PE20170920A1 - Piperidinilpirazolopirimidinonas y utilizacion de las mismas - Google Patents

Piperidinilpirazolopirimidinonas y utilizacion de las mismas

Info

Publication number
PE20170920A1
PE20170920A1 PE2017000789A PE2017000789A PE20170920A1 PE 20170920 A1 PE20170920 A1 PE 20170920A1 PE 2017000789 A PE2017000789 A PE 2017000789A PE 2017000789 A PE2017000789 A PE 2017000789A PE 20170920 A1 PE20170920 A1 PE 20170920A1
Authority
PE
Peru
Prior art keywords
hydrogen
piperidinylpyrazolopyrimidinones
alkyl
refers
inherited
Prior art date
Application number
PE2017000789A
Other languages
English (en)
Inventor
Manuel Ellermann
Gaelle Valot
Grande Yolanda Cancho
Jorma Hassfeld
Tom Kinzel
Johannes Kobberling
Kristin Beyer
Susanne Rohrig
Michael Sperzel
Jan Stampfuss
Imke Meyer
Maria Kollnberger
Nils Burkhardt
Karl-Heinz Schlemmer
Christian Stegmann
Joachim Schuhmacher
Matthias Werner
Jorg Heiermann
Willem Jan Hengeveld
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 PE20170920A1 publication Critical patent/PE20170920A1/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
    • A61K31/495—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
    • A61K31/535—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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D247/00—Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups C07D229/00 - C07D245/00
    • C07D247/02—Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups C07D229/00 - C07D245/00 having the nitrogen atoms in positions 1 and 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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

Abstract

Se refiere a un compuesto de formula (I-A) o (I-B), donde: R1 es hidrogeno o alquilo C1-C5; R2 es hidrogeno, alquilo C1-C4, entre otros; R3 es hidrogeno, halogeno, entre otros. Tambien se refiere a un procedimiento para su preparacion. Dichos compuestos son piperidinilpirazolopirimidinonas sustituidas utiles en el tratamiento de sangrado agudo y recurrente en pacientes con o sin trastornos hemostaticos hereditarios o adquiridos
PE2017000789A 2014-11-03 2015-10-30 Piperidinilpirazolopirimidinonas y utilizacion de las mismas PE20170920A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14191410 2014-11-03
EP15165918 2015-04-30

Publications (1)

Publication Number Publication Date
PE20170920A1 true PE20170920A1 (es) 2017-07-12

Family

ID=54365247

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017000789A PE20170920A1 (es) 2014-11-03 2015-10-30 Piperidinilpirazolopirimidinonas y utilizacion de las mismas

Country Status (17)

Country Link
US (1) US10118930B2 (es)
EP (1) EP3215505B1 (es)
JP (1) JP2017533235A (es)
KR (1) KR20170080647A (es)
CN (1) CN107108638A (es)
AU (1) AU2015342021B2 (es)
BR (1) BR112017009207A2 (es)
CA (1) CA2966259A1 (es)
HK (1) HK1243077A1 (es)
IL (1) IL251335A0 (es)
MX (1) MX2017005586A (es)
PE (1) PE20170920A1 (es)
RU (1) RU2713937C2 (es)
SG (1) SG11201703201PA (es)
TW (1) TW201627308A (es)
UY (1) UY36385A (es)
WO (1) WO2016071216A1 (es)

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* Cited by examiner, † Cited by third party
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CN114874209A (zh) * 2017-03-07 2022-08-09 豪夫迈·罗氏有限公司 噁二唑瞬时受体电位通道抑制剂
WO2018224455A1 (en) 2017-06-07 2018-12-13 Basf Se Substituted cyclopropyl derivatives
US11654057B2 (en) 2020-04-09 2023-05-23 Bio 54, Llc Devices for bleeding reduction and methods of making and using the same
US20240124443A1 (en) * 2021-02-05 2024-04-18 Scinnohub Pharmaceutical Co., Ltd Plasmin inhibitor, preparation method therefor, and application thereof
US11642324B1 (en) 2022-03-01 2023-05-09 Bio 54, Llc Topical tranexamic acid compositions and methods of use thereof

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RO121272B1 (ro) 1996-07-24 2007-02-28 The Du Pont Merck Pharmaceutical Company Azolotriazine şi pirimidine
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2527136A1 (en) * 2003-06-03 2004-12-09 Basf Aktiengesellschaft Substituted pyrazolopyrimidines, methods for the production thereof, use of the same for controlling pathogenic fungi, and agents containing said compounds
WO2006023000A1 (en) 2004-07-30 2006-03-02 Xanodyne Pharmaceuticals, Inc. Tranexamic acid formulations
RU2390523C2 (ru) * 2005-10-21 2010-05-27 Мицубиси Танабе Фарма Корпорейшн ПРОИЗВОДНОЕ ПИРАЗОЛ[1,5-a]ПИРИМИДИНА
EP1873157A1 (en) * 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
BRPI0713187A2 (pt) 2006-07-20 2012-10-16 Mehmet Kahraman método de inibir rho-quinase, método de tratamento de doença mediada por rho-quinase, composto e composição farmacêutica
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
AU2008287421A1 (en) 2007-08-10 2009-02-19 Glaxosmithkline Llc Nitrogen containing bicyclic chemical entities for treating viral infections
CA2706946A1 (en) 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
EA020825B1 (ru) 2009-04-07 2015-02-27 Эмерити Фарма Аб Аналоги изоксазол-3(2h)-она в качестве терапевтических агентов
WO2011140333A1 (en) 2010-05-07 2011-11-10 The Board Of Trustees Of The Leland Stanford Junior University Identification of stabilizers of multimeric proteins
WO2012047156A1 (en) * 2010-10-04 2012-04-12 Astrazeneca Ab Isoxazol-3(2h)-one analogs as plasminogen inhibitors and their use in the treatment of fibrinolysis related diseases
DK2649075T3 (en) 2010-12-08 2018-07-30 Us Health SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS
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CA2902686C (en) * 2013-04-25 2017-01-24 Beigene, Ltd. Fused heterocyclic compounds as protein kinase inhibitors
UY35809A (es) * 2013-11-05 2015-05-29 Bayer Pharma AG (aza)piridopirazolopirimidinonas e indazolopirimidinonas y sus usos

Also Published As

Publication number Publication date
RU2713937C2 (ru) 2020-02-11
AU2015342021B2 (en) 2020-02-27
WO2016071216A1 (en) 2016-05-12
UY36385A (es) 2016-06-01
EP3215505A1 (en) 2017-09-13
CN107108638A (zh) 2017-08-29
KR20170080647A (ko) 2017-07-10
TW201627308A (zh) 2016-08-01
AU2015342021A1 (en) 2017-05-04
RU2017119419A (ru) 2018-12-05
HK1243077A1 (zh) 2018-07-06
CA2966259A1 (en) 2016-05-12
US20170334917A1 (en) 2017-11-23
SG11201703201PA (en) 2017-05-30
JP2017533235A (ja) 2017-11-09
BR112017009207A2 (pt) 2019-10-01
IL251335A0 (en) 2017-05-29
EP3215505B1 (en) 2019-07-24
US10118930B2 (en) 2018-11-06
MX2017005586A (es) 2017-06-19
RU2017119419A3 (es) 2019-06-10

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