SV2016005234A - Análogos de cortistatina y síntesis y usos de los mismos - Google Patents

Análogos de cortistatina y síntesis y usos de los mismos

Info

Publication number
SV2016005234A
SV2016005234A SV2016005234A SV2016005234A SV2016005234A SV 2016005234 A SV2016005234 A SV 2016005234A SV 2016005234 A SV2016005234 A SV 2016005234A SV 2016005234 A SV2016005234 A SV 2016005234A SV 2016005234 A SV2016005234 A SV 2016005234A
Authority
SV
El Salvador
Prior art keywords
methods
same
modulation
activity
formula
Prior art date
Application number
SV2016005234A
Other languages
English (en)
Inventor
Matthew D Shair
Juergen Ramharter
Henry Efrem Pelish
Brian Bor-Jen Liau
Jae Young Ahn
Original Assignee
Harvard College
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Harvard College filed Critical Harvard College
Publication of SV2016005234A publication Critical patent/SV2016005234A/es

Links

Classifications

    • 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
    • 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
    • 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 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • 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

Landscapes

  • 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)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE PROPORCIONAN EN LA PRESENTE COMPUESTOS DE LA FÓRMULA (A), (B), (C), (D) Y (E), SALES FARMACÉUTICAMENTE ACEPTABLES, SALES DE AMINAS CUATERNARIAS, Y N-ÓXIDOS DE LOS MISMOS, Y COMPOSICIONES FARMACÉUTICAS DE LOS MISMOS: (VER FORMULA); SE CONTEMPLAN COMPUESTOS DE LA FÓRMULA (A), (B), (C), (D), Y (E) ÚTILES COMO AGENTES TERAPÉUTICOS PARA EL TRATAMIENTO DE UNA AMPLIA VARIEDAD DE CONDICIONES, EJ., INCLUYENDO, PERO NO LIMITADAS A, AFECCIONES ASOCIADAS CON LA ANGIOGÉNESIS Y CON CDK8 Y/O ACTIVIDAD DE LA QUINASA CDK19. ADEMÁS, SE PROPORCIONAN MÉTODOS PARA INHIBIR LA ACTIVIDAD DE LAS QUINASAS CDK19 Y/O CDK8, LOS MÉTODOS DE MODULACIÓN DE LA VÍA DE B-CATENINA, MÉTODOS DE MODULACIÓN DE LA ACTIVIDAD DE STAT1, MÉTODOS DE MODULACIÓN DE LA VÍA TGFB/BMP, MÉTODOS DE MODULACIÓN DE LA ACTIVIDAD DE HIF- 1-ALFA EN UNA CÉLULA, Y MÉTODOS DE AUMENTO DE LA EXPRESIÓN DE BIM PARA INDUCIR LA APOPTOSIS, UTILIZANDO UN COMPUESTO DE LA FÓRMULA (A), (B), (C), (D), O (E). ADEMÁS, SE PROPORCIONAN MUTANTES PUNTUALES EN CDK8 Y CDK19, Y MÉTODOS DE USO DE LOS MISMOS
SV2016005234A 2013-12-24 2016-06-24 Análogos de cortistatina y síntesis y usos de los mismos SV2016005234A (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
SV2016005234A true SV2016005234A (es) 2018-12-14

Family

ID=52350382

Family Applications (1)

Application Number Title Priority Date Filing Date
SV2016005234A SV2016005234A (es) 2013-12-24 2016-06-24 Análogos de cortistatina y síntesis y usos de los mismos

Country Status (30)

Country Link
US (3) US9994582B2 (es)
EP (2) EP3505521A1 (es)
JP (2) JP6494631B2 (es)
KR (1) KR20160101162A (es)
CN (2) CN106103452B (es)
AP (1) AP2016009324A0 (es)
AU (2) AU2014369834B2 (es)
BR (1) BR112016014760A2 (es)
CA (1) CA2934819A1 (es)
CL (1) CL2016001631A1 (es)
CR (1) CR20160291A (es)
DO (1) DOP2016000158A (es)
EA (2) EA201891279A1 (es)
EC (1) ECSP16062174A (es)
ES (1) ES2709480T3 (es)
GT (1) GT201600135A (es)
IL (1) IL246390A0 (es)
MD (1) MD20160089A2 (es)
MX (1) MX361652B (es)
MY (1) MY180383A (es)
NI (1) NI201600089A (es)
PE (1) PE20161405A1 (es)
PH (1) PH12016501258A1 (es)
RU (1) RU2016126503A (es)
SA (1) SA516371410B1 (es)
SG (2) SG11201605178WA (es)
SV (1) SV2016005234A (es)
TN (1) TN2016000240A1 (es)
WO (1) WO2015100420A1 (es)
ZA (1) ZA201603894B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2934819A1 (en) 2013-12-24 2015-07-02 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof
PE20161372A1 (es) 2014-02-03 2017-01-08 Vitae Pharmaceuticals Inc Inhibidores de dihidropirrolopiridina de ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
KR20180003597A (ko) * 2015-05-08 2018-01-09 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 코르티스타틴 유도체로의 치료를 위한 환자의 표적화된 선택
WO2016182932A1 (en) * 2015-05-08 2016-11-17 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
MA53943A (fr) 2015-11-20 2021-08-25 Vitae Pharmaceuticals Llc Modulateurs de ror-gamma
WO2017112823A1 (en) * 2015-12-23 2017-06-29 President And Fellows Of Harvard College Targeted selection of patients for treatment with specific cortistatin derivatives
EA201891511A1 (ru) * 2015-12-23 2018-12-28 Президент Энд Феллоус Оф Гарвард Колледж Аналоги кортистатина и их применения
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
US20190062340A1 (en) * 2016-02-19 2019-02-28 President And Fellows Of Harward College Cortistatin analogs
US11285144B2 (en) 2016-08-03 2022-03-29 The Broad Institute, Inc. Use of CDK8 inhibitors to treat diseases of inflammation and autoimmunity
EP3575297A4 (en) 2017-01-30 2021-07-28 Kyoto University NOVEL COMPOUND AND METHOD FOR PRODUCING REGULATORY T-CELLS
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
CN111225914B (zh) 2017-07-24 2022-10-11 生命医药有限责任公司 RORγ的抑制剂
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN111163775B (zh) 2017-10-02 2023-07-11 勃林格殷格翰国际有限公司 作为cdk8/cdk19抑制剂的新型[1,6]萘啶化合物和衍生物
CN113677341B (zh) * 2019-02-01 2024-07-05 南卡罗莱纳大学 双环吡啶组合物及其用于癌症治疗的方法
CN118056007A (zh) 2021-09-27 2024-05-17 国立大学法人京都大学 用于生产t细胞的方法
EP4438048A1 (en) 2021-11-24 2024-10-02 Regcell Co., Ltd. Pharmaceutical composition for treating or preventing t cell-related disorders
CN118591619A (zh) 2021-11-24 2024-09-03 雷格细胞股份有限公司 人诱导性调节性t细胞及其制作方法

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2886589A (en) 1957-08-05 1959-05-12 Merck & Co Inc 8-methyl-5-oxyphenyl hexahydroindan compounds
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4863457A (en) 1986-11-24 1989-09-05 Lee David A Drug delivery device
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4853224A (en) 1987-12-22 1989-08-01 Visionex Biodegradable ocular implants
US4997652A (en) 1987-12-22 1991-03-05 Visionex Biodegradable ocular implants
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5098443A (en) 1989-03-23 1992-03-24 University Of Miami Method of implanting intraocular and intraorbital implantable devices for the controlled release of pharmacological agents
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5185152A (en) 1990-01-10 1993-02-09 Peyman Gholam A Method and apparatus for controlled release drug delivery to the cornea and anterior chamber of the eye
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5410016A (en) 1990-10-15 1995-04-25 Board Of Regents, The University Of Texas System Photopolymerizable biodegradable hydrogels as tissue contacting materials and controlled-release carriers
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5378475A (en) 1991-02-21 1995-01-03 University Of Kentucky Research Foundation Sustained release drug delivery devices
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
IL105050A0 (en) 1992-03-27 1993-07-08 Lilly Co Eli Steroid derivatives
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
US5443505A (en) 1993-11-15 1995-08-22 Oculex Pharmaceuticals, Inc. Biocompatible ocular implants
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
SE9401108D0 (sv) 1994-03-31 1994-03-31 Leiras Oy Ophthalmic composition I
US5725493A (en) 1994-12-12 1998-03-10 Avery; Robert Logan Intravitreal medicine delivery
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5847172A (en) 1995-06-07 1998-12-08 Magainin Pharmaceuticals Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
US5554187A (en) 1995-08-18 1996-09-10 Rizzo, Iii; Joseph Medication dispensing intra-ocular lens system
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
US6074872A (en) 1996-05-15 2000-06-13 The Scripps Research Institute Cortistatin: nucleic acids that encode these neuropeptides
ZA978537B (en) 1996-09-23 1998-05-12 Focal Inc Polymerizable biodegradable polymers including carbonate or dioxanone linkages.
AU5902398A (en) 1996-12-31 1998-07-31 Human Genome Sciences, Inc. Cortistatin polypeptides
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6632457B1 (en) 1998-08-14 2003-10-14 Incept Llc Composite hydrogel drug delivery systems
US6667299B1 (en) 2000-03-16 2003-12-23 Hollis-Eden Pharmaceuticals, Inc. Pharmaceutical compositions and treatment methods
US20030060425A1 (en) 1998-11-24 2003-03-27 Ahlem Clarence N. Immune modulation method using steroid compounds
US6291516B1 (en) 1999-01-13 2001-09-18 Curis, Inc. Regulators of the hedgehog pathway, compositions and uses related thereto
AU775630B2 (en) 1999-04-30 2004-08-05 Arch Development Corporation Steroid derivatives
AU7736300A (en) 1999-09-30 2001-04-30 Hollis-Eden Pharmaceuticals, Inc. Therapeutic treatment of androgen receptor driven conditions
CA2386190C (en) 1999-10-13 2009-04-14 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
EP1223941B1 (en) 1999-10-25 2008-11-05 Hollis-Eden Pharmaceuticals Inc. Therapeutic treatments for blood cell deficiencies using sreroids
CN1827621A (zh) * 2000-03-31 2006-09-06 萨诺化学药物股份公司 雪花胺的新衍生物和类似物
CA2446904A1 (en) 2001-05-24 2003-04-03 Alexza Molecular Delivery Corporation Delivery of drug esters through an inhalation route
ITMI20011445A1 (it) 2001-07-06 2003-01-06 Europ Geie Analoghi della cortistantina capaci di legarsi selettivamente ai recettori dei secretagoghi dell'ormone della crescita
US20030236439A1 (en) 2002-01-30 2003-12-25 Gregory Agoston Non-steroidal analogs of 2-methoxyestradiol
EP1575981B1 (en) 2002-12-24 2009-06-10 The University of British Columbia Angiogenic acting tri-sulphate steroids and uses thereof
JP4719144B2 (ja) 2003-03-24 2011-07-06 ステリックス リミテッド ステロイドスルファターゼのインヒビターとしてのエストロゲン誘導体
EP1633367A2 (en) 2003-05-28 2006-03-15 EntreMed, Inc. Antiangiogenic agents
CN100448863C (zh) * 2003-07-24 2009-01-07 默克公司 抗生素化合物
US20070004689A1 (en) 2004-03-12 2007-01-04 Agoston Gregory E Antiangiogenic agents
GB0421106D0 (en) 2004-09-22 2004-10-27 Sterix Ltd Compound
PL1853619T3 (pl) 2005-03-02 2011-03-31 Univ Maryland 3-beta-Hydroksy-17-(1H-benzimidazol-1-ilo)-androsta-5,16-dien do zastosowania do leczenia choroby prostaty
CN101400690A (zh) 2006-01-09 2009-04-01 英国技术集团国际有限公司 低氧诱导因子-1调节剂和相关用途
WO2007082980A1 (es) 2006-01-23 2007-07-26 Consejo Superior De Investigaciones Científicas Composiciones y procedimientos para tratar trastornos inflamatorios e inmunitarios con cortistatina
WO2007103162A2 (en) 2006-03-01 2007-09-13 Samaritan Pharmaceuticals, Inc. Structure based drug design of steroidogenesis inhibitors
EP2029575B1 (en) * 2006-05-09 2014-10-22 Merck Sharp & Dohme Corp. Substituted spirocyclic cgrp receptor antagonists
EP1870405A1 (en) * 2006-06-22 2007-12-26 Bioprojet Carbonylated (Aza)cyclohexanes as dopamine D3 receptor ligands
WO2008064425A1 (en) 2006-11-30 2008-06-05 Solbec Pharmaceuticals Limited Glycoalkaloid and chemotherapeutic agent combinations and various uses thereof
CN101600711A (zh) 2006-12-22 2009-12-09 工业研究有限公司 核苷酶和磷酸化酶抑制剂的氮杂环丁烷类似物
WO2008109829A1 (en) 2007-03-07 2008-09-12 Infinity Pharmaceuticals, Inc. Cyclopamine lactam analogs and methods of use thereof
EP2205074A4 (en) * 2007-10-04 2013-07-31 Harvard College ANALOGUES OF THE MOENOMYCIN, METHODS OF SYNTHESIS AND USES THEREOF
WO2009137335A1 (en) * 2008-05-05 2009-11-12 The Scripps Research Institute Synthesis of (+) corstistatin a and related compounds
EP2334686B1 (en) 2008-08-28 2019-02-27 President and Fellows of Harvard College Cortistatin analogues and syntheses therof
US20120190659A1 (en) 2009-04-22 2012-07-26 Children's Medical Center Corporation Angiogenesis inhibitors
US8598344B2 (en) 2009-11-30 2013-12-03 Senex Biotechnology CDKI pathway inhibitors and uses thereof
RU2012152352A (ru) 2010-05-20 2014-06-27 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРАЗИН-7-КАРБОКСАМИДА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ JAK И SYK
EP2617720B1 (en) 2010-09-17 2016-03-30 Osaka University Novel cortistatin a analog and use thereof
US20130331414A1 (en) 2011-01-10 2013-12-12 Susana Valente Inhibitors of Retroviral Replication
EA028595B1 (ru) 2012-02-02 2017-12-29 Сенекс Биотекнолоджи Инк. Селективные ингибиторы cdk8/cdk19 и их применение в качестве противометастатических и химиопрофилактических агентов для лечения рака
WO2013122609A1 (en) 2012-02-17 2013-08-22 Genentech, Inc. Methods of using cdk8 antagonists
WO2014123900A1 (en) 2013-02-05 2014-08-14 Sirenas Marine Discovery Anti-cancer and anti-hiv compounds
WO2014134169A1 (en) 2013-02-26 2014-09-04 Senex Biotechnology, Inc. Inhibitors of cdk8/19 for use in treating estrogen receptor positive breast cancer
WO2014199377A1 (en) 2013-06-10 2014-12-18 Yeda Research And Development Co. Ltd. Compositions and methods for treating a hematological malignancy associated with an altered runx1 activity or expression
CA2921324C (en) 2013-09-18 2022-11-22 Bcn Peptides S.A. Cortistatin analogues for the treatment of inflammatory and/or immune diseases
CA2934819A1 (en) 2013-12-24 2015-07-02 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof

Also Published As

Publication number Publication date
EP3087080A1 (en) 2016-11-02
DOP2016000158A (es) 2016-10-16
BR112016014760A2 (pt) 2017-12-12
NI201600089A (es) 2016-08-18
AP2016009324A0 (en) 2016-07-31
EP3505521A1 (en) 2019-07-03
US20170029435A1 (en) 2017-02-02
EP3087080B1 (en) 2018-11-28
PE20161405A1 (es) 2017-01-18
US20180319814A1 (en) 2018-11-08
RU2016126503A3 (es) 2018-07-17
RU2016126503A (ru) 2018-01-30
CA2934819A1 (en) 2015-07-02
CN106103452A (zh) 2016-11-09
IL246390A0 (en) 2016-08-31
US9994582B2 (en) 2018-06-12
US20190185484A1 (en) 2019-06-20
SA516371410B1 (ar) 2019-02-13
PH12016501258A1 (en) 2016-08-15
JP6494631B2 (ja) 2019-04-03
GT201600135A (es) 2018-11-27
ZA201603894B (en) 2018-08-29
EA201891279A1 (ru) 2019-01-31
CN106103452B (zh) 2019-05-21
CR20160291A (es) 2017-02-24
US10508121B2 (en) 2019-12-17
CN110183461A (zh) 2019-08-30
TN2016000240A1 (en) 2017-10-06
MY180383A (en) 2020-11-28
MX361652B (es) 2018-12-13
AU2019201888A1 (en) 2019-04-11
ECSP16062174A (es) 2018-12-31
AU2014369834A1 (en) 2016-06-23
SG10201808151RA (en) 2018-10-30
KR20160101162A (ko) 2016-08-24
SG11201605178WA (en) 2016-07-28
JP2019108367A (ja) 2019-07-04
JP2017509586A (ja) 2017-04-06
EA030907B1 (ru) 2018-10-31
AU2014369834B2 (en) 2018-12-20
ES2709480T3 (es) 2019-04-16
MX2016008436A (es) 2016-12-16
WO2015100420A1 (en) 2015-07-02
US10273241B2 (en) 2019-04-30
EA201691167A1 (ru) 2016-11-30
CL2016001631A1 (es) 2017-02-24
MD20160089A2 (ro) 2016-12-31

Similar Documents

Publication Publication Date Title
SV2016005234A (es) Análogos de cortistatina y síntesis y usos de los mismos
CL2017000469A1 (es) Derivados de tetrahidronaftaleno que inhiben la proteina mcl-1
GT201400301A (es) 7h-pirrolo [2,3-d] pirimidinas-4- ( aminho-substituidas) novedosas como inhibidores de lrrk2
GT201400196A (es) Compuestos de heterociclilo
CR20160191A (es) Compuestos derivados de piridilo bicíclicos fusionados a anillo como inhibidores de fgfr4
CO7190242A2 (es) Moduladores del transporte nuclear y usos de los mismos
CR20150628A (es) Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedades
DOP2015000241A (es) Compuestos de biaril-amida como inhibidores de cinasa
CO2018004857A2 (es) Derivados de dihidroimidazopirazinona usados en el tratamiento del cáncer
SV2018005655A (es) "derivados de 8-[6-[3-(amino)propoxi]-3-piridil]1-isopropilimidazo[4,5-c]quinolin-2-ona como moduladores selectivos de la cinasa de la ataxia telangiectasia mutada (atm) para el tratamiento del cancer"
ES2636936T3 (es) Derivados de triazolo[4,5-d]pirimidina para el tratamiento de enfermedades tales como cáncer
CL2015002520A1 (es) Compuestos novedosos de pirimidina y piridina y su uso.
CL2012000589A1 (es) Compuestos derivados de pirrolo piridin carboxamidas, inhibidores de jak2; composición farmacéutica que los comprende; uso en el tratamiento de enfermedades mieloproliferativas o cáncer, tales como policitemia vera, trombocitopenia esencial, mieloma múltiple, entre otras.
CL2015002608A1 (es) Compuesto de amino-pirazol y usos medicinales relacionados.
ECSP14013215A (es) Compuestos novedosos
CL2019002900A1 (es) Análogos de benzoazepina como agentes inhibidores de la tirosina cinasa de bruton.
BR112015023013A2 (pt) inibidores de quinase cdk9
BR112015023078A2 (pt) inibidores de pirrolopirimindina cdk9 quinase
ECSP18056196A (es) Derivados de indano
CL2017002605A1 (es) Derivados de indol
ECSP099644A (es) Derivados de quinolina, composiciones farmacéuticas que los comprenden y el uso de tales en el tratamiento de enfermedades del sistema nervioso central y periférico
CU20100004A7 (es) Derivados de morfolino pirimidina utilizados en enfermedades relacionadas con mtor quinasa y/o pi3k
ECSP12012120A (es) Compuestos de pirazol como antagonistas de crth2.
CU20140140A7 (es) 7H-PIRROLO[2,3-d]PIRIMIDINAS 4-(AMINO-SUBSTITUIDAS) NOVEDOSAS COMO INHIBIDORES DE LRRK2
UY35792A (es) Compuestos derivados de piridilo bicíclicos fusionados a anillo como inhibidores de fgfr4