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WO1997038665A3 - Inhibitors of farnesyl-protein transferase - Google Patents

Inhibitors of farnesyl-protein transferase Download PDF

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Publication number
WO1997038665A3
WO1997038665A3 PCT/US1997/006487 US9706487W WO9738665A3 WO 1997038665 A3 WO1997038665 A3 WO 1997038665A3 US 9706487 W US9706487 W US 9706487W WO 9738665 A3 WO9738665 A3 WO 9738665A3
Authority
WO
WIPO (PCT)
Prior art keywords
farnesyl
protein transferase
inhibitors
protein
farnesylation
Prior art date
Application number
PCT/US1997/006487
Other languages
French (fr)
Other versions
WO1997038665A2 (en
Inventor
Neville J Anthony
Christopher Dinsmore
Robert P Gomez
John H Hutchinson
John S Wai
Theresa M Williams
Ian M Bell
Mark W Embrey
Thorsten E Fisher
Original Assignee
Merck & Co Inc
Neville J Anthony
Christopher Dinsmore
Robert P Gomez
John H Hutchinson
John S Wai
Theresa M Williams
Ian M Bell
Mark W Embrey
Thorsten E Fisher
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 GBGB9609981.7A external-priority patent/GB9609981D0/en
Application filed by Merck & Co Inc, Neville J Anthony, Christopher Dinsmore, Robert P Gomez, John H Hutchinson, John S Wai, Theresa M Williams, Ian M Bell, Mark W Embrey, Thorsten E Fisher filed Critical Merck & Co Inc
Priority to EP97921256A priority Critical patent/EP0944388A4/en
Priority to JP53738897A priority patent/JP2001519766A/en
Priority to AU27347/97A priority patent/AU715202B2/en
Publication of WO1997038665A2 publication Critical patent/WO1997038665A2/en
Publication of WO1997038665A3 publication Critical patent/WO1997038665A3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
PCT/US1997/006487 1996-04-03 1997-03-27 Inhibitors of farnesyl-protein transferase WO1997038665A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP97921256A EP0944388A4 (en) 1996-04-03 1997-03-27 Inhibitors of farnesyl-protein transferase
JP53738897A JP2001519766A (en) 1996-04-03 1997-03-27 Inhibitors of farnesyl protein transferase
AU27347/97A AU715202B2 (en) 1996-04-03 1997-03-27 Inhibitors of farnesyl-protein transferase

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US1479196P 1996-04-03 1996-04-03
US60/014,791 1996-04-03
GBGB9609981.7A GB9609981D0 (en) 1996-05-13 1996-05-13 Inhibitors of farnesyl-protien transferase
GB9609981.7 1996-05-13

Publications (2)

Publication Number Publication Date
WO1997038665A2 WO1997038665A2 (en) 1997-10-23
WO1997038665A3 true WO1997038665A3 (en) 1997-11-27

Family

ID=26309324

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/006487 WO1997038665A2 (en) 1996-04-03 1997-03-27 Inhibitors of farnesyl-protein transferase

Country Status (5)

Country Link
EP (1) EP0944388A4 (en)
JP (1) JP2001519766A (en)
AU (1) AU715202B2 (en)
CA (1) CA2249601A1 (en)
WO (1) WO1997038665A2 (en)

Cited By (5)

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Publication number Priority date Publication date Assignee Title
US7482367B2 (en) 2005-08-30 2009-01-27 Novartis Vaccines And Diagnostics, Inc. Substituted benzimidazoles and methods of their use
US7553854B2 (en) 2006-04-19 2009-06-30 Novartis Vaccines And Diagnostics, Inc. 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
US7576106B2 (en) 2005-10-11 2009-08-18 Chemocentryx, Inc. Piperidine derivatives and methods of use
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof

Families Citing this family (130)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2185307T3 (en) * 1998-02-02 2003-04-16 Lg Chemical Ltd FARNESIL TRANSFERASA INHIBITORS THAT HAVE A PIPERIDINIC STRUCTURE AND PROCEDURE FOR THEIR PREPARATION.
US6331541B1 (en) 1998-12-18 2001-12-18 Soo S. Ko N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
IL142768A0 (en) 1998-12-18 2002-03-10 Du Pont Pharm Co N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
WO2000035453A1 (en) 1998-12-18 2000-06-22 Du Pont Pharmaceuticals Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6525069B1 (en) 1998-12-18 2003-02-25 Bristol-Myers Squibb Pharma Co. N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
US6897234B2 (en) 1999-12-17 2005-05-24 Bristol-Myers Squibb Pharma Company N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
RU2398765C1 (en) * 2000-03-06 2010-09-10 Акадиа Фармасьютикалз, Инк. Azacyclic compounds to be used in treating serotonin-mediated diseases
JP2004517805A (en) 2000-06-30 2004-06-17 ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー N-ureidoheterocycloalkyl-piperidines as modulators of chemokine receptor activity
FR2819509B1 (en) 2001-01-18 2004-04-16 Servier Lab NOVEL CYCLOHEPTENE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2819510B1 (en) * 2001-01-18 2003-10-31 Servier Lab NOVEL CYCLO [C] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
FR2819511A1 (en) * 2001-01-18 2002-07-19 Servier Lab New N-substituted azepane or azepanone derivatives, are selective farnesyl transferase inhibitors useful for treating cancer diseases, restenosis or type I neurofibromatosis
FR2819512B1 (en) * 2001-01-18 2003-02-21 Servier Lab NOVEL CYCLO [D] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
EP1598338B9 (en) * 2001-04-18 2009-11-18 Euro-Celtique S.A. 1-(4-piperidinyl)-1,3-dihydro-2h-indole-2-one derivatives and related compounds as nociceptin analogs and orl1 ligands for the treatment of pain
US6624162B2 (en) 2001-10-22 2003-09-23 Pfizer Inc. Imidazopyridine compounds as 5-HT4 receptor modulators
ATE466014T1 (en) 2001-12-28 2010-05-15 Acadia Pharm Inc SPIROAZACYCLIC COMPOUNDS AS MONOAMINE RECEPTOR MODULATORS
MXPA03000145A (en) 2002-01-07 2003-07-15 Pfizer Oxo or oxy-pyridine compounds as 5-ht4 receptor modulators.
ES2193875B2 (en) 2002-04-09 2005-03-01 Laboratorios Del Dr. Esteve, S.A. DERIVATIVES OF BENZOXAZINONA, ITS PREPARATION AND ITS APPLICATION AS MEDICATIONS.
GB0211230D0 (en) 2002-05-16 2002-06-26 Medinnova Sf Treatment of heart failure
US7253186B2 (en) 2002-06-24 2007-08-07 Carl-Magnus Andersson N-substituted piperidine derivatives as serotonin receptor agents
US7538222B2 (en) 2002-06-24 2009-05-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
CA2490397A1 (en) 2002-06-24 2003-12-31 Acadia Pharmaceuticals Inc. N-substituted piperidine derivatives as serotonin receptor agents
TW200409637A (en) 2002-06-26 2004-06-16 Glaxo Group Ltd Compounds
CA2499494A1 (en) 2002-09-20 2004-04-01 Pfizer Inc. N-substituted piperidinyl-imidazopyridine compounds as 5-ht4 receptor modulators
DOP2003000703A (en) 2002-09-20 2004-03-31 Pfizer IMIDAZOPIRADINE COMPOUNDS AS 5-HT4 RECEIVER AGONISTS
US6919356B2 (en) 2002-09-26 2005-07-19 Bristol Myers Squibb Company N-substituted heterocyclic amines as modulators of chemokine receptor activity
SI2009000T1 (en) 2003-01-16 2011-09-30 Acadia Pharm Inc Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
KR100977242B1 (en) 2003-07-24 2010-08-24 유로-셀띠끄 소시에떼 아노님 Piperidine Compounds and Pharmaceutical Compositions Comprising the Same
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. Selective serotonin receptor inverse agonists as therapeutics for disease
US20050261278A1 (en) 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
EA200801608A1 (en) 2004-06-15 2008-10-30 Пфайзер Инк. DERIVATIVES OF BENZIMIDAZOLONIC CARBONIC ACID
US7737163B2 (en) 2004-06-15 2010-06-15 Pfizer Inc. Benzimidazolone carboxylic acid derivatives
US7790899B2 (en) 2004-09-27 2010-09-07 Acadia Pharmaceuticals, Inc. Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms
EP2289879B1 (en) 2004-09-27 2014-11-12 Acadia Pharmaceuticals Inc. Synthesis of a crystalline form of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide tartrate salt
UY29177A1 (en) 2004-10-25 2006-05-31 Astex Therapeutics Ltd SUBSTITUTED DERIVATIVES OF PURINA, PURINONA AND DEAZAPURINA, COMPOSITIONS THAT CONTAIN METHODS FOR THEIR PREPARATION AND ITS USES
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
ATE550019T1 (en) 2005-05-17 2012-04-15 Merck Sharp & Dohme CIS-4-Ä(4-CHLOROPHENYL)SULFONYLÜ-4-(2,5-DIFLUOROPHENYL)CYCLOHEXANEPROPANE ACID FOR THE TREATMENT OF CANCER
US7615556B2 (en) 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP3421471B1 (en) 2006-04-25 2021-05-26 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
WO2008084261A1 (en) 2007-01-10 2008-07-17 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
PL2134330T3 (en) 2007-03-19 2013-10-31 Acadia Pharm Inc Combinations of 5-ht2a inverse agonists and antagonists with antipsychotics
WO2008120759A1 (en) * 2007-03-30 2008-10-09 Japan Tobacco Inc. Urea compound and use thereof
ES2571533T3 (en) 2007-04-27 2016-05-25 Purdue Pharma Lp TRPV1 antagonists and uses thereof
KR20090130422A (en) 2007-04-27 2009-12-23 퍼듀 퍼머 엘피 Useful remedies for the treatment of pain
CN101754965B (en) 2007-05-21 2014-03-19 诺华股份有限公司 CSF-1R inhibitors, compositions, and methods of use
JP5501227B2 (en) 2007-06-27 2014-05-21 メルク・シャープ・アンド・ドーム・コーポレーション 4-Carboxybenzylamino derivatives as histone deacetylase inhibitors
EP2178534A4 (en) 2007-07-17 2011-03-30 Merck Sharp & Dohme SOLUBLE EPOXY HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND PROCESSING METHODS
PL2201012T3 (en) 2007-10-11 2014-11-28 Astrazeneca Ab Pyrrolo[2,3-d]pyrimidin derivatives as protein kinase b inhibitors
TWI433838B (en) 2008-06-25 2014-04-11 必治妥美雅史谷比公司 Piperidinyl derivative as a modulator of chemokine receptor activity
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
WO2010021693A2 (en) * 2008-08-18 2010-02-25 Yale University Mif modulators
EP2413932A4 (en) 2009-04-01 2012-09-19 Merck Sharp & Dohme HAMMER OF ACT ACTIVITY
NZ599343A (en) 2009-10-14 2014-05-30 Merck Sharp & Dohme Substituted piperidines that increase p53 activity and the uses thereof
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
WO2011093365A1 (en) * 2010-01-27 2011-08-04 協和発酵キリン株式会社 Nitrogenated heterocyclic compound
AU2011227643A1 (en) 2010-03-16 2012-09-20 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
US8642622B2 (en) 2010-06-16 2014-02-04 Bristol-Myers Squibb Company Piperidinyl compound as a modulator of chemokine receptor activity
JP5876423B2 (en) 2010-06-22 2016-03-02 塩野義製薬株式会社 Compounds having TRPV1 inhibitory activity and uses thereof
EP2584903B1 (en) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
EP2601293B1 (en) 2010-08-02 2017-12-06 Sirna Therapeutics, Inc. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
CA2807307C (en) 2010-08-17 2021-02-09 Merck Sharp & Dohme Corp. Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina)
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
WO2012036997A1 (en) 2010-09-16 2012-03-22 Schering Corporation Fused pyrazole derivatives as novel erk inhibitors
EP3766975A1 (en) 2010-10-29 2021-01-20 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acid (sina)
US8980924B2 (en) 2010-11-24 2015-03-17 The Trustees Of Columbia University In The City Of New York Non-retinoid RBP4 antagonist for treatment of age-related macular degeneration and stargardt disease
US9351965B2 (en) 2010-12-21 2016-05-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
JP6080837B2 (en) 2011-04-01 2017-02-15 アストラゼネカ アクチボラグ Therapeutic treatment
JP2014514321A (en) 2011-04-21 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Insulin-like growth factor 1 receptor inhibitor
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
AU2012293417A1 (en) 2011-08-10 2013-05-02 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
AU2012340200B2 (en) 2011-11-17 2017-10-12 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-Terminal Kinase (JNK)
PL2785349T5 (en) 2011-11-30 2023-01-30 Astrazeneca Ab Combination treatment of cancer
US9073856B2 (en) * 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
US9333202B2 (en) 2012-05-01 2016-05-10 The Trustees Of Columbia University In The City Of New York Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease
US20150299696A1 (en) 2012-05-02 2015-10-22 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
RU2660429C2 (en) 2012-09-28 2018-07-06 Мерк Шарп И Доум Корп. Novel compounds that are erk inhibitors
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
ME02925B (en) 2012-11-28 2018-04-20 Merck Sharp & Dohme COMPOSITIONS AND METHOD FOR THE TREATMENT OF CANCER
MX373639B (en) 2012-12-20 2020-05-04 Merck Sharp & Dohme SUBSTITUTED IMIDAZOPYRIDINES AS HUMAN DOUBLE MINUTE 2 INHIBITORS.
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
EP3495357B1 (en) 2013-03-14 2021-05-05 The Trustees of Columbia University in the City of New York 4-phenylpiperidines, their preparation and use
ES2700541T3 (en) 2013-03-14 2019-02-18 Univ Columbia Octahidrociclopentapirroles, its preparation and use
US9944644B2 (en) 2013-03-14 2018-04-17 The Trustees Of Columbia University In The City Of New York Octahydropyrrolopyrroles their preparation and use
WO2014151959A1 (en) 2013-03-14 2014-09-25 The Trustees Of Columbia University In The City Of New York N-alkyl-2-phenoxyethanamines, their preparation and use
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
AU2014337122B2 (en) 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
CN105849099B (en) 2013-10-18 2020-01-17 达纳-法伯癌症研究所股份有限公司 Polycyclic inhibitor of cyclin-dependent kinase 7 (CDK7)
EP3686200A3 (en) 2013-12-20 2020-09-09 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9434727B2 (en) 2014-04-30 2016-09-06 The Trustees Of Columbia University In The City Of New York Substituted 4-phenylpiperidines, their preparation and use
JO3589B1 (en) 2014-08-06 2020-07-05 Novartis Ag Protein kinase c inhibitors and methods of their use
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (en) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 Inhibitors of cyclin-dependent kinases
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP6850282B2 (en) 2015-07-20 2021-03-31 アカディア ファーマシューティカルズ インコーポレーテッド Preparation of N- (4-fluorobenzyl) -N- (1-methylpiperidin-4-yl) -N'-(4- (2-methylpropyloxy) phenylmethyl) carbamide and its tartrate and polymorphic form C how to
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
JOP20190055A1 (en) 2016-09-26 2019-03-24 Merck Sharp & Dohme Anti-cd27 antibodies
US10975084B2 (en) 2016-10-12 2021-04-13 Merck Sharp & Dohme Corp. KDM5 inhibitors
US11464768B2 (en) 2016-12-20 2022-10-11 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of Alzheimer's disease psychosis
KR102702926B1 (en) 2017-04-13 2024-09-06 사이로파 비.브이. Anti-SIRP alpha antibody
EP3615028A1 (en) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019094312A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
AU2019295632B2 (en) 2018-06-25 2025-03-06 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020033282A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
MX2021001486A (en) 2018-08-07 2021-07-15 Merck Sharp & Dohme Llc Prmt5 inhibitors.
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
WO2020140098A1 (en) 2018-12-28 2020-07-02 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
MX2024009122A (en) * 2022-01-25 2024-08-06 Merck Sharp & Dohme Llc PLASMA KALLIKERIN INHIBITORS.
US20250152585A1 (en) * 2022-02-16 2025-05-15 Duke Street Bio Limited Pharmaceutical compound
AU2024228641A1 (en) 2023-03-02 2025-07-24 Carcimun Biotech Gmbh Means and methods for diagnosing cancer and/or an acute inflammatory disease

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5478934A (en) * 1994-11-23 1995-12-26 Yuan; Jun Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands
WO1997018813A1 (en) * 1995-11-22 1997-05-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5639775A (en) * 1992-04-01 1997-06-17 The University Of Toledo 4-[4'-piperodinyl or 3'-pirrolidinyl] substituted imidazoles as H3 -receptor antagonists and therapeutic uses thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09500109A (en) * 1993-06-18 1997-01-07 メルク エンド カンパニー インコーポレーテッド Inhibitors of farnesyl protein transferase
RU95104898A (en) * 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Imedazole containing inhibitors of ferneside proteintansferase, and method of treatment diseases related therewith
US5576313A (en) * 1994-08-29 1996-11-19 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JPH10508005A (en) * 1994-09-29 1998-08-04 メルク エンド カンパニー インコーポレーテッド Thiol-free farnesyl-protein transferase inhibitors
US5491164A (en) * 1994-09-29 1996-02-13 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
IL117580A0 (en) * 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5710171A (en) * 1995-05-24 1998-01-20 Merck & Co., Inc. Bisphenyl inhibitors of farnesyl-protein transferase
HUP9901183A3 (en) * 1995-11-22 1999-11-29 Intrabiotics Pharmaceuticals Compositions and methods for the prevention and treatment of oral mucositis
AU706314B2 (en) * 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5639775A (en) * 1992-04-01 1997-06-17 The University Of Toledo 4-[4'-piperodinyl or 3'-pirrolidinyl] substituted imidazoles as H3 -receptor antagonists and therapeutic uses thereof
US5478934A (en) * 1994-11-23 1995-12-26 Yuan; Jun Certain 1-substituted aminomethyl imidazole and pyrrole derivatives: novel dopamine receptor subtype specific ligands
WO1997018813A1 (en) * 1995-11-22 1997-05-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP0944388A4 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7482367B2 (en) 2005-08-30 2009-01-27 Novartis Vaccines And Diagnostics, Inc. Substituted benzimidazoles and methods of their use
US7576106B2 (en) 2005-10-11 2009-08-18 Chemocentryx, Inc. Piperidine derivatives and methods of use
US7576218B2 (en) 2005-10-11 2009-08-18 Chemocentryx, Inc. 4-phenylpiperdine-pyrazole CCR1 antagonists
US7553854B2 (en) 2006-04-19 2009-06-30 Novartis Vaccines And Diagnostics, Inc. 6-O-substituted benzoxazole and benzothiazole compounds and methods of inhibiting CSF-1R signaling
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof

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EP0944388A4 (en) 2001-08-16
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EP0944388A2 (en) 1999-09-29
CA2249601A1 (en) 1997-10-23
AU2734797A (en) 1997-11-07
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