HUP0104607A2 - MEK inhibitor alkalmazása transzplantátumok kilökődésének megelőzésére - Google Patents

MEK inhibitor alkalmazása transzplantátumok kilökődésének megelőzésére

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Publication number
HUP0104607A2
HUP0104607A2 HU0104607A HUP0104607A HUP0104607A2 HU P0104607 A2 HUP0104607 A2 HU P0104607A2 HU 0104607 A HU0104607 A HU 0104607A HU P0104607 A HUP0104607 A HU P0104607A HU P0104607 A2 HUP0104607 A2 HU P0104607A2
Authority
HU
Hungary
Prior art keywords
group
hydrogen atom
alkyl
atom
hydroxyl
Prior art date
Application number
HU0104607A
Other languages
English (en)
Inventor
Richard Buell Gilbertsen
Original Assignee
Warner-Lambert Co.
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 Warner-Lambert Co. filed Critical Warner-Lambert Co.
Publication of HUP0104607A2 publication Critical patent/HUP0104607A2/hu
Publication of HUP0104607A3 publication Critical patent/HUP0104607A3/hu

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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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • 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
    • 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
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Compounds Of Unknown Constitution (AREA)

Abstract

A tal lm ny t rgya elj r s emlős"kben tültetett szervek, sejtek,végtagok és sz"vetek kil"kődésének gyógyító vagy megelőző kezelésére,amely elj r s szerint szelektív MEK inhibitort, előny"sen (I) vagy(II) ltal nos képletű vegyületet adagolunk. A képletekben R1 jelentésehidrogénatom, hidroxil-, 1-8 szénatomos alkil-, 1-8 szénatomosalkoxicsoport, halogénatom, trifluorometil-, vagy cianidcsoport. R2jelentése hidrogénatom. R3, R4 és R5 jelentése egym stól függetlenülhidrogénatom, hidroxilcsoport, halogénatom, trifluorometil-, 1-8szénatomos alkil-, 1-8 szénatomos alkoxi-, nitro-, cianid-, vagy -(Ovagy NH)m-(CH2)n-R9 képletű csoport. R9 jelentése hidrogénatom,hidroxil-, karboxil-, vagy NR10R11 képletű csoport; n értéke 0 és 4k"z"tti sz m; m értéke 0 vagy 1. R10 és R11 jelentése egyar nt, egymstól függetlenül hidrogénatom és 1-8 szénatomos alkilcsoport, R1ajelentése hidrogénatom, hidroxil-, 1-8 szénatomos alkil-, 1-8szénatomos alkoxicsoport, halogénatom, trifluoro-metil-, vagycianidcsoport. R2a jelentése hidrogénatom. R3a, R4a, és R5a jelentéseegyar nt, egym stól függetlenül hidrogénatom, hidroxilcsoport,halogénatom, trifluoro-metil-, 1-8 szénatomos alkil-, 1-8 szénatomosalkoxi-, nitro-, cianidcsoport, vagy (O vagy NH)m-(CH2)n-R9a-képletűcsoport. R9a jelentése hidrogénatom, hidroxil-, CO2H-, vagy NR10aR11a-képletű csoport; n értéke 0-4 k"z"tti sz m; és m értéke 0 vagy 1. R6ajelentése hidrogénatom, 1-8 szénatomos alkil-, (CO)-(1-8 szénatomosalkil)-csoport, aril-, aralkil-, vagy 3-10 szénatomoscikloalkilcsoport. R7a jelentése hidrogénatom, 1-8 szénatomos alkil-,2-8 szénatomos alkenil-, 2-8 szénatomos alkinil-, 3-10 szénatomos(cikloalkil vagy adott esetben egy heteroatommal helyettesítettcikloalkil-csoport, ahol a heteroatom jelentése oxigénatom, kénatom,vagy NR9a képletű csoport). Ó
HU0104607A 1998-12-15 1999-12-14 Use of a mek inhibitor for preventing transplant rejection HUP0104607A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11236998P 1998-12-15 1998-12-15
PCT/US1999/029591 WO2000035435A1 (en) 1998-12-15 1999-12-14 Use of a mek inhibitor for preventing transplant rejection

Publications (2)

Publication Number Publication Date
HUP0104607A2 true HUP0104607A2 (hu) 2002-04-29
HUP0104607A3 HUP0104607A3 (en) 2002-12-28

Family

ID=22343544

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0104607A HUP0104607A3 (en) 1998-12-15 1999-12-14 Use of a mek inhibitor for preventing transplant rejection

Country Status (10)

Country Link
EP (1) EP1140046A1 (hu)
JP (1) JP2002532414A (hu)
KR (1) KR20010101203A (hu)
AU (1) AU2180500A (hu)
CA (1) CA2346684A1 (hu)
HU (1) HUP0104607A3 (hu)
IL (1) IL143231A0 (hu)
TR (1) TR200101704T2 (hu)
WO (1) WO2000035435A1 (hu)
ZA (1) ZA200103765B (hu)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
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CN1219753C (zh) 2000-07-19 2005-09-21 沃尼尔·朗伯公司 4－碘苯氨基苯氧肟酸的氧合酯
IL149462A0 (en) 2001-05-09 2002-11-10 Warner Lambert Co Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor
AU2004283148A1 (en) 2003-10-21 2005-05-06 Warner-Lambert Company Llc Polymorphic form of N-[(R)-2,3-Dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-benzamide
KR100883289B1 (ko) 2004-06-11 2009-02-11 니뽄 다바코 산교 가부시키가이샤 암 치료용5-아미노-2,4,7-트리옥소-3,4,7,8-테트라히드로-2ｈ-피리도[2,3-ｄ]피리미딘 유도체 및 관련 화합물
US7378423B2 (en) 2004-06-11 2008-05-27 Japan Tobacco Inc. Pyrimidine compound and medical use thereof
EA025871B9 (ru) 2005-10-07 2017-08-31 Экселиксис, Инк. Ингибиторы mek и способы их применения
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
PE20080371A1 (es) 2006-05-19 2008-04-09 Wyeth Corp N-benzoil-y-n-bencilpirrolidin-3-ilaminas como antagonistas de histamina-3
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
US8993630B2 (en) 2008-11-10 2015-03-31 Bayer Intellectual Property Gmbh Substituted sulphonamido phenoxybenzamides
WO2011047795A1 (en) 2009-10-21 2011-04-28 Bayer Schering Pharma Aktiengesellschaft Substituted benzosulphonamides
CN102574782B (zh) 2009-10-21 2014-10-08 拜耳知识产权有限责任公司 取代的卤代苯氧基苯甲酰胺衍生物
WO2011047788A1 (en) 2009-10-21 2011-04-28 Bayer Schering Pharma Aktiengesellschaft Substituted benzosulphonamides
CA2816188A1 (en) 2010-10-29 2012-05-03 Marion Hitchcock Substituted phenoxypyridines
CR20200237A (es) 2012-10-12 2020-07-26 Exelixis Inc Proceso novedoso para la elaboración de compuestos para su uso en el tratamiento del cáncer (diviisional 2015-0245)
IL278194B2 (en) 2018-04-24 2023-12-01 Translational Drug Dev Llc Amide compounds as kinase inhibitors, compositions and methods of treatment
WO2020142745A1 (en) * 2019-01-04 2020-07-09 Translational Drug Development, Llc Methods of treating graft versus host disease and neoplastic disease with amide compounds

Family Cites Families (8)

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US5155110A (en) * 1987-10-27 1992-10-13 Warner-Lambert Company Fenamic acid hydroxamate derivatives having cyclooxygenase and 5-lipoxygenase inhibition
US5624946A (en) * 1994-07-05 1997-04-29 Williams; James Use of leflunomide to control and reverse chronic allograft rejection
US5525625A (en) * 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
WO1996031206A2 (en) * 1995-04-07 1996-10-10 Warner-Lambert Company Flavones and coumarins as agents for the treatment of atherosclerosis
US6251943B1 (en) * 1997-02-28 2001-06-26 Warner-Lambert Company Method of treating or preventing septic shock by administering a MEK inhibitor
EP0993437B1 (en) * 1997-07-01 2006-11-08 Warner-Lambert Company Llc 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as mek inhibitors
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WO1999034792A1 (en) * 1998-01-06 1999-07-15 The General Hospital Corporation Use of mek1 inhibitors as protective agents against damage due to ischemia

Also Published As

Publication number Publication date
TR200101704T2 (tr) 2001-11-21
HUP0104607A3 (en) 2002-12-28
WO2000035435A1 (en) 2000-06-22
CA2346684A1 (en) 2000-06-22
KR20010101203A (ko) 2001-11-14
AU2180500A (en) 2000-07-03
EP1140046A1 (en) 2001-10-10
IL143231A0 (en) 2002-04-21
ZA200103765B (en) 2002-05-09
JP2002532414A (ja) 2002-10-02
WO2000035435A9 (en) 2001-03-22

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