MD20160089A2 - Analogi ai cortistatinului, sinteza şi utilizările acestora - Google Patents
Analogi ai cortistatinului, sinteza şi utilizările acestora Download PDFInfo
- Publication number
- MD20160089A2 MD20160089A2 MDA20160089A MD20160089A MD20160089A2 MD 20160089 A2 MD20160089 A2 MD 20160089A2 MD A20160089 A MDA20160089 A MD A20160089A MD 20160089 A MD20160089 A MD 20160089A MD 20160089 A2 MD20160089 A2 MD 20160089A2
- Authority
- MD
- Moldova
- Prior art keywords
- methods
- modulating
- formula
- cdk8
- activity
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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
-
- 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
-
- 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)
Abstract
În prezenta cerere de brevet sunt prezentaţi compuşii cu formulele (A), (B), (C), (D) şi (E), sărurile acceptabile farmaceutice ale acestora, sărurile cuaternare de amine şi N-oxizii, precum şi compoziţiile farmaceutice ale acestora.Compuşii (A), (B), (C), (D) şi (E) sunt aplicabili ca agenţi terapeutici pentru tratarea unei game largi de stări, de exemplu, incluzând, dar fară a se limita la acestea, stările asociate cu angiogeneza şi cu activitatea kinazelor CDK8 şi/sau CDK19. De esemenea sunt prezentate metodele de inhibare a activităţii kinazelor CDK8 şi/sau CDK19, metodele de modulare a căii β-catenin, metodele de modulare a activităţii STAT1, metodele de modulare a căii TGF/β/BMP, metodele de modulare a activităţii HIF-1-alfa într-o celulă, precum şi metodele de creştere a expresiei BIM pentru a induce apoptoza, utilizând compuşii (A), (B), (C), (D) sau (E). În continuare sunt prezentaţi mutanţii punctiformi CDK8 şi CDK19 şi metodele de utilizare a acestora.
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 |
|---|---|
| MD20160089A2 true MD20160089A2 (ro) | 2016-12-31 |
Family
ID=52350382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MDA20160089A MD20160089A2 (ro) | 2013-12-24 | 2014-12-24 | Analogi ai cortistatinului, sinteza şi utilizările acestora |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US9994582B2 (ro) |
| EP (2) | EP3087080B1 (ro) |
| JP (2) | JP6494631B2 (ro) |
| KR (1) | KR20160101162A (ro) |
| CN (2) | CN106103452B (ro) |
| AP (1) | AP2016009324A0 (ro) |
| AU (2) | AU2014369834B2 (ro) |
| BR (1) | BR112016014760A2 (ro) |
| CA (1) | CA2934819A1 (ro) |
| CL (1) | CL2016001631A1 (ro) |
| CR (1) | CR20160291A (ro) |
| DO (1) | DOP2016000158A (ro) |
| EA (2) | EA030907B1 (ro) |
| EC (1) | ECSP16062174A (ro) |
| ES (1) | ES2709480T3 (ro) |
| GT (1) | GT201600135A (ro) |
| IL (1) | IL246390A0 (ro) |
| MD (1) | MD20160089A2 (ro) |
| MX (1) | MX361652B (ro) |
| MY (1) | MY180383A (ro) |
| NI (1) | NI201600089A (ro) |
| PE (1) | PE20161405A1 (ro) |
| PH (1) | PH12016501258A1 (ro) |
| RU (1) | RU2016126503A (ro) |
| SA (1) | SA516371410B1 (ro) |
| SG (2) | SG11201605178WA (ro) |
| SV (1) | SV2016005234A (ro) |
| TN (1) | TN2016000240A1 (ro) |
| WO (1) | WO2015100420A1 (ro) |
| ZA (1) | ZA201603894B (ro) |
Families Citing this family (28)
| 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 |
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