CA2934819A1 - Cortistatin analogues and syntheses and uses thereof - Google Patents

Cortistatin analogues and syntheses and uses thereof Download PDF

Info

Publication number
CA2934819A1
CA2934819A1 CA2934819A CA2934819A CA2934819A1 CA 2934819 A1 CA2934819 A1 CA 2934819A1 CA 2934819 A CA2934819 A CA 2934819A CA 2934819 A CA2934819 A CA 2934819A CA 2934819 A1 CA2934819 A1 CA 2934819A1
Authority
CA
Canada
Prior art keywords
optionally substituted
compound
hydrogen
attached
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2934819A
Other languages
English (en)
French (fr)
Inventor
Matthew D. Shair
Juergen Ramharter
Henry Efrem PELISH
Brian Bor-Jen Liau
Jae Young Ahn
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Harvard University
Original Assignee
Harvard University
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 University filed Critical Harvard University
Publication of CA2934819A1 publication Critical patent/CA2934819A1/en
Abandoned legal-status Critical Current

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 [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/26—Immunoglobulins [IG], 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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2934819A 2013-12-24 2014-12-24 Cortistatin analogues and syntheses and uses thereof Abandoned CA2934819A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361920674P 2013-12-24 2013-12-24
US61/920,674 2013-12-24
US201461935240P 2014-02-03 2014-02-03
US61/935,240 2014-02-03
US201461993329P 2014-05-15 2014-05-15
US61/993,329 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
CA2934819A1 true CA2934819A1 (en) 2015-07-02

Family

ID=52350382

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2934819A Abandoned CA2934819A1 (en) 2013-12-24 2014-12-24 Cortistatin analogues and syntheses and uses thereof

Country Status (30)

Country Link
US (3) US9994582B2 (enExample)
EP (2) EP3087080B1 (enExample)
JP (2) JP6494631B2 (enExample)
KR (1) KR20160101162A (enExample)
CN (2) CN106103452B (enExample)
AP (1) AP2016009324A0 (enExample)
AU (2) AU2014369834B2 (enExample)
BR (1) BR112016014760A2 (enExample)
CA (1) CA2934819A1 (enExample)
CL (1) CL2016001631A1 (enExample)
CR (1) CR20160291A (enExample)
DO (1) DOP2016000158A (enExample)
EA (2) EA030907B1 (enExample)
EC (1) ECSP16062174A (enExample)
ES (1) ES2709480T3 (enExample)
GT (1) GT201600135A (enExample)
IL (1) IL246390A0 (enExample)
MD (1) MD20160089A2 (enExample)
MX (1) MX361652B (enExample)
MY (1) MY180383A (enExample)
NI (1) NI201600089A (enExample)
PE (1) PE20161405A1 (enExample)
PH (1) PH12016501258A1 (enExample)
RU (1) RU2016126503A (enExample)
SA (1) SA516371410B1 (enExample)
SG (2) SG11201605178WA (enExample)
SV (1) SV2016005234A (enExample)
TN (1) TN2016000240A1 (enExample)
WO (1) WO2015100420A1 (enExample)
ZA (1) ZA201603894B (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201605178WA (en) 2013-12-24 2016-07-28 Harvard College Cortistatin analogues and syntheses and uses thereof
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
WO2016182932A1 (en) 2015-05-08 2016-11-17 President And Fellows Of Harvard College Cortistatin analogues, syntheses, and uses thereof
KR20180003597A (ko) * 2015-05-08 2018-01-09 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 코르티스타틴 유도체로의 치료를 위한 환자의 표적화된 선택
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
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3394072A4 (en) * 2015-12-23 2019-05-29 President and Fellows of Harvard College Cortistatin analogs and uses thereof
EP3394038A4 (en) * 2015-12-23 2019-08-21 President and Fellows of Harvard College TARGETED SELECTION OF PATIENTS FOR TREATMENT WITH SPECIFIC CORTISTATINE DERIVATIVES
TWI757266B (zh) 2016-01-29 2022-03-11 美商維它藥物有限責任公司 ROR-γ調節劑
CN109415382A (zh) * 2016-02-19 2019-03-01 哈佛学院院长等 皮质抑素类似物
US11285144B2 (en) 2016-08-03 2022-03-29 The Broad Institute, Inc. Use of CDK8 inhibitors to treat diseases of inflammation and autoimmunity
JP7142846B2 (ja) 2017-01-30 2022-09-28 国立大学法人京都大学 新規化合物及び制御性t細胞の製造方法
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
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN115716826A (zh) 2017-07-24 2023-02-28 生命医药有限责任公司 RORγ的抑制剂
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
ES2991429T3 (es) * 2019-02-01 2024-12-03 Univ South Carolina Compuestos de piridina bicíclicos para su uso en el tratamiento del cáncer
AU2020393896A1 (en) 2019-11-26 2022-06-23 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of CDK8 and CDK19
EP4410965A4 (en) 2021-09-27 2025-09-24 Univ Kyoto T LYMPHOCYTE PRODUCTION PROCESS
KR20240130083A (ko) 2021-11-24 2024-08-28 레그셀 가부시키가이샤 T세포 관련 질환을 치료 또는 예방하기 위한 의약 조성물
TW202330911A (zh) 2021-11-24 2023-08-01 日商雷格細胞股份有限公司 人類誘導性控制性t細胞及其製作方法
EP4497822A4 (en) 2022-03-23 2026-03-18 Univ Kyoto PROCESS FOR THE PRODUCTION OF REGULATORY T LYMPHOCYTES
CN120112629A (zh) 2022-09-26 2025-06-06 国立大学法人京都大学 T细胞产生方法
EP4596684A1 (en) 2022-09-26 2025-08-06 Regcell Co., Ltd. Induced regulatory t cells containing chimeric antigen receptor (car)
US20260232799A1 (en) 2023-02-08 2026-08-13 Regcell Co., Ltd. Pharmaceutical composition for treating or preventing pemphigus
CN121057812A (zh) 2023-03-29 2025-12-02 雷格细胞股份有限公司 人诱导性调节性t细胞及其制作方法以及用于治疗或预防t细胞相关疾病的药物组合物

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
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule 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
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 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
JP2002543216A (ja) 1999-04-30 2002-12-17 アーチ ディベロップメント コーポレイション ステロイド誘導体
AU7736300A (en) 1999-09-30 2001-04-30 Hollis-Eden Pharmaceuticals, Inc. Therapeutic treatment of androgen receptor driven conditions
DE60028411T2 (de) 1999-10-13 2007-01-04 Johns Hopkins University School Of Medicine Verbindungen zur regulierung des hedgehog-signalwegs, zusammensetzungen und verwendungen davon
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 Pharmaceuticals, Inc. 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
AU2003292939A1 (en) 2002-12-24 2004-07-22 The University Of British Columbia Angiogenic compounds and uses thereof
DE602004024966D1 (de) 2003-03-24 2010-02-25 Sterix Ltd Oestrogenderivate als steroid sulphatase inhibitoren
WO2005030120A2 (en) 2003-05-28 2005-04-07 Entremed, Inc. Antiangiogenic agents
DE602004025946D1 (de) * 2003-07-24 2010-04-22 Merck Sharp & Dohme Antibiotische verbindung
US20070004689A1 (en) 2004-03-12 2007-01-04 Agoston Gregory E Antiangiogenic agents
GB0421106D0 (en) 2004-09-22 2004-10-27 Sterix Ltd Compound
JP5130453B2 (ja) 2005-03-02 2013-01-30 ユニバーシティ オブ メリーランド,ボルティモア 新規なc−17−ヘテロアリールステロイドcyp17阻害剤/抗アンドロゲン:合成、インビトロ生物活性、薬物動態および抗腫瘍活性
US20090023666A1 (en) 2006-01-09 2009-01-22 BTG plc Modulators of Hypoxia Inducible Factor-1 and Related Uses
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
WO2007133491A1 (en) * 2006-05-09 2007-11-22 Merck & Co., Inc. 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
DK2114925T3 (da) 2006-12-22 2012-05-29 Ind Res Ltd Azetidin-analoger af nucleosidase- og phosphorylase-inhibitorer
EP2134719B1 (en) 2007-03-07 2013-07-17 Infinity Discovery, Inc. Cyclopamine lactam analogs and methods of use thereof
EP2205074A4 (en) * 2007-10-04 2013-07-31 Harvard College MOENOMYCIN ANALOGUE, SYNTHESIS PROCESS AND USE
CA2723689C (en) * 2008-05-05 2016-07-05 Ryan A. Shenvi Synthesis of (+) cortistatin a and related compounds
EP2334686B1 (en) 2008-08-28 2019-02-27 President and Fellows of Harvard College Cortistatin analogues and syntheses therof
JP2012524778A (ja) 2009-04-22 2012-10-18 プレジデント アンド フェロウズ オブ ハーバード カレッジ 血管新生阻害剤
US8598344B2 (en) 2009-11-30 2013-12-03 Senex Biotechnology CDKI pathway inhibitors and uses thereof
EP2571880A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolo [2, 3 - b]pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
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
CN104363913B (zh) 2012-02-02 2018-08-21 申内克斯生物科技公司 Cdk8/cdk19选择性抑制剂及其在癌症的抗转移和化学预防方法中的用途
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
EP2961409A1 (en) 2013-02-26 2016-01-06 Senex Biotechnology, Inc. Inhibitors of cdk8/19 for use in treating estrogen receptor positive breast cancer
EP3007686A4 (en) 2013-06-10 2017-03-15 Yeda Research and Development Co., Ltd. Compositions and methods for treating a hematological malignancy associated with an altered runx1 activity or expression
SG11201601036UA (en) 2013-09-18 2016-04-28 Bcn Peptides Sa Cortistatin analogues for the treatment of inflammatory and/or immune diseases
SG11201605178WA (en) 2013-12-24 2016-07-28 Harvard College Cortistatin analogues and syntheses and uses thereof

Also Published As

Publication number Publication date
US9994582B2 (en) 2018-06-12
TN2016000240A1 (en) 2017-10-06
EP3505521A1 (en) 2019-07-03
GT201600135A (es) 2018-11-27
CN110183461A (zh) 2019-08-30
JP2017509586A (ja) 2017-04-06
MY180383A (en) 2020-11-28
KR20160101162A (ko) 2016-08-24
US20180319814A1 (en) 2018-11-08
ES2709480T3 (es) 2019-04-16
CN106103452B (zh) 2019-05-21
JP2019108367A (ja) 2019-07-04
US10508121B2 (en) 2019-12-17
JP6494631B2 (ja) 2019-04-03
BR112016014760A2 (pt) 2017-12-12
US20190185484A1 (en) 2019-06-20
PE20161405A1 (es) 2017-01-18
AU2014369834B2 (en) 2018-12-20
SA516371410B1 (ar) 2019-02-13
SV2016005234A (es) 2018-12-14
AU2014369834A1 (en) 2016-06-23
CL2016001631A1 (es) 2017-02-24
MD20160089A2 (ro) 2016-12-31
CR20160291A (es) 2017-02-24
CN106103452A (zh) 2016-11-09
IL246390A0 (en) 2016-08-31
EP3087080A1 (en) 2016-11-02
ZA201603894B (en) 2018-08-29
PH12016501258A1 (en) 2016-08-15
RU2016126503A3 (enExample) 2018-07-17
US20170029435A1 (en) 2017-02-02
ECSP16062174A (es) 2018-12-31
US10273241B2 (en) 2019-04-30
EA030907B1 (ru) 2018-10-31
AP2016009324A0 (en) 2016-07-31
DOP2016000158A (es) 2016-10-16
RU2016126503A (ru) 2018-01-30
SG11201605178WA (en) 2016-07-28
SG10201808151RA (en) 2018-10-30
MX361652B (es) 2018-12-13
EA201691167A1 (ru) 2016-11-30
AU2019201888A1 (en) 2019-04-11
EP3087080B1 (en) 2018-11-28
MX2016008436A (es) 2016-12-16
WO2015100420A1 (en) 2015-07-02
NI201600089A (es) 2016-08-18
EA201891279A1 (ru) 2019-01-31

Similar Documents

Publication Publication Date Title
AU2014369834B2 (en) Cortistatin analogues and syntheses and uses thereof
CA3041563C (en) Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12)
AU2018202150B2 (en) Teatrahydro-and dihydro-isoquinoline prmt5 inhibitors and uses thereof
AU2017363313A1 (en) Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
WO2016182904A1 (en) Targeted selection of patients for treatment with cortistatin derivatives
CA2899363A1 (en) Prmt5 inhibitors and uses thereof
CA2918910A1 (en) Inhibitors of transcription factors and uses thereof
CA3157331A1 (en) A pyrazolopyrimidine derivative as a hck inhibitor for use in therapy, in particular myd88 mutated diseases
WO2019094732A1 (en) Inhibitors of cyclic-amp response element-binding protein
EP3448857A1 (en) Analogs of yohimbine and uses thereof
US10273240B2 (en) Cortistatin analogues, syntheses, and uses thereof
WO2023081141A1 (en) Thymidylate synthase inhibitors and uses thereof
AU2013364160A1 (en) PRMT5 inhibitors and uses thereof
AU2013364163A1 (en) Teatrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20210831