CO4940504A1 - THROMBIN INHIBITING COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THE MANUFACTURE OF SUCH COMPOUNDS - Google Patents

THROMBIN INHIBITING COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THE MANUFACTURE OF SUCH COMPOUNDS

Info

Publication number
CO4940504A1
CO4940504A1 CO97029802A CO97029802A CO4940504A1 CO 4940504 A1 CO4940504 A1 CO 4940504A1 CO 97029802 A CO97029802 A CO 97029802A CO 97029802 A CO97029802 A CO 97029802A CO 4940504 A1 CO4940504 A1 CO 4940504A1
Authority
CO
Colombia
Prior art keywords
alkyl
optionally substituted
chain
absent
hydrogen
Prior art date
Application number
CO97029802A
Other languages
Spanish (es)
Inventor
Derek Edward Brundish
Nigel Brown Lyndon
Darren Mark Legrand
Keith Allan Menear
Paul Smith Garrick
Mark Christopher Allen
Paul Ian Butler
Cockroft Xiao-Ling
Ian Timothy Will Matthews
Clive Victor Walker
William Bernard Wathey
Original Assignee
Novartis 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 Novartis Ag filed Critical Novartis Ag
Publication of CO4940504A1 publication Critical patent/CO4940504A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D417/14—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se relaciona con compuestos de lafórmula general Idonde Y es un grupo amino primario o secundario; R2 es el residuo de un aminoácido natural o sintético; R3 es hidrógeno o una cadena alquilo C1-C8 que puede estar sustituida por hidroxi o halógeno; y X es (CH2)n, donde n es 1, 2 ó 3, o bien es CH2N o representa una cadena de fenilo fundida que, de manera opcional se encuentra sustituida por uno o más grupos metoxo o una sal del mismo.Dichas composiciones pueden estar caracterizadas porque Y posee la fórmuladonde A y R se encuentran ausentes o A es un grupo metileno o etileno, y R es hidrógeno, halógeno, azida, COOR8 donde R8 es H o alquilo, donde R9 es H, alquilo, hidroxialquilo opcionalmente sustituido por 2-piranilo, carboxialquilo opcionalmente sustituido por terc.-butilo, amidoalquilo, OCH2CON(CH3)2, OCH2CONH(CH2)2OH o de forma OCH2CO, SO2 alquilo, SO2 arilo o NR10R11 donde R10 y R11 son, de manera independiente H, alquilo que, opcionalmente, se encuentra sustituido por OH, por COOR8 en donde R8 es H o alquilo, por un grupo amida o carbonilo o por un anillo heterocíclico, y/u opcionalmente interrumpido por O, o bien es CH3SO2, o junto con el átomo de nitrógeno forma una cadena cerrada que puede contener otro heteroátomo o R es SR12 donde R12 es hidrógeno o hidroxialquilo; B es CH o se encuentra ausente, siempre que B se encuentre ausente, A y R también se encuentran ausentes; R1 es hidrógeno, alquilo, alquilo opcionalmente sustituido por OH, hidroxilo esterificado, carboxilo, carboxialquilo, fenilo o NR10R11 y/u opcionalmente interrumpido por O, S, carboxilaminocarbonilo, o carbonilamino o es una cadena cerrada de fenilo que contiene uno o más heteroátomos o una cadena cerrada de ciclohexano o bicíclica que contiene uno o más heteroátomos; m es 0, 1, ó 2 y, cuando m es 1 y R 3s H, A puede formar una cadena cerrada de ciclopropano con el átomo C al cual se encuentra adherido R1. ...The present invention relates to compounds of the general formula Idonde Y is a primary or secondary amino group; R2 is the residue of a natural or synthetic amino acid; R3 is hydrogen or a C1-C8 alkyl chain which may be substituted by hydroxy or halogen; and X is (CH2) n, where n is 1, 2 or 3, or is CH2N or represents a fused phenyl chain which is optionally substituted by one or more methoxo groups or a salt thereof. may be characterized in that Y has the formula where A and R are absent or A is a methylene or ethylene group, and R is hydrogen, halogen, azide, COOR8 where R8 is H or alkyl, where R9 is H, alkyl, hydroxyalkyl optionally substituted by 2-pyranyl, carboxyalkyl optionally substituted by tert-butyl, amidoalkyl, OCH2CON (CH3) 2, OCH2CONH (CH2) 2OH or OCH2CO, SO2 alkyl, SO2 aryl or NR10R11 where R10 and R11 are independently H, alkyl which is optionally substituted by OH, by COOR8 where R8 is H or alkyl, by an amide or carbonyl group or by a heterocyclic ring, and / or optionally interrupted by O, or is CH3SO2, or together with the nitrogen atom forms a closed chain that may contain another heteroat as or R is SR12 where R12 is hydrogen or hydroxyalkyl; B is CH or is absent, provided that B is absent, A and R are also absent; R1 is hydrogen, alkyl, alkyl optionally substituted by OH, esterified hydroxyl, carboxyl, carboxyalkyl, phenyl or NR10R11 and / or optionally interrupted by O, S, carboxylaminocarbonyl, or carbonylamino or is a closed phenyl chain containing one or more heteroatoms or a closed cyclohexane or bicyclic chain containing one or more heteroatoms; m is 0, 1, or 2 and, when m is 1 and R 3s H, A can form a closed cyclopropane chain with the C atom to which R1 is attached. ...

CO97029802A 1996-06-01 1997-05-29 THROMBIN INHIBITING COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THE MANUFACTURE OF SUCH COMPOUNDS CO4940504A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9611461.6A GB9611461D0 (en) 1996-06-01 1996-06-01 New compounds

Publications (1)

Publication Number Publication Date
CO4940504A1 true CO4940504A1 (en) 2000-07-24

Family

ID=10794610

Family Applications (1)

Application Number Title Priority Date Filing Date
CO97029802A CO4940504A1 (en) 1996-06-01 1997-05-29 THROMBIN INHIBITING COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THE MANUFACTURE OF SUCH COMPOUNDS

Country Status (8)

Country Link
AR (1) AR008376A1 (en)
AU (1) AU2908197A (en)
CO (1) CO4940504A1 (en)
GB (1) GB9611461D0 (en)
ID (1) ID16990A (en)
PE (1) PE69498A1 (en)
WO (1) WO1997046553A1 (en)
ZA (1) ZA974779B (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040007672A (en) * 2001-06-12 2004-01-24 에스케이 주식회사 Novel Phenylalkyl Diamine and Amide Analogs
WO2003013571A1 (en) * 2001-08-10 2003-02-20 Palatin Technologies, Inc. Peptidomimetics of biologically active metallopeptides
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CA2725140A1 (en) * 2008-05-22 2009-11-26 Boehringer Ingelheim International Gmbh Alpha-substituted n-sulfonyl gylcine amides antagonists of ccr10, compositions containing the same and methods for using them
EP2640367A2 (en) 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
US20140378436A9 (en) 2010-11-24 2014-12-25 Exelixis, Inc. Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture
CN112679448B (en) * 2020-12-31 2022-08-19 苏州昊帆生物股份有限公司 Preparation method of N- (2-aminoethyl) morpholine

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH31294A (en) * 1992-02-13 1998-07-06 Thomae Gmbh Dr K Benzimidazolyl derivatives, pharmaceutical compositions containing these compounds and process for preparing them.
CA2150550A1 (en) * 1992-12-01 1994-06-09 Melissa S. Egbertson Fibrinogen receptor antagonists
FR2727413B1 (en) * 1994-11-25 1996-12-20 Synthelabo DERIVATIVES OF 5- (1H-IMIDAZOL-4-YL) -1-OXO-2- (PHENYLSULFONAMINO) - PENTYLPIPERIDINE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Also Published As

Publication number Publication date
WO1997046553A1 (en) 1997-12-11
ID16990A (en) 1997-11-27
AU2908197A (en) 1998-01-05
AR008376A1 (en) 2000-01-19
ZA974779B (en) 1997-12-01
PE69498A1 (en) 1998-11-27
GB9611461D0 (en) 1996-08-07

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