CU24399B1 - Nuevos compuestos macrocíclicos en calidad de inhibidores de cdk9, un proceso para su preparación y los compuestos intermediarios útiles en la preparación de estos compuestos - Google Patents
Nuevos compuestos macrocíclicos en calidad de inhibidores de cdk9, un proceso para su preparación y los compuestos intermediarios útiles en la preparación de estos compuestosInfo
- Publication number
- CU24399B1 CU24399B1 CU2016000152A CU20160152A CU24399B1 CU 24399 B1 CU24399 B1 CU 24399B1 CU 2016000152 A CU2016000152 A CU 2016000152A CU 20160152 A CU20160152 A CU 20160152A CU 24399 B1 CU24399 B1 CU 24399B1
- Authority
- CU
- Cuba
- Prior art keywords
- compounds
- preparation
- quality
- useful intermediate
- new macrocyclic
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 150000002678 macrocyclic compounds Chemical class 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 title 1
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
- C07C53/16—Halogenated acetic acids
- C07C53/18—Halogenated acetic acids containing fluorine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
<p>Nuevos compuestos macrocíclicos de la fórmula general (I) como se los describe y se los define en la memoria descriptiva. Métodos para prepararlos. Su uso en el tratamiento y/o la profilaxis de diversos trastornos, particularmente de los trastornos hiperproliferativos, de las enfermedades infecciosas inducidas por virus y/o de las enfermedades cardiovasculares. Compuestos intermedios útiles para preparar los compuestos de la fórmula general (I).</p>
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014000392 | 2014-04-11 | ||
| PCT/EP2015/057546 WO2015155197A1 (en) | 2014-04-11 | 2015-04-08 | Novel macrocyclic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CU20160152A7 CU20160152A7 (es) | 2017-04-05 |
| CU24399B1 true CU24399B1 (es) | 2019-04-04 |
Family
ID=52824234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU2016000152A CU24399B1 (es) | 2014-04-11 | 2015-04-08 | Nuevos compuestos macrocíclicos en calidad de inhibidores de cdk9, un proceso para su preparación y los compuestos intermediarios útiles en la preparación de estos compuestos |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9963464B2 (es) |
| EP (1) | EP3129387B1 (es) |
| JP (1) | JP6605493B2 (es) |
| KR (1) | KR102383938B1 (es) |
| CN (1) | CN106459084B (es) |
| AP (1) | AP2016009483A0 (es) |
| AR (1) | AR099999A1 (es) |
| AU (1) | AU2015243585B2 (es) |
| BR (1) | BR112016023554B1 (es) |
| CA (1) | CA2945237C (es) |
| CL (1) | CL2016002577A1 (es) |
| CR (1) | CR20160471A (es) |
| CU (1) | CU24399B1 (es) |
| DO (1) | DOP2016000278A (es) |
| EA (1) | EA032541B1 (es) |
| ES (1) | ES2743799T3 (es) |
| IL (1) | IL247966B (es) |
| MX (1) | MX376962B (es) |
| PE (1) | PE20161379A1 (es) |
| PH (1) | PH12016501968A1 (es) |
| SG (1) | SG11201608430RA (es) |
| SV (1) | SV2016005301A (es) |
| TN (1) | TN2016000435A1 (es) |
| TW (1) | TW201623312A (es) |
| UA (1) | UA119349C2 (es) |
| UY (1) | UY36072A (es) |
| WO (1) | WO2015155197A1 (es) |
| ZA (1) | ZA201607765B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017055196A1 (en) * | 2015-09-29 | 2017-04-06 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic sulfondiimine compounds |
| WO2017060167A1 (en) | 2015-10-08 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Novel modified macrocyclic compounds |
| AU2017252222B2 (en) * | 2016-04-22 | 2019-11-07 | Astrazeneca Ab | Macrocyclic Mcl-1 inhibitors for treating cancer |
| US10849903B2 (en) * | 2016-10-20 | 2020-12-01 | Pfizer Inc. | Anti-proliferative agents for treating PAH |
| EP3601236A1 (en) | 2017-03-28 | 2020-02-05 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| ES2900199T3 (es) | 2017-03-28 | 2022-03-16 | Bayer Ag | Novedosos compuestos macrocíclicos inhibidores de PTEFB |
| CN109251212A (zh) * | 2017-07-14 | 2019-01-22 | 上海长森药业有限公司 | 内环硫醚酰胺-芳基酰胺类化合物及其治疗乙型肝炎的用途 |
| CN111434665B (zh) * | 2019-01-11 | 2023-03-10 | 上海长森药业有限公司 | 内环硫脒酰胺-芳基酰胺类化合物及其治疗乙型肝炎的用途 |
| CN112321604A (zh) * | 2019-08-05 | 2021-02-05 | 华东理工大学 | 大环类jak2抑制剂及其应用 |
| JP7422242B2 (ja) | 2020-09-30 | 2024-01-25 | 旭化成ファーマ株式会社 | マクロサイクル化合物 |
| WO2023057812A1 (en) | 2021-10-04 | 2023-04-13 | Vincerx Pharma Gmbh | Compounds, pharmaceutical compositions, and methods for the treatment, prevention, or management of hyperproliferative disorder |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2311825T1 (sl) | 2000-12-21 | 2016-02-29 | Novartis Ag | Pirimidinamini kot angiogenetski modulatorji |
| DE10239042A1 (de) * | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| DE10349423A1 (de) | 2003-10-16 | 2005-06-16 | Schering Ag | Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| NZ555474A (en) | 2004-12-17 | 2010-10-29 | Astrazeneca Ab | 4-(4-(imidazol-4-yl) pyrimidin-2-ylamino) benzamides as CDK inhibitors |
| DE102006042143A1 (de) | 2006-09-08 | 2008-03-27 | Bayer Healthcare Aktiengesellschaft | Neue substituierte Bipyridin-Derivate und ihre Verwendung |
| WO2008060248A1 (en) * | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| MX2009006535A (es) | 2006-12-22 | 2009-06-26 | Novartis Ag | Derivados de indol-4-il-pirimidinil-2-il-amina y su uso como inhibidores de cinasa dependiente de ciclina. |
| AU2007336933A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as CDK inhibitors for the treatment of cancer, inflammation and viral infections |
| JP5693951B2 (ja) | 2007-04-24 | 2015-04-01 | アストラゼネカ エービー | プロテインキナーゼの阻害剤 |
| WO2008129080A1 (en) | 2007-04-24 | 2008-10-30 | Ingenium Pharmaceuticals Gmbh | 4, 6-disubstituted aminopyrimidine derivatives as inhibitors of protein kinases |
| JP5379787B2 (ja) | 2007-04-24 | 2013-12-25 | インゲニウム ファーマシューティカルズ ジーエムビーエイチ | プロテインキナーゼの阻害剤 |
| WO2008132138A1 (en) | 2007-04-25 | 2008-11-06 | Ingenium Pharmaceuticals Gmbh | Derivatives of 4,6-disubstituted aminopyrimidines |
| WO2009029998A1 (en) | 2007-09-06 | 2009-03-12 | Cytopia Research Pty Ltd | Retrometabolic compounds |
| GB0805477D0 (en) | 2008-03-26 | 2008-04-30 | Univ Nottingham | Pyrimidines triazines and their use as pharmaceutical agents |
| US8415381B2 (en) | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| MX2012010966A (es) | 2010-03-22 | 2013-01-29 | Lead Discovery Center Gmbh | Derivados de triazina disustituidos farmaceuticamente activos. |
| EP2681193B1 (en) | 2011-03-02 | 2016-01-06 | Lead Discovery Center GmbH | Pharmaceutically active disubstituted pyridine derivatives |
| EP2527332A1 (en) | 2011-05-24 | 2012-11-28 | Bayer Intellectual Property GmbH | 4-Aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group as CDK9 inhibitors |
| CA2848615C (en) | 2011-09-16 | 2020-02-25 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group |
| WO2013037896A1 (en) * | 2011-09-16 | 2013-03-21 | Bayer Intellectual Property Gmbh | Disubstituted 5-fluoro-pyrimidines |
| HK1213890A1 (zh) | 2012-10-18 | 2016-07-15 | Bayer Pharma Aktiengesellschaft | 含碸基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺 |
| CN104918918B (zh) | 2012-11-15 | 2017-10-24 | 拜耳药业股份公司 | 含磺亚胺基团的4‑(邻)‑氟苯基‑5‑氟嘧啶‑2‑基胺 |
| HUE032868T2 (en) | 2012-11-15 | 2017-11-28 | Bayer Pharma AG | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group |
| CN105492438B (zh) | 2013-07-04 | 2018-08-07 | 拜耳医药股份有限公司 | 磺亚胺取代的5-氟-n-(吡啶-2-基)吡啶-2-胺衍生物以及其作为cdk9激酶抑制剂的用途 |
| CN106232596A (zh) | 2014-03-13 | 2016-12-14 | 拜耳医药股份有限公司 | 含有砜基团的5‑氟‑n‑(吡啶‑2‑基)吡啶‑2‑胺衍生物 |
-
2015
- 2015-04-08 CU CU2016000152A patent/CU24399B1/es unknown
- 2015-04-08 AP AP2016009483A patent/AP2016009483A0/en unknown
- 2015-04-08 ES ES15715715T patent/ES2743799T3/es active Active
- 2015-04-08 BR BR112016023554-1A patent/BR112016023554B1/pt not_active IP Right Cessation
- 2015-04-08 KR KR1020167031177A patent/KR102383938B1/ko not_active Expired - Fee Related
- 2015-04-08 EP EP15715715.7A patent/EP3129387B1/en active Active
- 2015-04-08 CA CA2945237A patent/CA2945237C/en active Active
- 2015-04-08 TN TN2016000435A patent/TN2016000435A1/en unknown
- 2015-04-08 WO PCT/EP2015/057546 patent/WO2015155197A1/en not_active Ceased
- 2015-04-08 JP JP2016561318A patent/JP6605493B2/ja not_active Expired - Fee Related
- 2015-04-08 PE PE2016001962A patent/PE20161379A1/es unknown
- 2015-04-08 US US15/303,212 patent/US9963464B2/en active Active
- 2015-04-08 AU AU2015243585A patent/AU2015243585B2/en not_active Ceased
- 2015-04-08 EA EA201692034A patent/EA032541B1/ru not_active IP Right Cessation
- 2015-04-08 CR CR20160471A patent/CR20160471A/es unknown
- 2015-04-08 CN CN201580030721.XA patent/CN106459084B/zh not_active Expired - Fee Related
- 2015-04-08 SG SG11201608430RA patent/SG11201608430RA/en unknown
- 2015-04-08 MX MX2016013362A patent/MX376962B/es active IP Right Grant
- 2015-04-09 UY UY0001036072A patent/UY36072A/es not_active Application Discontinuation
- 2015-04-10 TW TW104111701A patent/TW201623312A/zh unknown
- 2015-04-10 AR ARP150101081A patent/AR099999A1/es unknown
- 2015-08-04 UA UAA201611295A patent/UA119349C2/uk unknown
-
2016
- 2016-09-22 IL IL247966A patent/IL247966B/en active IP Right Grant
- 2016-10-04 PH PH12016501968A patent/PH12016501968A1/en unknown
- 2016-10-11 SV SV2016005301A patent/SV2016005301A/es unknown
- 2016-10-11 DO DO2016000278A patent/DOP2016000278A/es unknown
- 2016-10-11 CL CL2016002577A patent/CL2016002577A1/es unknown
- 2016-11-10 ZA ZA2016/07765A patent/ZA201607765B/en unknown
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