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 JP53738897A priority Critical patent/JP2001519766A/en
Priority to AU27347/97A priority patent/AU715202B2/en
Priority to EP97921256A priority patent/EP0944388A4/en
Publication of WO1997038665A2 publication Critical patent/WO1997038665A2/en
Publication of WO1997038665A3 publication Critical patent/WO1997038665A3/en

Links

Classifications

    • 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
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon 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
    • 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
    • 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

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
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
EP97921256A EP0944388A4 (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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof

Families Citing this family (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1158277C (en) * 1998-02-02 2004-07-21 Lg化学株式会社 Farnesyl transferase inhibitors having a piperidine structure and process for preparation thereof
US6331541B1 (en) 1998-12-18 2001-12-18 Soo S. Ko 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
DE69926919D1 (en) 1998-12-18 2005-09-29 Bristol Myers Squibb Pharma Co N-UREIDOALKYLPIPERIDINES AS MODULATORS OF THE ACTIVITY OF CHEMOKIN RECEPTORS
CA2347770A1 (en) 1998-12-18 2000-06-22 Bristol-Myers Squibb Pharma Company 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
KR100879647B1 (en) * 2000-03-06 2009-01-20 아카디아 파마슈티칼스 인코포레이티드 Azacyclic compounds for use in the treatment of serotonin related diseases
IL153123A0 (en) 2000-06-30 2003-06-24 Bristol Myers Squibb Co N-ureidoheterocycloalkyl-piperidine derivatives and 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
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
FR2819512B1 (en) * 2001-01-18 2003-02-21 Servier Lab NOVEL CYCLO [D] AZEPANE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2819509B1 (en) * 2001-01-18 2004-04-16 Servier Lab NOVEL CYCLOHEPTENE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
MXPA03009600A (en) * 2001-04-18 2004-04-02 Euro Celtique Sa Nociceptin analogs.
US6624162B2 (en) 2001-10-22 2003-09-23 Pfizer Inc. Imidazopyridine compounds as 5-HT4 receptor modulators
MXPA04006280A (en) 2001-12-28 2004-09-27 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
AU2003247615B2 (en) 2002-06-24 2007-08-09 Acadia Pharmaceuticals Inc. N-substituted piperidine derivatives as serotonin receptor agents
TW200409637A (en) 2002-06-26 2004-06-16 Glaxo Group Ltd Compounds
DOP2003000703A (en) 2002-09-20 2004-03-31 Pfizer IMIDAZOPIRADINE COMPOUNDS AS 5-HT4 RECEIVER AGONISTS
CA2499494A1 (en) 2002-09-20 2004-04-01 Pfizer Inc. N-substituted piperidinyl-imidazopyridine compounds as 5-ht4 receptor modulators
US6919356B2 (en) 2002-09-26 2005-07-19 Bristol Myers Squibb Company N-substituted heterocyclic amines as modulators of chemokine receptor activity
ES2314362T3 (en) 2003-01-16 2009-03-16 Acadia Pharmaceuticals Inc. SELECTIVE INVESTING AGONISTS OF SEROTONINE 2A OR 2C RECEPTORS USED AS THERAPEUTIC AGENTS AGAINST NEURODEGENERATIVE DISEASES.
CN1829708A (en) 2003-07-24 2006-09-06 尤罗塞尔蒂克股份有限公司 Piperidine compounds and pharmaceutical compositions containing them
US20050261278A1 (en) 2004-05-21 2005-11-24 Weiner David M Selective serotonin receptor inverse agonists as therapeutics for disease
US7820695B2 (en) 2004-05-21 2010-10-26 Acadia Pharmaceuticals, Inc. 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
CN101031548B (en) 2004-09-27 2011-04-06 阿卡蒂亚药品公司 Salts of n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy) phenylmethyl) carbamide and their preparation
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
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
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
US8362075B2 (en) 2005-05-17 2013-01-29 Merck Sharp & Dohme Corp. Cyclohexyl sulphones for treatment of cancer
US7576106B2 (en) 2005-10-11 2009-08-18 Chemocentryx, Inc. Piperidine derivatives and methods of use
US7601844B2 (en) 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US7615556B2 (en) 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US8796293B2 (en) 2006-04-25 2014-08-05 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
PL2336120T3 (en) 2007-01-10 2014-12-31 Msd Italia Srl Combinations containing amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
MX2009009304A (en) 2007-03-01 2009-11-18 Novartis Ag Pim kinase inhibitors and methods of their use.
JP2010522198A (en) 2007-03-19 2010-07-01 アカドイア プハルマセウチカルス インコーポレーテッド Combination 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
EP2091936B1 (en) 2007-04-27 2013-05-15 Purdue Pharma LP Therapeutic agents useful for treating pain
CA2685967A1 (en) 2007-05-21 2008-11-21 Novartis Ag Csf-1r inhibitors, compositions, and methods of use
CA2690191C (en) 2007-06-27 2015-07-28 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
WO2009011872A1 (en) 2007-07-17 2009-01-22 Merck & Co., Inc. Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
RS53552B1 (en) 2007-10-11 2015-02-27 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
US9540322B2 (en) 2008-08-18 2017-01-10 Yale University MIF modulators
BRPI0917394A2 (en) * 2008-08-18 2019-09-24 Univ Yale mif modulators
US9643922B2 (en) 2008-08-18 2017-05-09 Yale University MIF modulators
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
PE20121172A1 (en) 2009-10-14 2012-09-05 Merck Sharp & Dohme PIPERIDINS SUBSTITUTED WITH ACTIVITY IN HDM2
US9180127B2 (en) 2009-12-29 2015-11-10 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
BR112012023021A2 (en) 2010-03-16 2016-05-31 Dana Farber Cancer Inst 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
US8921373B2 (en) 2010-06-22 2014-12-30 Shionogi & Co., Ltd. Compounds having TRPV1 antagonistic activity and uses thereof
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CA2805265A1 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. 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)
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
EP2632472B1 (en) 2010-10-29 2017-12-13 Sirna Therapeutics, Inc. Rna interference mediated inhibition of gene expression using short interfering nucleic acids (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
CA2831848C (en) 2011-04-01 2020-12-22 Astrazeneca Ab Combination comprising (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide and a taxane
IN2013MN02170A (en) 2011-04-21 2015-06-12 Piramal Entpr Ltd
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
WO2013063214A1 (en) 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP3569598A1 (en) 2011-11-17 2019-11-20 Dana Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
FI2785349T4 (en) 2011-11-30 2023-02-09 Combination treatment of cancer
WO2013112323A1 (en) * 2012-01-23 2013-08-01 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
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
WO2014052563A2 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. 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)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
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
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
MX363243B (en) 2012-11-28 2019-03-14 Merck Sharp & Dohme Compositions and methods for treating cancer.
BR112015013611A2 (en) 2012-12-20 2017-11-14 Merck Sharp & Dohme compound and pharmaceutical composition
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
ES2705247T3 (en) 2013-03-14 2019-03-22 Univ Columbia 4-phenylpiperidines, their preparation and use
US9637450B2 (en) 2013-03-14 2017-05-02 The Trustees Of Columbia University In The City Of New York Octahydrocyclopentapyrroles, 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
US9944644B2 (en) 2013-03-14 2018-04-17 The Trustees Of Columbia University In The City Of New York Octahydropyrrolopyrroles their preparation and use
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
ES2676734T3 (en) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Heteroatomic compounds useful for the treatment of proliferative diseases
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2933939C (en) 2013-12-20 2021-03-16 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
CN111393434B (en) 2014-04-30 2022-11-04 哥伦比亚大学董事会 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
JP6854762B2 (en) 2014-12-23 2021-04-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Inhibitor of cyclin-dependent kinase 7 (CDK7)
JP6861166B2 (en) 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Inhibitor of cyclin-dependent kinase
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CN107848972B (en) 2015-07-20 2021-06-18 阿卡蒂亚药品公司 Process for the preparation of N- (4-fluorobenzyl) -N- (1-methylpiperidin-4-yl) -N' - (4- (2-methylpropyloxy) phenylmethyl) urea and its tartrate salt and polymorph C
CA2996978A1 (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
EP3558311A1 (en) 2016-12-20 2019-10-30 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
MX2019012233A (en) 2017-04-13 2020-01-14 Aduro Biotech Holdings Europe Bv Anti-sirp alpha antibodies.
WO2018200977A1 (en) 2017-04-28 2018-11-01 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. Formulations of pimavanserin
WO2019094311A1 (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
US20210277009A1 (en) 2018-08-07 2021-09-09 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2020033284A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
WO2023156386A2 (en) * 2022-02-16 2023-08-24 Duke Street Bio Limited Pharmaceutical compound

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
EP0703905A1 (en) * 1993-06-18 1996-04-03 Merck & Co. Inc. 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
AU700175B2 (en) * 1994-09-29 1998-12-24 Merck & Co., Inc. Thiol-free inhibitors of farnesyl-protein transferase
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
IL124576A0 (en) * 1995-11-22 1999-01-26 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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof

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EP0944388A2 (en) 1999-09-29
AU2734797A (en) 1997-11-07
WO1997038665A2 (en) 1997-10-23
EP0944388A4 (en) 2001-08-16
JP2001519766A (en) 2001-10-23
CA2249601A1 (en) 1997-10-23

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