PE20161379A1 - Nuevos compuestos macrociclicos - Google Patents

Nuevos compuestos macrociclicos

Info

Publication number
PE20161379A1
PE20161379A1 PE2016001962A PE2016001962A PE20161379A1 PE 20161379 A1 PE20161379 A1 PE 20161379A1 PE 2016001962 A PE2016001962 A PE 2016001962A PE 2016001962 A PE2016001962 A PE 2016001962A PE 20161379 A1 PE20161379 A1 PE 20161379A1
Authority
PE
Peru
Prior art keywords
cyclic compounds
compounds
azeno
methene
difluoro
Prior art date
Application number
PE2016001962A
Other languages
English (en)
Inventor
Jiajun Xi
Gang Chen
Ping Gao
Kunzeng Zheng
Ulf Bomer
Ulrich Lucking
Gerhard Siemeister
Philip Lienau
Arne Scholz
Pierre Wasnaire
Christian Stegmann
Original Assignee
Bayer Pharma AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=52824234&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20161379(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20161379A1 publication Critical patent/PE20161379A1/es

Links

Classifications

    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente invencion se refiere a compuestos macrociclicos de formula (I), donde: A es -S-, -S(=O)-, entre otros; L es C2-C6-alquileno opcionalmente sustituido; X e Y son CH o N donde si uno es CH y el otro es N; R1 es C1-C6-alquilo, C3-C6-alquenilo opcionalmente sustituidos, entre otros; R2, R3 y R4 son H, F, entre otros. Son compuestos preferidos: (rac)-16,20-Difluoro-9-[(S-metilsulfonimidoil)metil]-2,3,4,5-tetrahidro-12H-13,17-(azeno)-11 ,7-(meteno)-1,6,12,14-benzodioxadiazaciclononadecino; 15,19-Difluoro-8-[(metilsulfanil)metil]-3,4-dihidro-2H,11H-12,16-(azeno)-10,6-(meteno)-1,5,11,13-benzodioxadiazaciclooctadecino, entre otros. Tambien se refiere a una combinacion, composicion farmaceutica, medicamento y proceso. Dichos compuestos inhiben la enzima quinasa dependiente de ciclina 9 (CDK9) siendo utiles en el tratamiento y/o profilaxis de trastornos hiperproliferativos, enfermedades infecciosas inducidas por virus, entre otros
PE2016001962A 2014-04-11 2015-04-08 Nuevos compuestos macrociclicos PE20161379A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2014000392 2014-04-11

Publications (1)

Publication Number Publication Date
PE20161379A1 true PE20161379A1 (es) 2017-01-15

Family

ID=52824234

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001962A PE20161379A1 (es) 2014-04-11 2015-04-08 Nuevos compuestos macrociclicos

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) MX2016013362A (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)

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CN108290903B (zh) * 2015-09-29 2021-09-03 拜耳医药股份有限公司 新的大环磺酰二亚胺化合物
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
PT3445767T (pt) * 2016-04-22 2020-05-13 Astrazeneca Ab Inibidores de mcl-1 macrocíclicos para o tratamento de cancro
RU2019111887A (ru) * 2016-10-20 2020-11-20 Пфайзер Инк. Антипролиферативные средства для лечения лаг
US11242356B2 (en) 2017-03-28 2022-02-08 Bayer Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
PL3601253T3 (pl) 2017-03-28 2022-01-17 Bayer Aktiengesellschaft Nowe hamujące ptefb związki makrocykliczne
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
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

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ES2556946T3 (es) 2000-12-21 2016-01-21 Novartis Ag Pirimidinaminas como moduladores de la angiogénesis
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
KR20070091018A (ko) 2004-12-17 2007-09-06 아스트라제네카 아베 Ｃｄｋ 억제제로서의4-(4-(이미다졸-4-일)피리미딘-2-일아미노)벤즈아미드
DE102006042143A1 (de) 2006-09-08 2008-03-27 Bayer Healthcare Aktiengesellschaft Neue substituierte Bipyridin-Derivate und ihre Verwendung
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CN105102434A (zh) 2012-10-18 2015-11-25 拜耳药业股份公司 含砜基团的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
LT2928878T (lt) 2012-11-15 2016-11-25 Bayer Pharma Aktiengesellschaft 5-fluor-n-(piridin-2-il)piridin-2-amino dariniai, turintys sulfoksimino grupę
WO2015001021A1 (en) 2013-07-04 2015-01-08 Bayer Pharma Aktiengesellschaft Sulfoximine substituted 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives and their use as cdk9 kinase inhibitors
US9856242B2 (en) 2014-03-13 2018-01-02 Bayer Pharma Aktiengesellscaft 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group

Also Published As

Publication number Publication date
EP3129387B1 (en) 2019-06-26
UA119349C2 (uk) 2019-06-10
AU2015243585B2 (en) 2019-08-01
CR20160471A (es) 2016-12-21
CU20160152A7 (es) 2017-04-05
CA2945237C (en) 2022-09-06
KR20160136449A (ko) 2016-11-29
UY36072A (es) 2015-11-30
CA2945237A1 (en) 2015-10-15
WO2015155197A1 (en) 2015-10-15
ZA201607765B (en) 2022-09-28
MX2016013362A (es) 2017-02-09
CL2016002577A1 (es) 2017-04-07
CN106459084A (zh) 2017-02-22
JP2017510598A (ja) 2017-04-13
EA032541B1 (ru) 2019-06-28
AU2015243585A1 (en) 2016-10-13
AR099999A1 (es) 2016-08-31
CU24399B1 (es) 2019-04-04
SG11201608430RA (en) 2016-11-29
BR112016023554A2 (pt) 2017-08-15
PH12016501968A1 (en) 2016-12-19
KR102383938B1 (ko) 2022-04-08
TW201623312A (zh) 2016-07-01
ES2743799T3 (es) 2020-02-20
BR112016023554B1 (pt) 2023-03-14
US9963464B2 (en) 2018-05-08
TN2016000435A1 (en) 2018-04-04
US20170029439A1 (en) 2017-02-02
IL247966B (en) 2021-02-28
JP6605493B2 (ja) 2019-11-13
AP2016009483A0 (en) 2016-10-31
DOP2016000278A (es) 2016-11-15
SV2016005301A (es) 2018-03-12
EA201692034A1 (ru) 2017-04-28
CN106459084B (zh) 2019-04-19
EP3129387A1 (en) 2017-02-15
IL247966A0 (en) 2016-11-30

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