh) 2018-03-01 2024-04-16 愛爾蘭商健生科學愛爾蘭無限公司 ２，４－二胺基喹唑啉衍生物及其醫學用途
CN110317202B (zh) * 2018-03-30 2021-12-24 江苏恒瑞医药股份有限公司 氰基吡咯并杂芳基类衍生物、其制备方法及其在医药上的应用
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
CN108295060A (zh) * 2018-04-08 2018-07-20 王长国 一种tlr7激动剂在增强cik细胞对肿瘤细胞杀伤力方面的应用
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
WO2019196918A1 (zh) * 2018-04-13 2019-10-17 罗欣药业(上海)有限公司 五元杂环并嘧啶类化合物、药物组合物及用途
WO2019204609A1 (en) 2018-04-19 2019-10-24 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
WO2019209811A1 (en) 2018-04-24 2019-10-31 Bristol-Myers Squibb Company Macrocyclic toll-like receptor 7 (tlr7) agonists
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
CN110526917B (zh) * 2018-05-25 2021-09-03 江苏恒瑞医药股份有限公司 一种吡唑并杂芳基类衍生物的可药用盐、晶型及其制备方法
JP2021526520A (ja) * 2018-05-25 2021-10-07 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Ｊｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．， Ｌｔｄ． ピラゾロヘテロアリール誘導体の塩酸塩の結晶形および調製方法
CN110526918B (zh) * 2018-05-25 2021-09-03 江苏恒瑞医药股份有限公司 一种吡唑并杂芳基类衍生物的晶型及制备方法
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
CR20200653A (es) 2018-07-03 2021-02-11 Gilead Sciences Inc Anticuerpos que se dirigen al gp120 de vih y métodos de uso
US11186579B2 (en) 2018-07-06 2021-11-30 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
JP7049519B2 (ja) 2018-07-06 2022-04-06 ギリアード サイエンシーズ， インコーポレイテッド 治療用複素環式化合物
BR112020026746A2 (pt) 2018-07-13 2021-03-30 Gilead Sciences, Inc. Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição.
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
US11554120B2 (en) 2018-08-03 2023-01-17 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor
SG11202101980VA (en) 2018-09-12 2021-03-30 Silverback Therapeutics Inc Methods and composition for the treatment of disease with immune stimulatory conjugates
CN111072667A (zh) * 2018-10-22 2020-04-28 罗欣药业(上海)有限公司 五元或六元杂环并嘧啶类化合物及其用途
CN112955435B (zh) 2018-10-24 2024-09-06 吉利德科学公司 Pd-1/pd-l1抑制剂
FI3873903T3 (fi) 2018-10-31 2024-03-26 Gilead Sciences Inc Substituoituja 6-azabentsiimidatsoliyhdisteitä HPK1-inhibiittoreina
KR102658602B1 (ko) 2018-10-31 2024-04-19 길리애드 사이언시즈, 인코포레이티드 Hpk1 억제 활성을 갖는 치환된 6-아자벤즈이미다졸 화합물
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
EP3934757B1 (en) 2019-03-07 2023-02-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
CA3129011C (en) 2019-03-07 2023-12-19 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
LT3938047T (lt) 2019-03-22 2022-10-10 Gilead Sciences, Inc. Tilteliniai tricikliniai karbamoilpiridono junginiai ir jų naudojimas farmacijoje
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
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202231277A (zh) 2019-05-21 2022-08-16 美商基利科學股份有限公司 鑑別對使用gp120 v3聚醣導向之抗體的治療敏感之hiv病患的方法
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
CA3140708A1 (en) 2019-06-18 2020-12-24 Helen Horton Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
WO2020257407A1 (en) 2019-06-19 2020-12-24 Silverback Therapeutics, Inc. Anti-mesothelin antibodies and immunoconjugates thereof
MX2021015452A (es) 2019-06-25 2022-02-11 Gilead Sciences Inc Proteinas de fusion flt3l-fc y metodos de uso.
TWI879779B (zh) 2019-06-28 2025-04-11 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3145791A1 (en) 2019-07-16 2021-01-21 Gilead Sciences, Inc. Hiv vaccines and methods of making and using
WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
WO2021026803A1 (en) 2019-08-14 2021-02-18 Novartis Ag Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
KR20220066887A (ko) 2019-09-19 2022-05-24 덴마크스 텍니스케 유니버시테트 면역 자극 미셀 조성물
KR20220074917A (ko) 2019-09-30 2022-06-03 길리애드 사이언시즈, 인코포레이티드 Hbv 백신 및 hbv를 치료하는 방법
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3151322A1 (en) 2019-10-01 2021-04-08 Silverback Therapeutics, Inc. Combination therapy with immune stimulatory conjugates
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX2022004370A (es) 2019-10-18 2022-05-06 Forty Seven Inc Terapias de combinacion para tratar sindromes mielodisplasicos y leucemia mieloide aguda.
WO2021087064A1 (en) 2019-10-31 2021-05-06 Forty Seven, Inc. Anti-cd47 and anti-cd20 based treatment of blood cancer
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
DK4069729T3 (da) 2019-12-06 2025-04-07 Prec Biosciences Inc Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet
JP7711068B2 (ja) 2019-12-24 2025-07-22 カルナバイオサイエンス株式会社 ジアシルグリセロールキナーゼ調節化合物
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115151548A (zh) 2020-01-27 2022-10-04 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物
WO2021154668A1 (en) 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US20230127326A1 (en) 2020-01-27 2023-04-27 Bristol-Myers Squibb Company C3-SUBSTITUTED 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
KR20220132591A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
KR20220132594A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
KR20220132592A (ko) 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
EP4097102A1 (en) 2020-01-27 2022-12-07 Bristol-Myers Squibb Company 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists
CN115279765B (zh) 2020-01-27 2024-11-12 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物
WO2021154662A1 (en) 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
IL295023A (en) 2020-02-14 2022-09-01 Jounce Therapeutics Inc Antibodies and fusion proteins that bind to ccr8 and their uses
EP4106819A1 (en) 2020-02-21 2022-12-28 Silverback Therapeutics, Inc. Nectin-4 antibody conjugates and uses thereof
AR121620A1 (es) 2020-03-20 2022-06-22 Gilead Sciences Inc Profármacos de nucleósidos 4’-c-sustituidos-2-halo-2’-deoxiadenosina y métodos de preparación y uso de los mismos
CR20220547A (es) 2020-05-01 2022-12-15 Gilead Sciences Inc Compuestos de 2,4-dioxopirimidina inhibidores de cd73
WO2021236944A1 (en) 2020-05-21 2021-11-25 Gilead Sciences, Inc. Pharmaceutical compositions comprising bictegravir
IL299508A (en) 2020-07-01 2023-02-01 Ars Pharmaceuticals Inc Anti-asgr1 antibody conjugates and uses thereof
JP7712352B2 (ja) 2020-08-07 2025-07-23 ギリアード サイエンシーズ， インコーポレイテッド ホスホンアミドヌクレオチド類似体のプロドラッグ及びその薬学的使用
US20240124486A1 (en) * 2020-09-27 2024-04-18 Shanghai Visonpharma Co., Ltd. Macrocyclic tlr7 agonist, preparation method therefor, pharmaceutical composition and use thereof
TW202406932A (zh) 2020-10-22 2024-02-16 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
EP4660325A3 (en) 2020-11-11 2026-02-25 Gilead Sciences, Inc. Methods of identifying hiv patients sensitive to therapy with gp120 cd4 binding site-directed antibodies
KR102514860B1 (ko) * 2020-12-01 2023-03-29 한국과학기술연구원 5-ht7 세로토닌 수용체 활성 저해용 바이페닐 피롤리딘 및 바이페닐 다이하이드로이미다졸 유도체 및 이를 유효성분으로 포함하는 약학 조성물
CA3215049A1 (en) 2021-04-10 2022-10-13 Baiteng ZHAO Folr1 binding agents, conjugates thereof and methods of using the same
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症
WO2022226317A1 (en) 2021-04-23 2022-10-27 Profoundbio Us Co. Anti-cd70 antibodies, conjugates thereof and methods of using the same
EP4337223A1 (en) 2021-05-13 2024-03-20 Gilead Sciences, Inc. Combination of a tlr8 modulating compound and anti-hbv sirna therapeutics
TW202313094A (zh) 2021-05-18 2023-04-01 美商基利科學股份有限公司 使用ＦＬＴ３Ｌ—Ｆｃ融合蛋白之方法
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
KR20240005901A (ko) 2021-06-23 2024-01-12 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
KR20240025616A (ko) 2021-06-23 2024-02-27 길리애드 사이언시즈, 인코포레이티드 다이아실글리세롤 키나제 조절 화합물
AU2022298639C1 (en) 2021-06-23 2025-07-17 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
TW202320857A (zh) 2021-07-06 2023-06-01 美商普方生物製藥美國公司 連接子、藥物連接子及其結合物及其使用方法
JP2024539252A (ja) 2021-10-28 2024-10-28 ギリアード サイエンシーズ， インコーポレイテッド ピリジジン－３（２ｈ）－オン誘導体
CA3235986A1 (en) 2021-10-29 2023-05-04 Gilead Science, Inc. Cd73 compounds
PL4445900T3 (pl) 2021-12-03 2025-09-22 Gilead Sciences, Inc. Związki terapeutyczne przeciwko zakażeniu wirusem hiv
KR20240113832A (ko) 2021-12-03 2024-07-23 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염 치료용 화합물
WO2023102529A1 (en) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
US20230203202A1 (en) 2021-12-08 2023-06-29 Dragonfly Therapeutics, Inc. Proteins binding nkg2d, cd16 and 5t4
WO2023107954A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Antibodies targeting 5t4 and uses thereof
EP4452414A2 (en) 2021-12-22 2024-10-30 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
EP4667056A1 (en) 2021-12-22 2025-12-24 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
KR102913194B1 (ko) * 2022-03-03 2026-01-19 서울대학교병원 안구건조증 또는 마이봄샘 기능장애의 예방, 개선, 또는 치료용 조성물
LT4245756T (lt) 2022-03-17 2024-11-25 Gilead Sciences, Inc. Ikaros cinko pirštų šeimos skaidymo medžiagos ir jų panaudojimas
AU2023240346A1 (en) 2022-03-24 2024-09-19 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TWI876305B (zh) 2022-04-05 2025-03-11 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
TWI856796B (zh) 2022-04-06 2024-09-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
US20230374036A1 (en) 2022-04-21 2023-11-23 Gilead Sciences, Inc. Kras g12d modulating compounds
IL317958A (en) 2022-07-01 2025-02-01 Gilead Sciences Inc CD73 compounds
WO2024006982A1 (en) 2022-07-01 2024-01-04 Gilead Sciences, Inc. Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection
JP2025523043A (ja) 2022-07-12 2025-07-17 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖ免疫原性ポリペプチド及びワクチン、並びにその使用
KR20250051732A (ko) 2022-08-26 2025-04-17 길리애드 사이언시즈, 인코포레이티드 광범위 중화 항체를 위한 투여 및 일정 요법
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY
US20240226130A1 (en) 2022-10-04 2024-07-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
EP4638436A1 (en) 2022-12-22 2025-10-29 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
EP4695260A1 (en) 2023-04-11 2026-02-18 Gilead Sciences, Inc. Kras modulating compounds
CN121358478A (zh) 2023-04-19 2026-01-16 吉利德科学公司 衣壳抑制剂的给药方案
KR20250175331A (ko) 2023-04-21 2025-12-16 길리애드 사이언시즈, 인코포레이티드 Prmt5 억제제 및 이의 용도
US20250011352A1 (en) 2023-05-31 2025-01-09 Gilead Sciences, Inc. Solid forms
WO2024249592A1 (en) 2023-05-31 2024-12-05 Gilead Sciences, Inc. Quinazolinyl-indazole derivatives as therapeutic compounds for hiv
CN116444522B (zh) * 2023-06-14 2023-08-25 齐泽(云南)生物科技有限公司 一种姜黄素腺嘌呤衍生化合物
CN116496277B (zh) * 2023-06-14 2023-08-25 齐泽(云南)生物科技有限公司 一种姜黄素2,6-二氨基嘌呤衍生化合物
AU2024306338A1 (en) 2023-06-30 2026-01-08 Gilead Sciences, Inc. Kras modulating compounds
AU2024300557A1 (en) 2023-07-26 2026-02-05 Gilead Sciences, Inc. Parp7 inhibitors
AU2024297978A1 (en) 2023-07-26 2026-02-05 Gilead Sciences, Inc. Parp7 inhibitors
AU2023460182A1 (en) 2023-07-28 2026-02-05 Gilead Sciences, Inc. Weekly regimen of lenacapavir for the treatment and prevention of hiv
AU2023462614A1 (en) 2023-08-23 2026-03-19 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
US20250101042A1 (en) 2023-09-08 2025-03-27 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2025054530A1 (en) 2023-09-08 2025-03-13 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
AR133955A1 (es) 2023-09-26 2025-11-19 Profoundbio Us Co Agentes de unión a ptk7, conjugados de éstos y métodos de uso de los mismos
WO2025080850A1 (en) 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
TW202530227A (zh) 2023-10-11 2025-08-01 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
WO2025080879A1 (en) 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20250154172A1 (en) 2023-11-03 2025-05-15 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20250230163A1 (en) 2023-12-22 2025-07-17 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
TW202547866A (zh) 2024-01-10 2025-12-16 丹麥商珍美寶股份有限公司 Ｓｌｉｔｒｋ６結合劑、其共軛物及使用彼之方法
US20250381289A1 (en) 2024-02-29 2025-12-18 Genmab A/S Egfr and c-met bispecific binding agents, conjugates thereof and methods of using the same
WO2025184447A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
US20250289822A1 (en) 2024-03-01 2025-09-18 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025184609A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Antiviral compounds
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
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
US20250345389A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
WO2025245003A1 (en) 2024-05-21 2025-11-27 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20260007683A1 (en) 2024-06-14 2026-01-08 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2026039365A1 (en) 2024-08-12 2026-02-19 Gilead Sciences, Inc. Kras modulating compounds

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4610699A (en) 1984-01-18 1986-09-09 Sumitomo Electric Industries, Ltd. Hard diamond sintered body and the method for producing the same
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
JPH07330770A (ja) 1994-06-03 1995-12-19 Japan Energy Corp プリン誘導体及びそれを有効成分とする治療剤
KR19990044383A (ko) 1996-07-03 1999-06-25 나가시마 카쭈시게, 노미야마 아키히코 신규 퓨린 유도체
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6329381B1 (en) 1997-11-28 2001-12-11 Sumitomo Pharmaceuticals Company, Limited Heterocyclic compounds
EP1040108B1 (en) 1997-12-19 2004-02-25 Schering Aktiengesellschaft Ortho-anthranilamide derivatives as anti-coagulants
TW572758B (en) 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
JP4160645B2 (ja) 1997-12-24 2008-10-01 大日本住友製薬株式会社 新規アデニン誘導体及びその医薬用途
JP4189048B2 (ja) 1997-12-26 2008-12-03 大日本住友製薬株式会社 複素環化合物
US20040247662A1 (en) 1998-06-25 2004-12-09 Dow Steven W. Systemic immune activation method using nucleic acid-lipid complexes
JP2000159767A (ja) 1998-11-26 2000-06-13 Sumitomo Pharmaceut Co Ltd ８−ヒドロキシアデニン誘導体の新規製造法
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
US20050226845A1 (en) 2004-03-10 2005-10-13 Chih-Ping Liu Method of treatment using interferon-tau
WO2002062767A1 (en) 2001-02-07 2002-08-15 Sumitomo Pharmaceuticals Company, Limited Novel quinazoline derivatives
ATE404561T1 (de) 2001-04-17 2008-08-15 Dainippon Sumitomo Pharma Co Neue adeninderivate
JP2004115416A (ja) 2002-09-25 2004-04-15 Japan Energy Corp 細胞の異常増殖に起因する疾患の治療剤
TWI349671B (en) 2002-09-27 2011-10-01 Dainippon Sumitomo Pharma Co Novel adenine derivative and its use
JP2004137157A (ja) 2002-10-16 2004-05-13 Sumitomo Pharmaceut Co Ltd 新規アデニン誘導体を有効成分として含有する医薬
US6960568B2 (en) 2002-12-17 2005-11-01 Yale University Nucleosides and related processes, pharmaceutical compositions and methods
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7176214B2 (en) 2003-05-21 2007-02-13 Bristol-Myers Squibb Company Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
JP2005089334A (ja) 2003-09-12 2005-04-07 Sumitomo Pharmaceut Co Ltd ８−ヒドロキシアデニン化合物
WO2005038056A1 (en) 2003-10-14 2005-04-28 Intermune, Inc. Combination therapy for the treatment of viral diseases
EP1697389A4 (en) 2003-10-24 2008-12-24 Eisai R&D Man Co Ltd COMPOUNDS AND METHODS FOR TREATING ILLNESS AND SUFFERING TOLL-LIKE RECEPTOR 2 RELATED DISORDERS
AU2004314706A1 (en) 2003-12-11 2005-08-11 University Of Miami Immunotherapy compositions, method of making and method of use thereof
JP4817599B2 (ja) 2003-12-25 2011-11-16 独立行政法人科学技術振興機構 免疫活性増強剤とこれを用いた免疫活性の増強方法
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
WO2005079419A2 (en) 2004-02-17 2005-09-01 The Regents Of The University Of California Methods of treating immunopathological disorders
US7592326B2 (en) 2004-03-15 2009-09-22 Karaolis David K R Method for stimulating the immune, inflammatory or neuroprotective response
JPWO2005092892A1 (ja) 2004-03-26 2008-02-14 大日本住友製薬株式会社 ８−オキソアデニン化合物
TWI392678B (zh) 2004-03-26 2013-04-11 Dainippon Sumitomo Pharma Co ９-取代-８-氧基腺嘌呤化合物
CA2566436C (en) 2004-05-13 2011-05-10 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
JP2008500338A (ja) 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び／又は予防する方法
EP1750715A1 (en) 2004-06-04 2007-02-14 Icos Corporation Methods for treating mast cell disorders
ES2392648T3 (es) 2004-12-30 2012-12-12 3M Innovative Properties Company Compuestos quirales sustituidos que contienen un núcleo 1,2-imidazo-4,5-c condensado
EP1885356A2 (en) 2005-02-17 2008-02-13 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
EP1863538A4 (en) 2005-03-09 2009-01-14 Baylor College Medicine DIRECT INVERSION OF CD4 + T CELL LYMPHOCYTE INHIBITOR FUNCTION VIA TOLL-TYPE 8 RECEIVER SIGNALING
US7498409B2 (en) 2005-03-24 2009-03-03 Schering Corporation Screening assay for TLR7, TLR8 and TLR9 agonists and antagonists
EP1888587A1 (en) 2005-05-04 2008-02-20 Pfizer Limited 2-amido-6-amino-8-oxopurine derivatives as toll-like receptor modulators for the treatment of cancer and viral infections, such as hepatitis c
CA2620182A1 (en) * 2005-08-22 2007-03-01 Dennis A. Carson Tlr agonists
WO2007028129A1 (en) 2005-09-02 2007-03-08 Pfizer Inc. Hydroxy substituted 1h-imidazopyridines and methods
TW200801003A (en) 2005-09-16 2008-01-01 Astrazeneca Ab Novel compounds
TW200745114A (en) 2005-09-22 2007-12-16 Astrazeneca Ab Novel compounds
EP1939201A4 (en) 2005-09-22 2010-06-16 Dainippon Sumitomo Pharma Co NEW ADENINE CONNECTION
JPWO2007034882A1 (ja) 2005-09-22 2009-03-26 大日本住友製薬株式会社 新規アデニン化合物
WO2007034881A1 (ja) 2005-09-22 2007-03-29 Dainippon Sumitomo Pharma Co., Ltd. 新規アデニン化合物
JPWO2007034817A1 (ja) 2005-09-22 2009-03-26 大日本住友製薬株式会社 新規アデニン化合物
EP1939200A4 (en) 2005-09-22 2010-06-16 Dainippon Sumitomo Pharma Co NEW ADENINE CONNECTION
JP5247458B2 (ja) 2005-11-04 2013-07-24 スリーエム・イノベイティブ・プロパティーズ・カンパニー ヒドロキシ及びアルコキシ置換１ｈ−イミダゾキノリン及び方法
US20090317825A1 (en) 2005-12-12 2009-12-24 Elan Pharma International Limited Assay for parkinson's disease therapeutics and enzymatically active parkin preparations useful therein
JP2009528989A (ja) 2006-02-17 2009-08-13 ファイザー・リミテッド Ｔｌｒ７変調剤としての３−デアザプリン誘導体
US8088788B2 (en) 2006-03-15 2012-01-03 3M Innovative Properties Company Substituted fused[1,2] imidazo[4,5-c] ring compounds and methods
US8329721B2 (en) 2006-03-15 2012-12-11 3M Innovative Properties Company Hydroxy and alkoxy substituted 1H-imidazonaphthyridines and methods
EP2017281A4 (en) 2006-04-14 2012-03-14 Kyowa Hakko Kirin Co Ltd AGONISTS AT TOLL-LIKE RECEPTOR 9
WO2007142755A2 (en) 2006-05-31 2007-12-13 The Regents Of The University Of California Purine analogs
US8138172B2 (en) 2006-07-05 2012-03-20 Astrazeneca Ab 8-oxoadenine derivatives acting as modulators of TLR7
ES2437871T3 (es) 2006-07-07 2014-01-14 Gilead Sciences, Inc. Moduladores del receptor tipo toll 7
JP5580592B2 (ja) 2006-09-11 2014-08-27 キュリス，インコーポレイテッド 亜鉛結合部分を含むキナゾリン系ｅｇｆｒインヒビター
WO2008036747A2 (en) 2006-09-21 2008-03-27 Amarillo Biosciences, Inc. Composition and method for immunomodulation
TW200831105A (en) 2006-12-14 2008-08-01 Astrazeneca Ab Novel compounds
ES2552471T3 (es) 2007-02-07 2015-11-30 The Regents Of The University Of California Conjugados de agonistas de TLR sintéticos y usos de los mismos
US20100120799A1 (en) 2007-02-19 2010-05-13 Smithkline Beecham Corporation Purine derivatives as immunomodulators
JP5480637B2 (ja) 2007-03-19 2014-04-23 アストラゼネカ・アクチエボラーグ Ｔｏｌｌ様受容体（ｔｌｒ７）モジュレーターとしての９−置換−８−オキソ−アデニン化合物
EP2139894B1 (en) 2007-03-19 2011-10-26 AstraZeneca AB 9-substituted-8-oxo-adenine compounds as toll-like receptor (tlr7) modulators
AR065784A1 (es) 2007-03-20 2009-07-01 Dainippon Sumitomo Pharma Co Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas.
US8044056B2 (en) 2007-03-20 2011-10-25 Dainippon Sumitomo Pharma Co., Ltd. Adenine compound
AU2008247165B2 (en) 2007-05-08 2011-11-03 Astrazeneca Ab Imidazoquinolines with immuno-modulating properties
JP5395068B2 (ja) 2007-06-29 2014-01-22 ギリアード サイエンシーズ， インコーポレイテッド トール様受容体７の調節物質としてのプリン誘導体およびその使用
ES2359123T3 (es) 2007-08-03 2011-05-18 Pfizer Limited Imidazopiridinonas.
WO2009062059A2 (en) * 2007-11-08 2009-05-14 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
PE20091236A1 (es) 2007-11-22 2009-09-16 Astrazeneca Ab Derivados de pirimidina como immunomoduladores de tlr7
UY31531A1 (es) 2007-12-17 2009-08-03 Sales derivadas de 8-oxoadenina composiciones farmacéuticas que las contienen y su uso en terapia como moduladores de receptor tipo toll (tlr)
AU2008347400B2 (en) 2008-01-15 2014-12-11 Meda Ab Treatment of colon diseases or prevention of colorectal carcinoma with imidazoquinoline derivatives
MX344330B (es) 2008-03-24 2016-12-13 4Sc Ag Imidazoquinolinas substituidas novedosas.
WO2009151910A2 (en) 2008-05-25 2009-12-17 Wyeth Combination product of receptor tyrosine kinase inhibitor and fatty acid synthase inhibitor for treating cancer
US8501734B2 (en) 2008-05-26 2013-08-06 Oncotyrol-Center For Personalized Cancer Medicine Gmbh (Ltd.) Medical intervention in haematological cancers
MX2011001315A (es) 2008-08-04 2011-03-15 Idera Pharmaceuticals Inc Modulacion de la expresion de los receptores del tipo toll 7 mediante oligonucleotidos antisentido.
UA103195C2 (uk) 2008-08-11 2013-09-25 Глаксосмитклайн Ллк Похідні пурину для застосування у лікуванні алергій, запальних та інфекційних захворювань
WO2010018132A1 (en) 2008-08-11 2010-02-18 Smithkline Beecham Corporation Compounds
EA201100114A1 (ru) 2008-08-11 2011-10-31 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Производные пурина для применения в лечении аллергических, воспалительных и инфекционных заболеваний
KR101616396B1 (ko) 2008-08-11 2016-04-28 글락소스미스클라인 엘엘씨 신규의 아데닌 유도체
WO2010018130A1 (en) 2008-08-11 2010-02-18 Smithkline Beecham Corporation Purine derivatives for use in the treatment of allergic, inflammatory and infectious diseases
BRPI0919937A2 (pt) 2008-10-24 2016-02-16 Glaxosmithkline Biolog Sa composto, e, método para melhorar a atividade de adjuvante de uma imidazoquinolina
SG173617A1 (en) 2009-02-11 2011-09-29 Univ California Toll-like receptor modulators and treatment of diseases
GB0908772D0 (en) 2009-05-21 2009-07-01 Astrazeneca Ab New salts 756
JP5913093B2 (ja) 2009-05-21 2016-04-27 アストラゼネカ アクチボラグ 新規ピリミジン誘導体と、癌とさらなる疾患の治療におけるそれらの使用
CA2768195A1 (en) 2009-08-07 2011-02-10 Glaxosmithkline Biologicals Sa Lipidated oxoadenine derivatives
CN102666541B (zh) 2009-10-22 2015-11-25 吉里德科学公司 用于治疗特别是病毒感染的嘌呤或脱氮嘌呤的衍生物
EP2507237A1 (en) 2009-12-03 2012-10-10 Dainippon Sumitomo Pharma Co., Ltd. Imidazoquinolines which act via toll - like receptors (tlr)
EA021048B1 (ru) 2010-02-10 2015-03-31 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Малеат 6-амино-2-{[(1s)-1-метилбутил]окси}-9-[5-(1-пиперидинил)пентил]-7,9-дигидро-8н-пурин-8-она
US8575340B2 (en) 2010-02-10 2013-11-05 Glaxosmithkline Llc Purine derivatives and their pharmaceutical uses
JP2013147428A (ja) 2010-04-27 2013-08-01 Dainippon Sumitomo Pharma Co Ltd 新規２−ヘテロアリール単環ピリミジン誘導体

Also Published As

Publication number Publication date
US8507507B2 (en) 2013-08-13
PT2491035T (pt) 2017-10-30
JP2013508373A (ja) 2013-03-07
EA020488B1 (ru) 2014-11-28
CR20120255A (es) 2012-07-02
JP5694345B2 (ja) 2015-04-01
NO2491035T3 (es) 2018-01-27
CL2012000988A1 (es) 2012-09-14
CA2777824C (en) 2016-11-29
ECSP12011915A (es) 2012-07-31
WO2011049825A1 (en) 2011-04-28
AU2010310813A1 (en) 2012-05-03
AP2012006227A0 (en) 2012-04-30
US8962652B2 (en) 2015-02-24
AU2010310813B2 (en) 2015-06-18
IL218747A (en) 2016-02-29
EP2491035B1 (en) 2017-08-30
IL218747A0 (en) 2012-06-28
PE20121091A1 (es) 2012-08-17
US20140128389A1 (en) 2014-05-08
IN2012DN02984A (es) 2015-07-31
ZA201202858B (en) 2012-12-27
SI2491035T1 (sl) 2017-10-30
KR20120105448A (ko) 2012-09-25
EA201290131A1 (ru) 2012-08-30
CA2777824A1 (en) 2011-04-28
AP3103A (en) 2015-01-31
EP2491035A1 (en) 2012-08-29
SG10201406813RA (en) 2014-11-27
KR101793300B1 (ko) 2017-11-02
US9161934B2 (en) 2015-10-20
PL2491035T3 (pl) 2018-01-31
CN102666541A (zh) 2012-09-12
US20110098248A1 (en) 2011-04-28
CN102666541B (zh) 2015-11-25
US20150126509A1 (en) 2015-05-07
CO6531469A2 (es) 2012-09-28
NZ598933A (en) 2013-04-26
BR112012009329A2 (pt) 2016-06-07
MX2012004706A (es) 2012-06-08

Similar Documents

Publication Publication Date Title
ES2644286T3 (es) Derivados de purina o deazapurina útiles para el tratamiento de (entre otros) infecciones víricas
AR091079A1 (es) Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
AR093584A1 (es) Inmunoglobulinas heterodimericas
PE20210668A1 (es) Analogos de carba-nucleosidos sustituidos con 2&#39;-fluoro antivirales
PE20230684A1 (es) Analogos de carba-nucleosidos sustituidos con 2&#39;-fluoro como inhibidores de la arn polimerasa
EA201170374A1 (ru) Производные замещенных трициклических кислот в качестве агонистов рецептора s1p1, применимые при лечении аутоиммунных и воспалительных заболеваний
JP2009533348A5 (es)
UY30169A1 (es) Nuevos productos farmacéuticos
CY1118319T1 (el) Αλατα και πολυμορφα της 8-φθορο-2-{4-[(μεθυλαμινο)μεθυλο]φαινυλο}-1,3,4,5-τετραϋδρο-6η-αζεπινο[5,4,3-cd]ινδολο-6-ονης
RU2011121876A (ru) Пиразолопиримидиновые соединения-ингибиторы jak и способы
MD4521B1 (ro) Compuşi antivirali pe bază de imidazolil-dihidroizocromeno-naftoimidazoli condensaţi
RU2015100198A (ru) Хиральный адъювант нуклеиновой кислоты
EP2621931A4 (en) TETRAZYCLIC INDOLE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C VIRUS INFECTIONS
NI200700043A (es) Inhibidores de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que los usan.
ECSP12012067A (es) Inhibidores del virus de la hepatitis c
WO2014022566A3 (en) Synthesis of deuterated ribo nucleosides, n-protected phosphoramidites, and oligonucleotides
MX348759B (es) Metodos y composiciones para inhibicion de polimerasa.
CO6470789A2 (es) N-[2´r)-2´-desoxi-2´fluoro-2´-metil-p-fenil-5´uridilil]-l-alanina 1 metiletil éster y proceso para su producción
BR112013020273A2 (pt) oligonucleotídeos antissenso
JP2012000112A5 (es)
UA110093C2 (uk) Карбануклеозидні аналоги для противірусного лікування
IN2014KN00943A (es)
PE20130399A1 (es) COMPUESTOS DE NUCLEO IMIDAZO[1,2-a]PIRAZINA O 5,6,7,8-TETRAHIDROIMIDAZO[1,2-a]PIRAZINA SUSTITUIDOS Y COMPOSICIONES DE LOS MISMOS, UTILES EN EL TRATAMIENTO DE ENFERMEDADES PARASITICAS
JP6968696B2 (ja) 異常なレベル及び／又は活性のｉｆｐ３５ファミリーのタンパク質に関連する疾患又は障害を治療及び／又は予防するための方法及び組成物
DOP2007000030A (es) Nuevos productos farmacéuticos