CU20160152A7 - 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
- CU20160152A7 CU20160152A7 CUP2016000152A CU20160152A CU20160152A7 CU 20160152 A7 CU20160152 A7 CU 20160152A7 CU P2016000152 A CUP2016000152 A CU P2016000152A CU 20160152 A CU20160152 A CU 20160152A CU 20160152 A7 CU20160152 A7 CU 20160152A7
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Hematology (AREA)
- Cardiology (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
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).
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 true CU20160152A7 (es) | 2017-04-05 |
| CU24399B1 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 |
|---|---|---|---|---|
| EP3356373B1 (en) * | 2015-09-29 | 2020-02-19 | Bayer Pharma Aktiengesellschaft | Novel macrocyclic sulfondiimine compounds |
| CN108368129B (zh) * | 2015-10-08 | 2021-08-17 | 拜耳医药股份有限公司 | 改性大环化合物 |
| JP6894449B2 (ja) * | 2016-04-22 | 2021-06-30 | アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ | 癌を治療するためのマクロ環状ｍｃｌ１阻害剤 |
| EP3804724B1 (en) * | 2016-10-20 | 2022-12-07 | Pfizer Inc. | Cdk inhibitors for treating pah |
| WO2018177889A1 (en) | 2017-03-28 | 2018-10-04 | 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 |
| MX2023003690A (es) | 2020-09-30 | 2023-06-15 | Asahi Kasei Pharma Corp | Compuesto macrociclico. |
| EP4412655A1 (en) | 2021-10-04 | 2024-08-14 | 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 |
|---|---|---|---|---|
| ATE430742T1 (de) | 2000-12-21 | 2009-05-15 | Smithkline Beecham Corp | Pyrimidinamine als angiogenesemodulatoren |
| 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 |
| US20090099160A1 (en) | 2004-12-17 | 2009-04-16 | David Andrews | 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 |
| 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 |
| WO2008079918A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Indol-4-yl-pyrimidinyl-2-yl-amine derivatives and use thereof as cyclin dependant kinase inhibitors |
| WO2008129070A1 (en) | 2007-04-24 | 2008-10-30 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| WO2008129071A1 (en) | 2007-04-24 | 2008-10-30 | Ingenium Pharmaceuticals Gmbh | Inhibitors of protein kinases |
| US8507498B2 (en) | 2007-04-24 | 2013-08-13 | Ingenium Pharmaceuticals Gmbh | 4, 6-disubstituted aminopyrimidine derivatives as inhibitors of protein kinases |
| 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 |
| CN102933561B (zh) | 2010-03-22 | 2016-05-11 | 利德发现中心有限责任公司 | 具有药学活性的二取代三嗪衍生物 |
| JP5947818B2 (ja) | 2011-03-02 | 2016-07-06 | リード ディスカバリー センター ゲーエムベーハー | 薬学的活性化二置換ピリジン誘導体 |
| 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 |
| EP2755956B1 (en) * | 2011-09-16 | 2016-05-18 | Bayer Intellectual Property GmbH | 2,4-disubstituted 5-fluoro-pyrimidines as selective cdk9 inhibtors |
| JP5976814B2 (ja) | 2011-09-16 | 2016-08-24 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | スルホキシイミン基を含有する二置換５−フルオロピリミジン誘導体 |
| CA2888381A1 (en) | 2012-10-18 | 2014-04-24 | Bayer Pharma Aktiengesellschaft | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group |
| CA2891244C (en) | 2012-11-15 | 2020-12-01 | Ulrich Lucking | 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfoximine group |
| SG11201503079PA (en) | 2012-11-15 | 2015-06-29 | Bayer Pharma AG | 5-FLUORO-<i>N</i>-(PYRIDIN-2-YL)PYRIDIN-2-AMINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP |
| CA2917096C (en) | 2013-07-04 | 2021-05-18 | Bayer Pharma Aktiengesellschaft | Sulfoximine substituted 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives and their use as cdk9 kinase inhibitors |
| CA2942119A1 (en) | 2014-03-13 | 2015-09-17 | Bayer Pharma Aktiengesellschaft | 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group |
-
2015
- 2015-04-08 CN CN201580030721.XA patent/CN106459084B/zh not_active Expired - Fee Related
- 2015-04-08 TN TN2016000435A patent/TN2016000435A1/en unknown
- 2015-04-08 SG SG11201608430RA patent/SG11201608430RA/en unknown
- 2015-04-08 KR KR1020167031177A patent/KR102383938B1/ko not_active Expired - Fee Related
- 2015-04-08 JP JP2016561318A patent/JP6605493B2/ja not_active Expired - Fee Related
- 2015-04-08 CR CR20160471A patent/CR20160471A/es unknown
- 2015-04-08 US US15/303,212 patent/US9963464B2/en active Active
- 2015-04-08 BR BR112016023554-1A patent/BR112016023554B1/pt not_active IP Right Cessation
- 2015-04-08 EP EP15715715.7A patent/EP3129387B1/en active Active
- 2015-04-08 WO PCT/EP2015/057546 patent/WO2015155197A1/en not_active Ceased
- 2015-04-08 CA CA2945237A patent/CA2945237C/en active Active
- 2015-04-08 EA EA201692034A patent/EA032541B1/ru not_active IP Right Cessation
- 2015-04-08 CU CU2016000152A patent/CU24399B1/es unknown
- 2015-04-08 ES ES15715715T patent/ES2743799T3/es active Active
- 2015-04-08 MX MX2016013362A patent/MX376962B/es active IP Right Grant
- 2015-04-08 AP AP2016009483A patent/AP2016009483A0/en unknown
- 2015-04-08 AU AU2015243585A patent/AU2015243585B2/en not_active Ceased
- 2015-04-08 PE PE2016001962A patent/PE20161379A1/es unknown
- 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 CL CL2016002577A patent/CL2016002577A1/es unknown
- 2016-10-11 SV SV2016005301A patent/SV2016005301A/es unknown
- 2016-10-11 DO DO2016000278A patent/DOP2016000278A/es unknown
- 2016-11-10 ZA ZA2016/07765A patent/ZA201607765B/en unknown
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