ECSP16062174A - Análogos de cortistatina y síntesis y usos de los mismos - Google Patents
Análogos de cortistatina y síntesis y usos de los mismosInfo
- Publication number
- ECSP16062174A ECSP16062174A ECIEPI201662174A ECPI201662174A ECSP16062174A EC SP16062174 A ECSP16062174 A EC SP16062174A EC IEPI201662174 A ECIEPI201662174 A EC IEPI201662174A EC PI201662174 A ECPI201662174 A EC PI201662174A EC SP16062174 A ECSP16062174 A EC SP16062174A
- Authority
- EC
- Ecuador
- Prior art keywords
- formula
- found
- compound
- cortistatin
- potent
- Prior art date
Links
Classifications
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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
-
- 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
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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
-
- 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)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
[0001] Se proporcionan en la presente nuevos análogos de cortistatina de la fórmula (A), (B) y (C), y sales farmacéuticamente aceptables, sales de amina cuaternaria, y N-óxidos de los mismos, sintetizados, en parte, por aminación reductiva de una cetona de la Fórmula (B) para proporcionar el producto aminado de la fórmula (A), como se representa en el Esquema 1, opcionalmente a través de un intermedio de imina de la fórmula (C). [0002] Además, se proporcionan nuevos análogos de cortistatina preparados por reducción de la cetona de la fórmula (B) para proporcionar un compuesto C3-hidroxilo de la Fórmula (D). Además se proporciona un compuesto de la fórmula (E), preparado por sustitución del compuesto de la Fórmula (D). Tales compuestos también se pueden convertir en un compuesto de la Fórmula (A) por tratamiento con una amina en condiciones adecuadas. [0003] Se ha encontrado sorprendentemente que los isómeros beta de la Fórmula (A), que se conoce como la Fórmula (A-1), se han encontrado como equipotentes, o más potentes, que la cortistatina A en la inhibición de la actividad de la quinasa CDK8 y la proliferación de las células AML, y también se ha encontrado que los isómeros alfa correspondientes de la fórmula (A), que se refiere como la Fórmula (A-2), también son muy potentes. Además, se ha descubierto que los compuestos de la Fórmula (B) se han encontrado activos contra el crecimiento de líneas celulares AML en cultivo y actividad de la quinasa CDK8 en las c
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 |
---|---|
ECSP16062174A true ECSP16062174A (es) | 2018-12-31 |
Family
ID=52350382
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECIEPI201662174A ECSP16062174A (es) | 2013-12-24 | 2016-07-20 | Análogos de cortistatina y síntesis y usos de los mismos |
Country Status (30)
Country | Link |
---|---|
US (3) | US9994582B2 (es) |
EP (2) | EP3087080B1 (es) |
JP (2) | JP6494631B2 (es) |
KR (1) | KR20160101162A (es) |
CN (2) | CN110183461A (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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE20161405A1 (es) | 2013-12-24 | 2017-01-18 | Harvard College | Analogos de cortistatina y sintesis y usos de los mismos |
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 |
CN107847763A (zh) * | 2015-05-08 | 2018-03-27 | 哈佛学院院长等 | 靶向选择适合于用皮质抑素衍生物治疗的患者 |
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 |
DK3331876T3 (da) | 2015-08-05 | 2021-01-11 | Vitae Pharmaceuticals Llc | Modulators of ror-gamma |
MA53943A (fr) | 2015-11-20 | 2021-08-25 | Vitae Pharmaceuticals Llc | Modulateurs 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 |
KR20180095051A (ko) * | 2015-12-23 | 2018-08-24 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 코르티스타틴 유사체 및 그의 용도 |
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 |
EP3416970A4 (en) * | 2016-02-19 | 2019-07-24 | President and Fellows of Harvard College | ANALOGUES OF CORTISTATIN |
US11285144B2 (en) | 2016-08-03 | 2022-03-29 | The Broad Institute, Inc. | Use of CDK8 inhibitors to treat diseases of inflammation and autoimmunity |
CN114921468A (zh) | 2017-01-30 | 2022-08-19 | 国立大学法人京都大学 | 新型化合物以及调节性t细胞的制造方法 |
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 |
AU2018307919B2 (en) | 2017-07-24 | 2022-12-01 | Vitae Pharmaceuticals, Llc | Inhibitors of RORϒ |
WO2019068613A1 (en) | 2017-10-02 | 2019-04-11 | Boehringer Ingelheim International Gmbh | NOVEL [1,6] NAPHTHYRIDINE COMPOUNDS AND DERIVATIVES AS CDK8 / CDK19 INHIBITORS |
EP3917523A4 (en) * | 2019-02-01 | 2022-10-19 | University of South Carolina | BICYCLIC PYRIDINE COMPOSITIONS AND METHODS OF USE THERE FOR CANCER THERAPY |
AR127141A1 (es) | 2021-09-27 | 2023-12-20 | Univ Kyoto | Método para producir células t |
CA3239019A1 (en) | 2021-11-24 | 2023-06-01 | Regcell Co., Ltd. | Human inducibility controllable t-cell and method for preparing same |
TW202334397A (zh) | 2021-11-24 | 2023-09-01 | 日商雷格細胞股份有限公司 | 用於治療或預防t細胞相關疾病之醫藥組合物 |
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