AR058205A1 - 5-fenil-3,6-dihidro-2-oxo-6h-[1,3,4] tiadiazinas sustituidas - Google Patents

5-fenil-3,6-dihidro-2-oxo-6h-[1,3,4] tiadiazinas sustituidas

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Publication number
AR058205A1
AR058205A1 ARP060105082A ARP060105082A AR058205A1 AR 058205 A1 AR058205 A1 AR 058205A1 AR P060105082 A ARP060105082 A AR P060105082A AR P060105082 A ARP060105082 A AR P060105082A AR 058205 A1 AR058205 A1 AR 058205A1
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AR
Argentina
Prior art keywords
hal
naso2a
so2naa
so2nha
nacoa
Prior art date
Application number
ARP060105082A
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English (en)
Inventor
Dieter Dorsch
Melanie Schultz
Andree Blaukat
Oliver Schadt
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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 AR058205A1 publication Critical patent/AR058205A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
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    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P35/00Antineoplastic agents
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/081,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/15Six-membered rings
    • C07D285/16Thiadiazines; Hydrogenated thiadiazines
    • C07D285/181,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
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  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
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  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
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  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos de la formula (1) en donde R1 es H, A, Hal, OH, OA, SH, SA, SOA, SO2A, NO2, NH2, NHA, NAA', SO2NH2, SO2NHA, SO2NAA', CONH2, CONHA, CONAA', NACOA', NASO2A', COOH, COOA o CN; R2 es H, A, Hal, SO2NH2, SO2NHA, SO2NAA', CONH2, CONHA, CONAA', NACOA', NASO2A', COOH, COOA o CN; R1 y R2 también son juntos metilendioxi; B es NHCOO(CH2)nR3 o NHCO(CH2)nR3; Q está ausente o es alquileno lineal o ramificado C1-4; R3 es R1, Het o alquilo no sustituido o mono-, di-, tri- o tetrasustituido con R4 con 1-6 átomos de C o cicloalquilo C3-8; R4 es A, Hal, OH, OA, SH, SA, SOA, SO2A, NO2, NH2, NHA, NAA', SO2NH2, SO2NHA, SO2NAA', CONH2, CONHA, CONAA', NACOA', NASO2A', COOH, COOA o CN; Het es un heterociclo saturado o aromático mono- o bicíclico con 1 a 4 átomos de N, O y/o , que no está sustituido o que puede estar mono-, di- o trisustituido con R4, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo); A, A' son cada uno, de modo independiente entre sí, alquilo no ramificado o ramificado C1-1, en donde 1-7 átomos de H pueden estar reemplazados por F, Cl, y/o Br; cicloalquilo C3-8 o cicloalquilalquileno C4-10; Hal es F, Cl, Br o I; m es 0 o 1; n es 0, 1, 2, o 3; así como sus derivados, solvatos, sales, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la Met-quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
ARP060105082A 2005-11-21 2006-11-21 5-fenil-3,6-dihidro-2-oxo-6h-[1,3,4] tiadiazinas sustituidas AR058205A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005055354A DE102005055354A1 (de) 2005-11-21 2005-11-21 Substituierte 5-Phenyl-3,6-dihydro-2-oxo-6H-[1,3,4]thiadiazine

Publications (1)

Publication Number Publication Date
AR058205A1 true AR058205A1 (es) 2008-01-23

Family

ID=37734761

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060105082A AR058205A1 (es) 2005-11-21 2006-11-21 5-fenil-3,6-dihidro-2-oxo-6h-[1,3,4] tiadiazinas sustituidas

Country Status (21)

Country Link
US (1) US7902186B2 (es)
EP (1) EP1951697B1 (es)
JP (1) JP5334586B2 (es)
KR (1) KR101424825B1 (es)
CN (1) CN101312956A (es)
AR (1) AR058205A1 (es)
AT (1) ATE517878T1 (es)
AU (1) AU2006314873B2 (es)
BR (1) BRPI0618806A2 (es)
CA (1) CA2630202C (es)
CY (1) CY1112031T1 (es)
DE (1) DE102005055354A1 (es)
DK (1) DK1951697T3 (es)
EA (1) EA015352B1 (es)
ES (1) ES2368001T3 (es)
IL (1) IL191360A (es)
PL (1) PL1951697T3 (es)
PT (1) PT1951697E (es)
SI (1) SI1951697T1 (es)
WO (1) WO2007057092A1 (es)
ZA (1) ZA200805406B (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005055355A1 (de) * 2005-11-21 2007-10-31 Merck Patent Gmbh 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate
DE102007025718A1 (de) * 2007-06-01 2008-12-04 Merck Patent Gmbh Pyridazinonderivate
DE102007026341A1 (de) * 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007041115A1 (de) * 2007-08-30 2009-03-05 Merck Patent Gmbh Thiadiazinonderivate
DE102007061963A1 (de) * 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
DE102008062826A1 (de) 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
DE102009003975A1 (de) * 2009-01-07 2010-07-08 Merck Patent Gmbh Benzothiazolonderivate
RU2458060C2 (ru) * 2009-05-22 2012-08-10 Государственное образовательное учреждение высшего профессионального образования "Уральский государственный технический университет - УПИ имени первого Президента России Б.Н. Ельцина" 5-(4'-гидроксифенил)- и 5-(2',5'-дигидроксифенил)-6н-1,3,4-тиадиазин-2-амины, гидрогалагениды, ингибирующие агрегацию тромбоцитов при внутривенном введении
CN111454232B (zh) * 2020-05-30 2021-11-23 南方医科大学 一种1,3,4-噻二嗪类化合物及其应用
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19502699A1 (de) * 1995-01-28 1996-08-01 Merck Patent Gmbh Arylalkyl-thiadiazinone
DE19533975A1 (de) * 1995-09-14 1997-03-20 Merck Patent Gmbh Arylalkyl-diazinone
GB9525262D0 (en) * 1995-12-11 1996-02-07 Bayer Ag Heterocyclylcarbonyl substituted benzofuranyl-ureas
DE19604388A1 (de) * 1996-02-07 1997-08-14 Merck Patent Gmbh Arylalkyl-diazinone
CA2382789A1 (en) 1999-08-27 2001-03-08 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
DE10150517A1 (de) * 2001-10-12 2003-04-17 Merck Patent Gmbh Verwendung von Phosphodiesterase IV-Inhibitoren
SK1862004A3 (en) 2001-10-31 2004-08-03 Type 4 phosphodiesterase inhibitors and uses thereof
KR100915287B1 (ko) * 2001-12-11 2009-09-03 교와 핫꼬 기린 가부시키가이샤 티아디아졸린 유도체
DE102005055355A1 (de) * 2005-11-21 2007-10-31 Merck Patent Gmbh 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate

Also Published As

Publication number Publication date
DK1951697T3 (da) 2011-09-26
KR101424825B1 (ko) 2014-08-01
EA200801365A1 (ru) 2008-10-30
US7902186B2 (en) 2011-03-08
ATE517878T1 (de) 2011-08-15
EP1951697B1 (de) 2011-07-27
CA2630202C (en) 2015-03-31
SI1951697T1 (sl) 2011-09-30
ZA200805406B (en) 2009-11-25
PT1951697E (pt) 2011-11-04
AU2006314873B2 (en) 2011-12-08
DE102005055354A1 (de) 2007-10-31
CN101312956A (zh) 2008-11-26
JP2009516657A (ja) 2009-04-23
IL191360A (en) 2013-10-31
WO2007057092A1 (de) 2007-05-24
US20080318936A1 (en) 2008-12-25
EA015352B1 (ru) 2011-06-30
KR20080070763A (ko) 2008-07-30
CY1112031T1 (el) 2015-11-04
BRPI0618806A2 (pt) 2011-09-13
ES2368001T3 (es) 2011-11-11
JP5334586B2 (ja) 2013-11-06
EP1951697A1 (de) 2008-08-06
AU2006314873A1 (en) 2007-05-24
PL1951697T3 (pl) 2011-11-30
CA2630202A1 (en) 2007-05-24

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