BR112016014760A2 - composto, composição farmacêutica, métodos para tratamento de uma condição, para inibir e validar atividade de cinase, para modular o trajeto de b-catenina e o trajeto de tgfb/bmp em uma célula, para modular a atividade de stat1 e de hif-1-alfa em uma célula, para aumentar a expressão de bim e para preparar um composto, mutante, e, proteína - Google Patents
composto, composição farmacêutica, métodos para tratamento de uma condição, para inibir e validar atividade de cinase, para modular o trajeto de b-catenina e o trajeto de tgfb/bmp em uma célula, para modular a atividade de stat1 e de hif-1-alfa em uma célula, para aumentar a expressão de bim e para preparar um composto, mutante, e, proteínaInfo
- Publication number
- BR112016014760A2 BR112016014760A2 BR112016014760A BR112016014760A BR112016014760A2 BR 112016014760 A2 BR112016014760 A2 BR 112016014760A2 BR 112016014760 A BR112016014760 A BR 112016014760A BR 112016014760 A BR112016014760 A BR 112016014760A BR 112016014760 A2 BR112016014760 A2 BR 112016014760A2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- 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
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- 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]
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/26—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against hormones ; against hormone releasing or inhibiting factors
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Diabetes (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
são fornecidos aqui compostos da fórmula (a), (b), (c), (d) e (e), (a), (c) (b), (d), (e) sais farmaceuticamente aceitáveis, sais de amina quaternários e n-óxidos destes farmaceuticamente aceitáveis e composições farmacêuticas dos mesmos. os compostos da fórmula (a), (b), (c), (d) e (e) são considerados úteis como terapêuticos para tratar uma variedade ampla de condições, por exemplo, que incluem, mas não se limitam a, condições associadas com a angiogênese e com atividade de cinase cdk8 e/ou cdk19. ainda são fornecidos métodos de inibir atividade de cinase cdk8 e/ou cdk19, métodos de modular o trajeto de ß-catenina, métodos de modular a atividade de stat1, métodos de modular o trajeto de tgfß/bmp, métodos de modular a atividade de hif-1-alfa em uma célula e métodos de aumentar a expressão de bim para induzir a apoptose, usando-se um composto da fórmula (a), (b), (c), (d) ou (e). ainda são fornecidos mutantes pontuais cdk8 e cdk19 e métoros de uso dos mesmos.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361920674P | 2013-12-24 | 2013-12-24 | |
US201461935240P | 2014-02-03 | 2014-02-03 | |
US201461993329P | 2014-05-15 | 2014-05-15 | |
PCT/US2014/072365 WO2015100420A1 (en) | 2013-12-24 | 2014-12-24 | Cortistatin analogues and syntheses and uses thereof |
Publications (1)
Publication Number | Publication Date |
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BR112016014760A2 true BR112016014760A2 (pt) | 2017-12-12 |
Family
ID=52350382
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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BR112016014760A BR112016014760A2 (pt) | 2013-12-24 | 2014-12-24 | composto, composição farmacêutica, métodos para tratamento de uma condição, para inibir e validar atividade de cinase, para modular o trajeto de b-catenina e o trajeto de tgfb/bmp em uma célula, para modular a atividade de stat1 e de hif-1-alfa em uma célula, para aumentar a expressão de bim e para preparar um composto, mutante, e, proteína |
Country Status (30)
Country | Link |
---|---|
US (3) | US9994582B2 (pt) |
EP (2) | EP3505521A1 (pt) |
JP (2) | JP6494631B2 (pt) |
KR (1) | KR20160101162A (pt) |
CN (2) | CN110183461A (pt) |
AP (1) | AP2016009324A0 (pt) |
AU (2) | AU2014369834B2 (pt) |
BR (1) | BR112016014760A2 (pt) |
CA (1) | CA2934819A1 (pt) |
CL (1) | CL2016001631A1 (pt) |
CR (1) | CR20160291A (pt) |
DO (1) | DOP2016000158A (pt) |
EA (2) | EA030907B1 (pt) |
EC (1) | ECSP16062174A (pt) |
ES (1) | ES2709480T3 (pt) |
GT (1) | GT201600135A (pt) |
IL (1) | IL246390A0 (pt) |
MD (1) | MD20160089A2 (pt) |
MX (1) | MX361652B (pt) |
MY (1) | MY180383A (pt) |
NI (1) | NI201600089A (pt) |
PE (1) | PE20161405A1 (pt) |
PH (1) | PH12016501258A1 (pt) |
RU (1) | RU2016126503A (pt) |
SA (1) | SA516371410B1 (pt) |
SG (2) | SG10201808151RA (pt) |
SV (1) | SV2016005234A (pt) |
TN (1) | TN2016000240A1 (pt) |
WO (1) | WO2015100420A1 (pt) |
ZA (1) | ZA201603894B (pt) |
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PE20161405A1 (es) | 2013-12-24 | 2017-01-18 | Harvard College | Analogos de cortistatina y sintesis y usos de los mismos |
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RU2017142394A (ru) * | 2015-05-08 | 2019-06-10 | Президент Энд Феллоус Оф Гарвард Колледж | Целевой отбор пациентов для лечения производными кортистатина |
EP3294298A4 (en) | 2015-05-08 | 2018-10-17 | President and Fellows of Harvard College | Cortistatin analogues, syntheses, and uses thereof |
EP3316889A4 (en) * | 2015-07-01 | 2018-11-14 | President and Fellows of Harvard College | Cortistatin analogues and syntheses and uses thereof |
EP3331876B1 (en) | 2015-08-05 | 2020-10-07 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
MX2018006223A (es) | 2015-11-20 | 2018-12-19 | Vitae Pharmaceuticals Inc | Moduladores de ror-gamma. |
EP3394038A4 (en) * | 2015-12-23 | 2019-08-21 | President and Fellows of Harvard College | TARGETED PATIENT SELECTION FOR TREATMENT WITH SPECIFIC CORTISTANTIDE DERIVATIVES |
SG11201805092WA (en) * | 2015-12-23 | 2018-07-30 | Harvard College | Cortistatin analogs and uses thereof |
TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
MX2018009998A (es) * | 2016-02-19 | 2018-12-10 | Harvard College | Analogos de cortistatina. |
US11285144B2 (en) | 2016-08-03 | 2022-03-29 | The Broad Institute, Inc. | Use of CDK8 inhibitors to treat diseases of inflammation and autoimmunity |
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CN107028956A (zh) * | 2017-03-06 | 2017-08-11 | 刘杰 | 一种治疗经期抑郁症的药物组合物 |
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