DE69615674D1 - Cyclobutan-derivate als inhibitoren der squalen-synthase und der protein farnesyltransferase - Google Patents

Cyclobutan-derivate als inhibitoren der squalen-synthase und der protein farnesyltransferase

Info

Publication number
DE69615674D1
DE69615674D1 DE69615674T DE69615674T DE69615674D1 DE 69615674 D1 DE69615674 D1 DE 69615674D1 DE 69615674 T DE69615674 T DE 69615674T DE 69615674 T DE69615674 T DE 69615674T DE 69615674 D1 DE69615674 D1 DE 69615674D1
Authority
DE
Germany
Prior art keywords
squalen
cyclobutan
synthase
inhibitors
derivatives
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE69615674T
Other languages
English (en)
Other versions
DE69615674T2 (de
Inventor
L Arendsen
R Baker
A Fakhoury
L Fung
S Garvey
J Mcclellan
J O'connor
N Prasad
W Rockway
H Rosenberg
H Stein
Wang Shen
M Stout
M Sullivan
J Augeri
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abbott Laboratories
Original Assignee
Abbott Laboratories
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 Abbott Laboratories filed Critical Abbott Laboratories
Publication of DE69615674D1 publication Critical patent/DE69615674D1/de
Application granted granted Critical
Publication of DE69615674T2 publication Critical patent/DE69615674T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/82—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/59—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/60—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
DE69615674T 1995-04-21 1996-04-18 Cyclobutan-derivate als inhibitoren der squalen-synthase und der protein farnesyltransferase Expired - Fee Related DE69615674T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US42835795A 1995-04-21 1995-04-21
US42655395A 1995-04-21 1995-04-21
US56452495A 1995-11-29 1995-11-29
US08/626,859 US5831115A (en) 1995-04-21 1996-04-12 Inhibitors of squalene synthase and protein farnesyltransferase
PCT/US1996/005529 WO1996033159A1 (en) 1995-04-21 1996-04-18 Cyclobutane derivatives as inhibitors of squalene synthase and protein farnesyltransferase

Publications (2)

Publication Number Publication Date
DE69615674D1 true DE69615674D1 (de) 2001-11-08
DE69615674T2 DE69615674T2 (de) 2002-07-11

Family

ID=27503744

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69615674T Expired - Fee Related DE69615674T2 (de) 1995-04-21 1996-04-18 Cyclobutan-derivate als inhibitoren der squalen-synthase und der protein farnesyltransferase

Country Status (7)

Country Link
US (1) US5831115A (de)
EP (2) EP1090908A3 (de)
JP (1) JPH11504017A (de)
AT (1) ATE206390T1 (de)
CA (1) CA2218597A1 (de)
DE (1) DE69615674T2 (de)
WO (1) WO1996033159A1 (de)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6403576B1 (en) * 1998-08-24 2002-06-11 The United States Of America As Represented By The Secretary Of The Navy Antifungal and antiparasitic compounds
US20030212008A1 (en) * 2000-02-29 2003-11-13 Palmer Peter Albert Farnesyl protein transferase inhibitor combinations with further anti-cancer agents
NZ534757A (en) 2002-03-12 2006-07-28 Merck & Co Inc Substituted amides
AU2003215024B2 (en) * 2002-03-26 2008-02-21 Merck Sharp & Dohme Corp. Spirocyclic amides as cannabinoid receptor modulators
JP4459629B2 (ja) 2002-04-12 2010-04-28 メルク エンド カムパニー インコーポレーテッド 二環式アミド
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7547693B2 (en) 2003-09-22 2009-06-16 Banyu Pharmaceutical Co. Ltd. Piperidine derivative
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
US8394765B2 (en) 2004-11-01 2013-03-12 Amylin Pharmaceuticals Llc Methods of treating obesity with two different anti-obesity agents
EP2286840A3 (de) 2004-11-01 2013-09-04 Amylin Pharmaceuticals, LLC Behandlung von Fettleibigkeit und von verwandten Krankheiten
US20090286723A1 (en) 2005-02-11 2009-11-19 Amylin Pharmaceuticals, Inc. Hybrid Polypeptides with Selectable Properties
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
EP1888050B1 (de) 2005-05-17 2012-03-21 Merck Sharp & Dohme Ltd. Cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropansäure zur Behandlug von Krebs
US8138206B2 (en) 2005-05-30 2012-03-20 Msd. K.K. Piperidine derivative
US20070148660A1 (en) * 2005-06-16 2007-06-28 The Regents Of The University Of California Treatment of maladaptive substance use with H-ras antagonists
WO2007018248A1 (ja) 2005-08-10 2007-02-15 Banyu Pharmaceutical Co., Ltd. ピリドン化合物
BRPI0614649A2 (pt) 2005-08-11 2011-04-12 Amylin Pharmaceuticals Inc polipeptìdeos hìbridos com propriedades selecionáveis
WO2007024004A1 (ja) 2005-08-24 2007-03-01 Banyu Pharmaceutical Co., Ltd. フェニルピリドン誘導体
JPWO2007029847A1 (ja) 2005-09-07 2009-03-19 萬有製薬株式会社 二環性芳香族置換ピリドン誘導体
KR20080048502A (ko) 2005-09-29 2008-06-02 머크 앤드 캄파니 인코포레이티드 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체
US8163770B2 (en) 2005-10-27 2012-04-24 Msd. K. K. Benzoxathiin derivative
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
US7442818B2 (en) * 2006-03-14 2008-10-28 David Rubin Method of making esters and catalysts therefore
TW200806284A (en) * 2006-03-31 2008-02-01 Alcon Mfg Ltd Prenyltransferase inhibitors for ocular hypertension control and the treatment of glaucoma
WO2008039327A2 (en) 2006-09-22 2008-04-03 Merck & Co., Inc. Method of treatment using fatty acid synthesis inhibitors
AU2007301126A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
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
MX2009007200A (es) 2007-01-10 2009-07-15 Angeletti P Ist Richerche Bio Indazoles sustituidos con amida como inhibidores de poli(adp-ribosa)polimerasa (parp).
EP2132177B1 (de) 2007-03-01 2013-07-17 Novartis AG Pim-kinase-hemmer und verfahren zu ihrer verwendung
JP5319518B2 (ja) 2007-04-02 2013-10-16 Ｍｓｄ株式会社 インドールジオン誘導体
EP2152700B1 (de) 2007-05-21 2013-12-11 Novartis AG Csf-1r-hemmer, zusammensetzungen und anwendungsverfahren
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
ES2393885T7 (es) 2007-06-04 2014-01-30 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
AU2008269154B2 (en) 2007-06-27 2014-06-12 Merck Sharp & Dohme Llc 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
JPWO2009110510A1 (ja) 2008-03-06 2011-07-14 Ｍｓｄ株式会社 アルキルアミノピリジン誘導体
CN101981025A (zh) 2008-03-28 2011-02-23 万有制药株式会社 具有黑色素浓缩激素受体拮抗作用的二芳基甲基酰胺衍生物
ES2522968T3 (es) 2008-06-04 2014-11-19 Synergy Pharmaceuticals Inc. Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
AU2009261248A1 (en) 2008-06-19 2009-12-23 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
AU2009270833B2 (en) 2008-07-16 2015-02-19 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
WO2010013595A1 (ja) 2008-07-30 2010-02-04 萬有製薬株式会社 ５員－５員又は５員－６員縮環シクロアルキルアミン誘導体
MX2011004258A (es) 2008-10-22 2011-06-01 Merck Sharp & Dohme Derivados de bencimidazol ciclicos novedosos utiles como agentes anti-diabeticos.
BRPI0919876A8 (pt) 2008-10-30 2016-02-10 Merck Sharp & Dohme Composto, composição farmacêutica, uso de um composto, e, método para intensificar a qualidade do sono, para tratar insônia, e para tratar ou controlar obesidade em um paciente mamífero que necessita do mesmo.
CA2741672A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2379547A1 (de) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidinderivate und verfahren zu deren anwendung
US20110243940A1 (en) 2008-12-16 2011-10-06 Schering Corporation Bicyclic pyranone derivatives and methods of use thereof
WO2010114780A1 (en) 2009-04-01 2010-10-07 Merck Sharp & Dohme Corp. Inhibitors of akt activity
JP6073677B2 (ja) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 縮合複素環式化合物およびそれらの使用
EA023838B1 (ru) 2009-10-14 2016-07-29 Мерк Шарп Энд Домэ Корп. ЗАМЕЩЕННЫЕ ПИПЕРИДИНЫ, КОТОРЫЕ ПОВЫШАЮТ АКТИВНОСТЬ p53, И ИХ ПРИМЕНЕНИЕ
WO2011077245A2 (en) * 2009-12-23 2011-06-30 Fondazione Centro San Raffaele Del Monte Tabor Compositions
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
CA2786314A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2791613A1 (en) 2010-03-16 2011-09-22 Dana-Farber Cancer Institute, Inc. Indazole compounds and their uses
EP2584903B1 (de) 2010-06-24 2018-10-24 Merck Sharp & Dohme Corp. Neue heterozyklische verbindungen als erk-hemmer
WO2012018754A2 (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 (de) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. Neue pyrazolo-[1,5-a-]pyrimidinderivate als mtor-hemmer
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2615916B1 (de) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Kondensierte pyrazolderivate als neue erk-hemmer
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
WO2012069605A1 (en) 2010-11-26 2012-05-31 Dr. August Wolff Gmbh & Co. Kg Arzneimittel Novel e,e-diene compounds and their use as medicaments and cosmetics
EP2654748B1 (de) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazolderivate als erk-hemmer
KR101668514B1 (ko) 2011-02-25 2016-10-21 머크 샤프 앤드 돔 코포레이션 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체
AU2012245971A1 (en) 2011-04-21 2013-10-17 Piramal Enterprises Limited A crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
US9023865B2 (en) 2011-10-27 2015-05-05 Merck Sharp & Dohme Corp. 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)
EP3453762B1 (de) 2012-05-02 2021-04-21 Sirna Therapeutics, Inc. Sina-zusammensetzungen
JP2015525782A (ja) 2012-08-02 2015-09-07 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 抗糖尿病性三環式化合物
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｅｒｋ阻害剤である新規化合物
WO2014063068A1 (en) 2012-10-18 2014-04-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063061A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
ME02925B (de) 2012-11-28 2018-04-20 Merck Sharp & Dohme Zusammensetzungen und verfahren zur behandlung von krebs
TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶
EP2951180B1 (de) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8-substituierte purine als hdm2-inhibitoren
RU2015140066A (ru) 2013-02-22 2017-03-30 Мерк Шарп И Доум Корп. Противодиабетические бициклические соединения
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
JP2016514671A (ja) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼのアゴニストおよびその使用
US10011637B2 (en) 2013-06-05 2018-07-03 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase C, method of making and using same
US20160194368A1 (en) 2013-09-03 2016-07-07 Moderna Therapeutics, Inc. Circular polynucleotides
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
WO2015164614A1 (en) 2014-04-23 2015-10-29 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
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
MX2017002610A (es) 2014-08-29 2017-10-11 Tes Pharma S R L INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA.
EP3236959A4 (de) 2014-12-23 2018-04-25 Dana Farber Cancer Institute, Inc. Hemmer der cyclinabhängigen kinase 7 (cdk7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
US20180134667A1 (en) 2016-10-14 2018-05-17 TES Pharma S.r.I. Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
WO2018106518A1 (en) 2016-12-06 2018-06-14 Merck Sharp & Dohme Corp. Antidiabetic heterocyclic compounds
EP3609922A2 (de) 2017-04-13 2020-02-19 Aduro Biotech Holdings, Europe B.V. Anti-sirp-alpha-antikörper
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
US11993602B2 (en) 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833667B1 (de) 2018-08-07 2024-03-13 Merck Sharp & Dohme LLC Prmt5-inhibitoren
MX2021005904A (es) 2018-11-20 2021-09-08 Tes Pharma S R L Inhibidores de la ácido alfa-amino-beta-carboximucónico semialdehído descarboxilasa.
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2021026047A1 (en) 2019-08-08 2021-02-11 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
US20230365533A1 (en) 2020-08-18 2023-11-16 Merck Sharp & Dohme Llc Bicycloheptane pyrrolidine orexin receptor agonists

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2115183A1 (en) 1993-02-12 1994-08-13 Takashi Nomoto Substituted amic acid derivatives
ATE177420T1 (de) * 1993-11-04 1999-03-15 Abbott Lab Cyclobutan-derivate als inhibitoren der squalen- synthetase und der protein-farnesyltransferase

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WO1996033159A1 (en) 1996-10-24
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ATE206390T1 (de) 2001-10-15
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