PE20170186A1 - Nuevos compuestos - Google Patents

Nuevos compuestos

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Publication number
PE20170186A1
PE20170186A1 PE2016001654A PE2016001654A PE20170186A1 PE 20170186 A1 PE20170186 A1 PE 20170186A1 PE 2016001654 A PE2016001654 A PE 2016001654A PE 2016001654 A PE2016001654 A PE 2016001654A PE 20170186 A1 PE20170186 A1 PE 20170186A1
Authority
PE
Peru
Prior art keywords
benzamide
alkyl
compounds
trifluorometoxy
morfolin
Prior art date
Application number
PE2016001654A
Other languages
English (en)
Inventor
Daniel Basting
Ludwig Zorn
Jens Geisler
Anja Giese
Stefan Golz
Andrea Hagebarth
Philip Lienau
Ningshu Liu
Ursula Monning
Manfred Mowes
Florian Puehler
Dirk Schneider
William J Scott
Franziska Siegel
Kai Thede
Eckhard Bender
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
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20170186A1 publication Critical patent/PE20170186A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE BENZAMIDA DE FORMULA (I) DONDE LA ES METILENO O ETILENO OPCIONALMENTE SUSTITUIDO; LB ES *N(H)-C(=O)** O *C(=O)-N(H)** DONDE "*" Y "**" INDICAN EL PUNTO DE UNION CON R2 Y FENILO, RESPECTIVAMENTE; R1 ES HETEROCICLOALQUILO DE 5 A 8 MIEMBROS, HETEROCICLOALQUENILO DE 4 A 10 MIEMBROS, ENTRE OTROS; R2 ES PIRIDINA, PIRAZINA, ENTRE OTROS; R3 ES PIRIDINA, PIRIMIDINA, TIOFENO, ENTRE OTROS; R4 ES H O ALQUILO C1-C3; R5 ES H, HALOGENO, CN, ENTRE OTROS; R6 ES ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 3-[(MORFOLIN-4-ILACETIL)AMINO]-N-[5-(PIRIMIDIN-5-IL)PIRIDIN-2-IL]-4-(TRIFLUOROMETOXI)BENZAMIDA; 3-({[1-(MORFOLIN-4-IL)CICLOPROPIL]CARBONIL}AMINO)-N-[5-(PIRIDIN-3-IL)-1,3,4-TIADIAZOL-2-IL]-4-(TRIFLUOROMETOXI)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LAS VIAS DE SENALIZACION DE LAS PROTEINAS WNT SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS HIPERPROLIFERATIVOS TAL COMO EL CANCER
PE2016001654A 2014-03-20 2015-03-18 Nuevos compuestos PE20170186A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461968172P 2014-03-20 2014-03-20
EP14185274 2014-09-18

Publications (1)

Publication Number Publication Date
PE20170186A1 true PE20170186A1 (es) 2017-04-01

Family

ID=51564537

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001654A PE20170186A1 (es) 2014-03-20 2015-03-18 Nuevos compuestos

Country Status (18)

Country Link
US (1) US20170107212A1 (es)
EP (1) EP3119759A1 (es)
JP (1) JP2017509650A (es)
KR (1) KR20160127138A (es)
CN (1) CN106458983A (es)
AP (1) AP2016009432A0 (es)
AU (1) AU2015233558A1 (es)
BR (1) BR112016021648A2 (es)
CA (1) CA2943002A1 (es)
CR (1) CR20160433A (es)
CU (1) CU20160138A7 (es)
DO (1) DOP2016000253A (es)
EA (1) EA201691881A1 (es)
MX (1) MX2016012175A (es)
PE (1) PE20170186A1 (es)
PH (1) PH12016501807A1 (es)
SG (1) SG11201606693SA (es)
WO (1) WO2015140195A1 (es)

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AP2016009433A0 (en) * 2014-03-20 2016-09-30 Bayer Pharma AG Inhibitors of the wnt signalling pathways
CA2942687A1 (en) 2014-03-20 2015-09-24 Samumed, Llc 5-substituted indazole-3-carboxamides and preparation and use thereof
SI3303330T1 (sl) 2015-06-03 2019-08-30 Bristol-Myers Squibb Company Agonisti 4-hidroksi-3-(heteroaril)piridin-2-on apj za uporabo pri zdravljenju kardiovaskularnih motenj
WO2017097215A1 (zh) * 2015-12-07 2017-06-15 杭州雷索药业有限公司 内嵌脲类结构的wnt通路抑制剂
US11542254B2 (en) 2016-03-25 2023-01-03 Universisity Of Utah Research Foundation Methods and composition of 4-substituted benzoylpiperazine-1-substituted carbonyls as beta-catenin/B-cell lymphoma 9 inhibitors
WO2017167150A1 (zh) * 2016-03-31 2017-10-05 苏州云轩医药科技有限公司 一种3-氟吡啶杂环化合物及其应用
CN115583938A (zh) * 2021-07-05 2023-01-10 南通聚太生物科技有限公司 靶向BCL9/β-连环蛋白互相作用的小分子化合物
KR20230066213A (ko) 2021-11-06 2023-05-15 윤보라 무선 이어폰 보안 시스템
TW202334157A (zh) * 2022-01-29 2023-09-01 大陸商杭州阿諾生物醫藥科技有限公司 一種Ｗｎｔ通路抑制劑化合物
WO2024022365A1 (zh) * 2022-07-28 2024-02-01 杭州阿诺生物医药科技有限公司 一种Wnt通路抑制剂化合物
WO2024022521A1 (zh) * 2022-07-28 2024-02-01 南通环聚泰生物科技有限公司 靶向BCL9/β-连环蛋白互相作用的小分子化合物
CN115850202B (zh) * 2022-12-26 2024-06-25 上海科技大学 一种卷曲受体7的小分子抑制剂及其制备方法和应用

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EA201691881A1 (ru) 2017-12-29
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EP3119759A1 (en) 2017-01-25
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MX2016012175A (es) 2017-01-19
AP2016009432A0 (en) 2016-09-30
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