AR069413A2 - Derivados de hetero- pentaciclo- fenilo fusionados, composicion farmaceutica que los comprende y usos para preparar un medicamento util para el tratamiento de una condicion mediada por p 38 - Google Patents

Derivados de hetero- pentaciclo- fenilo fusionados, composicion farmaceutica que los comprende y usos para preparar un medicamento util para el tratamiento de una condicion mediada por p 38

Info

Publication number
AR069413A2
AR069413A2 ARP080105084A ARP080105084A AR069413A2 AR 069413 A2 AR069413 A2 AR 069413A2 AR P080105084 A ARP080105084 A AR P080105084A AR P080105084 A ARP080105084 A AR P080105084A AR 069413 A2 AR069413 A2 AR 069413A2
Authority
AR
Argentina
Prior art keywords
unsubstituted
substituted
heteroalyl
heteroalkoxy
heteroalkynyl
Prior art date
Application number
ARP080105084A
Other languages
English (en)
Inventor
James Rizzi
Mark Munson
Youngboo Kim
Martha Rodriguez
David A Mareska
Ganghyeok Kim
Robert Groneberg
Guy Vigers
Chang Rao
Devan Balachari
Darren Harvey
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR069413A2 publication Critical patent/AR069413A2/es

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • 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
    • 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
    • C07D403/12—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
    • C07D405/12—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
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Dichos compuestos son utiles para tratamientos terapéuticos en enfermedades autoinmunes, proliferativas e infecciosas, inflamatorias, oseo-destructivas, viral y neurodegenerativas. Reivindicacion 1: Un compuesto derivado de hetero-pentaciclo-fenilo fusionados que incluye enantiomeros resueltos, diastereomeros, solvatos y sales farmacéuticamente aceptables de él, dicho compuesto caracterizado porque tiene la formula (1) en donde: Y es C o N; W es C, N, S, u O, siempre que W sea N, S, u O cuando Y es C, y que W sea C cuando Y es N; U es CH o N; V es C-E o N; X es O, S, SO, SO2, NR7, C=O, CHR7, -C=NOR1, -C=CHR1, o CHOR1; R1 es H, PO3H2, SO3H2, alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1, en donde dicho alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1 puede ser sustituido o no sustituido; Z es alquileno C1-4, o alquenileno o alquinileno C2-4, en donde dichos alquileno, alquenileno, o alquinileno pueden ser sustituidos o no sustituidos; R7 es H o metilo sustituido o no sustituido; Ar1 es arilo o heteroarilo, cada uno de los cuales puede ser sustituido o no sustituido; A es H, OH, un grupo protector de amina, Zn-NR2R3, Zn-NR2(C=O)R2, Zn-SO2R2, Zn-SOR2, Zn-SR2, Zn-OR2, Zn-(C=O)R2, Zn-(C=O)OR2, Zn-O-(C=O)R2, alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo o Zn-Ar1, en donde dicho alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo o Zn-Ar1 puede ser sustituido o no sustituido; R2 y R3 son independientemente H, OH, un grupo protector de amina, un grupo protector de alcohol, un grupo protector de ácido, un grupo protector de azufre, alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1, en donde dicho alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1 puede ser sustituido o no sustituido; o R2 junto con R3 y N forma un anillo de heterociclo saturado o parcialmente insaturado que tiene 1 o más heteroátomos en dicho anillo, en donde dicho heterociclo puede ser sustituido o no sustituido y en donde dicho heterociclo puede ser fusionado a un anillo aromático; B es H o NH2; E es H, Zn-NR2R3, Zn-(C=O)R4, Zn-(C=O)R5, Zn-NR5(C=O)R5, Zn-O(C=O)R5, Zn-OR5, Zn-SO2R5, Zn-SO2R4, Zn-SOR5, Zn-SR5, Zn-NH(C=O)NHR5, o R5; R4 es un aminoácido natural o no natural sustituido o no sustituido, un aminoácido natural o no natural protegido, NH(CHR6)(CH2)mOR5 donde m es un numero entero de 1 a 4, o NR2R3; R5 es H, OH, un grupo protector de amina, un grupo protector de alcohol, un grupo protector de ácido, un grupo protector de azufre, alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1, en donde dicho alquilo, alilo, alquenilo, alquinilo, heteroalquilo, heteroalilo, heteroalquenilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Zn-Ar1 puede ser sustituido o no sustituido; R6 es una cadena lateral de aminoácido natural, Zn-NR2R3, Zn-OR5, Zn-SO2R5, Zn-SOR5, o Zn-SR5; y n es 0 o 1; siempre que: cuando E es hidrogeno y el compuesto de la formula (1) es un compuesto de la formula (2) entonces A es diferente de H; cuando E es hidrogeno y el compuesto de la formula (1) es un compuesto de la formula (3) entonces el grupo de la formula (3) representada por Ar1 es arilo que puede ser sustituido o no sustituido, y A es diferente de H; y cuando E es H y el compuesto de la formula (1) es un compuesto de la formula (4) entonces A es OH, Zn-NR2R3, Zn-NR2(C=O)R2, Zn-SO2R2, Zn-SOR2, Zn-SR2, Zn-OR2, Zn-(C=O)R2, Zn-(C=O)OR2, Zn-O-(C=O)R2, alquilo, alilo, alquinilo, heteroalquilo, heteroalilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Z-Ar1, en donde dicho alquilo, alilo, alquinilo, heteroalquilo, heteroalilo, heteroalquinilo, alcoxi, heteroalcoxi, Zn-cicloalquilo, Zn-heterocicloalquilo, o Z-Ar1 puede ser sustituido o no sustituido; y con la condicion adicional de que el compuesto de la formula (1) no sea ácido 2-(1-metil-1H-indazol-5-ilamino)benzoico, ácido 5-(2,4-diclorofenoxi)-1H-indazol-1-acético, 3-metil-6-fenilsulfonilbenzisoxazol o 6-(2-cloro-4-trifluorometilfenoxi)-3-metilbencisoxazol.
ARP080105084A 2003-03-03 2008-11-21 Derivados de hetero- pentaciclo- fenilo fusionados, composicion farmaceutica que los comprende y usos para preparar un medicamento util para el tratamiento de una condicion mediada por p 38 AR069413A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10/378,164 US7135575B2 (en) 2003-03-03 2003-03-03 P38 inhibitors and methods of use thereof
US10/688,849 US20040180896A1 (en) 2003-03-03 2003-10-15 P38 inhibitors and methods of use thereof

Publications (1)

Publication Number Publication Date
AR069413A2 true AR069413A2 (es) 2010-01-20

Family

ID=32926418

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP040100656A AR043451A1 (es) 2003-03-03 2004-03-02 Compuestos de indazol como inhibidores de p38 y su empleo como medicamentos
ARP080105084A AR069413A2 (es) 2003-03-03 2008-11-21 Derivados de hetero- pentaciclo- fenilo fusionados, composicion farmaceutica que los comprende y usos para preparar un medicamento util para el tratamiento de una condicion mediada por p 38

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP040100656A AR043451A1 (es) 2003-03-03 2004-03-02 Compuestos de indazol como inhibidores de p38 y su empleo como medicamentos

Country Status (28)

Country Link
US (5) US7135575B2 (es)
EP (4) EP1997809B1 (es)
JP (2) JP5424657B2 (es)
KR (3) KR101236608B1 (es)
CN (2) CN101759645B (es)
AR (2) AR043451A1 (es)
AT (1) ATE410421T1 (es)
AU (1) AU2009225343B2 (es)
BR (2) BRPI0407993B8 (es)
CL (2) CL2004000416A1 (es)
CO (1) CO5670351A2 (es)
CY (4) CY1108661T1 (es)
DE (1) DE602004016970D1 (es)
DK (5) DK1997809T3 (es)
DO (1) DOP2009000155A (es)
EG (1) EG27049A (es)
ES (4) ES2534859T3 (es)
IL (3) IL170527A (es)
IS (1) IS2959B (es)
NO (1) NO20085373L (es)
NZ (3) NZ582796A (es)
PA (1) PA8596901A1 (es)
PL (1) PL219742B1 (es)
PT (4) PT1997809E (es)
SI (5) SI1606283T1 (es)
TW (2) TWI346663B (es)
UA (2) UA103873C2 (es)
ZA (1) ZA200507874B (es)

Families Citing this family (367)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7893101B2 (en) * 2002-03-20 2011-02-22 Celgene Corporation Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions thereof, and uses thereof
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
EP1606283B1 (en) * 2003-03-03 2008-10-08 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
US7553827B2 (en) * 2003-08-13 2009-06-30 Depuy Spine, Inc. Transdiscal administration of cycline compounds
US7429378B2 (en) * 2003-05-13 2008-09-30 Depuy Spine, Inc. Transdiscal administration of high affinity anti-MMP inhibitors
US8273347B2 (en) * 2003-05-13 2012-09-25 Depuy Spine, Inc. Autologous treatment of degenerated disc with cells
US7344716B2 (en) * 2003-05-13 2008-03-18 Depuy Spine, Inc. Transdiscal administration of specific inhibitors of pro-inflammatory cytokines
EP1663237B1 (en) * 2003-09-10 2013-06-19 Icagen, Inc. Fused ring heterocycles as potassium channel modulators
BRPI0415500A (pt) * 2003-10-17 2007-04-10 Incyte Corp hidroxamatos cìclicos substituìdos como inibidores de metaloproteinases de matriz
US8895540B2 (en) * 2003-11-26 2014-11-25 DePuy Synthes Products, LLC Local intraosseous administration of bone forming agents and anti-resorptive agents, and devices therefor
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
CN1926139A (zh) * 2004-02-27 2007-03-07 霍夫曼-拉罗奇有限公司 稠合吡唑衍生物
RU2006134022A (ru) * 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные индазола и содержащие их фармацевтические композиции
KR100844864B1 (ko) * 2004-02-27 2008-07-09 에프. 호프만-라 로슈 아게 헤테로아릴-융합 피라졸로 유도체
EP1773766B1 (en) * 2004-07-15 2014-04-02 Tetralogic Pharmaceuticals Corporation Iap binding compounds
PL1778686T3 (pl) * 2004-08-12 2009-04-30 Pfizer Pochodne triazolopirydynylosulfanylowe jako inhibitory kinazy MAP P38
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
US7517906B2 (en) 2005-02-25 2009-04-14 Tetralogic Pharmaceuticals Corporation Dimeric IAP inhibitors
CN101146575A (zh) * 2005-03-22 2008-03-19 依奈特制药公司 新类型的γδT细胞活化剂及其应用
US8362075B2 (en) * 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
JP2008542301A (ja) 2005-05-26 2008-11-27 メタバシス・セラピューティクス・インコーポレイテッド 脂肪性肝疾患の処置のための甲状腺ホルモン様薬剤
US8343953B2 (en) * 2005-06-22 2013-01-01 Astex Therapeutics Limited Pharmaceutical compounds
JP5345842B2 (ja) * 2005-06-23 2013-11-20 アステックス・セラピューティクス・リミテッド プロテインキナーゼモジュレーターとしてのピラゾール誘導体を含む医薬組み合わせ
ITRM20050344A1 (it) * 2005-06-30 2007-01-01 Luca Maria De Sali o complessi di sostanze metil-donatrici con acido fitico o suoi derivati e relativo metodo di sintesi.
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
US7999113B2 (en) 2005-08-11 2011-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN101248077B (zh) * 2005-08-25 2011-07-20 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
MX2008002588A (es) * 2005-08-25 2008-03-18 Hoffmann La Roche Inhibidores de p38-map-cinasa y los metodos para utilizarlos.
WO2007032556A1 (ja) * 2005-09-14 2007-03-22 Santen Pharmaceutical Co., Ltd. グルココルチコイド受容体結合活性を有する新規１，２−ジヒドロキノリン誘導体
EP1931668A2 (en) * 2005-09-16 2008-06-18 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b]pyridines as phosphodiesterase inhibitors
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
CN101365690A (zh) * 2005-10-12 2009-02-11 沃泰克斯药物股份有限公司 作为电压门控离子通道调控剂的联苯衍生物
US7939528B2 (en) * 2005-10-13 2011-05-10 Glaxosmithkline Llc Heterocycle compounds
DK2090575T3 (da) 2005-11-15 2011-05-23 Array Biopharma Inc Fremgangsmåder og mellemprodukter til fremstillingen af N4 phenylquinazolin-4-aminderivater
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
RU2008133161A (ru) * 2006-01-13 2010-02-20 Фармасайкликс, Инк. (Us) Ингибиторы тирозин киназ и их применение
RS52298B (en) * 2006-01-31 2012-12-31 Array Biopharma Inc. KINASE INHIBITORS AND PROCEDURE FOR THEIR USE
US8541406B2 (en) * 2006-02-07 2013-09-24 Nv Remynd Thiadiazole derivatives for the treatment of neurodegenerative diseases
CN107235980A (zh) 2006-05-04 2017-10-10 勃林格殷格翰国际有限公司 多晶型
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
WO2008005651A2 (en) * 2006-06-08 2008-01-10 Decode Chemistry, Inc. Cyclic carboxylic acid rhodanine derivatives for the treatment and prevention of tuberculosis
US7727978B2 (en) * 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
US20090298811A1 (en) * 2006-09-12 2009-12-03 Pfizer Inc Benzimidazolone derivatives
EP2076501B8 (en) 2006-09-25 2019-11-13 PTC Therapeutics, Inc. Crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid
US8008498B2 (en) * 2006-11-14 2011-08-30 Santen Pharmaceutical Co., Ltd. 1,2-dihydroquinoline derivative having substituted phenylamino lower alkyl group and ester-introduced phenyl group as substituents
TW200831085A (en) * 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
CA2676437A1 (en) * 2007-01-18 2008-07-24 Evolva Sa Substituted 1,3-dioxanes and their uses
DE102007009494A1 (de) * 2007-02-27 2008-08-28 Bayer Healthcare Ag Substituierte 4-Aryl-1, 4-dihydro-1,6-naphthyridinamide und ihre Verwendung
US20110105602A2 (en) 2007-03-08 2011-05-05 Daria Mochly-Rosen Mitochondrial Aldehyde Dehydrogenase-2 Modulators and Methods of Use Thereof
US8030344B2 (en) * 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
UA97837C2 (ru) * 2007-03-23 2012-03-26 Эбботт Гмбх Унд Ко. Кг Соединения хинолина для лечения нарушений, которые реагируют на модуляцию рецептора серотонина 5-ht6
WO2008118991A1 (en) * 2007-03-26 2008-10-02 University Of Southern California Usc Stevens Methods and compositions for inducing apoptosis by stimulating er stress
US8343995B2 (en) 2007-04-27 2013-01-01 Cydex Pharmaceuticals, Inc. Formulations containing clopidogrel and sulfoalkyl ether cyclodextrin and methods of use
EP2011786A1 (en) * 2007-07-05 2009-01-07 Laboratorios del Dr. Esteve S.A. Indane-amine derivatives, their preparation and use as medicaments
DE102007032347A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Aminoacyl-Prodrugs
US8202899B2 (en) * 2007-07-25 2012-06-19 Array Biopharma Inc. Pyrazole urea derivatives used as kinase inhibitors
TW200908984A (en) * 2007-08-07 2009-03-01 Piramal Life Sciences Ltd Pyridyl derivatives, their preparation and use
US8227492B2 (en) * 2007-08-07 2012-07-24 Cadila Healthcare Limited Sulfoxamine derivatives as factor Xa inhibitors
WO2009026579A1 (en) * 2007-08-23 2009-02-26 Cornell Research Foundation, Inc. Proteasome inhibitors and their use in treating pathogen infection and cancer
US20100292292A1 (en) * 2007-09-13 2010-11-18 Link Medicine Corporation Treatment of Neurodegenerative Diseases Using Indatraline Analogs
US8466187B2 (en) 2007-09-18 2013-06-18 Thermolife International, Llc Amino acid compositions
US10646508B1 (en) * 2007-09-18 2020-05-12 Thermolife International, Llc Method of safely administering nitrate dietary supplements and compositions
US10426750B1 (en) 2007-09-18 2019-10-01 Thermolife International, Llc Amino acid supplement formulations
US10435356B1 (en) 2007-09-18 2019-10-08 Thermolife International, Llc Amino acid compositions
JP2011503232A (ja) 2007-11-20 2011-01-27 ザ ブリガム アンド ウィメンズ ホスピタル インコーポレイテッド 免疫応答の調節
FR2924712B1 (fr) * 2007-12-06 2012-12-21 Univ Maine Derives du gossypol et de l'apogossypol, leurs preparations et leurs applications
EP2070929A1 (en) 2007-12-11 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
AR069650A1 (es) * 2007-12-14 2010-02-10 Actelion Pharmaceuticals Ltd Derivados de aminopirazol como agonistas no peptidicos del receptor alx humano
US8986696B2 (en) * 2007-12-21 2015-03-24 Depuy Mitek, Inc. Trans-capsular administration of p38 map kinase inhibitors into orthopedic joints
US20090162351A1 (en) * 2007-12-21 2009-06-25 Depuy Spine, Inc. Transdiscal administration of inhibitors of p38 MAP kinase
EP2257171B1 (en) * 2008-02-25 2016-02-10 Merck Sharp & Dohme Corp. Tetrahydro-1h-pyrrolo-fused pyridones
WO2009111277A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Imdizo [4. 5-b] pyridine derivatives used as raf inhibitors
EA022505B1 (ru) * 2008-03-25 2016-01-29 Эффектис Фармасьютиклз Аг Новые p2x7r антагонисты и их применение
US20090246234A1 (en) * 2008-04-01 2009-10-01 Benjamin Johnson Therapeutic Treatment Using Niacin for Skin Disorders
AR071175A1 (es) 2008-04-03 2010-06-02 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
US8501734B2 (en) * 2008-05-26 2013-08-06 Oncotyrol-Center For Personalized Cancer Medicine Gmbh (Ltd.) Medical intervention in haematological cancers
PT2318419E (pt) 2008-06-17 2015-08-25 Millennium Pharm Inc Compostos de ésteres de boronato e suas composições farmacêuticas
CN102123986B (zh) * 2008-06-25 2013-08-28 学校法人庆应义塾 药物组合物
MX2011001319A (es) * 2008-08-06 2011-04-05 Vertex Pharma Inhibidores de aminopiridina cinasa.
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
ES2477552T3 (es) 2008-09-08 2014-07-17 The Board Of Trustees Of The Leland Stanford Junior University Moduladores de la actividad de la aldehidodeshidrogenasa y métodos de uso de los mismos
EP2344195A2 (en) 2008-09-10 2011-07-20 Boehringer Ingelheim International GmbH Combination therapy for the treatment of diabetes and related conditions
KR100905419B1 (ko) * 2008-09-11 2009-07-02 연세대학교 산학협력단 세스퀴테르펜 유도체의 용도
EP3023097A1 (en) * 2008-10-01 2016-05-25 Novartis AG Smoothened antagonism for the treatment of hedgehog pathway-related disorders
CN102176906B (zh) * 2008-10-09 2014-07-02 新树株式会社 Panduratin衍生物或提琴形凹唇姜提取物的全新用途
AR074797A1 (es) * 2008-10-10 2011-02-16 Japan Tobacco Inc Compuesto de fluoreno , composiciones farmaceuticas , inhibidores de pdhk y pdhk2 , metodos de tratamiento , usos de los mismos y kit comercial
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
JP2012506856A (ja) * 2008-10-28 2012-03-22 ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ アルデヒドデヒドロゲナーゼのモジュレーターおよびその使用方法
DE102008059133A1 (de) * 2008-11-26 2010-05-27 Merck Patent Gmbh Difluorphenyl-diacylhydrazid-derivate
KR20100060189A (ko) * 2008-11-27 2010-06-07 국립암센터 에타크리닉 산을 포함하는 트란스글루타미나제 관련 질환 예방 또는 치료용 조성물 및 그를 이용하는 트란스글루타미나제 관련 질환 예방 또는 치료 방법
US8362080B2 (en) * 2008-12-18 2013-01-29 Baylor College Of Medicine Increasing glutathione levels for therapy
TWI432188B (zh) * 2008-12-19 2014-04-01 Merz Pharma Gmbh & Co Kgaa 供治療發炎性皮膚疾病之１－胺基－烷基環己烷衍生物類
CN107011345A (zh) 2008-12-23 2017-08-04 勃林格殷格翰国际有限公司 有机化合物的盐形式
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
PT2376077T (pt) * 2009-01-12 2017-06-23 Biokier Inc Composição e método para tratamento de diabetes
US9006288B2 (en) 2009-01-12 2015-04-14 Biokier, Inc. Composition and method for treatment of diabetes
US9314444B2 (en) * 2009-01-12 2016-04-19 Biokier, Inc. Composition and method for treatment of NASH
WO2010081488A1 (en) * 2009-01-15 2010-07-22 Humanitas Mirasole S.P.A. Nitric oxide furoxan derivative compounds endowed with antitumoral activity
US8993808B2 (en) 2009-01-21 2015-03-31 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
US20100204329A1 (en) * 2009-02-06 2010-08-12 Mcfaul William J Method of using and establishing an absorption rate level and a neuron firing level
US20120046364A1 (en) * 2009-02-10 2012-02-23 Metabasis Therapeutics, Inc. Novel Sulfonic Acid-Containing Thyromimetics, and Methods for Their Use
ES2345241B1 (es) 2009-03-16 2011-09-08 Lipopharma Therapeutics Uso de 2-hidroxiderivados de acidos grasos poliinsaturados como medicamentos.
EP2411001B1 (en) * 2009-03-23 2018-01-17 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
AR076752A1 (es) * 2009-05-07 2011-07-06 Gruenenthal Chemie Fenilureas y fenilamidas sustituidas como ligandos del receptor de vanilloides.
US8946204B2 (en) 2009-05-07 2015-02-03 Gruenenthal Gmbh Substituted phenylureas and phenylamides as vanilloid receptor ligands
EP3100728B1 (en) 2009-05-13 2019-11-20 Cydex Pharmaceuticals, Inc. Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same
CN102639133B (zh) 2009-06-12 2015-03-11 联合治疗公司 亚氨基糖和治疗布尼亚病毒性疾病以及披膜病毒性疾病的方法
US8283372B2 (en) 2009-07-02 2012-10-09 Tetralogic Pharmaceuticals Corp. 2-(1H-indol-3-ylmethyl)-pyrrolidine dimer as a SMAC mimetic
CN102066372B (zh) * 2009-08-24 2014-09-17 苏州爱斯鹏药物研发有限责任公司 含脲基的5，6元杂芳双环化合物作为激酶抑制剂
WO2011032320A1 (en) * 2009-09-21 2011-03-24 F. Hoffmann-La Roche Ag Novel alkene oxindole derivatives
CA2772188A1 (en) * 2009-09-23 2011-03-31 Pfizer Inc. Gpr 119 modulators
AU2010297557C1 (en) 2009-09-25 2017-04-06 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
US9457029B2 (en) 2009-11-27 2016-10-04 Boehringer Ingelheim International Gmbh Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin
CA2788078A1 (en) * 2010-01-26 2011-08-04 Yissum Research Development Company Of The Hebrew University Of Jerusale M Ltd. Compositions and methods for prevention and treatment of pulmonary hypertension
US8563610B2 (en) * 2010-02-04 2013-10-22 Rutgers, The State of New Jersey Polyunsaturated fatty acids interactions and oxidative stress disorders
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
EP2533642A4 (en) 2010-02-11 2013-08-07 Univ Vanderbilt BENZOOXAZOLE AND AZABENOX OXAZOLE AS ALLOSTERIC MGLUR4 POTENTRANS AND COMPOSITIONS AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTIONS
DK2534150T3 (en) 2010-02-12 2017-06-12 Chimerix Inc METHODS OF TREATING VIRUS INFECTION
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
US9616058B2 (en) 2010-02-24 2017-04-11 Oryzon Genomics, S.A. Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use
MX2012010212A (es) * 2010-03-08 2012-12-05 Spectrum Pharmaceuticals Inc Terapias inhibidoras de autofagia basadas en tioxantona para tratar el cancer.
JP5868948B2 (ja) * 2010-04-19 2016-02-24 オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． リジン特異的脱メチル化酵素１阻害薬およびその使用
US20130231360A1 (en) * 2010-04-22 2013-09-05 The Brigham And Women S Hospital, Inc. Beta-Carbolines as Inhibitors of Haspin and DYRK Kinases
CA2797601A1 (en) 2010-04-26 2011-11-10 Chimerix, Inc. Methods of treating retroviral infections and related dosage regimes
US20130035332A1 (en) * 2010-04-29 2013-02-07 Layton Mark E Substituted 1,3-Benzothiazol-2(3H)-Ones and [1,3]Thiazolo[5,4-B]Pyridin-2(IH)-Ones as Positive Allosteric Modulators of MGLUR2
KR101927068B1 (ko) 2010-05-05 2018-12-10 베링거 인겔하임 인터내셔날 게엠베하 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법
GB201008005D0 (en) * 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
EP2569273B1 (en) * 2010-05-14 2018-04-04 Agency For Science, Technology And Research Novel antimicrobial compounds and uses thereof
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
CN104557568B (zh) * 2010-05-27 2017-04-12 塔加西普特公司 烟碱受体非竞争性拮抗剂
GB201010359D0 (en) * 2010-06-21 2010-08-04 Univ Nottingham Compounds for treating proliferative disorders
CN102971005A (zh) 2010-06-24 2013-03-13 贝林格尔.英格海姆国际有限公司 糖尿病治疗
ES2691671T3 (es) * 2010-06-24 2018-11-28 Alkermes Pharma Ireland Limited Profármacos de compuestos NH-acídicos: derivados de éster, carbonato, carbamato y fosfonato
TW201204733A (en) * 2010-06-25 2012-02-01 Kowa Co Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same
US8846671B2 (en) * 2010-07-01 2014-09-30 Guangzhou Institute Of Biomedicine And Health, Chinese Academy Of Sciences Heterocyclic alkynyl benzene compounds and medical compositions and uses thereof
EP2593458A1 (en) * 2010-07-13 2013-05-22 Bayer Intellectual Property GmbH Bicyclic pyrimidines
US8987273B2 (en) 2010-07-28 2015-03-24 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-B]pyridazines
NO2598482T3 (es) 2010-07-29 2018-09-01
EP2598480B1 (en) 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
KR101760158B1 (ko) * 2010-07-29 2017-07-20 아스텔라스세이야쿠 가부시키가이샤 축환 피리딘 화합물
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
PL392436A1 (pl) * 2010-09-17 2012-03-26 Adamed Spółka Z Ograniczoną Odpowiedzialnością Pochodne arylosulfonamidów do leczenia chorób odśrodkowego układu nerwowego
WO2012042915A1 (en) * 2010-10-01 2012-04-05 Raqualia Pharma Inc. Sulfamoyl benzoic acid heterobicyclic derivatives as trpm8 antagonists
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
JP5826856B2 (ja) * 2010-10-20 2015-12-02 ビオタ サイエンティフィック マネージメント ピーティーワイ リミテッド ウイルスポリメラーゼ阻害剤
TWI537258B (zh) * 2010-11-05 2016-06-11 百靈佳殷格翰國際股份有限公司 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜環芳基羰基衍生物
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
HUE028967T2 (en) * 2010-11-24 2017-01-30 Merck Patent Gmbh Kinozalin carboxamide azetidines
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
US9096504B2 (en) * 2010-12-01 2015-08-04 Washington State University Controlled chemical release of hydrogen sulfide
US8796338B2 (en) 2011-01-07 2014-08-05 Elcelyx Therapeutics, Inc Biguanide compositions and methods of treating metabolic disorders
US9211263B2 (en) 2012-01-06 2015-12-15 Elcelyx Therapeutics, Inc. Compositions and methods of treating metabolic disorders
US9572784B2 (en) 2011-01-07 2017-02-21 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
US11974971B2 (en) 2011-01-07 2024-05-07 Anji Pharmaceuticals Inc. Compositions and methods for treating metabolic disorders
US9480663B2 (en) 2011-01-07 2016-11-01 Elcelyx Therapeutics, Inc. Biguanide compositions and methods of treating metabolic disorders
US11759441B2 (en) 2011-01-07 2023-09-19 Anji Pharmaceuticals Inc. Biguanide compositions and methods of treating metabolic disorders
BR112013017411B1 (pt) 2011-01-07 2022-03-22 Anji Pharma (Us) Llc Uso de uma composição compreendendo metformina ou um sal da mesma
EP2668951B9 (en) * 2011-01-25 2017-03-15 Viviabiotech, S.L. 1,2,4-oxadiazole derivatives as drugs modulating the glp-1 peptide receptor
WO2012107498A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative disorders
US20120208872A1 (en) * 2011-02-11 2012-08-16 Taipei Medical University Use of tea polyphenols for treating and/or preventing nicotine or nicotine-derived compounds or estrogen induced breast cancer
BR122021002201A8 (pt) * 2011-02-25 2023-04-11 Merck Sharp & Dohme Composto, composição, uso de um composto, e, método de tratamento de um distúrbio, condição ou doença
US8642655B2 (en) * 2011-03-09 2014-02-04 Benjamin Johnson Systems and methods for preventing cancer and treating skin lesions
SG193509A1 (en) 2011-03-18 2013-10-30 Corcept Therapeutics Inc Pyrimidine cyclohexyl glucocorticoid receptor modulators
US9018257B2 (en) * 2011-03-24 2015-04-28 Bar Ilan University 5-aminolevulinic acid derivatives, methods for their preparation and uses thereof
US8791112B2 (en) * 2011-03-30 2014-07-29 Arrien Pharmaceuticals Llc Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-B] pyridine and pyrazolo [3, 4-B] pyridine derivatives as protein kinase inhibitors
US8802731B2 (en) 2011-04-13 2014-08-12 Thermolife International, Llc N-acetyl beta alanine methods of use
EP2700643B1 (en) * 2011-04-19 2016-11-23 Daiichi Sankyo Company, Limited Tetrahydrothiazepine derivative
US10457659B2 (en) 2011-04-29 2019-10-29 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for increasing proliferation of adult salivary stem cells
EP2524694A1 (en) * 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
US8487008B2 (en) * 2011-06-22 2013-07-16 Universita Degli Studi Di Padova Treatment of muscular dystrophies and associated conditions by administration of monoamine oxidase inhibitors
WO2012177263A1 (en) 2011-06-24 2012-12-27 Intra-Cellular Therapies, Inc. Compounds and methods of prophylaxis and treatment regarding nictonic receptor antagonists
US8658677B2 (en) * 2011-07-07 2014-02-25 Aria Neurosciences Inc. Pyridyl-2-methylamino compounds, compositions and uses thereof
DK2731947T3 (en) 2011-07-15 2019-04-23 Boehringer Ingelheim Int SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES
UA113291C2 (xx) 2011-08-04 2017-01-10 Метаболіти транскломіфену і їх застосування
US8772277B2 (en) * 2011-08-04 2014-07-08 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound
CA2848726C (en) * 2011-08-19 2019-09-10 Emory University Bax agonist, compositions, and methods related thereto
SI2755483T1 (sl) 2011-09-14 2019-05-31 Samumed, Llc Indazol-3-karboksamidi in njihova uporaba kot inhibitorji signalne poti WNT/B-katenin
RU2622643C2 (ru) * 2011-09-14 2017-06-19 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные тетрагидротриазолопиримидина в качестве ингибиторов нейтрофильной эластазы человека
AU2012314587A1 (en) 2011-09-26 2014-03-06 Grünenthal GmbH Aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands
KR20140085470A (ko) * 2011-09-26 2014-07-07 그뤼넨탈 게엠베하 바닐로이드 수용체 리간드로서의 아민 치환된 메탄설폰아미드 유도체
PL2776394T3 (pl) 2011-10-20 2019-06-28 Oryzon Genomics, S.A. (hetero)arylowe związki cyklopropyloaminowe jako inhibitory lsd1
WO2013057320A1 (en) 2011-10-20 2013-04-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
BR112014010099A8 (pt) 2011-10-26 2018-01-16 Kempharm Inc ácido benzóico, derivados de ácidos benzóicos e ácidos carboxílicos heteroarílicos conjugados de hidromorfona, pró-fármacos, métodos de fabricação e uso dos mesmos.
EP2780316B1 (en) * 2011-11-13 2020-04-15 Blanchette Rockefeller Neurosciences Institute Esters of dcpla and methods of treatment using the same
HK1201871A1 (en) 2011-11-22 2015-09-11 Trustees Of Tufts College Small molecule enhancer for dendritic cell cancer vaccines
WO2013084153A1 (en) * 2011-12-05 2013-06-13 Glenmark Pharmaceuticals S.A. Pharmaceutical composition comprising a trpa1 antagonist and an anticholinergic agent
ES2832773T3 (es) 2012-01-06 2021-06-11 Anji Pharma Us Llc Composiciones de biguanida y métodos de tratamiento de trastornos metabólicos
NZ626578A (en) 2012-01-06 2016-11-25 Elcelyx Therapeutics Inc Compositions and methods for treating metabolic disorders
CN102603493B (zh) * 2012-01-17 2014-03-12 青岛农业大学 含氟邻烯丙基苯酚类化合物的制备方法及农用生物活性
CN106890185A (zh) * 2012-02-14 2017-06-27 利普生物药剂公司 具有短半衰期的选择性雌激素受体调节剂及其用途
CN102614177B (zh) * 2012-03-06 2014-08-06 北京伟峰益民科技有限公司 卢帕他定在制备治疗慢性阻塞性肺病药物组合物中的应用
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013144080A1 (en) * 2012-03-30 2013-10-03 Nestec S.A. 4-oxo-2-pentenoic acid and cardiovascular health
WO2013150529A2 (en) * 2012-04-02 2013-10-10 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd Indole, indoline derivatives, compositions comprising them and uses thereof
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
BR112014023670A8 (pt) * 2012-04-04 2017-07-25 Chiesi Farm Spa Composto, composição farmacêutica e suo de um composto
US8809376B2 (en) * 2012-04-30 2014-08-19 Boehringer Ingelheim International Gmbh Indanyloxydihydrobenzofuranylacetic acids
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
ES2929025T3 (es) 2012-05-14 2022-11-24 Boehringer Ingelheim Int Linagliptina, un derivado de xantina como inhibidor de dpp-4, para su uso en el tratamiento del SRIS y/o de la septicemia
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
US12226412B2 (en) 2012-05-25 2025-02-18 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US8859774B2 (en) 2012-05-25 2014-10-14 Corcept Therapeutics, Inc. Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
US20130345205A1 (en) * 2012-06-20 2013-12-26 Vanderbilt University Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors
CA2876979A1 (en) * 2012-06-20 2013-12-27 P. Jeffrey Conn Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors
WO2014015056A2 (en) 2012-07-17 2014-01-23 Washington University Anti-mucus drugs and uses therefor
CA2882292C (en) 2012-08-13 2023-10-17 The Rockefeller University Treatment and diagnosis of melanoma
CN113679717A (zh) 2012-08-22 2021-11-23 康奈尔大学 用于抑制肌成束蛋白的方法
WO2014032755A2 (en) * 2012-08-29 2014-03-06 Merck Patent Gmbh Ddr2 inhibitors for the treatment of osteoarthritis
US8859598B2 (en) * 2012-10-04 2014-10-14 Allergan, Inc. 1, 2, 4-oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
US9278081B2 (en) * 2012-10-04 2016-03-08 University Of The West Indies Extracts from Eucalyptus camaldulensis for the treatment of hyperglycemia and hypertension
HK1216502A1 (zh) 2012-11-02 2016-11-18 Repros Therapeutics Inc. 用於癌症治療的反式-克羅米芬
US9624214B2 (en) 2012-11-05 2017-04-18 Bayer Pharma Aktiengesellschaft Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use
WO2014081878A2 (en) * 2012-11-21 2014-05-30 Stategics, Inc. Substituted triazolo-pyrimidine compounds for modulating cell proliferation, differentiation and survival
BR112015012716A2 (pt) * 2012-12-05 2017-07-11 Chiesi Farm Spa derivados de feniletilpiridina como inibidores de pde4
EP2928886B1 (en) 2012-12-07 2016-11-02 Boehringer Ingelheim International GmbH New indanyloxydihydrobenzofuranylacetic acids
UY35212A (es) 2012-12-21 2014-06-30 Gilead Sciences Inc Inhibidores de la quinasa que regula la señal de la apoptosis
WO2014110086A2 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
CU20130027A7 (es) * 2013-02-28 2014-10-30 Ct De Neurociencias De Cuba Chaperoninas químicas como nuevos moduladores moleculares de la beta agregación proteica presente en las enfermedades conformacionales
JP6410790B2 (ja) 2013-03-14 2018-10-24 ザ ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティー ミトコンドリアアルデヒドデヒドロゲナーゼ−２調節因子およびその使用方法
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
EP2970133B1 (en) 2013-03-14 2018-10-24 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9346761B2 (en) 2013-03-14 2016-05-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
HRP20202008T1 (hr) 2013-03-14 2021-02-19 Epizyme, Inc. Inhibitori arginin-metiltransferaze i njihove uporabe
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
MX365315B (es) 2013-03-15 2019-05-29 Janssen Pharmaceutica Nv Derivados de piridina sustituidos útiles como inhibidores de c-fms quinasa.
US20140335079A1 (en) * 2013-05-07 2014-11-13 Emory University Solenopsin and derivatives, therapeutic compositions, and methods related thereto
WO2015002264A1 (ja) * 2013-07-03 2015-01-08 三菱化学フーズ株式会社 毛状疣贅病の予防および／または治療方法
KR20160033726A (ko) * 2013-07-18 2016-03-28 노파르티스 아게 헤테로방향족 고리-벤질-아미드-사이클 코어를 포함하는 오토탁신 억제제
US20150045435A1 (en) * 2013-08-06 2015-02-12 Indiana University Research And Technology Corporation Compounds and methods for treating diabetes
WO2015026574A1 (en) * 2013-08-20 2015-02-26 Bristol-Myers Squibb Company Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by aak1, such as alzheimer's disease, bipolar disorder, pain, schizophrenia
WO2015027160A2 (en) * 2013-08-22 2015-02-26 Northeastern University Allosteric modulators of the cannibinoid 1 receptor
BR112016005509B1 (pt) * 2013-09-13 2021-01-19 The Board Of Trustees Of The University Of Arkansas uso de uma composição
US9353078B2 (en) * 2013-10-01 2016-05-31 New York University Amino, amido and heterocyclic compounds as modulators of rage activity and uses thereof
AU2014340155B2 (en) 2013-10-22 2018-11-01 Massachusetts Institute Of Technology Lipid formulations for delivery of messenger RNA
US9796709B2 (en) * 2013-12-13 2017-10-24 Daiichi Sankyo Company, Limited 5-hydroxy-4-(trifluoromethyl)pyrazolopyridine derivative
MA39147B1 (fr) 2013-12-17 2019-12-31 Esteve Labor Dr Combinaisons d'inhibiteurs de la recapture de sérotonine-norépinéphrine (snri) et de ligands des récepteurs sigma
US9381171B2 (en) * 2013-12-19 2016-07-05 Samsung Electronics Co., Ltd. Composition including dapsone for preventing or treating side effect of steroid in subject and use of the composition
WO2015091934A1 (en) * 2013-12-20 2015-06-25 AbbVie Deutschland GmbH & Co. KG Oxindole derivatives carrying an amine-substituted piperidyl-azetidinyl substituent and use thereof for treating vasopressine-related diseases
CN104744446B (zh) * 2013-12-30 2019-06-25 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
EP3091970B1 (en) 2014-01-10 2020-10-28 Rgenix, Inc. Lxr agonists and uses thereof
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
CA2940144C (en) 2014-02-20 2023-06-13 Cornell University Substituted indazol-3-yl derivatives and pharmaceutical compositions thereof useful as inhibitor of fascin
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
US9526728B2 (en) 2014-02-28 2016-12-27 Boehringer Ingelheim International Gmbh Medical use of a DPP-4 inhibitor
JP2017508810A (ja) 2014-03-21 2017-03-30 バイエル・ファルマ・アクティエンゲゼルシャフト シアノ置換イミダゾ［１，２−ａ］ピリジンカルボキサミドおよびその使用
TWI746422B (zh) 2014-05-20 2021-11-21 美商千禧製藥公司 用於癌症治療的方法
EP3157520B1 (en) 2014-06-23 2019-09-04 Celgene Corporation Apremilast for the treatment of a liver disease or a liver function abnormality
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
TW201615221A (zh) * 2014-10-24 2016-05-01 朗齊生物醫學股份有限公司 炎症用藥臨床新應用
EP3215140A4 (en) * 2014-11-06 2018-05-02 The Arizona Board of Regents On Behalf of the University of Arizona Compositions and methods of diazeniumdiolate-based prodrugs for treating cancer
ES2882126T3 (es) * 2014-11-07 2021-12-01 Univ Northwestern Inhibición de ornitina aminotransferasa con análogos de GABA para el tratamiento de carcinoma hepatocelular
JP6462877B2 (ja) * 2014-12-02 2019-01-30 ケムファーム・インコーポレーテッド オキシモルホンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体、プロドラッグ、その製造法及び使用
CN107001361A (zh) 2014-12-02 2017-08-01 拜耳医药股份有限公司 杂芳基取代的咪唑并[1，2‑a]吡啶及其用途
CA2969540C (en) 2014-12-02 2023-03-21 Ignyta, Inc. Combinations for the treatment of neuroblastoma
JP6769962B2 (ja) * 2014-12-03 2020-10-14 オークランド ユニサービシーズ リミティド 癌治療のためのキナーゼ阻害剤プロドラッグ
WO2016094854A2 (en) * 2014-12-12 2016-06-16 Miradx Methods for treating or preventing cancer in a kras-variant patient and for diagnosing risk of developing multiple primary breast tumors
WO2016118741A1 (en) 2015-01-22 2016-07-28 Mitochon Pharmaceuticals Llc Induced expression of brain derived neurotrophic factor (bdnf) for treatment of neuromuscular, neurodegenerative, autoimmune, developmental and/or metabolic diseases
WO2016141341A1 (en) * 2015-03-04 2016-09-09 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant
US20180071376A1 (en) 2015-03-23 2018-03-15 The Brigham And Women`S Hospital, Inc. Tolerogenic nanoparticles for treating diabetes mellitus
WO2016172199A1 (en) * 2015-04-20 2016-10-27 Epizyme, Inc. Combination therapy for treating cancer
AU2016254049A1 (en) * 2015-04-30 2017-11-02 Musc Foundation For Research Development Oxindole compounds and pharmaceutical compositions thereof
US20160324914A1 (en) 2015-05-05 2016-11-10 Tocol Pharmaceuticals, Llc Use of rice bran oil distillate extract for prevention and mitigation of the effects of radiation
TWI713534B (zh) 2015-06-11 2020-12-21 日商第一三共股份有限公司 5-羥基-4-(三氟甲基)吡唑并吡啶衍生物之結晶及其用途
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024004A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024003A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10329309B2 (en) 2015-08-03 2019-06-25 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
US10195185B2 (en) 2015-08-03 2019-02-05 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US9675608B2 (en) * 2015-08-26 2017-06-13 Macau University Of Science And Technology Identification of natural small-molecules AMPK activators for treatment of cancers or multidrug-resistant cancers
JP6853819B2 (ja) * 2015-10-08 2021-03-31 スーチョウ ユンシュアン イーヤオ カジ ヨウシェン ゴンス Ｗｎｔシグナル伝達経路阻害剤およびその治療用途
GB201519450D0 (en) * 2015-11-03 2015-12-16 Univ Liverpool Novel treatment
KR20180080288A (ko) 2015-11-06 2018-07-11 사뮤메드, 엘엘씨 2-(1H-인다졸-3-일)-3H-이미다조[4,5-c]피리딘 및 그의 항-염증성 용도
US9549907B1 (en) * 2015-11-13 2017-01-24 Sovereign Pharmaceuticals, Llc Immediate release oral guaifenesin solution
US10765665B2 (en) * 2015-11-24 2020-09-08 Melin Jeffrey Composition comprising combination of rapamycin and an activator of AMP kinase and use thereof for treating diseases
ES2918589T3 (es) * 2015-11-25 2022-07-19 Convergene Llc Inhibidores de bromodomios BET bicíclicos y usos de los mismos
CN108697661A (zh) 2015-12-18 2018-10-23 亚尼塔公司 用于治疗癌症的组合
EP3426638B1 (en) * 2016-03-09 2020-05-06 Netherlands Translational Research Center B.V. Inhibitors of indoleamine 2,3-dioxygenase
HUE050890T2 (hu) * 2016-03-14 2021-01-28 Pliva Hrvatska D O O Nilotinib sók szilárd halmazállapotú formái
US10064834B2 (en) * 2016-05-09 2018-09-04 Texas Tech University System Carbidopa for the treatment of cancer
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
US20190054041A1 (en) * 2016-05-26 2019-02-21 Institute Of Tropical Bioscience And Biotechology Chinese Academy Of Tropical Agricultural Sciences Use of nootkatone
SMT202200486T1 (it) 2016-06-01 2023-01-13 Biosplice Therapeutics Inc Processo per la preparazione di n-(5-(3-(7-(3- fluorofen il)-3h-imidaz0[4,5-c]piridin-2-il)-1h-indazol-5- il)piridin-3-il)-3-metilbutanammide
EP3251668A1 (en) * 2016-06-02 2017-12-06 Pharmotech SA Cannabidiol compositions and uses thereof
CN109310697A (zh) 2016-06-10 2019-02-05 勃林格殷格翰国际有限公司 利格列汀和二甲双胍的组合
CA3035972A1 (en) * 2016-09-07 2018-03-15 Temple University - Of The Commonwealth System Of Higher Education Compositions and methods for treatment of insulin resistance
EP3446703A1 (en) * 2017-08-24 2019-02-27 Isofol Medical AB 6r]-mthf multiple bolus administration in 5-fluorouracil based chemotherapy
EP3446704A1 (en) 2017-08-24 2019-02-27 Isofol Medical AB [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy
MX391624B (es) 2016-10-21 2025-03-04 Samumed Llc Métodos de uso de indazol-3-carboxamidas y su uso como inhibidores de la ruta de señalización de wnt/b-catenina.
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
CN110198719A (zh) 2016-11-21 2019-09-03 维京治疗公司 治疗糖原贮积病的方法
WO2018109664A1 (en) * 2016-12-15 2018-06-21 Nestec Sa Compositions and methods that modulate digestibility in a companion animal
US10723716B2 (en) 2016-12-21 2020-07-28 New York University Alpha-helix mimetics as modulators of Abeta self-assembly
CN110198928B (zh) 2017-01-26 2023-08-29 勃林格殷格翰国际有限公司 苄氧基吡啶基环丙烷甲酸、其药物组合物和用途
CN110312714B (zh) 2017-01-26 2022-12-09 勃林格殷格翰国际有限公司 苄基氧基吡嗪基环丙烷甲酸、其药物组合物和用途
WO2018138028A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10919859B2 (en) 2017-01-26 2021-02-16 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018146008A1 (en) 2017-02-08 2018-08-16 Boehringer Ingelheim International Gmbh Indanylaminoazadihydrobenzofuranylacetic acids, pharmaceutical compositions for the treatment of diabetes
CA3053293C (en) 2017-02-14 2023-01-03 Isofol Medical Ab Methods for increasing blood plasma 2'-deoxyuridine (durd) and thymidylate synthase inhibition
US10517842B2 (en) * 2017-03-15 2019-12-31 Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Center Methods of modulating miRNA levels and compositions for use in the same
RU2675496C1 (ru) * 2017-03-31 2018-12-20 Федеральное государственное бюджетное учреждение науки Институт нефтехимии и катализа Российской академии наук Способ получения алкиловых эфиров гидроксибензойных кислот
KR102342620B1 (ko) 2017-03-31 2021-12-22 코어셉트 쎄라퓨틱스 인코포레이티드 자궁경부암을 치료하기 위한 글루코코르티코이드 수용체 조정제
US20180280319A1 (en) * 2017-04-04 2018-10-04 University Of The Sciences Compounds and compositions for treatment of breast cancer
FR3066393B1 (fr) * 2017-05-16 2019-07-19 Polyneuros Principe actif constitue par un melange de composes poly-lysine et utilisation dans la prevention des avc et le traitement de la phase inflammatoire post-avc
US11491150B2 (en) 2017-05-22 2022-11-08 Intra-Cellular Therapies, Inc. Organic compounds
WO2018226604A1 (en) 2017-06-05 2018-12-13 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis
KR102718538B1 (ko) 2017-07-19 2024-10-21 이그니타, 인코포레이티드 엔트렉티닙을 포함하는 약학적 조성물
US10639313B2 (en) * 2017-09-01 2020-05-05 Ndsu Research Foundation Compound for inhibition of delta-5-desaturase (D5D) and treatment of cancer and inflammation
EP3681505B1 (en) 2017-09-13 2024-12-18 Vanda Pharmaceuticals Inc. Improved treatment of atopic dermatitis with tradipitant
PT3691620T (pt) 2017-10-05 2022-10-06 Fulcrum Therapeutics Inc Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019077506A1 (en) 2017-10-17 2019-04-25 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS AND SOLID GALENIC FORMS
CA3079558A1 (en) 2017-10-20 2019-04-25 Eagle Research Labs Limited Dantrolene prodrugs and methods of their use
US11607458B2 (en) * 2017-10-25 2023-03-21 Georgia State University Research Foundation, Inc. Enrichment-triggered chemical delivery system
MX2020004946A (es) 2017-11-03 2020-09-25 Aclaris Therapeutics Inc Inhibidores jak de pirrolopiridina sustituidos y metodos para producir y utilizar los mismos.
EP3713575A4 (en) 2017-11-21 2021-08-25 Rgenix, Inc. POLYMORPHS AND THEIR USES
WO2019183004A1 (en) 2018-03-22 2019-09-26 Viking Therapeutics, Inc. Crystalline forms and methods of producing crystalline forms of a compound
AU2019242628A1 (en) 2018-03-26 2020-09-24 Clear Creek Bio, Inc. Compositions and methods for inhibiting dihydroorotate dehydrogenase
MX2020012831A (es) 2018-06-04 2021-04-28 Corcept Therapeutics Inc Moduladores del receptor de glucocorticoide de pirimidina ciclohexenilo.
CN112823005B (zh) 2018-08-10 2024-08-20 阿克拉瑞斯治疗股份有限公司 吡咯并嘧啶itk抑制剂
JP7546550B2 (ja) 2018-09-18 2024-09-06 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 抗腫瘍剤としてのキナゾリン誘導体
WO2020117962A1 (en) 2018-12-05 2020-06-11 Viking Therapeutics, Inc. Compositions for the treatment of fibrosis and inflammation
MX2021007322A (es) 2018-12-19 2021-07-07 Corcept Therapeutics Inc Formulaciones farmaceuticas que contienen relacorilant, un compuesto de azadecalina fusionado con heteroaril-cetona.
US11389432B2 (en) 2018-12-19 2022-07-19 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
US11234971B2 (en) 2018-12-19 2022-02-01 Corcept Therapeutics Incorporated Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent
SG11202108927UA (en) 2019-05-02 2021-09-29 Aclaris Therapeutics Inc Substituted pyrrolopyridines as jak inhibitors
KR102368413B1 (ko) * 2019-09-25 2022-02-28 경희대학교 산학협력단 시린가레지놀을 포함하는 신경병증성 통증 예방 또는 치료용 조성물
JP7569492B2 (ja) 2019-12-11 2024-10-18 コーセプト セラピューティクス， インコーポレイテッド 抗精神病薬誘発性体重増加のミリコリラントによる治療方法
NZ789129A (en) 2019-12-13 2025-03-28 Inspirna Inc Metal salts and uses thereof
WO2021189018A1 (en) 2020-03-20 2021-09-23 Clear Creek Bio, Inc. Methods of treating viral infections using inhibitors of nucleotide synthesis pathways
CA3182272A1 (en) 2020-05-06 2021-11-11 Corcept Therapeutics Incorporated Polymorphs of pyrimidine cyclohexyl glucocorticoid receptor modulators
AU2021266739B2 (en) 2020-05-06 2024-11-28 Corcept Therapeutics Incorporated Formulations of pyrimidine cyclohexyl glucocorticoid receptor modulators
US11071739B1 (en) 2020-09-29 2021-07-27 Genus Lifesciences Inc. Oral liquid compositions including chlorpromazine
CA3237722A1 (en) 2020-11-12 2022-05-19 Thermolife International, Llc Methods of increasing blood oxygen saturation
US11865139B2 (en) 2020-11-12 2024-01-09 Thermolife International, Llc Method of treating migraines and headaches
CN116848092A (zh) 2020-12-21 2023-10-03 科赛普特治疗公司 制备嘧啶环己基糖皮质激素受体调节剂的方法
WO2022134033A1 (en) 2020-12-25 2022-06-30 Corcept Therapeutics Incorporated Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators
CN113354558B (zh) * 2021-07-12 2022-03-11 无锡双启科技有限公司 一种2-氨基-5-氟苯腈的制备方法
WO2025056518A1 (en) * 2023-09-11 2025-03-20 Univerza V Ljubljani 5,6-DISUBSTITUTED ALKYL 1H AND 2H-INDAZOLES AS DUAL BUTYRYLCHOLINESTERASE AND p38α MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE AND INFLAMMATORY DISEASES

Family Cites Families (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3755332A (en) 1971-07-01 1973-08-28 Ciba Geigy Corp Substituted 4 indazolaminoquinolines
JPS5998060A (ja) * 1982-11-27 1984-06-06 Fujisawa Pharmaceut Co Ltd インダゾ−ル誘導体、その製造法および農薬
US4571255A (en) * 1983-12-29 1986-02-18 Ppg Industries, Inc. Subsituted phenoxybenzisoxazole herbicides
US5234942A (en) * 1984-10-19 1993-08-10 Ici Americas Inc. Heterocyclic amides and leucotriene antagonistic use thereof
GB8524157D0 (en) 1984-10-19 1985-11-06 Ici America Inc Heterocyclic amides
SU1545940A3 (ru) 1984-10-19 1990-02-23 Ай-Си-Ай Америказ Инк (Фирма) Способ получени гетероциклических кислот или их солей
PL265549A1 (en) 1985-03-26 1988-09-01 The method of manufacture of new heterocyclic amides
JPS6368568A (ja) * 1986-09-10 1988-03-28 Otsuka Pharmaceut Factory Inc ｐ−アミノフエノ−ル誘導体
NZ224714A (en) 1987-06-01 1990-03-27 Janssen Pharmaceutica Nv Substituted benzotriazole derivatives and pharmaceutical compositions
IE910278A1 (en) 1990-02-16 1991-08-28 Ici Plc Heterocyclic compounds
IL97102A0 (en) * 1990-02-16 1992-03-29 Ici Plc Heterocyclic compounds
US6194439B1 (en) * 1991-05-29 2001-02-27 Pfizer Inc. Tricyclic polyhydroxylic tyrosine kinase inhibitors
WO1994001415A1 (en) * 1992-07-03 1994-01-20 Kumiai Chemical Industry Co., Ltd. Condensed heterocyclic derivative and weedkiller
JPH0841032A (ja) * 1994-05-27 1996-02-13 Mochida Pharmaceut Co Ltd アロマターゼ阻害作用を有する新規なアゾールメチルフェニル誘導体
US5587392A (en) 1994-05-27 1996-12-24 Mochida Pharmaceutical Co., Ltd. Azolyl methyl phenyl derivatives having aromatase inhibitory activity
US6083949A (en) 1995-10-06 2000-07-04 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
NZ321738A (en) 1995-10-06 1999-11-29 Merck & Co Inc 3-pyridine-2-heterocyclic substituted imidazoles and medicaments having anti-cancer and cytokine inhibitory activity
HUP9903248A3 (en) 1996-09-04 2000-07-28 Pfizer Indazole derivatives and pharmaceutical compositions containing them with the effect of inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)
US6809097B1 (en) 1996-09-25 2004-10-26 Zeneca Limited Quinoline derivatives inhibiting the effect of growth factors such as VEGF
US5932570A (en) 1996-11-08 1999-08-03 Dupont Pharmaceuticals Company 1-(3-aminoindazol-5-yl)-3-phenylmethyl-cyclic ureas useful as HIV protease inhibitors
US6218386B1 (en) 1996-11-08 2001-04-17 Dupont Pharmaceuticals A1-(3-aminoindazol-5-yl)-3 butyl-cyclic urea useful as a HIV protease inhibitor
SK59699A3 (en) 1996-11-08 1999-12-10 Du Pont Pharm Co 1-(3-aminoindazol-5-yl)-3-phenylmethyl-cyclic ureas useful as hiv protease inhibitors
US5945418A (en) 1996-12-18 1999-08-31 Vertex Pharmaceuticals Incorporated Inhibitors of p38
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
DK1028954T3 (da) 1997-04-24 2003-10-27 Ortho Mcneil Pharm Inc Substituerede imidazoler egnede til behandling af inflammatoriske sygdomme
CA2288787A1 (en) 1997-05-22 1998-11-26 G.D. Searle And Co. Pyrazole derivatives as p38 kinase inhibitors
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
US6297239B1 (en) * 1997-10-08 2001-10-02 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
ES2221213T3 (es) 1997-10-20 2004-12-16 F. Hoffmann-La Roche Ag Inhibidores de kinasa biciclicos.
EP1028953A1 (en) 1997-11-03 2000-08-23 Boehringer Ingelheim Pharmaceuticals Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
US6329412B1 (en) * 1997-11-04 2001-12-11 Pfizer Inc Bisamidine compounds as antiproliferative agents
PL340799A1 (en) * 1997-11-04 2001-02-26 Pfizer Prod Inc Therapeutically active compounds based on a substitution of indazole bioisoster for cathechol in pde 4 inhibitors
JP2001521926A (ja) 1997-11-04 2001-11-13 ファイザー・プロダクツ・インク 治療上活性の化合物におけるカテコールのインダゾール生物学的等価物置換
CA2321419A1 (en) 1998-02-12 1999-08-19 Woo-Kyu Kim Catalyst compounds with beta-diiminate anionic ligands and processes for polymerizing olefins
US6589954B1 (en) * 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
GB9820767D0 (en) 1998-09-23 1998-11-18 Cerebrus Ltd Chemical compounds VIII
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
MXPA01008440A (es) 1999-02-22 2002-04-24 Boehringer Ingelheim Pharma Derivados heterociclicos policiclos como agentes anti-inflamatorios..
JP2002539206A (ja) 1999-03-12 2002-11-19 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症剤としての芳香族複素環化合物
CZ20013289A3 (cs) 1999-03-12 2002-01-16 Boehringer Ingelheim Pharmaceuticals, Inc. Sloučeniny výhodné jako protizánětové prostředky
EP2138179A1 (en) 1999-03-29 2009-12-30 Shire Canada Inc. Use of cytidine derivatives for the treatment of leukaemia
AU4063600A (en) * 1999-04-05 2000-10-23 Merck & Co., Inc. A method of treating cancer
BR0009870A (pt) 1999-04-21 2002-01-08 American Cyanamid Co Composto, métodos de inibir efeitos biológicos de uma proteìna-tirosina-quinase desregulada em um mamìfero necessitando do mesmo, de tratar, inibir o crescimento de, ou erradicar neoplasmas em um mamìfero necessitando do mesmo, de tratar, inibir o processo de, ou erradicar doença policìstica dos rins e pólipos colÈnicos em um mamìfero necessitando do mesmo, e, composição farmacêutica
US6355636B1 (en) 1999-04-21 2002-03-12 American Cyanamid Company Substituted 3-cyano-[1.7],[1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases
HUP0201261A3 (en) 1999-05-21 2003-12-29 Scios Inc Sunnyvale Indole-type derivatives as inhibitors of p38 kinase and pharmaceutical compositions containing them
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
CA2374737C (en) 1999-07-09 2008-02-12 Boehringer Ingelheim Pharmaceuticals, Inc. Novel process for synthesis of heteroaryl-substituted urea compounds
JP4234858B2 (ja) 1999-09-21 2009-03-04 東芝テック株式会社 負極性現像剤
US6743795B1 (en) 1999-11-27 2004-06-01 Dong Wha Pharm. Ind. Co. Ltd. 3-nitropyridine derivaives and the pharmaceutical compositions containing said derivatives
AU1899401A (en) * 1999-11-27 2001-06-04 Dong Wha Pharmaceutical Industrial Co., Ltd. Novel 5-pyrimidinecarboxamide derivatives and the pharmaceutical compositions containing said derivatives
EP1235804A1 (en) * 1999-11-27 2002-09-04 Dong Wha Pharmaceutical Industrial Co. Ltd. Novel 3-nitropyridine derivatives and the pharmaceutical compositions containing said derivatives
WO2001078648A2 (en) * 2000-04-17 2001-10-25 Dong Wha Pharm. Ind. Co., Ltd. 6-methylnicotinamide derivatives as antiviral agents
JP2004529859A (ja) 2000-11-20 2004-09-30 サイオス インコーポレイテッド インドール誘導体とｐ３８キナーゼの阻害剤としてのその使用方法
US7102009B2 (en) * 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
TW593278B (en) * 2001-01-23 2004-06-21 Wyeth Corp 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands
EP1370559B1 (en) 2001-03-09 2006-04-19 Pfizer Products Inc. Triazolopyridines as anti-inflammatory agents
JPWO2002100833A1 (ja) * 2001-06-12 2004-09-24 住友製薬株式会社 Ｒｈｏキナーゼ阻害剤
DE60238999D1 (de) 2001-09-26 2011-03-03 Pfizer Italia Srl Aminoindazolderivate mit kinaseinhibierender wirkung, verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammensetzungen
EP1438048A1 (en) 2001-10-18 2004-07-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
AU2002353186A1 (en) 2001-12-19 2003-06-30 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
DE60319066T2 (de) 2002-02-25 2009-02-26 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield 1,4-disubstituierte benzokondensierte cycloalkyl-harnstoffverbindungen zur behandlung von zytokinvermittelten erkrankungen
FR2836914B1 (fr) 2002-03-11 2008-03-14 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
WO2003087072A1 (fr) 2002-03-29 2003-10-23 Mochida Pharmaceutical Co., Ltd. Agent therapeutique destine a des troubles endotheliaux
CA2492911A1 (en) 2002-07-19 2004-01-29 Memory Pharmaceuticals Corporation 6-amino-1h-indazole and 4-aminobenzofuran compounds as phosphodiesterase 4 inhibitors
CN1678589A (zh) 2002-09-05 2005-10-05 安万特医药股份有限公司 作为药物的新氨基吲唑衍生物与含有它们的药物组合物
RU2005115842A (ru) 2002-10-24 2006-03-10 Мерк Патент ГмбХ (DE) Производные метиленмочевины
CA2503646C (en) 2002-10-28 2011-09-27 Bayer Healthcare Ag Heteroaryloxy-substituted phenylaminopyrimidines as rho-kinase inhibitors
US7196082B2 (en) 2002-11-08 2007-03-27 Merck & Co. Inc. Ophthalmic compositions for treating ocular hypertension
AU2003293376A1 (en) 2002-12-10 2004-06-30 Imclone Systems Incorporated Anti-angiogenic compounds and their use in cancer treatment
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
EP1606283B1 (en) * 2003-03-03 2008-10-08 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
GB0320244D0 (en) 2003-05-06 2003-10-01 Aventis Pharma Inc Pyrazoles as inhibitors of tumour necrosis factor
US7129252B2 (en) * 2003-06-16 2006-10-31 Guoqing P Chen Six membered amino-amide derivatives an angiogenisis inhibitors
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
US20090048301A1 (en) * 2003-07-09 2009-02-19 Imclone Systems Incorporated Heterocyclic compounds and their use as anticancer agents
SG146624A1 (en) 2003-09-11 2008-10-30 Kemia Inc Cytokine inhibitors
CA2547837A1 (en) 2003-12-18 2005-07-14 Boehringer Ingelheim Pharmaceuticals, Inc. Polymorph of birb 796, a p38map kinase inhibitor
EP1699783B1 (en) * 2003-12-22 2012-07-25 Eli Lilly And Company Opioid receptor antagonists
US20060264431A1 (en) 2005-05-11 2006-11-23 Array Biopharma Inc. P38 inhibitors and methods of use thereof
RS52298B (en) 2006-01-31 2012-12-31 Array Biopharma Inc. KINASE INHIBITORS AND PROCEDURE FOR THEIR USE

Also Published As

Publication number Publication date
CN101759645A (zh) 2010-06-30
SI1606283T1 (sl) 2009-04-30
US8017641B2 (en) 2011-09-13
AR043451A1 (es) 2005-07-27
EP1997809A2 (en) 2008-12-03
SI1997809T1 (sl) 2014-09-30
DK1997809T3 (da) 2014-07-21
CL2004000416A1 (es) 2005-01-14
PT1997811E (pt) 2015-07-29
EP1997811B1 (en) 2015-04-08
BRPI0407993A (pt) 2006-03-07
US20040176325A1 (en) 2004-09-09
EP1997811A2 (en) 2008-12-03
PT1997809E (pt) 2014-08-26
BRPI0419305B1 (pt) 2019-10-22
EP1997810A2 (en) 2008-12-03
PT1997810E (pt) 2013-11-07
IL170527A (en) 2011-11-30
TWI346663B (en) 2011-08-11
IL215917A0 (en) 2011-12-29
US20090143422A1 (en) 2009-06-04
TW200510416A (en) 2005-03-16
CY1116207T1 (el) 2017-02-08
EP2039685A3 (en) 2009-12-02
NZ582796A (en) 2011-05-27
EP1997809A3 (en) 2009-09-09
DK2039685T3 (da) 2013-03-25
AU2009225343B2 (en) 2012-08-23
US7799782B2 (en) 2010-09-21
CY1115441T1 (el) 2017-01-04
CY1114554T1 (el) 2016-10-05
ES2534859T3 (es) 2015-04-29
DK1997810T3 (da) 2013-10-21
HK1146664A1 (zh) 2011-06-30
ES2484866T3 (es) 2014-08-12
CL2009000234A1 (es) 2009-04-24
UA103873C2 (ru) 2013-12-10
CN100579976C (zh) 2010-01-13
PL400577A1 (pl) 2013-02-18
EP1997809B1 (en) 2014-05-14
ATE410421T1 (de) 2008-10-15
BRPI0407993B1 (pt) 2018-05-22
ES2433096T3 (es) 2013-12-09
JP2009102395A (ja) 2009-05-14
ES2315641T3 (es) 2009-04-01
EP1997811A3 (en) 2009-09-09
IL196847A0 (en) 2011-07-31
US20040180896A1 (en) 2004-09-16
BRPI0419305B8 (pt) 2021-05-25
AU2009225343A1 (en) 2009-11-05
ZA200507874B (en) 2007-03-28
UA86196C2 (uk) 2009-04-10
JP5424657B2 (ja) 2014-02-26
HK1084673A1 (en) 2006-08-04
DE602004016970D1 (de) 2008-11-20
JP2012251003A (ja) 2012-12-20
NZ542616A (en) 2009-02-28
JP5687259B2 (ja) 2015-03-18
TW200936590A (en) 2009-09-01
CY1108661T1 (el) 2014-04-09
US7135575B2 (en) 2006-11-14
KR20120037022A (ko) 2012-04-18
SI1997810T1 (sl) 2013-12-31
US20090136596A1 (en) 2009-05-28
DK1606283T3 (da) 2009-02-09
SI2039685T1 (sl) 2013-04-30
NO20085373L (no) 2005-11-29
KR101236608B1 (ko) 2013-02-22
KR20110091532A (ko) 2011-08-11
KR20090021231A (ko) 2009-02-27
PT1606283E (pt) 2008-12-29
NZ572694A (en) 2010-04-30
EP1997810A3 (en) 2009-12-02
PA8596901A1 (es) 2004-11-26
SI1997811T1 (sl) 2015-07-31
PL219742B1 (pl) 2015-07-31
TWI343386B (en) 2011-06-11
US20090149459A1 (en) 2009-06-11
DOP2009000155A (es) 2010-09-15
EP2039685B1 (en) 2012-12-26
IS2959B (is) 2017-02-15
DK1997811T3 (en) 2015-07-06
CO5670351A2 (es) 2006-08-31
CN101759645B (zh) 2014-06-25
IS8810A (is) 2009-03-16
US8518983B2 (en) 2013-08-27
EP2039685A2 (en) 2009-03-25
BRPI0407993B8 (pt) 2021-05-25
EG27049A (en) 2015-04-28
CN1784396A (zh) 2006-06-07
EP1997810B1 (en) 2013-07-31

Similar Documents

Publication Publication Date Title
AR069413A2 (es) Derivados de hetero- pentaciclo- fenilo fusionados, composicion farmaceutica que los comprende y usos para preparar un medicamento util para el tratamiento de una condicion mediada por p 38
CA2517517A1 (en) P38 inhibitors and methods of use thereof
PE20190705A1 (es) COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING
PE20090042A1 (es) Analogos de ciclopamina
EA200900358A1 (ru) Энантиомерно чистые фосфоиндолы в качестве ингибиторов hiv
AR062680A1 (es) Sintesis de 2-(piridin-2-ilamino) pirido [2,3-d] pirimidin-7-onas
PE20040479A1 (es) Inhibidores de proteasa del vih y composiciones que los contienen
AR037898A1 (es) Compuesto de benzamida, uso de un compuesto de benzamida en la fabricacion de un medicamento, proceso para su preparacion y composicion farmaceutica que lo comprende
PE20020592A1 (es) Quinolonas como agentes antimicrobianos
AR057716A1 (es) Inhibidores de las serina proteasas y composiciones farmaceuticas
RS20090249A (en) Spiroketone acetyl-coa carboxylase inhibotors
AR071959A1 (es) Derivado de benceno o tiofeno y su uso como inhibidor de vap-1
AR025276A1 (es) El uso de un compuesto que es un derivado de 2-amino-1,3-tiazol, un compuesto que es un derivado de 2-amino-1,3-tiazol, un procedimiento para producirlo y una composicion farmaceutica que lo comprende
PA8591701A1 (es) Derivados de pirrolopirimidina
AR029151A1 (es) Una sal cuaternaria de piperidina, su uso, un proceso para su preparacion, y una composicion farmaceutica que la contiene
RU2004122102A (ru) Новые производные бензимидазола и их применение в качестве лекарственных препаратов
PE20090276A1 (es) Compuestos derivados de imidazoquinolina como moduladores de tlr7
AR036586A1 (es) Nuevas dihidro-pteridinonas, procedimientos para su preparacion, su utilizacion como medicamentos y las formulaciones farmaceuticas que las contienen
PE20070798A1 (es) Compuestos heterociclicos como inhibidores de aspartil proteasas
PE20001403A1 (es) Derivados de pirrolidina como antagonistas del receptor ccr-3
PE20070138A1 (es) Compuestos heterociclicos como inhibidores de aspartil proteasas
DOP2003000694A (es) Nuevos derivados de benzoimidazol utiles como agentes antiproliferativos
AR057408A1 (es) Agonistas del receptor de niacina composiciones que contienen tales compuestos y procedimientos para tratamiento
PE20010964A1 (es) Derivados de tiazolilamida
CO4810375A1 (es) Derivados de 9-amino-3-ceto eritromicina

Legal Events

Date Code Title Description
FA Abandonment or withdrawal
FC Refusal