AR085316A1 - Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas - Google Patents

Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas

Info

Publication number
AR085316A1
AR085316A1 ARP120100389A ARP120100389A AR085316A1 AR 085316 A1 AR085316 A1 AR 085316A1 AR P120100389 A ARP120100389 A AR P120100389A AR P120100389 A ARP120100389 A AR P120100389A AR 085316 A1 AR085316 A1 AR 085316A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
cycloalkyl
aryl
heteroaryl
Prior art date
Application number
ARP120100389A
Other languages
English (en)
Inventor
Ying Zhang
Marika Nespi
Todd Ewing
Jack Lin
Jiazhong Zhang
Guoxian Wu
Songyuan Shi
Prabha N Ibrahim
Hanna Cho
Chao Zhang
Wayne Spevak
Original Assignee
Plexxikon 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46638904&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR085316(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Plexxikon Inc filed Critical Plexxikon Inc
Publication of AR085316A1 publication Critical patent/AR085316A1/es

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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/535—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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

Composición farmacéutica y proceso de preparación.Reivindicación 1: Un compuesto de fórmula (1), o sales, hidratos, solvatos, tautómeros e isómeros de los mismos aceptables farmacéuticamente; donde: Y1 se selecciona del grupo que consiste en CN, halógeno, -OH, alquilo C1-6 sustituido opcionalmente, alcoxi C1-6 sustituido opcionalmente, cicloalquilo C3-6 sustituido opcionalmente, haloalquilo C1-6 sustituido opcionalmente, haloalcoxi C1-6 sustituido opcionalmente, arilo sustituido opcionalmente y heteroarilo sustituido opcionalmente; opcionalmente donde los dos sustituyentes adyacentes en el anillo de arilo o heteroarilo junto con los átomos a los cuales están unidos forman un anillo de 5 ó 6 miembros sustituido opcionalmente que tiene de 0 a 3 heteroátomos adicionales seleccionados de N, O ó S; Y2 es H, halógeno, CN, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, haloalcoxi C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo C3-8-alquilo C0-4 o (R2)(R3)N-, donde R2 y R3 son seleccionados cada uno por separado del grupo que consiste en H, alquilo C1-6, alcoxi C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo C3-8-alquilo C0-4, heterocicloalquilo y heterocicloalquilo-alquilo C1-4; o R2 y R3 tomados junto con el átomo de nitrógeno al cual están unidos forman un anillo de tres a ocho miembros que tiene de 0 - 2 heteroátomos adicionales como miembros de anillo seleccionados de N, O ó S; donde Y2 es sustituido opcionalmente con uno a tres grupos seleccionados por separado de Re; Q es seleccionado de H, F, Cl o CH3; Z es -N(R4)(R5) o -C(R6)(R7)(R8), donde R4 y R5 son seleccionados cada uno por separado del grupo que consiste en H, alquilo C1-6 sustituido opcionalmente, cicloalquilo C3-8 sustituido opcionalmente, cicloalquilo C3-8 alquilo sustituido opcionalmente, heterocicloalquilo sustituido opcionalmente, heterocicloalquilalquilo sustituido opcionalmente, arilo sustituido opcionalmente, arilalquilo sustituido opcionalmente, heteroarilo sustituido opcionalmente y heteroarilalquilo sustituido opcionalmente; o R4 y R5 tomados junto con el átomo de nitrógeno al cual están unidos forman un anillo de cuatro a ocho miembros que tiene de 0 - 2 heteroátomos adicionales como miembros de anillo seleccionados de N, O ó S, donde el anillo de cuatro a ocho miembros es sustituido opcionalmente; R6, R7 y R8 son cada uno por separado H, alquilo C1-6 sustituido opcionalmente, haloalquilo C1-6 sustituido opcionalmente, haloalcoxi C1-6 sustituido opcionalmente, cicloalquilo C3-8 sustituido opcionalmente, cicloalquilo C3-8 alquilo sustituido opcionalmente, arilo sustituido opcionalmente, arilalquilo sustituido opcionalmente, heterocicloalquilo sustituido opcionalmente, heterocicloalquilalquilo sustituido opcionalmente, heteroarilo sustituido opcionalmente, heteroarilalquilo sustituido opcionalmente o -X2R9, donde X2 es -NR10, O ó S; R10 es H, alquilo C1-6 o arilo; y R9 es H, alquilo C1-6, haloalquilo C1-6, haloalcoxi C1-6, cicloalquilo C3-8, cicloalquilalquilo C3-8, arilo, arilalquilo, heteroarilo o heteroarilalquilo, donde R9 es sustituido opcionalmente con 1 a 3 sustituyentes Re; o dos opciones cualesquiera de los grupos R6, R7 y R8 grupos tomados junto con el átomo de carbono al cual están unidos forma un anillo no aromático de 3 a 8 miembros sustituido opcionalmente que tiene de 0 a 2 heteroátomos seleccionados de N, O ó S; proporcionado en cada aparición, como mínimo dos opciones cualesquiera de los grupos R6, R7 y R8 no son simultáneamente hidrógeno; y en el entendido de que cuando (i) Y1 es halógeno, -CH3, -CN, -OMe o 2-metoxipirimidin-5-il, Z es otro aparte de dimetilamino, dietilamino, 1-pirrolodina, 1-piperidinilo, 4-morfolinilo, isopropilo, -CH(CH3)(CH2CH3), -CH(CH3)(CH2CH2CH3), ciclobutilo, ciclopentilo o ciclohexilo; y (ii) cuando Y1 es 1-metil-4-pirazolilo, 3-metilsulfonilfenilo o 3-metilsulfonilaminofenilo, Z es otro aparte de ciclopropilo, ciclobutilo, ciclopentilo o ciclohexilo.
ARP120100389A 2011-02-07 2012-02-07 Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas AR085316A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161440339P 2011-02-07 2011-02-07

Publications (1)

Publication Number Publication Date
AR085316A1 true AR085316A1 (es) 2013-09-25

Family

ID=46638904

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100389A AR085316A1 (es) 2011-02-07 2012-02-07 Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas

Country Status (35)

Country Link
US (3) US9624213B2 (es)
EP (1) EP2672967B1 (es)
JP (3) JP5941069B2 (es)
KR (1) KR101911972B1 (es)
CN (1) CN103517710B (es)
AR (1) AR085316A1 (es)
AU (1) AU2012214762B2 (es)
BR (1) BR112013020041B1 (es)
CA (1) CA2826123C (es)
CL (1) CL2013002228A1 (es)
CO (1) CO6781514A2 (es)
CR (1) CR20130374A (es)
CY (1) CY1121511T1 (es)
DK (1) DK2672967T3 (es)
EA (1) EA028821B9 (es)
EC (1) ECSP13012869A (es)
ES (1) ES2696023T3 (es)
HR (1) HRP20181779T1 (es)
HU (1) HUE040136T2 (es)
IL (1) IL227698B (es)
LT (1) LT2672967T (es)
MA (1) MA34948B1 (es)
MX (1) MX358128B (es)
MY (1) MY162950A (es)
PE (1) PE20141360A1 (es)
PL (1) PL2672967T3 (es)
PT (1) PT2672967T (es)
RS (1) RS58455B1 (es)
SG (1) SG192686A1 (es)
SI (1) SI2672967T1 (es)
TR (1) TR201816421T4 (es)
TW (1) TWI640521B (es)
UY (1) UY33899A (es)
WO (1) WO2012109075A1 (es)
ZA (1) ZA201305856B (es)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US20100190777A1 (en) 2007-07-17 2010-07-29 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
CN105237530A (zh) 2009-04-03 2016-01-13 豪夫迈罗氏公司 丙烷-1-磺酸{3-[5-(4-氯-苯基)-1H-吡咯并[2,3-b]吡啶-3-羰基]-2,4-二氟-苯基}-酰胺组合物及其用途
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011057022A1 (en) 2009-11-06 2011-05-12 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
RU2012125070A (ru) 2009-11-18 2013-12-27 Плексксикон, Инк. Соединения и способы модулирования киназы и показания к их применению
RU2012131373A (ru) 2009-12-23 2014-01-27 Плексксикон, Инк. Соединения и способы модулирования киназы, а также показания для такого модулирования
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
PT2672967T (pt) * 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
WO2012158957A2 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
JP2015502958A (ja) * 2011-12-09 2015-01-29 オンコメッド ファーマシューティカルズ インコーポレイテッド がんの処置のための併用療法
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
WO2013142817A2 (en) 2012-03-23 2013-09-26 Dennis Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
US9150570B2 (en) * 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
TWI601725B (zh) 2012-08-27 2017-10-11 加拓科學公司 取代的氮雜吲哚化合物及其鹽、組合物和用途
WO2014039714A2 (en) 2012-09-06 2014-03-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
JP6832846B2 (ja) 2014-09-15 2021-02-24 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ヘテロ環化合物およびその用途
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
RU2730506C2 (ru) 2015-05-06 2020-08-24 Плексксикон Инк. Твердые формы соединения, модулирующего киназы
CA2984899C (en) 2015-05-06 2021-06-15 Plexxikon Inc. Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases
CN107801378A (zh) * 2015-05-22 2018-03-13 普莱希科公司 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904
CN107771178B (zh) * 2015-05-22 2021-04-06 普莱希科公司 杂环化合物的合成
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG10201912386RA (en) 2015-09-21 2020-02-27 Plexxikon Inc Heterocyclic compounds and uses thereof
WO2017066193A1 (en) * 2015-10-15 2017-04-20 Princeton Drug Discovery, Llc Novel inhibitors of protein kinases
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US9938273B2 (en) 2015-12-07 2018-04-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
JP6921846B6 (ja) 2016-03-16 2021-09-15 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節およびその適応症のための化合物および方法
GEP20227339B (en) 2016-04-04 2022-01-25 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)- pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydro-xypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3439663B1 (en) 2016-04-04 2024-07-17 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3024603A1 (en) 2016-05-18 2017-11-23 Charles Todd Eary Process for the preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
US11020398B2 (en) 2016-08-24 2021-06-01 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CA3047784A1 (en) * 2016-12-23 2018-06-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
JP7300394B2 (ja) * 2017-01-17 2023-06-29 ヘパリジェニックス ゲーエムベーハー 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
JP2020511467A (ja) 2017-03-20 2020-04-16 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ブロモドメインを阻害する４−（１−（１，１−ジ（ピリジン−２−イル）エチル）−６−（３，５−ジメチルイソオキサゾール−４−イル）−１Ｈ−ピロロ［３，２−ｂ］ピリジン−３−イル）安息香酸の結晶形
JP7309614B2 (ja) 2017-05-02 2023-07-18 ノバルティス アーゲー 組み合わせ療法
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
KR102615829B1 (ko) 2017-07-25 2023-12-20 플렉시콘 인코퍼레이티드 키나제를 조정하는 화합물의 제제
TW202410896A (zh) 2017-10-10 2024-03-16 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
CA3080197C (en) * 2017-10-27 2023-12-19 Plexxikon Inc. Formulations of a compound modulating kinases
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
TWI802635B (zh) 2018-01-18 2023-05-21 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
US11858927B2 (en) 2018-01-31 2024-01-02 Heparegenix Gmbh Protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
CN112119072A (zh) 2018-03-20 2020-12-22 普莱希科公司 用于ido和tdo调节的化合物和方法，以及其适应症
RU2687107C1 (ru) * 2018-06-18 2019-05-07 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" Ингибитор braf киназы n-(3-(5-(4-хлорофенил)-1h-пиразоло[3,4-b]пиридин-3-карбонил)-2,4-дифторофенил) пропан-1-сульфонамид
US11731968B2 (en) 2018-06-21 2023-08-22 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
US11912701B2 (en) 2018-07-16 2024-02-27 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN111434661B (zh) * 2019-01-11 2023-09-12 爱科诺生物医药(香港)有限公司 具有细胞坏死抑制活性的芳香杂环化合物及其应用
TWI849043B (zh) * 2019-01-25 2024-07-21 英屬開曼群島商百濟神州有限公司 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途
CA3136224A1 (en) 2019-04-09 2020-10-15 Plexxikon Inc. Condensed azines for ep300 or cbp modulation and indications therefor
US20220160723A1 (en) * 2019-04-18 2022-05-26 The Regents Of The University Of California Pharmacological mitigation of late-stage toxemia
WO2020214987A1 (en) * 2019-04-18 2020-10-22 Brown University Neurogenesis
JP2022544074A (ja) 2019-07-29 2022-10-17 ヘパリジェニックス ゲーエムベーハー 肝臓再生を促進または肝細胞死を縮減もしくは防止するためのヘテロアリール置換ピラゾロ－ピリジンタンパク質キナーゼ阻害剤
CN110889859A (zh) * 2019-11-11 2020-03-17 珠海上工医信科技有限公司 一种用于眼底图像血管分割的u型网络
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
CR20220299A (es) 2019-12-20 2022-08-05 Pfizer Derivados de becimidazol
CA3161339A1 (en) 2019-12-27 2021-07-01 Schrodinger, Inc. Cyclic compounds and methods of using same
CA3164361A1 (en) 2020-01-15 2021-07-22 Heparegenix Gmbh 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases
JP2023522949A (ja) 2020-04-23 2023-06-01 オプナ バイオ ソシエテ アノニム Ｃｄ７３調節のための化合物及び方法並びにそれらの表示
WO2022040512A1 (en) 2020-08-21 2022-02-24 Plexxikon Inc. Combinational drug anticancer therapies
WO2022055963A1 (en) 2020-09-10 2022-03-17 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法

Family Cites Families (352)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2234705A (en) 1940-04-12 1941-03-11 Eastman Kodak Co Cellulose organic derivative composition containing esters of monoalkoxy benzoic acids
US2413258A (en) 1942-07-07 1946-12-24 United Gas Improvement Co Polystyrene-type resins plasticized with high boiling fatty acid alkyl esters
GB1198301A (en) 1966-10-21 1970-07-08 Minnesota Mining & Mfg Perfluoroalkylsulfonamides
DE2413258A1 (de) 1974-03-20 1975-10-02 Bayer Ag Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide
AU7915675A (en) 1974-03-20 1976-09-23 Bayer Ag Alkoxycarbonylphenylureas
GB1573212A (en) 1976-04-15 1980-08-20 Technicon Instr Immunoassay for gentamicin
US4301159A (en) 1980-06-20 1981-11-17 Shionogi & Co., Ltd. N-(Diethylaminoethyl)-2-alkoxy-benzamide derivatives
AU547405B2 (en) 1981-07-08 1985-10-17 Sanofi Amidobenzamides
US4664504A (en) 1983-01-20 1987-05-12 Tokyo Shibaura Denki Kabushiki Kaisha Image forming apparatus
US4568649A (en) 1983-02-22 1986-02-04 Immunex Corporation Immediate ligand detection assay
US4626513A (en) 1983-11-10 1986-12-02 Massachusetts General Hospital Method and apparatus for ligand detection
AU567140B2 (en) 1984-01-06 1987-11-12 Shionogi & Co., Ltd. Sulphonamido-benzamide derivatives
EP0154734B1 (en) 1984-03-15 1990-08-29 Immunex Corporation Immediate ligand detection assay, a test kit and its formation
IT1196133B (it) 1984-06-06 1988-11-10 Ausonia Farma Srl Derivati furanici con attivita' antiulcera
JPS6135946U (ja) 1984-07-23 1986-03-05 栄一 早乙女 栽培ハウス固定用杭抜
US4714693A (en) 1986-04-03 1987-12-22 Uop Inc. Method of making a catalyst composition comprising uniform size metal components on carrier
DE3642315A1 (de) 1986-12-11 1988-06-23 Boehringer Mannheim Gmbh Neue pyrrolobenzimidazole, verfahren zu ihrer herstellung sowie arzneimittel
US5688655A (en) 1988-02-10 1997-11-18 Ict Pharmaceuticals, Inc. Method of screening for protein inhibitors and activators
US5700637A (en) 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US6054270A (en) 1988-05-03 2000-04-25 Oxford Gene Technology Limited Analying polynucleotide sequences
US5658775A (en) 1988-05-17 1997-08-19 Sloan-Kettering Institute For Cancer Research Double copy retroviral vector
JP2528706B2 (ja) 1988-05-30 1996-08-28 ゼリア新薬工業株式会社 ジヒドロピリジン化合物の製剤組成物
CA1339354C (en) 1988-09-01 1997-08-26 The Whitehead Institute For Biomedical Research Recombinant retroviruses with amphotropic and ecotropic host ranges
US5703055A (en) 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
US5527681A (en) 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5143854A (en) 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5744101A (en) 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5800992A (en) 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
WO1991018088A1 (en) 1990-05-23 1991-11-28 The United States Of America, Represented By The Secretary, United States Department Of Commerce Adeno-associated virus (aav)-based eucaryotic vectors
DE4022414A1 (de) 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
US5958930A (en) 1991-04-08 1999-09-28 Duquesne University Of The Holy Ghost Pyrrolo pyrimidine and furo pyrimidine derivatives
AU1537292A (en) 1991-04-16 1992-11-17 Nippon Shinyaku Co. Ltd. Method of manufacturing solid dispersion
WO1993002556A1 (en) 1991-07-26 1993-02-18 University Of Rochester Cancer therapy utilizing malignant cells
US5632957A (en) 1993-11-01 1997-05-27 Nanogen Molecular biological diagnostic systems including electrodes
GB9127531D0 (en) 1991-12-31 1992-02-19 Fujisawa Pharmaceutical Co Heterocyclic compound
FR2687402B1 (fr) 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
JPH05236997A (ja) 1992-02-28 1993-09-17 Hitachi Ltd ポリヌクレオチド捕捉用チップ
JPH06135946A (ja) 1992-10-30 1994-05-17 Otsuka Pharmaceut Co Ltd ピラジン誘導体
AU686115B2 (en) 1992-11-02 1998-02-05 Fujisawa Pharmaceutical Co., Ltd. Imidazo (I,2-a) pyridine derivatives as bradykinin antagonists, pharmaceuticals and processes for their preparation
GB9226855D0 (en) 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation
US5700809A (en) 1993-03-01 1997-12-23 Merck Sharp & Dohme, Ltd. Pyrrolo-pyridine derivatives
CA2156410A1 (en) 1993-03-01 1994-09-15 Raymond Baker Pyrrolo-pyridine derivatives
US5576319A (en) 1993-03-01 1996-11-19 Merck, Sharp & Dohme Ltd. Pyrrolo-pyridine derivatives
WO1994020497A1 (en) 1993-03-01 1994-09-15 Merck Sharp & Dohme Limited Pyrrolo-pyridine derivatives
JP3394777B2 (ja) 1993-05-27 2003-04-07 セレクタイド コーポレーション 位相学的に分離された、コードされた固相ライブラリー
US5840485A (en) 1993-05-27 1998-11-24 Selectide Corporation Topologically segregated, encoded solid phase libraries
IT1265057B1 (it) 1993-08-05 1996-10-28 Dompe Spa Tropil 7-azaindolil-3-carbossiamidi
US5631236A (en) 1993-08-26 1997-05-20 Baylor College Of Medicine Gene therapy for solid tumors, using a DNA sequence encoding HSV-Tk or VZV-Tk
US5426039A (en) 1993-09-08 1995-06-20 Bio-Rad Laboratories, Inc. Direct molecular cloning of primer extended DNA containing an alkane diol
GB9319297D0 (en) 1993-09-17 1993-11-03 Wellcome Found Indole derivatives
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US5965452A (en) 1996-07-09 1999-10-12 Nanogen, Inc. Multiplexed active biologic array
US6468742B2 (en) 1993-11-01 2002-10-22 Nanogen, Inc. Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip
US5486525A (en) 1993-12-16 1996-01-23 Abbott Laboratories Platelet activating factor antagonists: imidazopyridine indoles
US5360882A (en) 1994-02-04 1994-11-01 Isp Investments Inc. Eutectic compositions of divinyl imidazolidone and vinyl caprolactam
EP1195372A1 (en) 1994-04-18 2002-04-10 Mitsubishi Pharma Corporation N-heterocyclic substituted benzamide derivatives with antihypertensive activity
GB9408577D0 (en) 1994-04-29 1994-06-22 Fujisawa Pharmaceutical Co New compound
US5807522A (en) 1994-06-17 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods for fabricating microarrays of biological samples
GB9412719D0 (en) 1994-06-24 1994-08-17 Erba Carlo Spa Substituted azaindolylidene compounds and process for their preparation
US5763198A (en) 1994-07-22 1998-06-09 Sugen, Inc. Screening assays for compounds
GB9416162D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
ATE189895T1 (de) 1994-08-10 2000-03-15 Merck Sharp & Dohme Tetrahydropyridinylmethylderivate von pyrrolo(2,3-b)pyridine
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9420521D0 (en) 1994-10-12 1994-11-30 Smithkline Beecham Plc Novel compounds
US5556752A (en) 1994-10-24 1996-09-17 Affymetrix, Inc. Surface-bound, unimolecular, double-stranded DNA
US5830645A (en) 1994-12-09 1998-11-03 The Regents Of The University Of California Comparative fluorescence hybridization to nucleic acid arrays
US5837815A (en) 1994-12-15 1998-11-17 Sugen, Inc. PYK2 related polypeptide products
GB2298199A (en) 1995-02-21 1996-08-28 Merck Sharp & Dohme Synthesis of azaindoles
GB9503400D0 (en) 1995-02-21 1995-04-12 Merck Sharp & Dohme Therpeutic agents
US5959098A (en) 1996-04-17 1999-09-28 Affymetrix, Inc. Substrate preparation process
US6117681A (en) 1995-03-29 2000-09-12 Bavarian Nordic Research Inst. A/S Pseudotyped retroviral particles
GB2299581A (en) 1995-04-07 1996-10-09 Merck Sharp & Dohme 3-(Tetrahydropyridin-1-yl-methyl)pyrrolo[2,3-b]pyridine derivatives as ligands for dopamine receptor subtypes
GB9507291D0 (en) 1995-04-07 1995-05-31 Merck Sharp & Dohme Therapeutic agents
GB9511220D0 (en) 1995-06-02 1995-07-26 Glaxo Group Ltd Solid dispersions
US6110456A (en) 1995-06-07 2000-08-29 Yale University Oral delivery or adeno-associated viral vectors
US5856174A (en) 1995-06-29 1999-01-05 Affymetrix, Inc. Integrated nucleic acid diagnostic device
WO1997003967A1 (en) 1995-07-22 1997-02-06 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
US5866411A (en) 1995-09-08 1999-02-02 Pedersen; Finn Skou Retroviral vector, a replication system for said vector and avian or mammalian cells transfected with said vector
US5747276A (en) 1995-09-15 1998-05-05 The Scripps Research Institute Screening methods for the identification of novel antibiotics
US5721118A (en) 1995-10-31 1998-02-24 The Regents Of The University Of California, San Diego Mammalian artificial chromosomes and methods of using same
US6022963A (en) 1995-12-15 2000-02-08 Affymetrix, Inc. Synthesis of oligonucleotide arrays using photocleavable protecting groups
US6013440A (en) 1996-03-11 2000-01-11 Affymetrix, Inc. Nucleic acid affinity columns
US6025155A (en) 1996-04-10 2000-02-15 Chromos Molecular Systems, Inc. Artificial chromosomes, uses thereof and methods for preparing artificial chromosomes
US5804585A (en) 1996-04-15 1998-09-08 Texas Biotechnology Corporation Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
US5908401A (en) 1996-05-08 1999-06-01 The Aps Organization, Llp Method for iontophoretic delivery of antiviral agents
US5725838A (en) 1996-05-31 1998-03-10 Resolution Pharmaceuticals, Inc. Radiolabeled D4 receptor ligands
US6057100A (en) 1996-06-07 2000-05-02 Eos Biotechnology, Inc. Oligonucleotide arrays
EP0923577A2 (en) 1996-06-25 1999-06-23 Takeda Chemical Industries, Ltd. Oxazolone derivatives and their use as anti-helicobacter pylori agent
DE69737631T3 (de) 1996-08-12 2011-08-18 Mitsubishi Tanabe Pharma Corp. MEDIKAMENTE ENTHALTEND Rho-KINASE INHIBITOREN
JPH10130269A (ja) 1996-09-04 1998-05-19 Nippon Chemiphar Co Ltd カルボリン誘導体
JPH1087629A (ja) 1996-09-18 1998-04-07 Fujisawa Pharmaceut Co Ltd 新規イソキノリン誘導体、およびその医薬用途
ATE264318T1 (de) 1996-11-19 2004-04-15 Amgen Inc Aryl und heteroaryl substituierte kondensierte pyrrole als entzündunghemmende mittel
US6294330B1 (en) 1997-01-31 2001-09-25 Odyssey Pharmaceuticals Inc. Protein fragment complementation assays for the detection of biological or drug interactions
CA2283434A1 (en) 1997-03-07 1998-09-11 Tropix, Inc. Protease inhibitor assay
US5977131A (en) 1997-04-09 1999-11-02 Pfizer Inc. Azaindole-ethylamine derivatives as nicotinic acetylcholine receptor binding agents
WO1998047899A1 (en) 1997-04-24 1998-10-29 Ortho-Mcneil Corporation, Inc. Substituted pyrrolopyridines useful in the treatment of inflammatory diseases
US6096718A (en) 1997-06-05 2000-08-01 Gene Targeting Corp. Tissue specific adenovirus vectors for breast cancer treatment
SG72827A1 (en) 1997-06-23 2000-05-23 Hoffmann La Roche Phenyl-and aminophenyl-alkylsulfonamide and urea derivatives
AU8096798A (en) 1997-06-27 1999-01-19 Resolution Pharmaceuticals Inc. Dopamine d4 receptor ligands
US6235769B1 (en) 1997-07-03 2001-05-22 Sugen, Inc. Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
US6826296B2 (en) 1997-07-25 2004-11-30 Affymetrix, Inc. Method and system for providing a probe array chip design database
EP0901786B1 (en) 1997-08-11 2007-06-13 Pfizer Products Inc. Solid pharmaceutical dispersions with enhanced bioavailability
US6161776A (en) 1997-08-12 2000-12-19 Nibco Inc. Multi-layered, porous mat turf irrigation apparatus and method
WO1999009217A1 (en) 1997-08-15 1999-02-25 Hyseq, Inc. Methods and compositions for detection or quantification of nucleic acid species
ATE319986T1 (de) 1997-09-11 2006-03-15 Bioventures Inc Verfahren zur herstellung von arrays hoher dichte
US6178384B1 (en) 1997-09-29 2001-01-23 The Trustees Of Columbia University In The City Of New York Method and apparatus for selecting a molecule based on conformational free energy
US6465178B2 (en) 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
CZ299156B6 (cs) 1997-12-22 2008-05-07 Bayer Corporation Substituované heterocyklické mocoviny, farmaceutické prípravky je obsahující a jejich použití
BR9814327A (pt) 1997-12-23 2000-10-03 Warner Lambert Co Compostos de tiouréia e benzamida, composições e pro-cessos para tratamento ou prevenção de doenças infla-matórias e arteriosclerose
AU3367999A (en) 1998-04-02 1999-10-25 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
JP2002510628A (ja) 1998-04-02 2002-04-09 メルク エンド カムパニー インコーポレーテッド 性腺刺激ホルモン放出ホルモン拮抗薬
CA2326185A1 (en) 1998-04-02 1999-10-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1999051595A1 (en) 1998-04-02 1999-10-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EP1071423A1 (en) 1998-04-02 2001-01-31 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU3118399A (en) 1998-04-02 1999-10-25 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
ATE340870T1 (de) 1998-04-03 2006-10-15 Compound Therapeutics Inc Adressierbare protein arrays
US6048695A (en) 1998-05-04 2000-04-11 Baylor College Of Medicine Chemically modified nucleic acids and methods for coupling nucleic acids to solid support
EP1085846A2 (en) 1998-06-08 2001-03-28 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
US6113913A (en) 1998-06-26 2000-09-05 Genvec, Inc. Recombinant adenovirus
JP3720264B2 (ja) 1998-08-17 2005-11-24 千寿製薬株式会社 緑内障予防・治療剤
CN1261098C (zh) 1998-08-28 2006-06-28 西奥斯股份有限公司 p38－α激酶的抑制剂
PT1107973E (pt) 1998-08-28 2004-03-31 Astrazeneca Ab Novas tieno¬2,3-d| pirimidinodionas processo para a sua preparacao e sua utilizacao em terapia
PL347138A1 (en) 1998-09-18 2002-03-25 Basf Ag 4-aminopyrrolopyrimidines as kinase inhibitors
US6594527B2 (en) 1998-09-18 2003-07-15 Nexmed Holdings, Inc. Electrical stimulation apparatus and method
US6350786B1 (en) 1998-09-22 2002-02-26 Hoffmann-La Roche Inc. Stable complexes of poorly soluble compounds in ionic polymers
US6277628B1 (en) 1998-10-02 2001-08-21 Incyte Genomics, Inc. Linear microarrays
IT1303759B1 (it) 1998-11-17 2001-02-23 Dompe Spa Procedimento migliorato per la preparazione di acido 7-azaindolil-3-carbossilico.
US6277489B1 (en) 1998-12-04 2001-08-21 The Regents Of The University Of California Support for high performance affinity chromatography and other uses
US20010001449A1 (en) 1998-12-30 2001-05-24 Thomas R. Kiliany Low-pressure hydrocracking process
CA2366260A1 (en) 1999-03-05 2000-09-14 Masahiro Imoto Heterocyclic compounds having effect of activating .alpha.4.beta.2 nicotinic acetylcholine receptors
US6792306B2 (en) 2000-03-10 2004-09-14 Biophoretic Therapeutic Systems, Llc Finger-mounted electrokinetic delivery system for self-administration of medicaments and methods therefor
BR0009083B1 (pt) 1999-03-17 2011-11-01 derivado de amida compreendendo um núcleo de quinazolinona, processo para a preparação de um derivado de amida, composição farmacêutica, e, uso de um derivado de amida.
AR028475A1 (es) 1999-04-22 2003-05-14 Wyeth Corp Derivados de azaindol y uso de los mismos para la manufactura de un medicamento para el tratamiento de la depresion.
US6653309B1 (en) 1999-04-26 2003-11-25 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme technical field of the invention
US6221653B1 (en) 1999-04-27 2001-04-24 Agilent Technologies, Inc. Method of performing array-based hybridization assays using thermal inkjet deposition of sample fluids
FR2793793B1 (fr) 1999-05-19 2004-02-27 Adir Nouveaux derives dimeriques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6492406B1 (en) 1999-05-21 2002-12-10 Astrazeneca Ab Pharmaceutically active compounds
TWI234557B (en) 1999-05-26 2005-06-21 Telik Inc Novel naphthalene ureas as glucose uptake enhancers
US7049312B1 (en) 1999-06-03 2006-05-23 Abbott Gmbh & Co. Kg Benzothiazinone and benzoxazinone compounds
CN1193026C (zh) 1999-07-30 2005-03-16 艾博特股份有限两合公司 2－吡唑啉－5－酮
US6653151B2 (en) 1999-07-30 2003-11-25 Large Scale Proteomics Corporation Dry deposition of materials for microarrays using matrix displacement
WO2001024236A1 (en) 1999-09-27 2001-04-05 Infineon Technologies North America Corp. Semiconductor structures having a capacitor and manufacturing methods
GB9924962D0 (en) 1999-10-21 1999-12-22 Mrc Collaborative Centre Allosteric sites on muscarinic receptors
EP1106603A3 (en) 1999-12-06 2003-11-19 Fuji Photo Film Co., Ltd. DNA chip and reactive solid carrier
DE60021423T2 (de) 1999-12-21 2006-04-13 Sugen, Inc., San Diego 4-substituierte 7-aza-indolin-2-one und ihre verwendung als proteinkinaseinhibitoren
DK1255536T3 (da) 1999-12-22 2006-10-30 Sugen Inc Indolinonderivater til modulation af c-kit-tyrosinproteinkinase
FR2805259B1 (fr) 2000-02-17 2002-03-29 Inst Nat Sante Rech Med Nouveaux derives d'aminoacides n-mercaptoacyles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US20020061892A1 (en) 2000-02-22 2002-05-23 Tao Wang Antiviral azaindole derivatives
JP2001278886A (ja) 2000-03-28 2001-10-10 Dai Ichi Seiyaku Co Ltd ベンゾオキサジン誘導体及びこれを含有する医薬
GB0007934D0 (en) 2000-03-31 2000-05-17 Darwin Discovery Ltd Chemical compounds
US6335342B1 (en) 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
AU2001266575A1 (en) 2000-06-26 2002-01-08 Lilly Icos Llc Chemical compounds
PT1294724E (pt) 2000-06-26 2006-07-31 Pfizer Prod Inc Compostos pirrolo (2,3-d ) pirimidina como agentes imunosupressivos
BR0113574A (pt) 2000-08-31 2003-07-22 Pfizer Prod Inc Derivados de pirazol e uso dos mesmos como inibidores de proteìna quinase
PL365746A1 (en) 2001-02-27 2005-01-10 Astrazeneca Ab Pharmaceutical formulation comprising bicalutamide
KR100865262B1 (ko) 2001-04-11 2008-10-24 센주 세이야꾸 가부시키가이샤 시각 기능 장애 개선제
US6559169B2 (en) 2001-04-24 2003-05-06 Wyeth Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan
GB0114417D0 (en) 2001-06-13 2001-08-08 Boc Group Plc Lubricating systems for regenerative vacuum pumps
EP1267111A1 (en) 2001-06-15 2002-12-18 Dsm N.V. Pressurized fluid conduit
US20040171630A1 (en) 2001-06-19 2004-09-02 Yuntae Kim Tyrosine kinase inhibitors
US7291639B2 (en) 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
SE0102300D0 (sv) 2001-06-26 2001-06-26 Astrazeneca Ab Compounds
US20030091974A1 (en) 2001-06-29 2003-05-15 Alain Moussy Method for screening compounds capable of depleting mast cells
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
UA75425C2 (en) 2001-07-09 2006-04-17 Piperazine oxime derivatives with antagonistic activity to nk-1 receptor, use thereof, a pharmaceutical composition based thereon, a method for producing and a method for producing intermediary compounds
GB0117583D0 (en) 2001-07-19 2001-09-12 Astrazeneca Ab Novel compounds
US6858860B2 (en) 2001-07-24 2005-02-22 Seiko Epson Corporation Apparatus and method for measuring natural period of liquid
GB0118479D0 (en) 2001-07-28 2001-09-19 Astrazeneca Ab Novel compounds
JP2003073357A (ja) 2001-09-03 2003-03-12 Mitsubishi Pharma Corp アミド化合物を含有するＲｈｏキナーゼ阻害剤
AU2002334355A1 (en) 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
WO2003028724A1 (en) 2001-10-04 2003-04-10 Smithkline Beecham Corporation Chk1 kinase inhibitors
WO2003037862A1 (fr) 2001-10-30 2003-05-08 Nippon Shinyaku Co., Ltd. Derives amide, et medicaments correspondants
US20030119839A1 (en) 2001-12-13 2003-06-26 Nan-Horng Lin Protein kinase inhibitors
GEP20063909B (en) 2002-01-22 2006-08-25 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES
CN101607958A (zh) 2002-02-01 2009-12-23 阿斯特拉曾尼卡有限公司 喹唑啉化合物
US20030236277A1 (en) 2002-02-14 2003-12-25 Kadow John F. Indole, azaindole and related heterocyclic pyrrolidine derivatives
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
US6884889B2 (en) 2002-03-25 2005-04-26 Bristol-Myers Squibb Co. Processes for the preparation of antiviral 7-azaindole derivatives
DE60331219D1 (de) 2002-03-28 2010-03-25 Eisai R&D Man Co Ltd Azaindole als hemmstoffe von c-jun n-terminalen kinasen
CA2480317A1 (en) 2002-03-28 2003-10-09 Eisai Co., Ltd. 7-azaindoles as inhibitors of c-jun n-terminal kinases for the treatment of neurodegenerative disorders
JP2005526831A (ja) 2002-04-09 2005-09-08 アステックス テクノロジー リミテッド 医薬化合物
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
EP1554269A1 (en) 2002-07-09 2005-07-20 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
TW200403243A (en) 2002-07-18 2004-03-01 Wyeth Corp 1-Heterocyclylalkyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
EP1388341A1 (en) 2002-08-07 2004-02-11 Aventis Pharma Deutschland GmbH Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals
US6878887B2 (en) 2002-08-07 2005-04-12 Matsushita Electric Industrial Co., Ltd. Anti-malfunction mechanism for variable output device
EP1388541A1 (en) 2002-08-09 2004-02-11 Centre National De La Recherche Scientifique (Cnrs) Pyrrolopyrazines as kinase inhibitors
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
CN102516417B (zh) 2002-09-06 2014-12-10 天蓝制药公司 用于传递治疗剂的以环糊精为基础的聚合物
CA2503905A1 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
US6766199B2 (en) 2002-10-10 2004-07-20 Proventure (Far East), Limited Skin/hair treatment method and system
US7183241B2 (en) 2002-10-15 2007-02-27 Exxonmobil Research And Engineering Company Long life lubricating oil composition with very low phosphorus content
GB0226370D0 (en) 2002-11-12 2002-12-18 Novartis Ag Organic compounds
SE0203654D0 (sv) 2002-12-09 2002-12-09 Astrazeneca Ab New compounds
MXPA05006354A (es) 2002-12-13 2005-08-26 Smithkline Beecham Corp Antagonistas ccr5 como agentes terapeuticos.
AU2003297048A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Cyclohexyl compounds as ccr5 antagonists
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
US7696225B2 (en) 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
SE0300120D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
SE0300119D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
US20050085463A1 (en) 2003-01-23 2005-04-21 Weiner David M. Use of N-desmethylclozapine to treat human neuropsychiatric disease
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
CN101091695B (zh) 2003-02-03 2011-01-19 诺瓦提斯公司 药物制剂
EP1592690A1 (en) 2003-02-14 2005-11-09 Wyeth Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
SE0300456D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
WO2004078923A2 (en) 2003-02-28 2004-09-16 Plexxikon, Inc. Pyk2 crystal structure and uses
EP1599475A2 (en) 2003-03-06 2005-11-30 Eisai Co., Ltd. Jnk inhibitors
EP1628975A2 (en) 2003-05-16 2006-03-01 Eisai Co., Ltd. Jnk inhibitors
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
ATE412650T1 (de) 2003-07-11 2008-11-15 Warner Lambert Co Isethionat salz eines selektiven cdk4 inhibitors
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
NZ545326A (en) 2003-07-17 2009-12-24 Plexxikon Inc PPAR active compounds
CL2004001884A1 (es) 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
WO2005028624A2 (en) 2003-09-15 2005-03-31 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
JP2007506741A (ja) 2003-09-23 2007-03-22 メルク　エンド　カムパニー　インコーポレーテッド 向代謝性グルタミン酸受容体のピラゾール系調節剤
KR100793095B1 (ko) 2003-10-01 2008-01-10 주식회사 프로메디텍 Ｂａｃｅ 저해효능을 가진 신규한 술폰 아미드 유도체
JP4758349B2 (ja) 2003-10-08 2011-08-24 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
EP1696920B8 (en) 2003-12-19 2015-05-06 Plexxikon Inc. Compounds and methods for development of ret modulators
JP5697294B2 (ja) 2003-12-24 2015-04-08 デュポン ニュートリション バイオサイエンシーズ エーピーエス 糖脂質アシル基転移酵素変異体及びその製造方法
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
CN1918158B (zh) 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
GB0403635D0 (en) 2004-02-18 2004-03-24 Devgen Nv Pyridinocarboxamides with improved activity as kinase inhibitors
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
WO2005086904A2 (en) 2004-03-08 2005-09-22 Amgen Inc. Therapeutic modulation of ppar (gamma) activity
KR20050091462A (ko) 2004-03-12 2005-09-15 한국과학기술연구원 푸로피리미딘 화합물 및 이를 포함하는 ｄｄｒ2 티로신키나아제 활성 저해제
EP2332940B1 (en) 2004-03-30 2012-10-31 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
KR20070002081A (ko) 2004-04-02 2007-01-04 버텍스 파마슈티칼스 인코포레이티드 Ｒｏｃｋ 및 기타 단백질 키나아제의 억제제로서 유용한아자인돌
WO2006078287A2 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
WO2005115363A2 (en) 2004-05-25 2005-12-08 Yale University Method for treating skeletal disorders resulting from fgfr malfunction
WO2005116035A1 (en) 2004-05-27 2005-12-08 Pfizer Products Inc. Pyrrolopyrimidine derivatives useful in cancer treatment
WO2005115374A1 (en) 2004-05-29 2005-12-08 7Tm Pharma A/S Crth2 receptor ligands for therapeutic use
JP2008503473A (ja) 2004-06-17 2008-02-07 プレキシコン，インコーポレーテッド Ｃ−ｋｉｔ活性を調節する化合物
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
AU2005260689B2 (en) 2004-06-30 2012-05-10 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7140816B2 (en) 2004-07-20 2006-11-28 H&S Tool, Inc. Multi-functional tube milling head
EP2239262A3 (en) 2004-07-27 2011-10-19 SGX Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7709645B2 (en) 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CA2573362A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7361764B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US20060024361A1 (en) 2004-07-28 2006-02-02 Isa Odidi Disintegrant assisted controlled release technology
WO2006010637A2 (en) 2004-07-30 2006-02-02 Gpc Biotech Ag Pyridinylamines
EP1786813A2 (en) 2004-09-03 2007-05-23 Plexxikon, Inc. Bicyclic heteroaryl pde4b inhibitors
JP2008521829A (ja) 2004-11-30 2008-06-26 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
WO2006060535A2 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
ATE524467T1 (de) 2005-04-25 2011-09-15 Merck Patent Gmbh Neuartige aza-heterozyklen als kinase-inhibitoren
FR2884821B1 (fr) 2005-04-26 2007-07-06 Aventis Pharma Sa Pyrrolopyridines substitues, compositions les contenant, procede de fabrication et utilisation
NZ563444A (en) 2005-05-17 2011-04-29 Plexxikon Inc Pyrrolo(2,3-b)pyridine derivatives as protein kinase inhibitors
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
EP1883625A2 (en) 2005-05-23 2008-02-06 Teva Pharmaceutical Industries Ltd Amorphous cinacalcet hydrochloride and preparation thereof
US8067638B2 (en) 2005-06-21 2011-11-29 Mitsui Chemicals, Inc. Amide derivative and insecticide containing the same
NZ565255A (en) 2005-06-22 2010-04-30 Plexxikon Inc Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
US20080194622A1 (en) 2005-06-23 2008-08-14 Astrazeneca Ab Quinoline 3-Sulfonate Esters as Nk3 Receptor Modulators
DE102005034406A1 (de) 2005-07-22 2007-02-01 Ratiopharm Gmbh Neue Salze von Rosiglitazon
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
US20070072904A1 (en) 2005-09-07 2007-03-29 Jack Lin PPAR active compounds
JP2009509932A (ja) 2005-09-07 2009-03-12 プレキシコン，インコーポレーテッド Ｐｐａｒ活性化合物
AU2006287521A1 (en) 2005-09-07 2007-03-15 Plexxikon, Inc. PPARactive compounds
CN101494979A (zh) 2006-03-20 2009-07-29 沃泰克斯药物股份有限公司 药物组合物
US7963673B2 (en) 2006-05-30 2011-06-21 Finn Bruce L Versatile illumination system
WO2008058341A1 (en) 2006-11-15 2008-05-22 Cytopia Research Pty Ltd Inhibitors of kinase activity
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
GB0624084D0 (en) 2006-12-01 2007-01-10 Selamine Ltd Ramipril amino acid salts
US8093246B2 (en) 2006-12-14 2012-01-10 Lexicon Pharmaceuticals, Inc. O-linked pyrimidin-4-amine-based compounds, compositions comprising them, and methods of their use to treat cancer
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
MX2009009290A (es) 2007-03-08 2009-09-10 Plexxikon Inc Compuestos activos en ppar.
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
EP2155166A2 (en) 2007-05-11 2010-02-24 F. Hoffmann-Roche AG Pharmaceutical compositions for poorly soluble drugs
CL2008001540A1 (es) 2007-05-29 2009-05-22 Sgx Pharmaceuticals Inc Compuestos derivados de pirrolopiridinas y pirazolopiridinas; composicion farmaceutica; y uso en el tratamiento del cancer.
US20100190777A1 (en) 2007-07-17 2010-07-29 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP5769963B2 (ja) 2007-07-23 2015-08-26 ファーマシェン エス．エー． ジヒドロピリジンカルシウムチャンネルアンタゴニストを含む薬学的組成物とその調製方法
CA2639416C (en) 2007-09-11 2019-12-31 F. Hoffmann-La Roche Ag Diagnostic test for susceptibility to b-raf kinase inhibitors
PE20091561A1 (es) 2008-02-29 2009-10-30 Array Biopharma Inc Compuestos inhibidores de raf y metodos para su uso
AR072657A1 (es) 2008-02-29 2010-09-15 Genentech Inc Compuestos inhibidores de raf y metodos para su uso
CA2716949A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
US20110003809A1 (en) 2008-02-29 2011-01-06 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
WO2009115084A2 (de) 2008-03-20 2009-09-24 Schebo Biotech Ag Neue pyrrolopyrimidin-derivate und deren verwendungen
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
CN102112478A (zh) 2008-06-10 2011-06-29 普莱希科公司 用于激酶调节的5h-吡咯[2，3-b]吡嗪衍生物和其适应症
BRPI0917459B1 (pt) 2008-08-20 2017-09-12 Zoetis Services Llc N-methyl-1- [trans-4- [methyl (7h-pyrrol [2,3-d] pyridol [2,3-d] pyrimidine compounds, use of these in therapy and crystalline a form of n-methyl- pyrimidin-4-yl) amino] cyclohexyl} methanosulphonamide
UY32251A (es) 2008-11-20 2010-05-31 Glaxosmithkline Llc Compuestos quimicos
US8129404B2 (en) 2009-03-11 2012-03-06 Plexxikon Inc. Compounds and uses thereof
TW201036973A (en) * 2009-03-11 2010-10-16 Plexxikon Inc Compounds and uses thereof
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
CN105237530A (zh) 2009-04-03 2016-01-13 豪夫迈罗氏公司 丙烷-1-磺酸{3-[5-(4-氯-苯基)-1H-吡咯并[2,3-b]吡啶-3-羰基]-2,4-二氟-苯基}-酰胺组合物及其用途
WO2010129467A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
WO2011057022A1 (en) 2009-11-06 2011-05-12 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2011060216A1 (en) 2009-11-12 2011-05-19 Concert Pharmaceuticals Inc. Substituted azaindoles
RU2012125070A (ru) * 2009-11-18 2013-12-27 Плексксикон, Инк. Соединения и способы модулирования киназы и показания к их применению
RU2012131373A (ru) 2009-12-23 2014-01-27 Плексксикон, Инк. Соединения и способы модулирования киназы, а также показания для такого модулирования
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
US8779150B2 (en) * 2010-07-21 2014-07-15 Hoffmann-La Roche Inc. Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
US8709419B2 (en) 2010-08-17 2014-04-29 Hoffmann-La Roche, Inc. Combination therapy
FR2964757B1 (fr) 2010-09-09 2013-04-05 Giroptic Dispositif optique pour la capture d'images selon un champ de 360°
WO2012037060A1 (en) * 2010-09-13 2012-03-22 Concert Pharmaceuticals Inc. Substituted azaindoles
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
PT2672967T (pt) * 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
WO2012138809A1 (en) 2011-04-05 2012-10-11 Dawei Zhang Heterocyclic compounds as kinase inhibitors
WO2012158957A2 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
US20130172375A1 (en) 2011-12-13 2013-07-04 Hoffmann-La Roche Inc. Pharmaceutical composition
US9134807B2 (en) 2012-03-02 2015-09-15 Microsoft Technology Licensing, Llc Pressure sensitive key normalization
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2014039714A2 (en) 2012-09-06 2014-03-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2014100620A2 (en) 2012-12-21 2014-06-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
MX2015012456A (es) 2013-03-15 2016-02-03 Plexxikon Inc Compuestos heterociclicos y usos de los mismos.
CN105228983A (zh) 2013-05-30 2016-01-06 普莱希科公司 用于激酶调节的化合物及其适应症
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP6832846B2 (ja) 2014-09-15 2021-02-24 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ヘテロ環化合物およびその用途
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2984899C (en) 2015-05-06 2021-06-15 Plexxikon Inc. Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases
RU2730506C2 (ru) 2015-05-06 2020-08-24 Плексксикон Инк. Твердые формы соединения, модулирующего киназы
CN107771178B (zh) 2015-05-22 2021-04-06 普莱希科公司 杂环化合物的合成
CN107801378A (zh) 2015-05-22 2018-03-13 普莱希科公司 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG10201912386RA (en) 2015-09-21 2020-02-27 Plexxikon Inc Heterocyclic compounds and uses thereof
US9938273B2 (en) 2015-12-07 2018-04-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP6921846B6 (ja) 2016-03-16 2021-09-15 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節およびその適応症のための化合物および方法
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
JP2020511467A (ja) 2017-03-20 2020-04-16 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ブロモドメインを阻害する４−（１−（１，１−ジ（ピリジン−２−イル）エチル）−６−（３，５−ジメチルイソオキサゾール−４−イル）−１Ｈ−ピロロ［３，２−ｂ］ピリジン−３−イル）安息香酸の結晶形
WO2018226846A1 (en) 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
KR102615829B1 (ko) 2017-07-25 2023-12-20 플렉시콘 인코퍼레이티드 키나제를 조정하는 화합물의 제제
EP3694855A1 (en) 2017-10-13 2020-08-19 Plexxikon Inc. Solid forms of a compound for modulating kinases
CA3080197C (en) 2017-10-27 2023-12-19 Plexxikon Inc. Formulations of a compound modulating kinases
CN112119072A (zh) 2018-03-20 2020-12-22 普莱希科公司 用于ido和tdo调节的化合物和方法，以及其适应症
CA3136224A1 (en) 2019-04-09 2020-10-15 Plexxikon Inc. Condensed azines for ep300 or cbp modulation and indications therefor
WO2021113625A1 (en) 2019-12-06 2021-06-10 Plexxikon Inc. Compounds and methods for cd73 modulation and indications therefor
WO2021202900A1 (en) 2020-04-02 2021-10-07 Plexxikon Inc. 1,6-naphthyridine compounds and methods for csk modulation and indications therefor
JP2023522949A (ja) 2020-04-23 2023-06-01 オプナ バイオ ソシエテ アノニム Ｃｄ７３調節のための化合物及び方法並びにそれらの表示
WO2022040512A1 (en) 2020-08-21 2022-02-24 Plexxikon Inc. Combinational drug anticancer therapies
WO2022061251A1 (en) 2020-09-18 2022-03-24 Plexxikon Inc. Compounds and methods for kras modulation and indications therefor

Also Published As

Publication number Publication date
US20170157120A1 (en) 2017-06-08
AU2012214762A1 (en) 2013-04-11
UY33899A (es) 2012-09-28
US11337976B2 (en) 2022-05-24
CA2826123C (en) 2016-08-09
PL2672967T3 (pl) 2019-04-30
JP2017160224A (ja) 2017-09-14
CN103517710B (zh) 2017-05-31
WO2012109075A1 (en) 2012-08-16
JP2014504640A (ja) 2014-02-24
IL227698B (en) 2018-01-31
ECSP13012869A (es) 2013-12-31
JP5941069B2 (ja) 2016-06-29
EP2672967A4 (en) 2014-08-20
KR101911972B1 (ko) 2018-10-25
RS58455B1 (sr) 2019-04-30
TR201816421T4 (tr) 2018-11-21
ES2696023T3 (es) 2019-01-11
MA34948B1 (fr) 2014-03-01
DK2672967T3 (da) 2019-01-02
BR112013020041A2 (pt) 2016-10-25
KR20140064712A (ko) 2014-05-28
US20140128373A1 (en) 2014-05-08
TW201309693A (zh) 2013-03-01
IL227698A0 (en) 2013-09-30
JP6359720B2 (ja) 2018-07-18
NZ613786A (en) 2015-09-25
HRP20181779T1 (hr) 2018-12-28
JP2016138119A (ja) 2016-08-04
CL2013002228A1 (es) 2014-03-07
EA028821B1 (ru) 2018-01-31
PT2672967T (pt) 2018-12-07
ZA201305856B (en) 2021-05-26
MY162950A (en) 2017-07-31
CY1121511T1 (el) 2020-05-29
US9624213B2 (en) 2017-04-18
CR20130374A (es) 2013-11-18
PE20141360A1 (es) 2014-10-13
BR112013020041B1 (pt) 2021-11-23
EA028821B9 (ru) 2018-10-31
LT2672967T (lt) 2018-12-10
TWI640521B (zh) 2018-11-11
US12076322B2 (en) 2024-09-03
EP2672967B1 (en) 2018-10-17
HUE040136T2 (hu) 2019-02-28
SI2672967T1 (sl) 2018-12-31
CN103517710A (zh) 2014-01-15
EP2672967A1 (en) 2013-12-18
US20230277534A1 (en) 2023-09-07
CA2826123A1 (en) 2012-08-16
SG192686A1 (en) 2013-09-30
EA201391019A1 (ru) 2014-01-30
AU2012214762B2 (en) 2015-08-13
MX2013009068A (es) 2013-12-16
CO6781514A2 (es) 2013-10-31
MX358128B (es) 2018-08-06

Similar Documents

Publication Publication Date Title
AR085316A1 (es) Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas
PE20190811A1 (es) Derivados de pirazolopirimidinas como inhibidor de quinasa
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
AR080785A1 (es) Derivados de imidazo[1,2-a]pirimidina ,proceso para prepararlos e intermediarios de dicha sintesis, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de patologias del sistema nervioso central,tales como esquizofrenia y parkinson, entre otros.
AR087328A1 (es) Derivados de imidazo[1,2-b]piridazina e imidazo[4,5-b]piridina como inhibidores de jak
AR067413A1 (es) Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer
AR084849A1 (es) Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
AR085958A1 (es) 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer
ES2669189T3 (es) Compuestos de carbazol útiles como inhibidores del bromodominio
NZ627036A (en) Piperidino-pyrimidine derivatives for the treatment of viral infections
AR077975A1 (es) Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
PE20130188A1 (es) Pirrolidinonas heteroaromaticas fusionadas como inhibidores de syk
AR081369A1 (es) Compuestos de 2-5-6-7-tetrahidro-(1,4) oxazepin-3-ilamina o 2,3,6,7-tetrahidro-(1,4) oxazepin-5-ilamina, sus procesos de obtencion y composiciones farmaceuticas que los contienen
AR077695A1 (es) Derivados de pirimidina como inhibidores del factor ixa
AR083358A1 (es) Compuestos de furo[3,2-d]pirimidina
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
AR082885A1 (es) Compuestos y composiciones para la inhibicion de nampt
AR086983A1 (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
AR081978A1 (es) Derivados fusionados de pirimidina para la inhibicion de la actividad quinasa de tirosina
AR071512A1 (es) Derivados de imidazolidinona como inhibidores de 11b-hsd1
AR085398A1 (es) Ureas asimetricas y usos medicos de las mismas
AR076008A1 (es) Derivados de hidroximetil-isoxazol moduladores de receptores gaba a, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para el tratamiento del alzheimer y otros trastornos cognitivos.
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
PE20141553A1 (es) Compuestos de triazolopiridina como inhibidores de la ped10a

Legal Events

Date Code Title Description
FC Refusal