AR055376A1 - Derivados de 1-acildihidropirazol - Google Patents

Derivados de 1-acildihidropirazol

Info

Publication number
AR055376A1
AR055376A1 ARP060103562A ARP060103562A AR055376A1 AR 055376 A1 AR055376 A1 AR 055376A1 AR P060103562 A ARP060103562 A AR P060103562A AR P060103562 A ARP060103562 A AR P060103562A AR 055376 A1 AR055376 A1 AR 055376A1
Authority
AR
Argentina
Prior art keywords
mono
phet1
het1
nhcoo
het
Prior art date
Application number
ARP060103562A
Other languages
English (en)
Inventor
Dieter Dorsch
Oliver Schadt
Andree Blaukat
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR055376A1 publication Critical patent/AR055376A1/es

Links

Classifications

    • 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
    • C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07D417/14—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

Abstract

Los compuestos de la formula (1), en donde: R1 es Ar o Het, R2 es -[C(R4)2]n-Ar o -[C(R4)2]n-Het, R3, R3a, R3b, R3c, R3d son en cada caso, de modo independiente entre sí, H o A; R4 es H, A u OR3; A es alquilo no ramificado o ramificado con C1-10, en donde 1-7 átomos de H pueden estar reemplazados por F, Cl y/o Br; y/o en donde uno o dos grupos CH2 pueden estar reemplazados por O, S, SO, SO2 y/o CH=CH; o alquilo cíclico con C3-7; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA, CO-Het1, Het1, O[C(R3)2]pN(R3), O[C(R3)2]pHet1, NHCONH[C(R3)2]pN(R3), NHCOO[C(R3)2]pN(R3), NHCOO[C(R3)2]pHet1, CHO y/o COA; Het es un heterociclo saturado, insaturado, o aromático mono-, bi- o tricíclico con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, O[C(R3)2]pN(R3), O[C(R3)2]pHet1, NHCONH[C(R3)2]pN(R3), NHCOO[C(R3)2]pN(R3), NR3COA, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo) Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, HaI y/o =O (oxígeno del carbonilo); HaI es F, Cl, Br o I; m es 0, 1 o 2; n es 1 o 2, p es 1, 2, 3 o 4; así como sus derivados, solvatos, sales, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones; en donde se excluyen los compuestos: 1-bencilcarbonil-3-fenil-4,5-dihidro-1H-pirazol y 1-bencilcarbonil-3-(4-cloro-fenil)-4,5-dihidro-1H-pirazol. Son inhibidores de las tirosina quinasas, en especial de la Met- quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
ARP060103562A 2005-08-16 2006-08-16 Derivados de 1-acildihidropirazol AR055376A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005038537A DE102005038537A1 (de) 2005-08-16 2005-08-16 1-Acyldihydropyrazolderivate

Publications (1)

Publication Number Publication Date
AR055376A1 true AR055376A1 (es) 2007-08-22

Family

ID=37308912

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060103562A AR055376A1 (es) 2005-08-16 2006-08-16 Derivados de 1-acildihidropirazol

Country Status (14)

Country Link
US (1) US7875644B2 (es)
EP (1) EP1917248B1 (es)
JP (1) JP5174665B2 (es)
KR (1) KR20080039992A (es)
CN (1) CN101243048A (es)
AR (1) AR055376A1 (es)
AU (1) AU2006281700B2 (es)
BR (1) BRPI0616999A2 (es)
CA (1) CA2619039C (es)
DE (1) DE102005038537A1 (es)
ES (1) ES2548517T3 (es)
MX (1) MX2008002104A (es)
WO (1) WO2007019933A1 (es)
ZA (1) ZA200802421B (es)

Families Citing this family (17)

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Publication number Priority date Publication date Assignee Title
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
US20100105729A1 (en) * 2006-10-06 2010-04-29 Kalypsys, Inc. Aryl-substituted heterocyclic pde4 inhibitors as anti-inflammatory agents
US8283351B2 (en) * 2007-04-02 2012-10-09 Institute For Oneworld Health Cyclic and acyclic hydrazine derivatives compositions including them and uses thereof
WO2008137408A1 (en) 2007-04-30 2008-11-13 Genentech, Inc. Pyrazole inhibitors of wnt signaling
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102008025750A1 (de) * 2008-05-29 2009-12-03 Merck Patent Gmbh Dihydropyrazolderivate
DE102009003975A1 (de) 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
WO2011055561A1 (ja) * 2009-11-06 2011-05-12 独立行政法人科学技術振興機構 蛋白質架橋阻害剤およびその用途
JP5246715B2 (ja) * 2009-01-27 2013-07-24 独立行政法人科学技術振興機構 蛋白質架橋阻害剤およびその用途
US8791114B2 (en) * 2011-07-01 2014-07-29 Merck Patent Gmbh Dihydropyrazoles
CN102391272B (zh) * 2011-09-30 2014-07-02 浙江工业大学 1,4-二取代基-1,4-二氢苯并吡喃[4,3-c]吡唑类化合物
AU2013243737B2 (en) 2012-04-03 2016-06-30 Novartis Ag Tyrosine kinase inhibitor combinations and their use
WO2013149581A1 (en) 2012-04-03 2013-10-10 Novartis Ag Combination products with tyrosine kinase inhibitors and their use
WO2014174478A1 (en) 2013-04-26 2014-10-30 Novartis Ag Pharmaceutical combinations of a pkc inhibitor and a c-met receptor tyrosine kinase inhibitor
CN103265535B (zh) * 2013-05-14 2015-06-17 浙江医药高等专科学校 抗肿瘤化合物、其制备方法和用途
CN106749192B (zh) * 2017-01-16 2019-05-17 南京医科大学 一种烟酰二氢吡唑类化合物及其药物用途
CN109912574A (zh) * 2019-05-06 2019-06-21 合肥工业大学 一种二氢吡唑类化合物及其制备方法和用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH05112555A (ja) * 1991-10-18 1993-05-07 Nippon Bayeragrochem Kk 選択的殺虫性ピラゾリン類
WO2001032173A1 (fr) * 1999-10-29 2001-05-10 Yamanouchi Pharmaceutical Co., Ltd. Inhibiteurs de neurocytotoxicite de l'acide kainique
AU2003249597B2 (en) * 2002-03-08 2007-06-28 Merck Sharp & Dohme Corp. Mitotic kinesin inhibitors

Also Published As

Publication number Publication date
JP5174665B2 (ja) 2013-04-03
ES2548517T3 (es) 2015-10-19
EP1917248B1 (de) 2015-08-19
DE102005038537A1 (de) 2007-02-22
CA2619039A1 (en) 2007-02-22
EP1917248A1 (de) 2008-05-07
WO2007019933A1 (de) 2007-02-22
AU2006281700B2 (en) 2012-01-19
BRPI0616999A2 (pt) 2011-07-05
AU2006281700A1 (en) 2007-02-22
CN101243048A (zh) 2008-08-13
MX2008002104A (es) 2008-04-17
CA2619039C (en) 2014-03-18
US7875644B2 (en) 2011-01-25
ZA200802421B (en) 2009-01-28
KR20080039992A (ko) 2008-05-07
JP2009504694A (ja) 2009-02-05
US20080249095A1 (en) 2008-10-09

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