RU2418800C2 - Пирроло[2, 3-в]пиридиновые производные в качестве ингибиторов протеинкиназ - Google Patents

Пирроло[2, 3-в]пиридиновые производные в качестве ингибиторов протеинкиназ Download PDF

Info

Publication number
RU2418800C2
RU2418800C2 RU2008100933/04A RU2008100933A RU2418800C2 RU 2418800 C2 RU2418800 C2 RU 2418800C2 RU 2008100933/04 A RU2008100933/04 A RU 2008100933/04A RU 2008100933 A RU2008100933 A RU 2008100933A RU 2418800 C2 RU2418800 C2 RU 2418800C2
Authority
RU
Russia
Prior art keywords
phenyl
pyridin
pyrrolo
carbonyl
difluoro
Prior art date
Application number
RU2008100933/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2008100933A (ru
Inventor
Прабха Н. ИБРАХИМ (US)
Прабха Н. Ибрахим
Дин Р. АРТИС (US)
Дин Р. Артис
Райан БРЕМЕР (US)
Райан Бремер
Шумейе МАМО (US)
Шумейе МАМО
Марика НЕСПИ (US)
Марика Неспи
Чао ЖАНГ (US)
Чао Жанг
Джиажонг ЖАНГ (US)
Джиажонг ЖАНГ
Йонг-Лианг ЖУ (US)
Йонг-Лианг Жу
Джеймс ЦАЙ (US)
Джеймс Цай
Клаус-Питер ХЕРТ (US)
Клаус-Питер ХЕРТ
Гидеон БОЛЛАГ (US)
Гидеон Боллаг
Уэйн СПЕВАК (US)
Уэйн СПЕВАК
Ханна ЧО (US)
Ханна Чо
Сэмьюэл Дж. ДЖИЛЛЕТ (US)
Сэмьюэл Дж. ДЖИЛЛЕТ
Гуоксиам ВУ (US)
Гуоксиам ВУ
Хонгьяо ЖУ (US)
Хонгьяо ЖУ
Шенгхуа ШИ (US)
Шенгхуа Ши
Original Assignee
Плекссикон, Инк.
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=37033831&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2418800(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Плекссикон, Инк. filed Critical Плекссикон, Инк.
Publication of RU2008100933A publication Critical patent/RU2008100933A/ru
Application granted granted Critical
Publication of RU2418800C2 publication Critical patent/RU2418800C2/ru

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P13/12—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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • A61P25/06—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C37/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring
    • C07C37/62—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom of a six-membered aromatic ring by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
    • C07C39/24—Halogenated derivatives
    • C07C39/26—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms
    • C07C39/27—Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms all halogen atoms being bound to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/56—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups
    • C07C47/565—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups all hydroxy groups bound to the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
RU2008100933/04A 2005-06-22 2006-06-21 Пирроло[2, 3-в]пиридиновые производные в качестве ингибиторов протеинкиназ RU2418800C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US69296005P 2005-06-22 2005-06-22
US60/692,960 2005-06-22
US73152805P 2005-10-28 2005-10-28
US60/731,528 2005-10-28

Related Child Applications (1)

Application Number Title Priority Date Filing Date
RU2011101140/04A Division RU2565071C2 (ru) 2005-06-22 2006-06-21 ПИРРОЛО[2,3-b]ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕИНКИНАЗ

Publications (2)

Publication Number Publication Date
RU2008100933A RU2008100933A (ru) 2009-07-27
RU2418800C2 true RU2418800C2 (ru) 2011-05-20

Family

ID=37033831

Family Applications (3)

Application Number Title Priority Date Filing Date
RU2011101140/04A RU2565071C2 (ru) 2005-06-22 2006-06-21 ПИРРОЛО[2,3-b]ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕИНКИНАЗ
RU2008100933/04A RU2418800C2 (ru) 2005-06-22 2006-06-21 Пирроло[2, 3-в]пиридиновые производные в качестве ингибиторов протеинкиназ
RU2012150759A RU2629999C2 (ru) 2005-06-22 2012-11-28 Пирроло[2,3-B]пиридиновые производные в качестве ингибиторов протеинкиназ

Family Applications Before (1)

Application Number Title Priority Date Filing Date
RU2011101140/04A RU2565071C2 (ru) 2005-06-22 2006-06-21 ПИРРОЛО[2,3-b]ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕИНКИНАЗ

Family Applications After (1)

Application Number Title Priority Date Filing Date
RU2012150759A RU2629999C2 (ru) 2005-06-22 2012-11-28 Пирроло[2,3-B]пиридиновые производные в качестве ингибиторов протеинкиназ

Country Status (35)

Country Link
US (10) US7863288B2 (US07863288-20110104-C00024.png)
EP (3) EP3088400A1 (US07863288-20110104-C00024.png)
JP (1) JP5007304B2 (US07863288-20110104-C00024.png)
KR (1) KR101125919B1 (US07863288-20110104-C00024.png)
CN (3) CN102603581B (US07863288-20110104-C00024.png)
AR (2) AR054624A1 (US07863288-20110104-C00024.png)
AT (1) ATE518860T1 (US07863288-20110104-C00024.png)
AU (1) AU2006261993B2 (US07863288-20110104-C00024.png)
BR (1) BRPI0611863B1 (US07863288-20110104-C00024.png)
CA (1) CA2613015C (US07863288-20110104-C00024.png)
CR (2) CR9677A (US07863288-20110104-C00024.png)
CY (2) CY1111996T1 (US07863288-20110104-C00024.png)
DE (1) DE122012000043I1 (US07863288-20110104-C00024.png)
DK (2) DK2395004T3 (US07863288-20110104-C00024.png)
EC (1) ECSP088121A (US07863288-20110104-C00024.png)
ES (2) ES2565992T3 (US07863288-20110104-C00024.png)
HK (2) HK1114610A1 (US07863288-20110104-C00024.png)
HU (2) HUE027370T2 (US07863288-20110104-C00024.png)
IL (1) IL188248A (US07863288-20110104-C00024.png)
LU (1) LU92035I2 (US07863288-20110104-C00024.png)
MA (1) MA29612B1 (US07863288-20110104-C00024.png)
MX (1) MX2007016463A (US07863288-20110104-C00024.png)
MY (2) MY153898A (US07863288-20110104-C00024.png)
NO (2) NO333913B1 (US07863288-20110104-C00024.png)
NZ (1) NZ565255A (US07863288-20110104-C00024.png)
PE (1) PE20070100A1 (US07863288-20110104-C00024.png)
PL (2) PL2395004T3 (US07863288-20110104-C00024.png)
PT (1) PT1893612E (US07863288-20110104-C00024.png)
RS (1) RS52010B (US07863288-20110104-C00024.png)
RU (3) RU2565071C2 (US07863288-20110104-C00024.png)
SI (2) SI2395004T1 (US07863288-20110104-C00024.png)
TW (3) TWI522337B (US07863288-20110104-C00024.png)
UA (1) UA95244C2 (US07863288-20110104-C00024.png)
WO (2) WO2007002325A1 (US07863288-20110104-C00024.png)
ZA (4) ZA200711152B (US07863288-20110104-C00024.png)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
EA037372B1 (ru) * 2011-08-01 2021-03-22 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
RU2782458C2 (ru) * 2016-12-23 2022-10-27 Эрвинэс Оперейшнс, Инк. Соединения и способы нацеленного расщепления полипептидов быстропрогрессирующей фибросаркомы
US11883393B2 (en) 2019-12-19 2024-01-30 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

Families Citing this family (407)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1696920T3 (pl) 2003-12-19 2015-03-31 Plexxikon Inc Związki i sposoby opracowywania modulatorów Ret
ATE508129T1 (de) 2004-03-30 2011-05-15 Vertex Pharma Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
JP4834553B2 (ja) 2004-09-17 2011-12-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 医薬組成物
BRPI0610066A2 (pt) 2005-05-17 2010-05-25 Plexxikon Inc compostos que modulam atividade de c-kit e c-fms e usos para estes
BRPI0611863B1 (pt) 2005-06-22 2021-11-23 Plexxikon, Inc Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
JP5071374B2 (ja) 2005-07-14 2012-11-14 アステラス製薬株式会社 ヘテロ環ヤヌスキナーゼ３阻害剤
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
EP1938842A4 (en) * 2005-09-01 2013-01-09 Eisai R&D Man Co Ltd METHOD FOR PRODUCING A PHARMACEUTICAL COMPOSITION COMPRISING IMPROVED CRASHING CHARACTERISTICS
PT3184526T (pt) 2005-12-13 2018-12-19 Incyte Holdings Corp Derivados de pirrolo[2,3-d]pirimidina como inibidores da cinase janus
BRPI0722364A2 (pt) 2006-01-17 2011-08-16 Vertex Pharma azaindóis, composição farmacêutica e usos dos referidos compostos
US20070208053A1 (en) * 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
BRPI0709866B8 (pt) 2006-04-03 2021-05-25 Astellas Pharma Inc compostos héteros e composição farmacêutica compreendendo ditos compostos
RU2448708C3 (ru) 2006-05-18 2017-09-28 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое средство против рака щитовидной железы
CN101448827A (zh) * 2006-05-22 2009-06-03 阿斯利康(瑞典)有限公司 吲哚衍生物
EA015700B1 (ru) * 2006-07-06 2011-10-31 Солвей Фармасьютикалс Б.В. Азаиндольные производные с сочетанием частичного агонизма к никотиновому ацетилхолиновому рецептору и ингибирования обратного захвата дофамина
US7964728B2 (en) * 2006-07-06 2011-06-21 Solvay Pharmaceuticals B.V. Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
PT2526933E (pt) 2006-09-22 2015-06-23 Pharmacyclics Inc Inibidores da tirosina-quinase de bruton
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) * 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
AU2007336811A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
EP2815750A1 (en) 2006-12-21 2014-12-24 Vertex Pharmaceuticals Incorporated 5-cyano-4-(pyrrolo [2,3b] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors
US20120101113A1 (en) 2007-03-28 2012-04-26 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
IL295053A (en) * 2007-03-28 2022-09-01 Pharmacyclics Llc Broton tyrosine kinase inhibitors
ES2529790T3 (es) 2007-04-13 2015-02-25 Dana-Farber Cancer Institute, Inc. Métodos de tratamiento de cáncer resistente a agentes terapéuticos de ERBB
GB0710528D0 (en) * 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
US20080312259A1 (en) 2007-06-13 2008-12-18 Incyte Corporation SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE
BRPI0814423B1 (pt) * 2007-07-17 2022-04-19 Plexxikon, Inc Compostos que modulam quinase e composição farmacêutica compreendendo os mesmos
MX2010001636A (es) * 2007-08-14 2010-03-15 Hoffmann La Roche Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos.
JP5558353B2 (ja) 2007-08-17 2014-07-23 ユニバーシティー オブ メリーランド，ボルティモア Ｌｃｋｓｈ２ドメイン結合の小分子阻害剤
CA2639416C (en) 2007-09-11 2019-12-31 F. Hoffmann-La Roche Ag Diagnostic test for susceptibility to b-raf kinase inhibitors
DE102007045919B4 (de) 2007-09-26 2018-07-05 Bayer Intellectual Property Gmbh Wirkstoffkombinationen mit insektiziden und akariziden Eigenschaften
DE102007045956A1 (de) 2007-09-26 2009-04-09 Bayer Cropscience Ag Wirkstoffkombination mit insektiziden und akariziden Eigenschaften
AU2008317406B2 (en) 2007-10-25 2013-07-18 Merck Sharp & Dohme Corp. Therapeutic compounds
EP2242755B1 (en) 2008-01-08 2012-09-12 Array Biopharma, Inc. Pyrrolopyridines as kinase inhibitors
US8426396B2 (en) * 2008-01-08 2013-04-23 Shriners Hospitals For Children Treatment for achondroplasia
CN101965347B (zh) 2008-01-09 2013-01-02 阵列生物制药公司 作为激酶抑制剂的吡唑并吡啶
AU2009206775A1 (en) * 2008-01-22 2009-07-30 Merck Patent Gmbh Protein kinase inhibitors and use thereof
CN101945877B (zh) * 2008-02-25 2013-07-03 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
CL2009000447A1 (es) 2008-02-29 2010-01-04 Array Biopharma Inc Y Genentech Inc Compuestos derivados de (1h-pirrolo{2,3-b}piridin-5-il)-sulfonamido-benzamida sustituida; procedimiento de preparacion; composicion farmaceutica; y su uso en el tratamiento del cancer, a travez de la inhibicion de raf.
WO2009111280A1 (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
AU2009222144A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. Pyrazole [3, 4-b] pyridine Raf inhibitors
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
US8158636B2 (en) 2008-05-19 2012-04-17 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
CN102036982A (zh) * 2008-05-21 2011-04-27 巴斯夫欧洲公司 作为杀真菌剂的取代吡啶-4-基甲基磺酰胺
JP2011521924A (ja) * 2008-05-28 2011-07-28 ビーエーエスエフ ソシエタス・ヨーロピア 殺菌剤としての置換ピリジン−４−イル−メチルスルホンアミド
JP5767965B2 (ja) * 2008-06-10 2015-08-26 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼを調節する５ｈ−ピロロ［２，３−ｂ］ピラジン誘導体、およびその適応症
WO2009152087A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor
AR072008A1 (es) * 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
US9447049B2 (en) 2010-03-01 2016-09-20 University Of Tennessee Research Foundation Compounds for treatment of cancer
WO2009157196A1 (ja) 2008-06-25 2009-12-30 武田薬品工業株式会社 アミド化合物
AU2009270856B2 (en) 2008-07-16 2013-07-25 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors
DE102008052943A1 (de) 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
US8592448B2 (en) 2008-11-20 2013-11-26 OSI Pharmaceuticals, LLC Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
AU2009324894B2 (en) * 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
US8318446B2 (en) * 2008-12-05 2012-11-27 California Institute Of Technology DNA-damage-induced proteolysis
US8017555B2 (en) * 2009-02-10 2011-09-13 Divergence, Inc. Compositions and methods for controlling nematodes
CN102421776A (zh) * 2009-03-11 2012-04-18 普莱希科公司 抑制Raf激酶的吡咯并[2，3-b]吡啶衍生物
EP2406260A1 (en) * 2009-03-11 2012-01-18 Plexxikon, Inc. Pyrrolo [2, 3-b]pyridine derivatives for the inhibition of raf kinases
WO2010111527A1 (en) * 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
AR078033A1 (es) * 2009-04-03 2011-10-12 Plexxikon Inc Una dispersion solida, que contiene al compuesto {3-[5-(4-(cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico, composiciones y formulaciones que comprenden a dicha dispersion solida; metodos para fabricar dicha dispersion solida, formas 1 y 2 de
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
ES2487542T3 (es) 2009-05-22 2014-08-21 Incyte Corporation Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus
CN106967070A (zh) 2009-05-22 2017-07-21 因塞特控股公司 作为jak抑制剂的化合物
US9034875B2 (en) 2009-05-26 2015-05-19 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
DK2435432T6 (da) 2009-05-26 2023-12-18 Abbvie Ireland Unlimited Co Apoptose-inducerende midler til behandling af cancer og immune og autoimmune sygdomme
US20220315555A1 (en) 2009-05-26 2022-10-06 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
US8546399B2 (en) 2009-05-26 2013-10-01 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
GEP20156325B (en) 2009-06-17 2015-07-10 Vertex Pharma Inhibitors of influenza viruses replication
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
MX2012002317A (es) 2009-08-24 2012-06-25 Ascepion Pharmaceuticals Inc Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa.
US20120157451A1 (en) 2009-08-28 2012-06-21 Genentech, Inc Raf inhibitor compounds and methods of use thereof
JP2013503189A (ja) 2009-08-28 2013-01-31 アレイ バイオファーマ、インコーポレイテッド Ｒａｆ阻害化合物およびその使用方法
JP2013503187A (ja) 2009-08-28 2013-01-31 アレイ バイオファーマ、インコーポレイテッド Ｒａｆ阻害化合物およびその使用方法
JP2013503193A (ja) 2009-08-28 2013-01-31 ジェネンテック， インコーポレイテッド Ｒａｆ阻害剤化合物およびその使用方法
WO2011025968A1 (en) 2009-08-28 2011-03-03 Array Biopharma Inc. 1h-pyrazolo [ 3, 4-b] pyridine compounds for inhibiting raf kinase
CN102712646A (zh) * 2009-08-28 2012-10-03 阵列生物制药公司 Raf抑制剂化合物及其使用方法
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
CA2778707A1 (en) 2009-10-23 2011-04-28 Mannkind Corporation Cancer immunotherapy and method of treatment
ES2633317T3 (es) 2009-11-06 2017-09-20 Plexxikon, Inc. Compuestos y métodos para la modulación de quinasas, e indicaciones para ello
WO2011060216A1 (en) 2009-11-12 2011-05-19 Concert Pharmaceuticals Inc. Substituted azaindoles
SG10201407718WA (en) 2009-11-18 2015-01-29 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
DE102009058280A1 (de) * 2009-12-14 2011-06-16 Merck Patent Gmbh Thiazolderivate
WO2011079133A2 (en) 2009-12-23 2011-06-30 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
JP2013516479A (ja) 2010-01-06 2013-05-13 ジョゼフ・ピー・エリコ 標的薬物を開発する方法および組成物
US8658170B2 (en) 2010-01-06 2014-02-25 Joseph P. Errico Combination therapy with MDM2 and EFGR inhibitors
US9163015B2 (en) * 2010-02-11 2015-10-20 Vanderbilt University Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US11084811B2 (en) 2010-03-01 2021-08-10 Oncternal Therapeutics, Inc. Compounds for treatment of cancer
TWI766281B (zh) 2010-03-10 2022-06-01 美商英塞特控股公司 作為jak1抑制劑之哌啶-4-基三亞甲亞胺衍生物
WO2011119842A1 (en) 2010-03-25 2011-09-29 The J. David Gladstone Institutes Compositions and methods for treating neurological disorders
DK2558446T5 (da) * 2010-04-16 2019-12-09 Ac Immune Sa Nye forbindelser til behandling af sygdomme associerede med amyloid- eller amyloidlignende proteiner
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
CN102917707A (zh) * 2010-05-06 2013-02-06 默沙东公司 可用作faah调节剂的氮杂吲哚衍生物
US20130072495A1 (en) 2010-05-14 2013-03-21 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
AR081039A1 (es) * 2010-05-14 2012-05-30 Osi Pharmaceuticals Llc Inhibidores biciclicos fusionados de quinasa
KR102132405B1 (ko) 2010-05-20 2020-07-09 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
EP2576566B1 (en) * 2010-05-28 2015-10-28 Merck Sharp & Dohme B.V. Thieno(2,3b)pyrazine compounds as b-raf inhibitors
EA201890869A3 (ru) 2010-06-03 2019-03-29 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk)
EP2580336B1 (en) 2010-06-09 2017-05-10 Bayer CropScience NV Methods and means to modify a plant genome at a nucleotide sequence commonly used in plant genome engineering
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
EP2598660B1 (en) 2010-07-26 2017-03-15 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures
EP2598661B1 (en) 2010-07-26 2017-09-27 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
US20120045433A1 (en) 2010-08-17 2012-02-23 Kapil Dhingra Combination therapy
US8709419B2 (en) 2010-08-17 2014-04-29 Hoffmann-La Roche, Inc. Combination therapy
US20120208837A1 (en) 2010-09-13 2012-08-16 Roger Tung Substituted azaindoles
UA113500C2 (xx) 2010-10-29 2017-02-10 Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб
CA2811805A1 (en) 2010-10-29 2012-05-03 Abbvie Inc. Solid dispersions containing an apoptosis-inducing agent
KR101236731B1 (ko) 2010-11-02 2013-02-25 한국과학기술원 아자인돌 화합물, 이를 포함하는 ｐｉ３ｋ 저해제용 약학 조성물 및 ｐｉ３ｋ와 연관된 질환 치료용 약학 조성물
AR083933A1 (es) 2010-11-19 2013-04-10 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
KR101923364B1 (ko) 2010-11-23 2018-11-30 애브비 인코포레이티드 아폽토시스­유도제의 염 및 결정형
DK2642999T3 (en) 2010-11-23 2017-01-09 Abbvie Ireland Unlimited Co METHODS OF TREATMENT FOR USING selectivity-VE BCL-2 INHIBITORS
US9296811B2 (en) 2010-12-02 2016-03-29 University of Pittsburgh—of the Commonwealth System of Higher Education Methods for treating a tumor using an antibody that specifically binds HMW-MAA
US9295669B2 (en) 2010-12-14 2016-03-29 Hoffman La-Roche Inc. Combination therapy for proliferative disorders
MX2013006836A (es) 2010-12-16 2013-09-26 Vertex Pharma Inhibidores de la replicacion de los virus de la influenza.
JP2014505052A (ja) 2011-01-06 2014-02-27 ベータ ファルマ カナダ インコーポレーテッド 癌の治療および予防用の新規なウレア
MA34948B1 (fr) * 2011-02-07 2014-03-01 Plexxikon Inc Composes et procedes de modulation de kinase, et leurs indications
EP2672963A4 (en) 2011-02-08 2015-06-24 Childrens Medical Center METHOD FOR THE TREATMENT OF MELANOMA
US9993480B2 (en) 2011-02-18 2018-06-12 Novartis Pharma Ag mTOR/JAK inhibitor combination therapy
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
US20140199292A1 (en) * 2011-03-15 2014-07-17 Inserm (Institut National De La Sante Et De La Recherche Medicale) Compositions and methods for inhibiting tumor development caused by chemotherapy induced senescence
CN103857395A (zh) 2011-04-01 2014-06-11 基因泰克公司 Akt抑制剂化合物和阿比特龙的组合及使用方法
WO2012138809A1 (en) * 2011-04-05 2012-10-11 Dawei Zhang Heterocyclic compounds as kinase inhibitors
CA2828946C (en) 2011-04-18 2016-06-21 Eisai R&D Management Co., Ltd. Therapeutic agent for tumor
AU2012253525B2 (en) * 2011-05-10 2016-09-22 Brunangelo Falini Hairy cell leukemia biomarkers and methods of using same
JP2014513724A (ja) 2011-05-16 2014-06-05 オーエスアイ・ファーマシューティカルズ，エルエルシー 融合二環キナーゼ阻害剤
RU2631487C2 (ru) 2011-05-17 2017-09-22 Плексксикон Инк. Модуляция киназ и показания к её применению
EP2714688B1 (en) 2011-05-26 2016-02-24 Daiichi Sankyo Company, Limited Heterocyclic compounds as protein kinase inhibitors
ES2841809T3 (es) 2011-06-03 2021-07-09 Eisai R&D Man Co Ltd Biomarcadores para pronosticar y evaluar el grado de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib
US8877742B2 (en) 2011-06-10 2014-11-04 Glaxosmithkline Intellectual Property Limited Compounds
EA201490042A1 (ru) 2011-06-20 2014-10-30 Инсайт Корпорейшн Азетидинил-фенил-, пиридил- или пиразинилкарбоксамидные производные как ингибиторы jak
WO2013010136A2 (en) 2011-07-13 2013-01-17 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
TW201840336A (zh) 2011-08-01 2018-11-16 美商建南德克公司 利用pd-1軸結合拮抗劑及mek抑制劑治療癌症之方法
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
WO2013029043A1 (en) * 2011-08-25 2013-02-28 Reaction Biology Corp. Selective kinase inhibitors
CN104053442B (zh) 2011-08-26 2017-06-23 润新生物公司 某些化学实体、组合物及方法
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
JP6093768B2 (ja) * 2011-09-14 2017-03-08 ニューファーマ， インコーポレイテッド 特定の化学的実体、組成物、および方法
EP2570127A1 (en) 2011-09-16 2013-03-20 Sanofi Compositions and methods for treating cancer using PI3KB beta inhibitor and MAPK pathway inhibitor, including MEK and RAF inhibitors
CN103930111A (zh) 2011-09-19 2014-07-16 霍夫曼-拉罗奇有限公司 包含c-met拮抗剂和b-raf拮抗剂的组合治疗
EP2771011A4 (en) * 2011-10-24 2015-04-15 Glaxosmithkline Ip No 2 Ltd CHEMICAL COMPOUNDS
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
SI2797888T1 (sl) 2011-12-31 2017-01-31 BeiGene, Ltd. Mourant Ozannes Corporate Services (Cayman) Limited Zlite triciklične spojine kot inhibitorji kinaze raf
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
CN102603734A (zh) * 2012-01-19 2012-07-25 盛世泰科生物医药技术(苏州)有限公司 一种蛋白激酶抑制剂及其应用
WO2013112950A2 (en) 2012-01-25 2013-08-01 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9216170B2 (en) 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9527852B2 (en) 2012-03-28 2016-12-27 Neuropore Therapies, Inc. Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
MY168958A (en) * 2012-04-23 2019-01-28 Genentech Inc Intermediates and processes for preparing compounds
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
EP2858501A4 (en) * 2012-05-22 2015-12-09 Merck Sharp & Dohme TRK-A KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
US10077474B2 (en) * 2012-05-29 2018-09-18 Abbott Molecular, Inc. Method of designing primers, method of detecting single nucleotide polymorphisms (SNPs), method of distinguishing SNPs, and related primers, detectable oligonucleotides, and kits
US9150570B2 (en) * 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
EP2855459B1 (en) 2012-05-31 2020-04-29 F.Hoffmann-La Roche Ag Aminoquinazoline and pyridopyrimidine derivatives
CA3015208C (en) 2012-06-04 2024-01-02 Pharmacyclics Llc Crystalline forms of a bruton's tyrosine kinase inhibitor
JP2015522037A (ja) 2012-07-03 2015-08-03 ラシオファルム ゲーエムベーハー ベムラフェニブコリン塩の固体形態
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
WO2014024077A1 (en) * 2012-08-07 2014-02-13 Aurigene Discovery Technologies Limited 5-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
BR112015003418A2 (pt) 2012-08-17 2017-07-04 Hoffmann La Roche produto farmacêutico, conjunto, métodos para estender a duração da resposta ao tratamento, de retardar ou prevenir o desenvolvimento de resistência ao tratamento, para a seleção de uma terapia e para otimizar a eficácia terapêutica.
CN103626765B (zh) * 2012-08-27 2016-08-10 广东东阳光药业有限公司 取代的氮杂吲哚化合物及其盐、组合物和用途
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
AU2013312477B2 (en) 2012-09-06 2018-05-31 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2014047648A1 (en) 2012-09-24 2014-03-27 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN103613591B (zh) * 2012-09-29 2016-04-13 上海科州药物研发有限公司 作为cMet抑制剂的化合物及其制备方法和用途
US9163021B2 (en) 2012-10-04 2015-10-20 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
EA028605B1 (ru) * 2012-10-08 2017-12-29 Атрива Терапьютикс Гмбх Комбинация озельтамивира и ингибитора mek для лечения вирусных заболеваний
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
BR112015011171A2 (pt) 2012-11-15 2017-07-11 Pharmacyclics Inc compostos de pirrolopirimidina como inibidores da quinase
SG11201503695XA (en) 2012-11-15 2015-06-29 Incyte Corp Sustained-release dosage forms of ruxolitinib
US9260426B2 (en) * 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
US9725703B2 (en) 2012-12-20 2017-08-08 Biomatrica, Inc. Formulations and methods for stabilizing PCR reagents
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
HUE036739T2 (hu) 2012-12-21 2018-07-30 Plexxikon Inc Vegyületek és eljárások kináz modulációra, és azok indikációi
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
NZ710079A (en) 2013-01-15 2020-01-31 Incyte Holdings Corp Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
WO2014130856A2 (en) * 2013-02-21 2014-08-28 Wayne Rothbaum Treatment of skeletal-related disorders
KR20150118159A (ko) 2013-02-22 2015-10-21 에프. 호프만-라 로슈 아게 암의 치료 방법 및 약물 내성의 예방 방법
CN109568312A (zh) * 2013-03-05 2019-04-05 田纳西大学研究基金会 用于治疗癌症的化合物
HUE057262T2 (hu) 2013-03-06 2022-04-28 Incyte Holdings Corp Eljárás és köztitermékek JAK inhibitor elõállítására
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
CA2900951A1 (en) 2013-03-14 2014-10-02 Ratiopharm Gmbh Solid state forms of vemurafenib hydrochloride
PL2970265T3 (pl) 2013-03-15 2018-11-30 Plexxikon Inc. Heterocykliczne związki i ich zastosowania
CA2904770A1 (en) 2013-03-15 2014-09-18 Sanofi Anti-tumoral composition comprising a pi3kbeta inhibitor and a raf inhibitor, to overcome cancer cells resistance
JP2016520528A (ja) 2013-03-15 2016-07-14 ジェネンテック， インコーポレイテッド 癌の治療及び抗癌剤耐性の防止方法
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
US9206188B2 (en) 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
AU2014266223B2 (en) 2013-05-14 2020-06-25 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
SG11201509338QA (en) 2013-05-30 2015-12-30 Plexxikon Inc Compounds for kinase modulation, and indications therefor
WO2015002729A2 (en) 2013-06-13 2015-01-08 Biomatrica, Inc. Cell stabilization
JP6380862B2 (ja) 2013-06-28 2018-08-29 ベイジーン リミテッド 複数種類のキナーゼの阻害剤としての縮合三環式アミド系化合物
TWI680760B (zh) * 2013-07-12 2020-01-01 印度商皮拉馬爾企業有限公司 治療黑色素瘤的藥物組合
US9421208B2 (en) 2013-08-02 2016-08-23 Pharmacyclics Llc Methods for the treatment of solid tumors
US9655854B2 (en) 2013-08-07 2017-05-23 Incyte Corporation Sustained release dosage forms for a JAK1 inhibitor
ES2709509T3 (es) 2013-08-12 2019-04-16 Pharmacyclics Llc Procedimientos para el tratamiento de cáncer amplificado por HER2
AR097431A1 (es) 2013-08-23 2016-03-16 Incyte Corp Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
EP3046557A1 (en) 2013-09-20 2016-07-27 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
CA2925124A1 (en) 2013-09-30 2015-04-02 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
EP3421468B1 (en) 2013-11-13 2020-11-04 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
RS59144B1 (sr) 2013-11-13 2019-09-30 Vertex Pharma Inhibitori replikacije virusa influence
US9856214B2 (en) * 2013-11-15 2018-01-02 The Wistar Institute Of Anatomy And Biology EBNA1 inhibitors and their method of use
WO2015075749A1 (en) * 2013-11-22 2015-05-28 Laurus Labs Private Limited Novel processes for the preparation of vemurafenib
CZ2013943A3 (cs) 2013-11-27 2015-06-03 Zentiva, K.S. Krystalické formy vemurafenibu
CN104710417B (zh) * 2013-12-11 2020-09-08 上海科州药物研发有限公司 氮杂吲哚类衍生物及其合成方法
CA3168002A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Cancer treatment using combinations of erk and raf inhibitors
CN104739823A (zh) * 2013-12-28 2015-07-01 复旦大学附属华山医院 淫羊藿素在制备维罗非尼增敏剂中的用途
EP3094736A4 (en) 2014-01-14 2017-10-25 Dana-Farber Cancer Institute, Inc. Compositions and methods for identification, assessment, prevention, and treatment of melanoma using pd-l1 isoforms
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2015143400A1 (en) 2014-03-20 2015-09-24 Pharmacyclics, Inc. Phospholipase c gamma 2 and resistance associated mutations
WO2015156674A2 (en) 2014-04-10 2015-10-15 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
CN106535900A (zh) * 2014-05-06 2017-03-22 加利福尼亚大学董事会 使用braf抑制剂的伤口愈合
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
WO2015181628A1 (en) * 2014-05-27 2015-12-03 Eisai R&D Management Co., Ltd. Treatment of acute myeloid leukemia with an hck inhibitor
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
WO2015191632A1 (en) 2014-06-10 2015-12-17 Biomatrica, Inc. Stabilization of thrombocytes at ambient temperatures
JP2017517558A (ja) * 2014-06-13 2017-06-29 ジェネンテック， インコーポレイテッド 癌薬剤耐性の治療方法及び防止方法
US20230190750A1 (en) 2014-06-13 2023-06-22 Genentech, Inc. Methods of treating and preventing cancer drug resistance
TW201613919A (en) 2014-07-02 2016-04-16 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
WO2016000615A1 (en) * 2014-07-02 2016-01-07 Sunshine Lake Pharma Co., Ltd. Heteroaryl compounds and pharmaceutical applications thereof
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
CN106573060A (zh) 2014-07-15 2017-04-19 豪夫迈·罗氏有限公司 使用pd‑1轴结合拮抗剂和mek抑制剂治疗癌症的组合物
AU2015296215A1 (en) 2014-08-01 2017-03-23 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
US9545407B2 (en) 2014-08-07 2017-01-17 Pharmacyclics Llc Formulations of a bruton's tyrosine kinase inhibitor
ES2926687T3 (es) 2014-08-28 2022-10-27 Eisai R&D Man Co Ltd Derivado de quinolina muy puro y método para su producción
AU2015318233B2 (en) 2014-09-15 2020-03-12 Plexxikon Inc. Heterocyclic compounds and uses thereof
ES2881195T3 (es) 2014-09-26 2021-11-29 Gilead Sciences Inc Derivados de aminotriazina útiles como compuestos inhibidores de quinasas que se unen a TANK
EP3204516B1 (en) 2014-10-06 2023-04-26 Dana-Farber Cancer Institute, Inc. Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response
WO2016073771A2 (en) * 2014-11-06 2016-05-12 Ohio State Innovation Foundation Pyrrolopyrimidine derivatives as mps1/ttk kinase inhibitors
WO2016083956A1 (en) * 2014-11-29 2016-06-02 Shilpa Medicare Limited Substantially pure vemurafenib and its salts
EP3256470B1 (en) * 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3236959A4 (en) 2014-12-23 2018-04-25 Dana Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
HUE064614T2 (hu) 2015-02-25 2024-04-28 Eisai R&D Man Co Ltd Eljárás egy kinolin-származék keserû ízének elnyomására
KR20170122220A (ko) 2015-03-03 2017-11-03 파마싸이클릭스 엘엘씨 브루톤 타이로신 키나제 저해제의 약제학적 제제
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
WO2016164641A1 (en) 2015-04-08 2016-10-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CZ2015250A3 (cs) 2015-04-14 2016-10-26 Zentiva, K.S. Amorfní formy vemurafenibu
ES2774178T3 (es) 2015-05-06 2020-07-17 Plexxikon Inc Síntesis de derivados de 1h-pirrolo[2,3-B] piridina que modulan cinasas
KR102630889B1 (ko) 2015-05-06 2024-01-30 다이이치 산쿄 인코포레이티드 키나제를 조절하는 화합물의 고형 형태
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP6771491B2 (ja) 2015-05-14 2020-10-21 ザ ウィスター インスティテュート オブ アナトミー アンド バイオロジー Ｅｂｎａ１阻害剤およびその使用方法
US9814714B2 (en) 2015-05-22 2017-11-14 Plexxikon Inc. Kinase modulation, and indications therefor
US9776998B2 (en) 2015-05-22 2017-10-03 Plexxikon Inc. Synthesis of heterocyclic compounds
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
LT3307734T (lt) * 2015-06-09 2020-05-11 Abbvie Inc. Branduolinio receptoriaus moduliatoriai (ror), skirti uždegiminių ir autoimuninių ligų gydymui
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
AU2016279474B2 (en) 2015-06-16 2021-09-09 Eisai R&D Management Co., Ltd. Anticancer agent
LT3322706T (lt) 2015-07-16 2021-03-10 Array Biopharma, Inc. Pakeistieji pirazolo[1,5-a]piridino junginiai, kaip ret kinazės inhibitoriai
CN107922396B (zh) * 2015-07-20 2022-08-05 建新公司 集落刺激因子-1受体(csf-1r)抑制剂
WO2017019664A1 (en) * 2015-07-28 2017-02-02 University Of Iowa Research Foundation Compositions and methods of treating cancer
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Ｐｉｍ激酶抑制劑之鹽
US9771363B2 (en) 2015-09-21 2017-09-26 Plexxikon Inc. Heterocyclic compounds and uses thereof
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
WO2017066193A1 (en) * 2015-10-15 2017-04-20 Princeton Drug Discovery, Llc Novel inhibitors of protein kinases
BR112018008357A2 (pt) 2015-10-26 2018-11-27 Array Biopharma Inc mutações de ponto em câncer resistente a inibidor de trk e métodos relacionados às mesmas
KR20180081591A (ko) 2015-11-19 2018-07-16 제넨테크, 인크. B-raf 억제제 및 면역 체크포인트 억제제를 사용하여 암을 치료하는 방법
SG11201804711RA (en) 2015-12-07 2018-07-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CN113588501A (zh) 2015-12-08 2021-11-02 生物马特里卡公司 降低红细胞沉降速率
US10116776B2 (en) 2015-12-14 2018-10-30 Red.Com, Llc Modular digital camera and cellular phone
US10316049B2 (en) 2015-12-17 2019-06-11 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
WO2017147316A1 (en) * 2016-02-25 2017-08-31 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
WO2017161045A1 (en) 2016-03-16 2017-09-21 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
AU2017246554B2 (en) 2016-04-04 2022-08-18 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-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
WO2017176744A1 (en) 2016-04-04 2017-10-12 Loxo Oncology, Inc. Methods of treating pediatric cancers
AU2017249229A1 (en) 2016-04-15 2018-10-04 Genentech, Inc. Diagnostic and therapeutic methods for cancer
HRP20230704T1 (hr) 2016-05-18 2023-10-27 Loxo Oncology, Inc. Priprava (s)-n-(5-((r)-2-(2,5-difluorfenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
WO2017218544A1 (en) * 2016-06-13 2017-12-21 Chemocentryx, Inc. Methods of treating pancreatic cancer
US11179484B2 (en) 2016-06-24 2021-11-23 University Of Iowa Research Foundation Compositions and methods of treating melanoma
RS60451B1 (sr) 2016-07-01 2020-07-31 Fermion Oy Novi postupci za dobijanje vemurafeniba
EP3484856B1 (en) 2016-07-12 2023-11-15 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
CN109715631B (zh) * 2016-09-16 2022-02-18 德国亥姆霍兹慕尼黑中心健康与环境研究中心（有限公司） Traf 6抑制剂
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
EP3308773A1 (en) 2016-10-11 2018-04-18 Recordati Industria Chimica E Farmaceutica SPA Formulations of cysteamine and cysteamine derivatives
EP3528798A4 (en) 2016-10-19 2020-10-21 United States Government as Represented by The Department of Veterans Affairs COMPOSITIONS AND METHODS OF TREATMENT OF CANCER
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
IL266751B (en) 2016-11-23 2022-07-01 Chemocentryx Inc A method for the treatment of focal segmental tuberous sclerosis
EP3554258B1 (en) 2016-12-15 2023-07-19 Société des Produits Nestlé S.A. Compositions and methods that modulate phosphorus or enzymes in a companion animal
EP3558991A2 (en) 2016-12-23 2019-10-30 Plexxikon Inc. Compounds and methods for cdk8 modulation and indications therefor
US11040027B2 (en) 2017-01-17 2021-06-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
CA3049136C (en) 2017-01-18 2022-06-14 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
EP3571199A1 (en) 2017-01-23 2019-11-27 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
JP7341060B2 (ja) 2017-02-10 2023-09-08 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Ｍａｐｋ経路の活性化に関連付けられる癌の処置のための方法及び医薬組成物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
AU2018237047A1 (en) 2017-03-20 2019-10-17 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
WO2018175324A1 (en) 2017-03-20 2018-09-27 The Broad Institute, Inc. Compounds and methods for regulating insulin secretion
WO2018183762A1 (en) * 2017-03-29 2018-10-04 United States Government As Represented By The Department Of Veterans Affairs Methods and compositions for treating cancer
CA3058183A1 (en) 2017-03-30 2018-10-04 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
CA3060147A1 (en) * 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
WO2018210661A1 (en) * 2017-05-15 2018-11-22 Basf Se Heteroaryl compounds as agrochemical fungicides
US11161845B2 (en) * 2017-05-19 2021-11-02 Nflection Therapeutics, Inc. Pyrrolopyridine-aniline compounds for treatment of dermal disorders
MA49140A (fr) 2017-05-19 2020-03-25 Nflection Therapeutics Inc Composés hétéroaromatiques-aniline fusionnés pour le traitement de troubles dermiques
US10428067B2 (en) 2017-06-07 2019-10-01 Plexxikon Inc. Compounds and methods for kinase modulation
JP7221227B2 (ja) 2017-06-30 2023-02-13 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 発毛を調節するための組成物及び方法
EP3658189A1 (en) 2017-07-25 2020-06-03 Plexxikon Inc. Formulations of a compound modulating kinases
CN109384785B (zh) * 2017-08-10 2021-09-28 浙江海正药业股份有限公司 吡咯并吡啶酮类衍生物、其制备方法及其在医药上的用途
AU2018329925A1 (en) 2017-09-08 2020-03-05 F. Hoffmann-La Roche Ag Diagnostic and therapeutic methods for cancer
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
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
JP2020536919A (ja) 2017-10-11 2020-12-17 ケモセントリックス， インコーポレイテッド Ｃｃｒ２アンタゴニストによる巣状分節性糸球体硬化症の治療
AU2018347516A1 (en) 2017-10-12 2020-05-07 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
US10717735B2 (en) 2017-10-13 2020-07-21 Plexxikon Inc. Solid forms of a compound for modulating kinases
IL274027B2 (en) 2017-10-26 2023-12-01 Xynomic Pharmaceuticals Inc B–RAF kinase inhibitor salt crystals
BR112020007972A2 (pt) 2017-10-27 2020-10-20 Plexxikon, Inc. formulações de composto que modula quinases
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
MX2020006273A (es) 2017-12-15 2020-09-14 Revolution Medicines Inc Compuestos policiclicos como inhibidores alostericos de shp2.
WO2019133810A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
US11524963B2 (en) 2018-01-18 2022-12-13 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
JP7060694B2 (ja) 2018-01-18 2022-04-26 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物
JP6997876B2 (ja) 2018-01-18 2022-02-04 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物
CN112105608B (zh) 2018-01-30 2023-07-14 因赛特公司 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法
CN111788195B (zh) 2018-01-31 2023-11-21 海帕瑞吉尼克斯股份有限公司 用于促进肝脏再生或减少或预防肝细胞死亡的蛋白激酶mkk4抑制剂
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
JP2021518367A (ja) 2018-03-20 2021-08-02 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． Ｉｄｏおよびｔｄｏ調節のための化合物および方法、ならびにそれらのための兆候
AU2019245420A1 (en) 2018-03-30 2020-11-12 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
WO2019195682A1 (en) * 2018-04-05 2019-10-10 Beth Israel Deaconess Medical Center, Inc. Aryl hydrocarbon receptor modulators and uses thereof
EP3560516A1 (en) * 2018-04-27 2019-10-30 Bergen Teknologioverforing AS Combination therapy including beta-sitosterol in combination with at least one of a braf inhibitor, a mek inhibitor or an erk inhibitor and methods and use thereof
EP3793546A4 (en) 2018-05-17 2021-12-08 The Wistar Institute CRYSTALLINE FORMS OF EBNA1-INHIBITOR AND METHOD OF MANUFACTURING AND USING THEREOF
GB201808321D0 (en) * 2018-05-21 2018-07-11 Univ College Dublin Nat Univ Ireland Dublin Compositions and uses thereof
US11731968B2 (en) 2018-06-21 2023-08-22 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
GB2612522B (en) * 2018-07-06 2023-08-02 The Regents Of The Univ Of Colorado A Body Corporate Existing Under The Laws Of The State Of Colorad Genetically encoded system for constructing and detecting biologically active agents
CA3104246A1 (en) 2018-07-16 2020-01-23 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
US20210253571A1 (en) * 2018-07-19 2021-08-19 Medshine Discovery Inc. Azaindole derivative and use thereof as fgfr and c-met inhibitor
AU2019314302A1 (en) 2018-07-31 2021-01-28 Loxo Oncology, Inc. Spray-dried dispersions and formulations of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1H-pyrazole-4-carboxamide
US11964988B2 (en) 2018-09-10 2024-04-23 Array Biopharma Inc. Fused heterocyclic compounds as RET kinase inhibitors
US20210244716A1 (en) 2018-10-03 2021-08-12 Jyväskylän Yliopisto Vemurafenib and salts thereof for use in the treatment of enteroviral infections
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN112867803A (zh) 2018-10-16 2021-05-28 诺华股份有限公司 单独的或与免疫标志物组合的肿瘤突变负荷作为生物标志物用于预测对靶向疗法的应答
SG11202104404XA (en) * 2018-11-16 2021-05-28 California Inst Of Techn Erk inhibitors and uses thereof
WO2020106306A1 (en) 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
JP2022510368A (ja) * 2018-12-03 2022-01-26 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング タンキラーゼのインヒビターとしての４－ヘテロアリールカルボニル－ｎ－（フェニルまたはヘテロアリール）ピペリジン－１－カルボキサミド
US20220041579A1 (en) 2018-12-19 2022-02-10 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of fgfr tyrosine kinases
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
MX2021009426A (es) * 2019-02-11 2021-09-10 Merck Patent Gmbh Derivados de indazolil-isoxazol para el tratamiento de enfermedades tales como cancer.
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
KR20220018475A (ko) 2019-04-09 2022-02-15 플렉시콘 인코퍼레이티드 Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US20220227760A1 (en) * 2019-05-29 2022-07-21 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
EP3976607A4 (en) * 2019-05-31 2023-07-19 Fochon Biosciences, Ltd. SUBSTITUTED PYRROLO[2,3-B]PYRIDINE AND PYRAZOLO[3,4-B]PYRIDINE DERIVATIVES AS PROTEIN KINAS INHIBITORS
WO2021018820A1 (en) 2019-07-29 2021-02-04 Heparegenix Gmbh Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
AR119765A1 (es) 2019-08-14 2022-01-12 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2
US20220347182A1 (en) * 2019-10-02 2022-11-03 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for the treatment of osteoarthritis
MX2022004390A (es) 2019-10-11 2022-08-08 Incyte Corp Aminas biciclicas como inhibidores de la cinasa dependiente de ciclina 2 (cdk2).
CN111004210A (zh) * 2019-10-23 2020-04-14 中山大学 化合物单晶及其制备方法
AU2020413333A1 (en) 2019-12-27 2022-06-16 Schrödinger, Inc. Cyclic compounds and methods of using same
EP4087657A1 (en) 2020-01-08 2022-11-16 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof
EP4090659B1 (en) 2020-01-15 2024-06-12 HepaRegeniX GmbH 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases
JP2023510220A (ja) * 2020-01-17 2023-03-13 テグ－キョンプク メディカル イノベーション ファウンデーション 新規化合物、その調製方法、及びその使用
AU2021213317A1 (en) 2020-01-28 2022-06-30 Centre National De La Recherche Scientifique Antisense oligonucleotide targeting LINC00518 for treating melanoma
EP4135700A4 (en) * 2020-04-15 2024-04-17 Pyramid Biosciences, Inc. METHOD FOR THE PRODUCTION OF TYROSINE RECEPTOR KINASE INHIBITORS
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
KR20210135092A (ko) * 2020-05-04 2021-11-12 아주대학교산학협력단 톨-유사 수용체 7/9 억제 기능이 있는 길항성 소분자 화합물
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11529335B2 (en) 2020-07-31 2022-12-20 University Of Iowa Research Foundation Compositions and methods for treating cancer
AU2021327375A1 (en) 2020-08-21 2023-03-16 Opna Bio SA Combinational drug anticancer therapies
US20230365584A1 (en) 2020-09-10 2023-11-16 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
WO2022063101A1 (zh) * 2020-09-23 2022-03-31 劲方医药科技(上海)有限公司 芳甲酰取代的三环化合物及其制法和用途
CN114478528A (zh) * 2020-10-28 2022-05-13 劲方医药科技(上海)有限公司 芳甲酰取代的三环化合物及其制法和用途
KR20230110286A (ko) * 2020-11-17 2023-07-21 포천 바이오사이언시스, 리미티드 단백질 키나제 억제제로서 치환된 피롤로 [2,3-b] 피리딘 및 피라졸로 [3,4-b] 피리딘 유도체
EP4234558A1 (en) * 2020-12-07 2023-08-30 Zhejiang Longcharm Bio-Tech Pharma. Co., Ltd. Pyrrolopyridine compound and application thereof
EP4255420A1 (en) * 2020-12-07 2023-10-11 Lieber Institute, Inc. Compounds for inhibiting inositol hexakisphosphate kinase (ip6k) and methods of use thereof
EP4267573A1 (en) 2020-12-23 2023-11-01 Genzyme Corporation Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
CN112574200B (zh) * 2021-02-26 2021-06-11 安润医药科技（苏州）有限公司 Btk和/或btk的突变体c481s的小分子抑制剂
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
JP2024511373A (ja) 2021-03-18 2024-03-13 ノバルティス アーゲー がんのためのバイオマーカーおよびその使用
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
TW202304890A (zh) * 2021-04-14 2023-02-01 美商百歐克斯製藥公司 Klk5雙環雜芳香族抑制劑
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023059786A1 (en) * 2021-10-06 2023-04-13 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of ulk1 and methods of use
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN116768896A (zh) * 2022-03-15 2023-09-19 劲方医药科技(上海)有限公司 Btk抑制剂的晶型及其酸式盐和其酸式盐的晶型
WO2023178240A2 (en) * 2022-03-16 2023-09-21 The Children's Medical Center Corporation Pyk2 inhibition modulates immune cell function
WO2024003350A1 (en) 2022-06-30 2024-01-04 Universite De Strasbourg Combination therapy for melanoma
CN115141197B (zh) * 2022-07-27 2024-03-26 安徽医科大学 一种3-芳杂环取代苯基衍生物及其制备方法与用途
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
WO2024111671A1 (ja) * 2022-11-25 2024-05-30 ゼノリス プライベート リミテッド 核酸アプタマー

Family Cites Families (166)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3124610A (en) * 1964-03-10 Preparation of intermediates
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
US3067237A (en) * 1959-04-14 1962-12-04 Sterling Drug Inc Lower-alkyl mono-or bis-(alkanesulfonamido) benzoate esters
GB1141949A (en) 1966-02-23 1969-02-05 Sterling Drug Inc 7-azaindole derivatives
BR6794063D0 (pt) * 1966-10-21 1973-09-18 Minnesota Mining & Mfg Processo para preparar perfluoral-quilsulfonamidas n-substituidas e composicoes herbicidas e fitoreguladoras nelas baseadas
IL46853A0 (en) * 1974-03-20 1975-05-22 Bayer Ag Novel alkoxycarbonylphenylureas,their preparation and their use as herbicides
DE2413258A1 (de) * 1974-03-20 1975-10-02 Bayer Ag Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide
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
EP0142152B1 (en) * 1983-11-14 1991-03-20 The Dow Chemical Company Novel substituted 1,2,4-triazolo- [1,5-a] pyrimidine-2-sulfonamides and compositions and methods of controlling undesired vegetation and suppressing the nitrification of ammonium nitrogen in soil
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
US4714693A (en) 1986-04-03 1987-12-22 Uop Inc. Method of making a catalyst composition comprising uniform size metal components on carrier
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
JP3082204B2 (ja) * 1988-09-01 2000-08-28 ホワイトヘッド・インスティチュート・フォー・バイオメディカル・リサーチ 両栄養性および環境栄養性宿主域を持つ組換え体レトロウイルス
US5703055A (en) * 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
US5744101A (en) * 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
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
US5527681A (en) * 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5800992A (en) * 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
US5360822A (en) * 1990-02-07 1994-11-01 Nippon Shinyaku Co. Ltd. Sulfonanilide derivatives and medicine
AU7906691A (en) * 1990-05-23 1991-12-10 United States of America, as represented by the Secretary, U.S. Department of Commerce, The Adeno-associated virus (aav)-based eucaryotic vectors
DE4022414A1 (de) 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
US5124335A (en) 1991-01-30 1992-06-23 Merck & Co., Inc. Substituted pyrollo-fused 6 membered heterocycles as angiotensin ii antagonists
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
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
US5576319A (en) * 1993-03-01 1996-11-19 Merck, Sharp & Dohme Ltd. Pyrrolo-pyridine derivatives
BR9406128A (pt) * 1993-03-01 1996-02-27 Merck Sharp & Dohme Uso de um composto processo para o tratamento e/ou prevençao de distúrbios psicóticos composto composiçao farmacêutica processos para a preparaçao de um composto e de uma composiçao farmacêutica
ES2134929T3 (es) * 1993-03-01 1999-10-16 Merck Sharp & Dohme Derivados de pirrolo-piridina como ligandos para receptores de dopamina.
US5549614A (en) * 1993-03-18 1996-08-27 Tunis; Scott W. Apparatus for folding flexible intraocular lenses
ES2204921T3 (es) * 1993-05-27 2004-05-01 Selectide Corporation Bibliotecas de fase solida codificadas, segregadas topologicamente.
US5840485A (en) * 1993-05-27 1998-11-24 Selectide Corporation Topologically segregated, encoded solid phase libraries
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
JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
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
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
US5763198A (en) * 1994-07-22 1998-06-09 Sugen, Inc. Screening assays for compounds
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9416162D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
DE4430212A1 (de) * 1994-08-28 1996-02-29 Merck Patent Gmbh Ortho-substituierte Benzoesäure-Derivate
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
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
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
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
WO1997016533A1 (en) * 1995-10-31 1997-05-09 The Regents Of The University Of California 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
PT948495E (pt) * 1996-11-19 2004-08-31 Amgen Inc Agentes anti-inflamatorios de pirrolo fundido substituidos em arilo e heteroarilo
US6294330B1 (en) * 1997-01-31 2001-09-25 Odyssey Pharmaceuticals Inc. Protein fragment complementation assays for the detection of biological or drug interactions
US6243980B1 (en) * 1997-03-07 2001-06-12 Tropix, Inc. Protease inhibitor assay
US5977131A (en) 1997-04-09 1999-11-02 Pfizer Inc. Azaindole-ethylamine derivatives as nicotinic acetylcholine receptor binding agents
US6096718A (en) * 1997-06-05 2000-08-01 Gene Targeting Corp. Tissue specific adenovirus vectors for breast cancer treatment
KR20010014183A (ko) 1997-06-27 2001-02-26 Fujisawa Pharmaceutical Co 술폰아미드 화합물 및 그의 의약 용도
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
US6161776A (en) * 1997-08-12 2000-12-19 Nibco Inc. Multi-layered, porous mat turf irrigation apparatus and method
IL134702A (en) * 1997-09-11 2004-03-28 Bioventures Inc High density arrays and methods of making the same
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
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
US6288234B1 (en) * 1998-06-08 2001-09-11 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
US6113913A (en) * 1998-06-26 2000-09-05 Genvec, Inc. Recombinant adenovirus
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
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
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
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
ES2219319T3 (es) * 1999-03-17 2004-12-01 Astrazeneca Ab Derivados de amida.
GB9906566D0 (en) 1999-03-23 1999-05-19 Zeneca Ltd Chemical compounds
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
TWI234557B (en) * 1999-05-26 2005-06-21 Telik Inc Novel naphthalene ureas as glucose uptake enhancers
US6653151B2 (en) * 1999-07-30 2003-11-25 Large Scale Proteomics Corporation Dry deposition of materials for microarrays using matrix displacement
US20010008765A1 (en) * 1999-12-06 2001-07-19 Fuji Photo Film Co., Ltd. DNA chip and reactive solid carrier
JP5004392B2 (ja) * 1999-12-22 2012-08-22 スージェン， インク． インドリノン化合物を用いてｃ−ｋｉｔチロシン蛋白質キナーゼ機能を調節する方法
NZ519380A (en) 1999-12-28 2004-10-29 Eisai Co Ltd Heterocyclic compounds having sulfonamide groups
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
JP4255285B2 (ja) 2001-02-21 2009-04-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 インテグリン発現抑制を介した血管新生抑制剤の効果を検定する方法
CN101310771B (zh) 2001-04-11 2012-08-08 千寿制药株式会社 视觉功能障碍改善剂
WO2002085896A1 (en) 2001-04-24 2002-10-31 Wyeth Antidepressant azaheterocyclylmethyl 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
WO2002102783A1 (en) 2001-06-19 2002-12-27 Merck & Co., Inc. 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
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
WO2003028724A1 (en) 2001-10-04 2003-04-10 Smithkline Beecham Corporation Chk1 kinase inhibitors
JPWO2003037862A1 (ja) 2001-10-30 2005-02-17 日本新薬株式会社 アミド誘導体及び医薬
US20030236277A1 (en) 2002-02-14 2003-12-25 Kadow John F. Indole, azaindole and related heterocyclic pyrrolidine derivatives
US6884889B2 (en) 2002-03-25 2005-04-26 Bristol-Myers Squibb Co. Processes for the preparation of antiviral 7-azaindole derivatives
JP2005534619A (ja) 2002-03-28 2005-11-17 エーザイ株式会社 Ｃ−ｊｕｎｎ−末端キナーゼ阻害剤としてのアザインドール
IL164187A0 (en) 2002-03-28 2005-12-18 Eisai Co Ltd 7-Azaindole derivatives and pharmaceutical compositions containing the same
GB0212785D0 (en) * 2002-05-31 2002-07-10 Glaxo Group Ltd Compounds
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
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
US6878887B2 (en) * 2002-08-07 2005-04-12 Matsushita Electric Industrial Co., Ltd. Anti-malfunction mechanism for variable output device
SE0202463D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
EP2277551B1 (en) 2002-09-06 2013-05-08 Cerulean Pharma Inc. Cyclodextrin-based polymers for delivering the therapeutic agents covalently bound thereto
US20040142864A1 (en) 2002-09-16 2004-07-22 Plexxikon, Inc. Crystal structure of PIM-1 kinase
DE60323133D1 (de) * 2002-12-13 2008-10-02 Smithkline Beecham Corp Cyclohexylverbindungen als ccr5-antagonisten
JP2006511554A (ja) * 2002-12-13 2006-04-06 スミスクライン ビーチャム コーポレーション Ｃｃｒ５アンタゴニストとしてのピペリジン誘導体
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
CA2515571A1 (en) * 2003-02-14 2004-09-02 Wyeth Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
US20050170431A1 (en) * 2003-02-28 2005-08-04 Plexxikon, Inc. PYK2 crystal structure and uses
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
PL1696920T3 (pl) 2003-12-19 2015-03-31 Plexxikon Inc Związki i sposoby opracowywania modulatorów Ret
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
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
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
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
ATE508129T1 (de) 2004-03-30 2011-05-15 Vertex Pharma Als inhibitoren von jak und anderen proteinkinasen geeignete azaindole
US7498342B2 (en) * 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
CA2570817A1 (en) * 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
EP1765819B1 (en) 2004-06-30 2014-03-12 Vertex Pharmaceuticals Inc. Azaindoles useful as inhibitors of protein kinases
AU2005269387A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP2264033A1 (en) * 2004-07-27 2010-12-22 SGX Pharmaceuticals, Inc. 3,5-DIPHENYL-SUBSTITUTED PYRROLO[2,3b]PYRIDINES USEFUL AS KINASE INHIBITORS
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
GB0419192D0 (en) * 2004-08-27 2004-09-29 Merck Sharp & Dohme Therapeutic agents
US8859581B2 (en) 2005-04-25 2014-10-14 Merck Patent Gmbh Azaheterocyclic compounds as kinase inhibitors
BRPI0610066A2 (pt) * 2005-05-17 2010-05-25 Plexxikon Inc compostos que modulam atividade de c-kit e c-fms e usos para estes
CN101228161B (zh) 2005-05-20 2012-10-10 沃泰克斯药物股份有限公司 适用作蛋白激酶抑制剂的吡咯并吡啶类
BRPI0611863B1 (pt) * 2005-06-22 2021-11-23 Plexxikon, Inc Composto, bem como composição e kit compreendendo o mesmo, composto intermediário na preparação do mesmo, método para tratamento e uso do mesmo
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
US20070218138A1 (en) * 2006-03-20 2007-09-20 Bittorf Kevin J Pharmaceutical Compositions
WO2008063888A2 (en) * 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) * 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
TW200908968A (en) * 2007-05-29 2009-03-01 Sgx Pharmaceuticals Inc Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BARTON et al. The chemistry of pentavalent organobismuth reagents. Part X. Stadies on the phenylation and oxidation of phenols. TETRAHEDRON. Vol.43, n. 2, 1987, p.323-332. *
LANGHAM et al. Metalationof Halogen-Metal Interconversion Reaction of Some Halogenated Phenyl Ethers. J. Am. Chem. Soc. vol.63, 1941, p.545-549. HEACOCK et al. Orientation and Relative Reaction rate Factors in aromatic Substitution by the Benzensulfonimido Radical. J. Am. Chem. Soc. Vol.82, 1960,p.3460-3463. *
PIERCE et al. Local anaesthetics.l.beta-Monoalkylaminoethyl Esters of Alkoxybenzoic Acid. J. Am. Chem. Soc. Vol.64, 1942, p.1691-1694. CUTTIN et al. Discovery and evalution of a series of 3-Acylindole Imidazopyridine Platelet-Activating Factor Antagonists. J. Med. Chem. Vol.41, 1998, p.74-95. *

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA037372B1 (ru) * 2011-08-01 2021-03-22 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
RU2782458C2 (ru) * 2016-12-23 2022-10-27 Эрвинэс Оперейшнс, Инк. Соединения и способы нацеленного расщепления полипептидов быстропрогрессирующей фибросаркомы
US11986531B2 (en) 2016-12-23 2024-05-21 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
RU2795146C2 (ru) * 2017-01-31 2023-04-28 Эрвинэс Оперейшнс, Инк. Лиганды цереблона и бифункциональные соединения, содержащие их
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
US11883393B2 (en) 2019-12-19 2024-01-30 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

Also Published As

Publication number Publication date
CN102206216B (zh) 2014-11-12
US20120053177A1 (en) 2012-03-01
CN102603581B (zh) 2015-06-24
TW201514140A (zh) 2015-04-16
RS52010B (en) 2012-04-30
IL188248A0 (en) 2008-04-13
TWI473808B (zh) 2015-02-21
IL188248A (en) 2012-04-30
NO2014006I1 (no) 2014-06-02
AR078519A2 (es) 2011-11-16
CY1111996T1 (el) 2015-08-05
PE20070100A1 (es) 2007-03-10
US20120022098A1 (en) 2012-01-26
PT1893612E (pt) 2011-11-21
US20180111929A1 (en) 2018-04-26
HUS1200009I1 (hu) 2018-09-28
PL1893612T3 (pl) 2012-01-31
JP5007304B2 (ja) 2012-08-22
MY153898A (en) 2015-04-15
TWI432193B (zh) 2014-04-01
HK1164866A1 (zh) 2012-09-28
LU92035I2 (fr) 2012-08-28
CA2613015A1 (en) 2007-01-04
AR054624A1 (es) 2007-07-04
UA95244C2 (ru) 2011-07-25
ES2565992T3 (es) 2016-04-08
PL2395004T3 (pl) 2016-08-31
US20130261117A1 (en) 2013-10-03
RU2011101140A (ru) 2012-07-20
AU2006261993A1 (en) 2007-01-04
CR9677A (es) 2008-03-26
MA29612B1 (fr) 2008-07-01
NZ565255A (en) 2010-04-30
EP2395004A3 (en) 2012-04-04
AU2006261993B2 (en) 2011-11-17
CN102206216A (zh) 2011-10-05
EP2395004A2 (en) 2011-12-14
RU2629999C2 (ru) 2017-09-05
US20110059963A1 (en) 2011-03-10
JP2008546797A (ja) 2008-12-25
US8415469B2 (en) 2013-04-09
SI2395004T1 (sl) 2016-05-31
CN102603581A (zh) 2012-07-25
CA2613015C (en) 2012-04-03
EP1893612A1 (en) 2008-03-05
SI1893612T1 (sl) 2012-03-30
US20150290205A1 (en) 2015-10-15
ZA201202024B (en) 2016-02-24
RU2565071C2 (ru) 2015-10-20
CN101243084B (zh) 2012-03-07
CN101243084A (zh) 2008-08-13
MX2007016463A (es) 2008-03-04
ATE518860T1 (de) 2011-08-15
TW200804370A (en) 2008-01-16
KR101125919B1 (ko) 2012-06-12
TWI522337B (zh) 2016-02-21
ZA201202026B (en) 2012-11-28
WO2007002325A1 (en) 2007-01-04
DK1893612T3 (da) 2011-11-21
CY2012021I2 (el) 2015-08-05
US8470818B2 (en) 2013-06-25
RU2008100933A (ru) 2009-07-27
ZA201202025B (en) 2022-03-30
CR20130216A (es) 2013-07-02
BRPI0611863A2 (pt) 2008-12-02
MY147410A (en) 2012-11-30
NO333913B1 (no) 2013-10-21
CY2012021I1 (el) 2015-08-05
WO2007002433A1 (en) 2007-01-04
HK1114610A1 (en) 2008-11-07
KR20080030619A (ko) 2008-04-04
US20160176865A1 (en) 2016-06-23
US20130303534A1 (en) 2013-11-14
TW201345906A (zh) 2013-11-16
RU2012150759A (ru) 2014-06-10
ES2371397T3 (es) 2011-12-30
US20100256365A1 (en) 2010-10-07
EP3088400A1 (en) 2016-11-02
ZA200711152B (en) 2012-06-27
EP2395004B1 (en) 2016-01-20
LU92035I9 (US07863288-20110104-C00024.png) 2019-01-04
US20100249118A1 (en) 2010-09-30
EP1893612B1 (en) 2011-08-03
NO2014006I2 (no) 2014-03-20
US8143271B2 (en) 2012-03-27
US7863288B2 (en) 2011-01-04
DE122012000043I1 (de) 2012-09-13
DK2395004T3 (en) 2016-03-21
ECSP088121A (es) 2008-02-20
HUE027370T2 (en) 2016-10-28
BRPI0611863B1 (pt) 2021-11-23
NO20076659L (no) 2008-03-18

Similar Documents

Publication Publication Date Title
RU2418800C2 (ru) Пирроло[2, 3-в]пиридиновые производные в качестве ингибиторов протеинкиназ
EP1773310B1 (en) Alpha, beta-unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides and therapeutic uses thereof
RU2435757C2 (ru) Производные 3-циклил-2-(4-сульфамоилфенил)-n-циклилпропионамида, применимые для лечения нарушенной переносимости глюкозы и диабета
ES2581848T3 (es) Derivados de pirrolo[2,3-d]pirimidina como inhibidores de quinasas relacionadas con tropomiosina
RU2368608C2 (ru) Производные пиперидина в качестве модуляторов хемокинового рецептора ccr5
CN103435524B (zh) 作为有生理学价值的硝酰氧基供体的n-羟基磺酰胺衍生物
BG100247A (bg) Фенилхетероциклени съединения като инхибитори на циклооксигеназа-2
AU2007310897A1 (en) Oxadiazole and thiadiazole compounds and their use as nicotinic acetylcholine receptor modulators
WO2008079906A1 (en) Pyrrolo [2, 3-b] pyridine derivatives as kinase modulators
JP5592360B2 (ja) イミダゾピリミジノンおよびその使用
CA2623045A1 (en) Sulfonamide derivatives as glycokinase activators useful in the treatment of type 2 diabetes
HRP20140098T1 (hr) Derivati piridin-4-ila kao agonisti s1p1/edg1
HRP20080070T3 (en) Pyrrazolo-pyrimidine derivatives
RU2007106037A (ru) Производные пиримидисульфонамида в качестве модуляторов рецепторов хемокинов
CA2581865A1 (en) Indazolone derivatives as 11b-hsd1 inhibitors
HRP20151126T1 (hr) DERIVATI IMIDAZO[2,1-b][1,3,4]TIADIAZOLA
ES2367332T3 (es) Agentes antiparasitarios de benzofurano.
RU2014126341A (ru) СОЕДИНЕНИЯ ТИЕНИЛ[3, 2-d]ПИРИМИДИН-4-ОН, СПОСОБ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И ИХ ПРИМЕНЕНИЕ
HRP20151183T1 (hr) N-[4-(1h-pirazolo[3,4-b]pirazin-6-il)-fenil]-sulfonamidi i njihova uporaba kao lijekova
RU2003129060A (ru) Замещенные пиразоло-и тиазолопиримидины
Suta et al. Modern approaches for SO 2 insertion in heterocyclic synthesis (microreview)
Elattar et al. Sulfones in heterocyclic synthesis: advances in the chemistry of phenyl sulfonylacetophenone
Mukku et al. A facile microwave-assisted synthesis of oxazoles and diastereoselective oxazolines using aryl-aldehydes, p-toluenesulfonylmethyl isocyanide under controlled basic conditions
RU2013129993A (ru) Новое производное пуринилпиридиниламино-2,4-дифторфенилсульфонамида, его фармацевтически приемлемая соль, способ его получения и фармацевтическая композиция, обладающая ингибирующей активностью в отношении raf-киназы, содержащая данное соединение в качестве активного ингредиента
Dobrydnev et al. Updating the CSIC reaction (2003–2020)

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20110622

NF4A Reinstatement of patent

Effective date: 20121020

ND4A Extension of patent duration

Free format text: CLAIMS: 1-5, 9, 10, 49, 57, 58, 60-62

Extension date: 20281004

PD4A Correction of name of patent owner