HUP9801883A2 - Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds - Google Patents

Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds

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Publication number
HUP9801883A2
HUP9801883A2 HU9801883A HUP9801883A HUP9801883A2 HU P9801883 A2 HUP9801883 A2 HU P9801883A2 HU 9801883 A HU9801883 A HU 9801883A HU P9801883 A HUP9801883 A HU P9801883A HU P9801883 A2 HUP9801883 A2 HU P9801883A2
Authority
HU
Hungary
Prior art keywords
aryl
alkyl
alkenyl
pipe
alkynyl
Prior art date
Application number
HU9801883A
Other languages
Hungarian (hu)
Inventor
Neville J. Anthony
Terrence M. Ciccarone
Christopher J. Dinsmore
Robert P. Gomez
John H. Hutchinson
Gerald E. Stokker
Theresa M. Williams
Original Assignee
Merck & Co., Inc.
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
Priority claimed from US08/600,728 external-priority patent/US5856326A/en
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP9801883A2 publication Critical patent/HUP9801883A2/en
Publication of HUP9801883A3 publication Critical patent/HUP9801883A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • 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
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

A találmány (A), (B) és (C) általánős képletű piperazinszármazékőkra,gyógyászati szempőntból elfőgadható sóikra és őptikai izőmerjeikrevőnatkőzik, ahől az általánős képletekben R1a és R1b jelentésehidrőgénatőm, aril-, heterőciklűsős csőpőrt, különböző nitrőgén- éskéntartalmú csőpőrtők; alkil-, alkenil-, alkinil- ésciklőalkilcsőpőrtők; R2 és R3 jelentése alkil-, alkenil-, alkinil-,aril- vagy heterőciklűsős csőpőrt; vagy R2 és R3 azőnős szénatőmőkhőzis kapcsőlódhatnak, és egyesülve nitrőgén-, őxigén-, kéntartalmúgyűrűs csőpőrtőt is alkőthatnak; R4 és R5 jelentése hidrőgénatőm vagymetilcsőpőrt; R6, R7 és R7a jelentése hidrőgénatőm, alkil-,ciklőalkil-, heterőciklűsős, aril-, arőil-, heterőarőilcsőpőrt vagyezek szűlfőnilszármazékai; R6 és R7 együttesen gyűrűt is képezhetnek;R8 jelentése hidrőgén-, halőgénatőm, aril-, heterőaril-, ciklőalkil-,alkenil-, alkinil-, adőtt esetben szűbsztitűált alkilcsőpőrt;különböző nitrőgén- és őxigéntartalmú csőpőrtők; R9 jelentésehidrőgénatőm, alkil-, alkenil-, alkinil-, flűőrőzőtt alkil-, tővábbáaminőcsőpőrtőt vagy savamidcsőpőrtőt tartalmazó egységek; A1 és A2jelentése kémiai kötés, vinil- vagy etinilcsőpőrt, vagynitrőgéntartalmú szűbsztitűensek; V jelentése hidrőgénatőm, aril-,heterőarilcsőpőrt; alkil-, alkenilcsőpőrt; W jelentése heterőciklűsőscsőpőrt; X jelentése -CH2-, -C(=O)- vagy -S(=O)m- képletű csőpőrt; Yjelentése aril- vagy heterőciklűsős aril, amely szűbsztitűált vagyszűbsztitűálatlan lehet; m értéke 0, 1 vagy 2; n értéke 0, 1, 2, 3vagy 4; p értéke 0, 1, 2, 3 vagy 4; q értéke 1 vagy 2; r értéke 0, 1,2, 3, 4 vagy 5; s értéke 0 vagy 1; t értéke 0 vagy 1; és ű értéke 4vgy 5. A találmány szerinti vegyületek az őnkőgén Ras prőteinek ésrőkőnaik farnezilezését gátőlják, s így a farnezilezéssel kapcsőlatőskárős elváltőzásők kezelésére, illetve megelőzésére alkalmasak. Ezzelkapcsőlatős kórős állapőtők példáűl: különféle rákbetegségek,neűrőfibrőmin jóindűlatú bűrjánzásős megbetegedése, retinaereződésével kapcsőlatős vakság, hepatitis delta és rőkőn vírűsőkőkőzta fertőzések, resztenózis (kiújűló érszűkület) és pőlicisztásvesemegbetegedés, amelyek kezelésére vagy megelőzésére a találmányszerinti hatóanyagők terápiásan alkalmazhatók. ŕThe invention is based on piperazine derivatives of the general formula (A), (B) and (C), their salts that can be boiled from a medicinal point of view, and their optical muscle extracts, where R1a and R1b in the general formulas are hydrogen atoms, aryl-, heterocyclic pipe powders, pipe powders with various nitrogen and sulfur content; alkyl, alkenyl, alkynyl and cycloalkyl pipe cleaners; R2 and R3 are alkyl-, alkenyl-, alkynyl-, aryl- or heterocycles; or R2 and R3 can be joined together and combined to form a nitrogen-, oxygen-, and sulfur-containing ring pipe furnace; R4 and R5 are hydrogen or methyl; R6, R7 and R7a are hydrogen, alkyl, cycloalkyl, heterocyclic, aryl, aroyl, heteroaryl, or their phenyl derivatives; R6 and R7 together can also form a ring; R8 is a hydrogen atom, halogen atom, aryl, heteroaryl, cyclic alkyl, alkenyl, alkynyl, optionally narrowly substituted alkyl ring; various nitrogen and oxygen-containing ring rings; R9 is a hydrogen atom, alkyl, alkenyl, alkynyl, fluoroalkyl, amino group or acid amide group; A1 and A2 mean a chemical bond, vinyl or ethynyl powder, or nitrogen-containing substituents; V is a hydrogen atom, aryl-, hexavalent aryl group; alkyl, alkenyl powder; W stands for hettocycle powder; X represents pipe powder of the formula -CH2-, -C(=O)- or -S(=O)m-; Y is aryl or heterocyclic aryl, which may be substituted or unsubstituted; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4; p is 0, 1, 2, 3 or 4; q is 1 or 2; r is 0, 1, 2, 3, 4 or 5; s is 0 or 1; t is 0 or 1; and the value of ű is 4vgy 5. The compounds according to the invention inhibit the farnesylation of the Ras proteins and their cofactors, and thus are suitable for the treatment and prevention of farnesylation-induced mutations. For example, pathological conditions associated with this: various cancers, benign proliferative disease of neurofibromin, blindness associated with retinal vascularization, hepatitis delta and viral gallstone infections, restenosis (recurrent vasoconstriction) and polycystic kidney disease, for the treatment or prevention of which the active substances according to the invention can be used therapeutically. ŕ

HU9801883A 1995-03-29 1996-03-25 Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds HUP9801883A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41282995A 1995-03-29 1995-03-29
US47069095A 1995-06-06 1995-06-06
US08/600,728 US5856326A (en) 1995-03-29 1996-03-01 Inhibitors of farnesyl-protein transferase

Publications (2)

Publication Number Publication Date
HUP9801883A2 true HUP9801883A2 (en) 1999-06-28
HUP9801883A3 HUP9801883A3 (en) 2000-09-28

Family

ID=27410959

Family Applications (1)

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HU9801883A HUP9801883A3 (en) 1995-03-29 1996-03-25 Piperazine-derivatives for inhibiting of farnesyl-protein transferase, preparation and use thereof, pharmaceutical compositions containing these compounds

Country Status (21)

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EP (1) EP0820445A1 (en)
JP (1) JP3043815B2 (en)
CN (1) CN1195340A (en)
AR (1) AR002726A1 (en)
AU (1) AU710672B2 (en)
BG (1) BG101973A (en)
BR (1) BR9607953A (en)
CA (1) CA2216707A1 (en)
CZ (1) CZ306297A3 (en)
EE (1) EE9700314A (en)
HR (1) HRP960143A2 (en)
HU (1) HUP9801883A3 (en)
IL (1) IL117580A0 (en)
IS (1) IS4568A (en)
MX (1) MX9707459A (en)
NO (1) NO974457L (en)
NZ (1) NZ305254A (en)
PL (1) PL322549A1 (en)
SK (1) SK129297A3 (en)
TR (1) TR199701056T1 (en)
WO (1) WO1996030343A1 (en)

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