JP2016500110A5 - - Google Patents

Download PDF

Info

Publication number
JP2016500110A5
JP2016500110A5 JP2015544142A JP2015544142A JP2016500110A5 JP 2016500110 A5 JP2016500110 A5 JP 2016500110A5 JP 2015544142 A JP2015544142 A JP 2015544142A JP 2015544142 A JP2015544142 A JP 2015544142A JP 2016500110 A5 JP2016500110 A5 JP 2016500110A5
Authority
JP
Japan
Prior art keywords
wee1
cancer
pharmaceutically acceptable
acceptable salt
inhibitor
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.)
Granted
Application number
JP2015544142A
Other languages
English (en)
Other versions
JP6290237B2 (ja
JP2016500110A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2013/071377 external-priority patent/WO2014085216A1/en
Publication of JP2016500110A publication Critical patent/JP2016500110A/ja
Publication of JP2016500110A5 publication Critical patent/JP2016500110A5/ja
Application granted granted Critical
Publication of JP6290237B2 publication Critical patent/JP6290237B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Claims (14)

  1. WEE1キナーゼ関連癌と診断された患者の中からWEE1阻害剤で処置される患者の同定を補助するための方法であって、
    (a)前記患者から得られた癌細胞を含む生体試料中の、および対照試料中の、PKMYT1の遺伝子発現レベルを測定し;
    (b)前記患者試料中の前記遺伝子発現レベルが、前記対照試料中の前記遺伝子発現レベルを上回るかまたは下回るかを判定し;
    (c)WEE1阻害剤での処置に対して、前記患者試料からの予測的バイオマーカーのレベルが前記対照試料のレベルを下回る前記患者を選択すること
    を含む方法。
  2. 前記対照試料が、疾患がないかまたはWEE1キナーゼ関連癌と診断されていない1以上の対象から得られる、請求項1に記載の方法。
  3. 前記WEE1阻害剤が、WEE1−1もしくは医薬的に許容可能なその塩またはWEE1−2もしくは医薬的に許容可能なその塩である、請求項1に記載の方法。
  4. 前記WEE1阻害剤が、WEE1−1または医薬的に許容可能なその塩である、請求項3に記載の方法。
  5. 前記WEE1阻害剤が、WEE1−2または医薬的に許容可能なその塩である、請求項3に記載の方法。
  6. WEE1阻害剤での処置に感受性がある癌患者の同定を補助するための方法であって、
    (a)前記患者から得られた癌細胞を含む生体試料中の、および対照試料中の、PKMYT1の遺伝子発現レベルを測定し;
    (b)前記患者試料中の前記遺伝子発現レベルが、前記対照試料中の前記遺伝子発現レベルを上回るかまたは下回るかを判定し;
    (c)WEE1阻害剤での処置に対して、前記患者試料からのPKMYT1のレベルが前記対照試料のレベルを下回る、前記感受性がある患者を選択すること
    を含む方法。
  7. 前記対照試料が、疾患がないかまたはWEE1キナーゼ関連癌と診断されていない1以上の対象から得られる、請求項6に記載の方法。
  8. 前記WEE1阻害剤が、WEE1−1もしくは医薬的に許容可能なその塩またはWEE
    1−2もしくは医薬的に許容可能なその塩である、請求項6に記載の方法。
  9. 前記WEE1阻害剤が、WEE1−1または医薬的に許容可能なその塩である、請求項8に記載の方法。
  10. 前記WEE1阻害剤が、WEE1−2または医薬的に許容可能なその塩である、請求項8に記載の方法。
  11. 前記癌が、乳癌、肺癌、膵臓癌、結腸癌、卵巣癌、急性白血病、慢性リンパ性白血病、慢性骨髄性白血病およびホジキンリンパ腫からなる群から選択されるWEE1キナーゼ関連癌である、請求項6に記載の方法。
  12. WEE1キナーゼ関連癌の処置を必要とするWEE1キナーゼ関連癌患者を処置するためのWEE1阻害剤であって、前記WEE1阻害剤が、WEE1−1もしくは医薬的に許容可能なその塩またはWEE1−2もしくは医薬的に許容可能なその塩であり、処置される前記患者の癌細胞がPKMYT1の低発現を特徴とする、WEE1阻害剤
  13. 前記WEE1阻害剤が、WEE1−1または医薬的に許容可能なその塩である、請求項12に記載のWEE1阻害剤
  14. 生体試験試料中でPKMYT1の発現産物を検出可能な検出剤を含む、WEE1阻害剤での処置に感受性のある癌患者を同定するためのキット。
JP2015544142A 2012-11-28 2013-11-22 癌を処置するための組成物および方法 Active JP6290237B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261730795P 2012-11-28 2012-11-28
US61/730,795 2012-11-28
PCT/US2013/071377 WO2014085216A1 (en) 2012-11-28 2013-11-22 Compositions and methods for treating cancer

Publications (3)

Publication Number Publication Date
JP2016500110A JP2016500110A (ja) 2016-01-07
JP2016500110A5 true JP2016500110A5 (ja) 2017-01-05
JP6290237B2 JP6290237B2 (ja) 2018-03-07

Family

ID=50828365

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015544142A Active JP6290237B2 (ja) 2012-11-28 2013-11-22 癌を処置するための組成物および方法

Country Status (23)

Country Link
US (1) US9655899B2 (ja)
EP (1) EP2925888B1 (ja)
JP (1) JP6290237B2 (ja)
KR (1) KR102161331B1 (ja)
AU (1) AU2013352568B2 (ja)
BR (1) BR112015012295A8 (ja)
CA (1) CA2892361A1 (ja)
CY (1) CY1119676T1 (ja)
DK (1) DK2925888T3 (ja)
ES (1) ES2651347T3 (ja)
HK (1) HK1209798A1 (ja)
HR (1) HRP20180002T1 (ja)
HU (1) HUE035662T2 (ja)
LT (1) LT2925888T (ja)
ME (1) ME02925B (ja)
MX (1) MX363243B (ja)
NO (1) NO2941224T3 (ja)
PL (1) PL2925888T3 (ja)
PT (1) PT2925888T (ja)
RS (1) RS56680B1 (ja)
RU (1) RU2660349C2 (ja)
SI (1) SI2925888T1 (ja)
WO (1) WO2014085216A1 (ja)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AR091424A1 (es) 2012-06-13 2015-02-04 Incyte Corp Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr)
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為fgfr抑制劑之雙環雜環
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MX2017010673A (es) 2015-02-20 2018-03-21 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr).
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
WO2017078752A1 (en) * 2015-11-06 2017-05-11 The Penn State Research Foundation Compositions and methods relating to cancer
US10280348B2 (en) * 2017-01-31 2019-05-07 Prc-Desoto International, Inc. Low density aerospace compositions and sealants
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11299493B2 (en) 2017-10-09 2022-04-12 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
WO2019074981A1 (en) 2017-10-09 2019-04-18 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AND USES THEREOF
CA3099116A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
MA52494A (fr) 2018-05-04 2021-03-10 Incyte Corp Formes solides d'un inhibiteur de fgfr et leurs procédés de préparation
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
AU2020271837A1 (en) 2019-04-09 2021-11-18 Nuvation Bio Inc. Heterocyclic compounds and uses thereof
EP3952878A4 (en) * 2019-04-09 2023-01-04 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AND USES THEREOF
EP3952879A4 (en) * 2019-04-09 2023-01-04 Nuvation Bio Inc. HETEROCYCLIC COMPOUNDS AND USES THEREOF
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
PE20221085A1 (es) 2019-10-14 2022-07-05 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
IL294084A (en) * 2019-12-20 2022-08-01 Recurium Ip Holdings Llc conjunctions
IL294081A (en) * 2019-12-20 2022-08-01 Recurium Ip Holdings Llc conjunctions
KR20230017167A (ko) * 2020-04-01 2023-02-03 엔진 바이오사이언시즈 피티이. 엘티디. 암을 치료하기 위한 방법 및 조성물
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CN113735863A (zh) * 2021-09-29 2021-12-03 武汉九州钰民医药科技有限公司 Wee1抑制剂adavosertib的制备工艺
PT118269A (pt) 2022-10-20 2024-04-22 Univ Aveiro Pkmyt1 for use in regenerative medicine

Family Cites Families (393)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3126375A (en) 1964-03-24 Chioacyl
US2789118A (en) 1956-03-30 1957-04-16 American Cyanamid Co 16-alpha oxy-belta1, 4-pregnadienes
US2990401A (en) 1958-06-18 1961-06-27 American Cyanamid Co 11-substituted 16alpha, 17alpha-substituted methylenedioxy steroids
US3048581A (en) 1960-04-25 1962-08-07 Olin Mathieson Acetals and ketals of 16, 17-dihydroxy steroids
US3749712A (en) 1970-09-25 1973-07-31 Sigma Tau Ind Farmaceuti Triamcinolone acetonide esters and process for their preparation
SE378110B (ja) 1972-05-19 1975-08-18 Bofors Ab
US3996359A (en) 1972-05-19 1976-12-07 Ab Bofors Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith
SE378109B (ja) 1972-05-19 1975-08-18 Bofors Ab
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4294926A (en) 1979-06-15 1981-10-13 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4319039A (en) 1979-06-15 1982-03-09 Merck & Co., Inc. Preparation of ammonium salt of hypocholesteremic fermentation product
US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
JPS5889191A (ja) 1981-11-20 1983-05-27 Sankyo Co Ltd 3−ヒドロキシ−ml−236b誘導体の製造法
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4911165A (en) 1983-01-12 1990-03-27 Ethicon, Inc. Pliabilized polypropylene surgical filaments
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US5525464A (en) 1987-04-01 1996-06-11 Hyseq, Inc. Method of sequencing by hybridization of oligonucleotide probes
US5202231A (en) 1987-04-01 1993-04-13 Drmanac Radoje T Method of sequencing of genomes by hybridization of oligonucleotide probes
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4820850A (en) 1987-07-10 1989-04-11 Merck & Co., Inc. Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
US5030447A (en) 1988-03-31 1991-07-09 E. R. Squibb & Sons, Inc. Pharmaceutical compositions having good stability
US5700637A (en) 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US4916239A (en) 1988-07-19 1990-04-10 Merck & Co., Inc. Process for the lactonization of mevinic acids and analogs thereof
EP0360390A1 (en) 1988-07-25 1990-03-28 Glaxo Group Limited Spirolactam derivatives
GB8822228D0 (en) 1988-09-21 1988-10-26 Southern E M Support-bound oligonucleotides
US5118853A (en) 1988-10-13 1992-06-02 Sandoz Ltd. Processes for the synthesis of 3-disubstituted aminoacroleins
US5290946A (en) 1988-10-13 1994-03-01 Sandoz Ltd. Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes
MX18467A (es) 1988-11-23 1993-07-01 Pfizer Agentes terapeuticos de quinuclidinas
US4929437A (en) 1989-02-02 1990-05-29 Merck & Co., Inc. Coenzyme Q10 with HMG-CoA reductase inhibitors
US5164372A (en) 1989-04-28 1992-11-17 Fujisawa Pharmaceutical Company, Ltd. Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same
US5189164A (en) 1989-05-22 1993-02-23 Sandoz Ltd. Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof
US5744101A (en) 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5143854A (en) 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5527681A (en) 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5547839A (en) 1989-06-07 1996-08-20 Affymax Technologies N.V. Sequencing of surface immobilized polymers utilizing microflourescence detection
US5242974A (en) 1991-11-22 1993-09-07 Affymax Technologies N.V. Polymer reversal on solid surfaces
US5424186A (en) 1989-06-07 1995-06-13 Affymax Technologies N.V. Very large scale immobilized polymer synthesis
US6551784B2 (en) 1989-06-07 2003-04-22 Affymetrix Inc Method of comparing nucleic acid sequences
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
DE3924454A1 (de) 1989-07-24 1991-02-07 Cornelis P Prof Dr Hollenberg Die anwendung von dna und dna-technologie fuer die konstruktion von netzwerken zur verwendung in der chip-konstruktion und chip-produktion (dna chips)
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
FI97540C (fi) 1989-11-06 1997-01-10 Sanofi Sa Menetelmä terapeuttisesti käyttökelpoisten, aromaattisesti substituoitujen piperidiini- ja piperatsiinijohdannaisten valmistamiseksi
FR2654725B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2654726B1 (fr) 1989-11-23 1992-02-14 Rhone Poulenc Sante Nouveaux derives de l'isoindolone et leur preparation.
EP0430881A3 (en) 1989-11-29 1991-10-23 Ciba-Geigy Ag Photochromic compounds, process for their preparation and their use
GB8929070D0 (en) 1989-12-22 1990-02-28 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
US5232929A (en) 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
UA41251C2 (uk) 1990-01-04 2001-09-17 Пфайзер, Інк. Гідровані азотвмісні гетероциклічні сполуки, похідні піперидину, фармацевтична композиція та спосіб пригнічення активності речовини р в організмі
US5321032A (en) 1990-02-15 1994-06-14 Fujisawa Pharmaceutical Co., Ltd. Peptide compounds and pharmaceutical compositions thereof
US5288644A (en) 1990-04-04 1994-02-22 The Rockefeller University Instrument and method for the sequencing of genome
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
CA2084193C (en) 1990-06-01 1998-04-07 John A. Lowe, Iii 3-amino-2-aryl quinuclidines
EP0540526B1 (en) 1990-07-23 1994-12-28 Pfizer Inc. Quinuclidine derivatives
ATE121389T1 (de) 1990-09-28 1995-05-15 Pfizer Ringverknüpfte analoge von stickstoffenthaltenden nichtaromatischen heterocyclen.
GB9023116D0 (en) 1990-10-24 1990-12-05 Fujisawa Pharmaceutical Co Peptide compounds,processes for preparation thereof and pharmaceutical composition comprising the same
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
DE69114117T2 (de) 1990-12-21 1996-03-21 Fujisawa Pharmaceutical Co Neue Verwendung von Peptidderivat.
EP0566589A1 (en) 1991-01-10 1993-10-27 Pfizer Inc. N-alkyl quinuclidinium salts as substance p antagonists
ATE154354T1 (de) 1991-02-11 1997-06-15 Merck Sharp & Dohme Azabicyclische verbindungen, diese enthaltende pharmazeutische zubereitungen und ihre therapeutische verwendung
ATE115581T1 (de) 1991-03-01 1994-12-15 Pfizer 1-azabicyclo(3.2.2>nonan-3-aminderivate.
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
CZ293955B6 (cs) 1991-03-26 2004-08-18 Pfizeráinc Postup přípravy substituovaných piperidinů
FR2677361A1 (fr) 1991-06-04 1992-12-11 Adir Nouveaux peptides et pseudopeptides, derives de tachykinines, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
FR2676055B1 (fr) 1991-05-03 1993-09-03 Sanofi Elf Composes polycycliques amines et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676053B1 (fr) 1991-05-03 1993-08-27 Sanofi Elf Nouveaux composes dialkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant.
FR2676443B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole et leur preparation.
FR2676442B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveau derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2676446B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole, leur preparation et les compositions pharmaceutiques qui les contiennent.
FR2676447B1 (fr) 1991-05-17 1993-08-06 Rhone Poulenc Rorer Sa Nouveaux derives du thiopyranopyrrole et leur preparation.
WO1992020661A1 (en) 1991-05-22 1992-11-26 Merck & Co., Inc. N, n-diacylpiperazines
WO1992020676A1 (en) 1991-05-22 1992-11-26 Pfizer Inc. Substituted 3-aminoquinuclidines
US5807867A (en) 1991-05-31 1998-09-15 Pfizer Inc. Quinuclidine derivatives
GB9113219D0 (en) 1991-06-19 1991-08-07 Fujisawa Pharmaceutical Co Peptide compound,processes for preparation thereof and pharmaceutical composition comprising the same
RU2114848C1 (ru) 1991-06-20 1998-07-10 Пфайзер Инк. Фторалкоксибензиламинные производные азотсодержащих гетероциклов, фармацевтическая композиция, способ ингибирования действия вещества р у млекопитающих
TW202432B (ja) 1991-06-21 1993-03-21 Pfizer
US5288730A (en) 1991-06-24 1994-02-22 Merck Sharp & Dohme Limited Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
EP0536817A1 (en) 1991-07-05 1993-04-14 MERCK SHARP & DOHME LTD. Azabicyclic compounds as tachykinin antagonists
EP0593557B1 (en) 1991-07-05 1996-01-31 MERCK SHARP & DOHME LTD. Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
CA2110514A1 (en) 1991-07-05 1993-01-21 Raymond Baker Aromatic compounds, pharmaceutical compositions containing them and their use in therapy
JPH06509090A (ja) 1991-07-10 1994-10-13 メルク シヤープ エンド ドーム リミテツド 芳香族化合物、それらを含む組成物、及び治療におけるそれらの使用
US5495047A (en) 1991-07-10 1996-02-27 Merck, Sharp & Dohme (Ltd.) Fused tricyclic compounds, pharmaceutical compositions containing them and their use in therapy
MY110227A (en) 1991-08-12 1998-03-31 Ciba Geigy Ag 1-acylpiperindine compounds.
EP0528495A1 (en) 1991-08-20 1993-02-24 Merck Sharp & Dohme Ltd. Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
PT533280E (pt) 1991-09-20 2001-01-31 Glaxo Group Ltd Novas utilizacoes medicas para antagonistas de taquiquinina
US5527808A (en) 1991-09-26 1996-06-18 Pfizer Inc. Fused tricyclic nitrogen containing heterocycles
JP2553020B2 (ja) 1991-11-07 1996-11-13 吉富製薬株式会社 キヌクリジン化合物およびその医薬用途
DK0613458T3 (da) 1991-11-12 1998-02-09 Pfizer Acykliske ethylendiaminderivater som substans P receptorantagonister
US5384261A (en) 1991-11-22 1995-01-24 Affymax Technologies N.V. Very large scale immobilized polymer synthesis using mechanically directed flow paths
US5324633A (en) 1991-11-22 1994-06-28 Affymax Technologies N.V. Method and apparatus for measuring binding affinity
US5412087A (en) 1992-04-24 1995-05-02 Affymax Technologies N.V. Spatially-addressable immobilization of oligonucleotides and other biological polymers on surfaces
CA2083891A1 (en) 1991-12-03 1993-06-04 Angus Murray Macleod Heterocyclic compounds, compositions containing them and their use in therapy
HU9203780D0 (en) 1991-12-12 1993-03-29 Sandoz Ag Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them
GB9200535D0 (en) 1992-01-10 1992-02-26 Fujisawa Pharmaceutical Co New compound
GB9201179D0 (en) 1992-01-21 1992-03-11 Glaxo Group Ltd Chemical compounds
US5328927A (en) 1992-03-03 1994-07-12 Merck Sharpe & Dohme, Ltd. Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them
JP2656702B2 (ja) 1992-03-23 1997-09-24 ファイザー製薬株式会社 ペプチド性キヌクリジン
ATE173767T1 (de) 1992-04-03 1998-12-15 Perkin Elmer Corp Proben zusammensetzung und verfahren
FR2689888B1 (fr) 1992-04-10 1994-06-10 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent.
CA2133077A1 (en) 1992-04-15 1993-10-28 Raymond Baker Azacyclic compounds
GB2266529A (en) 1992-05-01 1993-11-03 Merck Sharp & Dohme Tetrahydroisoquinoline derivatives
DE69331190T2 (de) 1992-05-18 2002-04-18 Pfizer Überbrückte azabicyclische derivate als substanz p antagonisten
GB9211193D0 (en) 1992-05-27 1992-07-08 Merck Sharp & Dohme Therapeutic agents
CA2099233A1 (en) 1992-06-29 1993-12-30 Conrad P. Dorn Morpholine and thiomorpholine tachykinin receptor antagonists
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5719147A (en) 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
AU4713293A (en) 1992-07-13 1994-01-31 Merck Sharp & Dohme Limited Heterocyclic amide derivatives as tachykinin derivatives
EP1251170A3 (en) 1992-07-17 2002-10-30 Ribozyme Pharmaceuticals, Inc. Method and reagent for treatment of NF-kappaB dependent animal diseases
GB2268931A (en) 1992-07-22 1994-01-26 Merck Sharp & Dohme Azabicyclic tachykinin-receptor antagonists
US5561130A (en) 1992-07-28 1996-10-01 Merck Sharp & Dohme Limited Azacyclic compounds
GB2269170A (en) 1992-07-29 1994-02-02 Merck Sharp & Dohme Azatricyclic tachykinin antagonists
AU4718093A (en) 1992-07-31 1994-03-03 Merck Sharp & Dohme Limited Substituted amines as tachykinin receptor antagonists
EP0654029A1 (en) 1992-08-04 1995-05-24 Pfizer Inc. 3-benzylamino-2-phenyl-piperidine derivatives as substance p receptor antagonists
GB9216911D0 (en) 1992-08-10 1992-09-23 Merck Sharp & Dohme Therapeutic agents
CA2140640A1 (en) 1992-08-13 1994-03-03 David C. Horwell Tachykinin antagonists
ATE208376T1 (de) 1992-08-19 2001-11-15 Pfizer Substituierte benzylamin-stickstoff enthaltende nichtaromatische heterocyclen
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
ATE161530T1 (de) 1992-09-04 1998-01-15 Takeda Chemical Industries Ltd Kondensierte heterozyklische verbindungen, deren herstellung und verwendung
WO1994005625A1 (en) 1992-09-10 1994-03-17 Merck Sharp & Dohme Limited Alcohols and ethers with aromatic substituents as tachykinin-antagonists
GB9220286D0 (en) 1992-09-25 1992-11-11 Merck Sharp & Dohme Therapeutic agents
JP2656699B2 (ja) 1992-10-21 1997-09-24 ファイザー製薬株式会社 置換ベンジルアミノキヌクリジン
GB9222262D0 (en) 1992-10-23 1992-12-09 Merck Sharp & Dohme Therapeutic agents
GB9222486D0 (en) 1992-10-26 1992-12-09 Merck Sharp & Dohme Therapeutic agents
WO1994010165A1 (en) 1992-10-28 1994-05-11 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
JP2656700B2 (ja) 1992-10-28 1997-09-24 ファイザー製薬株式会社 置換キヌクリジン誘導体
US5554501A (en) 1992-10-29 1996-09-10 Beckman Instruments, Inc. Biopolymer synthesis using surface activated biaxially oriented polypropylene
US5554627A (en) 1992-10-30 1996-09-10 Merck, Sharp & Dohme Ltd. Tachykinin antagonists
US5503980A (en) 1992-11-06 1996-04-02 Trustees Of Boston University Positional sequencing by hybridization
DE69307340T2 (de) 1992-11-12 1997-04-24 Pfizer Chinuclidin derivat als substanz p antagonist
US5261188A (en) 1992-11-23 1993-11-16 The Standard Products Company Belt weatherstrip with bulb
JP2722279B2 (ja) 1992-12-10 1998-03-04 ファイザー・インク. アミノメチレンで置換した非芳香族複素環式化合物及びサブスタンスpのアンタゴニストとしての使用
US5604260A (en) 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
JPH08504435A (ja) 1992-12-14 1996-05-14 メルク シヤープ エンド ドーム リミテツド タキキニン受容体拮抗剤としての4−アミノメチル/チオメチル/スルホニルメチル−4−フェニルピペリジン
GB9226581D0 (en) 1992-12-21 1993-02-17 Merck Sharp & Dohme Therapeutic agents
CA2111902A1 (en) 1992-12-21 1994-06-22 Jack Beuford Campbell Antitumor compositions and methods of treatment
GB9300051D0 (en) 1993-01-04 1993-03-03 Merck Sharp & Dohme Therapeutic agents
EP0764645A1 (en) 1993-01-15 1997-03-26 G.D. Searle & Co. Novel 3,4-diaryl furans and analogs thereof having use as anti-inflammatory agents
EP0610793A1 (en) 1993-02-08 1994-08-17 Takeda Chemical Industries, Ltd. Tetracyclic morpholine derivatives and their use or analgesics
CA2152925A1 (en) 1993-02-18 1994-09-01 Raymond Baker Azacyclic compounds compositions containing them and their use as tachykinin antagonists
AU6140694A (en) 1993-02-22 1994-09-14 Merck Sharp & Dohme Limited Aromatic compounds, compositions containing them and their use in therapy
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
US5298627A (en) 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5688806A (en) 1993-03-04 1997-11-18 Pfizer Inc. Spiroazacyclic derivatives as substance P antagonists
US5409944A (en) 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
DE4311230C2 (de) 1993-04-02 1996-12-19 Mannesmann Ag Nicht-spurgebundenes Fahrzeug mit Elektromotor
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
US5496833A (en) 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
WO1994026735A1 (en) 1993-05-06 1994-11-24 Merrell Dow Pharmaceuticals Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines useful as tachykinin antagonists
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
IL109646A0 (en) 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
US5380738A (en) 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
EP0702681A1 (en) 1993-06-07 1996-03-27 Merck & Co. Inc. Spiro-substituted azacycles as neurokinin antagonists
US5436265A (en) 1993-11-12 1995-07-25 Merck Frosst Canada, Inc. 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents
GB9602877D0 (en) 1996-02-13 1996-04-10 Merck Frosst Canada Inc 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5837832A (en) 1993-06-25 1998-11-17 Affymetrix, Inc. Arrays of nucleic acid probes on biological chips
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
DE69413822T2 (de) 1993-07-15 1999-02-25 Pfizer Benzyloxychinuclidine als substanz p antagonisten
GB9315808D0 (en) 1993-07-30 1993-09-15 Merck Sharp & Dohme Therapeutic agents
TW365603B (en) 1993-07-30 1999-08-01 Rhone Poulenc Rorer Sa Novel perhydroisoindole derivatives, their preparation and pharmaceutical compositions which contain them
GB9317987D0 (en) 1993-08-26 1993-10-13 Glaxo Group Ltd Chemical compounds
DE69433744T2 (de) 1993-09-17 2004-10-14 Pfizer Inc. 3-amino-5-carboxy-substituierte piperidine und 3-amino-4-carboxy-substituierte pyrrolidine als tachykinin-antagonisten
US5703065A (en) 1993-09-17 1997-12-30 Pfizer Inc. Heteroarylamino and heteroarylsulfonamido substituted 3-benyzlaminomethyl piperidines and related compounds
IL111002A (en) 1993-09-22 1998-09-24 Glaxo Group Ltd History of piperidine, their preparation and the pharmaceutical preparations containing them
US5728830A (en) 1993-09-22 1998-03-17 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
PT723538E (pt) 1993-10-15 2002-05-31 Schering Corp Compostos triciclicos de carbamato uteis para a ainibicao da funcao da proteina g e para o tratamento de doencas proliferativas
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
NZ275646A (en) 1993-10-15 1998-02-26 Schering Corp Tricyclic sulphonamide derivatives and medicaments
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5470710A (en) 1993-10-22 1995-11-28 University Of Utah Automated hybridization/imaging device for fluorescent multiplex DNA sequencing
US5472672A (en) 1993-10-22 1995-12-05 The Board Of Trustees Of The Leland Stanford Junior University Apparatus and method for polymer synthesis using arrays
ES2157994T3 (es) 1993-10-25 2001-09-01 Parke Davis & Co Inhibidores tetra y pentapeptidos sustituidos de la proteina farnesiltransferasa.
US6156501A (en) 1993-10-26 2000-12-05 Affymetrix, Inc. Arrays of modified nucleic acid probes and methods of use
AU7947594A (en) 1993-10-27 1995-05-22 Merck Sharp & Dohme Limited Substituted amides as tachykinin antagonists
US5429807A (en) 1993-10-28 1995-07-04 Beckman Instruments, Inc. Method and apparatus for creating biopolymer arrays on a solid support surface
US5344991A (en) 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
EP0677039B1 (en) 1993-11-04 1999-03-10 Abbott Laboratories Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
AU681454B2 (en) 1993-11-05 1997-08-28 Warner-Lambert Company Substituted DI- and tripeptide inhibitors of protein:farnesyl transferase
US6403577B1 (en) 1993-11-17 2002-06-11 Eli Lilly And Company Hexamethyleneiminyl tachykinin receptor antagonists
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
IT1271462B (it) 1993-12-03 1997-05-28 Menarini Farma Ind Antagonisti delle tachichinine,procedimento per la loro preparazione e loro impiego in formulazioni farmaceutiche.
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
EP0736007A4 (en) 1993-12-21 1997-03-19 Lilly Co Eli NON-PEPTIDE ANTAGONISTS OF TACHYKININ RECEPTORS
DK0737192T3 (da) 1993-12-29 2001-11-26 Merck Sharp & Dohme Substituerede morpholinderivater og deres anvendelse som terapeutiske midler
WO1995018129A1 (en) 1993-12-29 1995-07-06 Pfizer Inc. Diazabicyclic neurokinin antagonists
AU685212B2 (en) 1994-01-13 1998-01-15 Merck Sharp & Dohme Limited Gem-disubstituted azacyclic tachykinin antagonists
JPH09508376A (ja) 1994-01-28 1997-08-26 メルク シヤープ エンド ドーム リミテツド アラルキル置換アザシクロ系の治療薬
US5393790A (en) 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
US5631734A (en) 1994-02-10 1997-05-20 Affymetrix, Inc. Method and apparatus for detection of fluorescently labeled materials
GB9402688D0 (en) 1994-02-11 1994-04-06 Merck Sharp & Dohme Therapeutic agents
US5610165A (en) 1994-02-17 1997-03-11 Merck & Co., Inc. N-acylpiperidine tachykinin antagonists
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
WO1995024612A1 (de) 1994-03-07 1995-09-14 International Business Machines Corporation Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper
HUT77406A (hu) 1994-03-15 1998-04-28 Eisai Co., Ltd., 1-(4-Amino-5-tio-pent-2-en)-il oldalláncot tartalmazó peptidomimetikumok és az ezeket tartalmazó gyógyszerkészítmények
FR2718136B1 (fr) 1994-03-29 1996-06-21 Sanofi Sa Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant.
IL113196A0 (en) 1994-03-31 1995-06-29 Bristol Myers Squibb Co Imidazole derivatives and pharmaceutical compositions containing the same
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5610145A (en) 1994-04-15 1997-03-11 Warner-Lambert Company Tachykinin antagonists
EP0694535A1 (en) 1994-04-29 1996-01-31 Eli Lilly And Company Non-peptidyl tachykinin receptor antagonists
CA2189141A1 (en) 1994-05-05 1995-11-16 Karen Elizabeth Haworth Morpholine derivatives and their use as antagonists of tachikinins
RO115355B1 (ro) 1994-05-07 2000-01-28 Boehringer Ingelheim Kg Derivati de aminoacizi
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5571639A (en) 1994-05-24 1996-11-05 Affymax Technologies N.V. Computer-aided engineering system for design of sequence arrays and lithographic masks
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
JPH10501228A (ja) 1994-06-06 1998-02-03 ワーナー−ランバート・コンパニー タキキニン(nk▲下1▼)受容体アンタゴニスト
CA2150992A1 (en) 1994-06-10 1995-12-11 Philip Arthur Hipskind Cyclohexyl tachykinin receptor antagonists
CN1150419A (zh) 1994-06-10 1997-05-21 罗纳-布朗克罗莱尔股份有限公司 新的法呢基转移酶抑制剂、其制法及其药物组合物
US5807522A (en) 1994-06-17 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods for fabricating microarrays of biological samples
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
HUT77948A (hu) 1994-07-12 1998-12-28 Eli Lilly And Co., Heterociklusos tachikinin-receptor antagonisták
CA2154116A1 (en) 1994-07-22 1996-01-23 Philip Arthur Hipskind 1-aryl-2-acetamidopentanone derivatives for use as tachykinin receptor antagonists
GB9415997D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9415996D0 (en) 1994-08-08 1994-09-28 Merck Sharp & Dohme Therapeutic agents
TW432061B (en) 1994-08-09 2001-05-01 Pfizer Res & Dev Lactams
WO1996005529A1 (en) 1994-08-09 1996-02-22 Micron Optics, Inc. Temperature compensated fiber fabry-perot filters
EP0776884B1 (en) 1994-08-11 2000-01-05 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
AU3192495A (en) 1994-08-12 1996-03-07 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
WO1996005181A1 (en) 1994-08-15 1996-02-22 Merck Sharp & Dohme Limited Morpholine derivatives and their use as therapeutic agents
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
DE4429653C2 (de) 1994-08-20 1997-04-03 Anton Dr More Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl
NZ292683A (en) 1994-08-25 1998-07-28 Merrell Pharma Inc Piperidine derivatives
EP0699655B1 (en) 1994-08-29 1997-09-24 Akzo Nobel N.V. Process for the preparation of quaternary diesters
GB9417956D0 (en) 1994-09-02 1994-10-26 Merck Sharp & Dohme Therapeutic agents
GB9418545D0 (en) 1994-09-15 1994-11-02 Merck Sharp & Dohme Therapeutic agents
US5457107A (en) 1994-09-16 1995-10-10 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
WO1996010562A1 (en) 1994-09-30 1996-04-11 Novartis Ag 1-acyl-4-aliphatylaminopiperidine compounds
TW397825B (en) 1994-10-14 2000-07-11 Novartis Ag Aroyl-piperidine derivatives
FR2725986B1 (fr) 1994-10-21 1996-11-29 Adir Nouveaux derives de piperidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5556752A (en) 1994-10-24 1996-09-17 Affymetrix, Inc. Surface-bound, unimolecular, double-stranded DNA
DE69534213T2 (de) 1994-10-25 2006-01-12 Astrazeneca Ab Therapeutisch wirksame Heterocyclen
GB9421709D0 (en) 1994-10-27 1994-12-14 Zeneca Ltd Therapeutic compounds
JP4319251B2 (ja) 1994-11-22 2009-08-26 エヌエックスピー ビー ヴィ 半導体素子を有し導体トラックが形成されている基板が接着層により結合されている支持本体を有する半導体装置
CA2162786A1 (en) 1994-11-22 1996-05-23 Philip Arthur Hipskind Heterocyclic tachykinin receptor antagonists
FR2727411B1 (fr) 1994-11-30 1997-01-03 Rhone Poulenc Rorer Sa Nouveaux derives de perhydroisoindole, leur preparation et les compositions pharmaceutiques qui les contiennent
JPH10510261A (ja) 1994-12-09 1998-10-06 ワーナー−ランバート・カンパニー タンパク質:ファルネシルトランスフェラーゼの置換テトラーおよびペンタペプチド阻害剤
IL116323A0 (en) 1994-12-13 1996-03-31 Sandoz Ag Tachykinin antagonists their preparation and pharmaceutical compositions containing them
GB9426103D0 (en) 1994-12-23 1995-02-22 Merck Sharp & Dohme Therapeutic agents
CN1176652A (zh) 1995-01-09 1998-03-18 马格拉国际有限公司 胶乳表面的耐磨图象印刷
EP0802912B1 (en) 1995-01-12 2004-10-13 Glaxo Group Limited Piperidine derivatives having tachykinin antagonist activity
AU4915796A (en) 1995-01-12 1996-07-31 University Of Pittsburgh Inhibitors of prenyl transferases
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2729951B1 (fr) 1995-01-30 1997-04-18 Sanofi Sa Nouveaux composes heterocycliques, procede pour leur preparation et compositions pharmaceutiques en contenant
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
GB9505491D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
GB9505492D0 (en) 1995-03-18 1995-05-03 Merck Sharp & Dohme Therapeutic agents
US5554641A (en) 1995-03-20 1996-09-10 Horwell; David C. Nonpeptides as tachykinin antagonists
GB9505692D0 (en) 1995-03-21 1995-05-10 Glaxo Group Ltd Chemical compounds
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
DE69628484T2 (de) 1995-03-24 2004-05-19 Takeda Chemical Industries, Ltd. Zyklische Verbindungen, ihre Herstellung und ihre Verwendung als Tachykininrezeptorantagonisten
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
US5565568A (en) 1995-04-06 1996-10-15 Eli Lilly And Company 2-acylaminopropanamides as tachykinin receptor antagonists
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
WO1996031501A1 (en) 1995-04-07 1996-10-10 Schering Corporation Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
HUP9802036A3 (en) 1995-04-13 1999-06-28 Aventis Pharmaceuticals Inc Br Novel substituted piperazine derivatives having tachykinin receptor antagonists activity, process for producing them an pharmaceutical compositions containing them
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
US5624711A (en) 1995-04-27 1997-04-29 Affymax Technologies, N.V. Derivatization of solid supports and methods for oligomer synthesis
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
AU706021B2 (en) 1995-05-25 1999-06-03 Fujisawa Pharmaceutical Co., Ltd. Piperazine derivatives
US5545531A (en) 1995-06-07 1996-08-13 Affymax Technologies N.V. Methods for making a device for concurrently processing multiple biological chip assays
WO1997000252A1 (en) 1995-06-16 1997-01-03 Warner-Lambert Company Tricyclic inhibitors of protein farnesyltransferase
GB9513117D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513118D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
GB9513121D0 (en) 1995-06-28 1995-08-30 Merck Sharp & Dohme Therapeutic agents
DE69612003T2 (de) 1995-07-07 2001-06-21 Pfizer Substituierte benzolaktamverbindungen als substanz-p-antagonisten
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
AT402617B (de) 1995-07-11 1997-07-25 Datacon Schweitzer & Zeindl Gm Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
US5569588A (en) 1995-08-09 1996-10-29 The Regents Of The University Of California Methods for drug screening
TW340842B (en) 1995-08-24 1998-09-21 Pfizer Substituted benzylaminopiperidine compounds
US5661028A (en) 1995-09-29 1997-08-26 Lockheed Martin Energy Systems, Inc. Large scale DNA microsequencing device
US6020343A (en) 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
WO1997014671A1 (en) 1995-10-18 1997-04-24 Merck & Co., Inc. Cyclopentyl tachykinin receptor antagonists
PT873123E (pt) 1995-11-06 2003-08-29 Univ Pittsburgh Inibidores de proteina-isoprenil-transferase
DE19541283A1 (de) 1995-11-06 1997-05-07 Boehringer Ingelheim Kg Neue Aminosäurederivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
GB9523244D0 (en) 1995-11-14 1996-01-17 Merck Sharp & Dohme Therapeutic agents
DE59609305D1 (de) 1995-11-17 2002-07-11 Biotechnolog Forschung Gmbh Epothilon-Derivate und deren Herstellung
CA2238081A1 (en) 1995-11-22 1997-05-29 S. Jane Desolms Inhibitors of farnesyl-protein transferase
JP2000500760A (ja) 1995-11-23 2000-01-25 メルク シヤープ エンド ドーム リミテツド スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用
GB9524157D0 (en) 1995-11-25 1996-01-24 Pfizer Ltd Therapeutic agents
RU2135494C1 (ru) 1995-12-01 1999-08-27 Санкио Компани Лимитед Гетероциклические соединения и композиция на их основе, проявляющая антагонистическое действие в отношении рецепторов тахикинина
ES2175137T3 (es) 1995-12-08 2002-11-16 Janssen Pharmaceutica Nv Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de laproteina farnesil-transferasa.
GB9525296D0 (en) 1995-12-11 1996-02-07 Merck Sharp & Dohme Therapeutic agents
US6022963A (en) 1995-12-15 2000-02-08 Affymetrix, Inc. Synthesis of oligonucleotide arrays using photocleavable protecting groups
PL185597B1 (pl) 1995-12-22 2003-06-30 Schering Corp Tricykliczne amidy, środek farmaceutyczny i ich zastosowania
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
US5744349A (en) * 1996-03-05 1998-04-28 Washington University DNA sequences encoding human Myt1 kinase
WO1997038665A2 (en) 1996-04-03 1997-10-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AP1009A (en) 1996-04-12 2001-09-21 Searle & Co Substituted benzenesulfonamide derivatives as products of COX-2 inhibitors.
GEP20012500B (en) 1996-05-22 2001-07-25 Warner Lambert Co Inhibitors of Protein Farnesyl Transferase
AU709409B2 (en) 1996-07-15 1999-08-26 Bristol-Myers Squibb Company Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
US5861419A (en) 1996-07-18 1999-01-19 Merck Frosst Canad, Inc. Substituted pyridines as selective cyclooxygenase-2 inhibitors
US6020194A (en) * 1996-10-04 2000-02-01 California Institute Of Technology DNA encoding a Myt1 polypeptide
WO1999001124A1 (en) 1996-12-03 1999-01-14 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
WO1998029119A1 (en) 1996-12-30 1998-07-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP1003374A4 (en) 1996-12-30 2000-05-31 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
ID29970A (id) 1998-11-23 2001-10-25 Novartis Ag Metode untuk mengobati penyakit neovaskuler okuler
EP1151002A4 (en) 1999-01-29 2002-05-02 Imclone Systems Inc KDR-SPECIFIC ANTIBODIES AND USES THEREOF
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
EP1187633A4 (en) 1999-04-08 2005-05-11 Arch Dev Corp USE OF ANTI-VEGF ANTIBODY FOR INCREASING IRRADIATION IN CANCER THERAPY
US6077674A (en) 1999-10-27 2000-06-20 Agilent Technologies Inc. Method of producing oligonucleotide arrays with features of high purity
AU2001240861B2 (en) 2000-03-20 2006-03-30 Merck Frosst Canada Ltd Sulphonamido-substituted bridged bicycloalkyl derivatives
GB0012671D0 (en) 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
GB0025173D0 (en) 2000-10-13 2000-11-29 Merck Sharp & Dohme Therapeutic agents
JP3880051B2 (ja) 2000-11-02 2007-02-14 メルク シャープ エンド ドーム リミテッド γ−セクレターゼ阻害剤としてのスルファミド
UA74849C2 (en) 2000-11-17 2006-02-15 Lilly Co Eli Lactam
GB0108592D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
GB0108591D0 (en) 2001-04-05 2001-05-23 Merck Sharp & Dohme Therapeutic agents
US6958334B2 (en) 2001-04-10 2005-10-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
EP1379251B1 (en) 2001-04-10 2008-07-09 Merck & Co., Inc. Inhibitors of akt activity
AU2002251266A1 (en) 2001-04-10 2002-10-28 Merck Sharp And Dohme Limited Inhibitors of akt activity
JP2004527531A (ja) 2001-04-10 2004-09-09 メルク エンド カムパニー インコーポレーテッド 癌を治療する方法
GB0119152D0 (en) 2001-08-06 2001-09-26 Merck Sharp & Dohme Therapeutic agents
WO2003013526A1 (en) 2001-08-08 2003-02-20 Merck & Co. Inc. Anticoagulant compounds
EA006225B1 (ru) 2001-08-21 2005-10-27 Мерк Шарп Энд Домэ Лимитед Новые циклогексилсульфоны
WO2003032809A2 (en) 2001-10-15 2003-04-24 The Medstar Research Institute Modulation of akt-dependent response to prevent restenosis
AU2002346882A1 (en) 2001-10-26 2003-05-06 Novartis Ag Methods for the treatment of osteoarthritis and compositions thereof
CA2465491A1 (en) 2001-11-07 2003-05-15 Merck & Co., Inc. Mitotic kinesin inhibitors
ATE424388T1 (de) 2001-12-06 2009-03-15 Merck & Co Inc Mitotische kinesinhemmer
WO2003050122A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
ATE447577T1 (de) 2001-12-06 2009-11-15 Merck & Co Inc Mitotische kinesin-hemmer
DE60232994D1 (de) 2001-12-06 2009-08-27 Merck & Co Inc Inhibitoren von mitotischem kinesin
WO2003050064A2 (en) 2001-12-06 2003-06-19 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003105855A1 (en) 2002-01-11 2003-12-24 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003079973A2 (en) 2002-03-08 2003-10-02 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1494676B1 (en) 2002-04-08 2013-05-08 Merck Sharp & Dohme Corp. Fused quinoxaline derivatives as inhibitors of akt activity
WO2003086394A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
EP1496906A4 (en) 2002-04-08 2006-05-03 Merck & Co Inc INHIBITORS OF AKT ACTIVITY
CA2481229C (en) 2002-04-08 2010-09-21 Merck & Co., Inc. Substituted pyrazine inhibitors of akt
US20060142178A1 (en) 2002-04-08 2006-06-29 Barnett Stanley F Method of treating cancer
GB0209991D0 (en) 2002-05-01 2002-06-12 Merck Sharp & Dohme Therapeutic agents
GB0209995D0 (en) 2002-05-01 2002-06-12 Merck Sharp & Dohme Therapeutic agents
GB0209997D0 (en) 2002-05-01 2002-06-12 Merck Sharp & Dohme Therapeutic agents
EP1503998B1 (en) 2002-05-01 2009-07-01 MERCK SHARP & DOHME LTD. Heteroaryl substituted spirocyclic sufamides for inhibition of gamma secretase
EP1509507A4 (en) 2002-05-23 2006-09-13 Merck & Co Inc INHIBITORS OF MITOTIC KINESIN
JP2006506401A (ja) 2002-05-23 2006-02-23 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害薬
US7301028B2 (en) 2002-06-14 2007-11-27 Merck & Co., Inc. Mitotic kinesin inhibitors
GB0223040D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
WO2004037171A2 (en) 2002-10-18 2004-05-06 Merck & Co., Inc. Mitotic kinesin inhibitors
JP2006507299A (ja) 2002-10-30 2006-03-02 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害薬
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
GB0225475D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
GB0225474D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
EP1585391A4 (en) 2002-12-06 2006-03-15 Pharmacia Corp MITONEET POLYPEPTIDES FROM MITOCHONDRIUM MEMBRANES, MODULATORS THEREOF, AND METHOD OF USE THEREOF
WO2004058148A2 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1578724A4 (en) 2002-12-20 2006-11-29 Merck & Co Inc INHIBITORS OF MITOTIC KINESINE
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
CN1809354A (zh) 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
WO2004096135A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
WO2004096129A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
WO2004096130A2 (en) 2003-04-24 2004-11-11 Merck & Co., Inc. Inhibitors of akt activity
EP1638951B1 (en) 2003-05-16 2008-02-13 MERCK SHARP & DOHME LTD. Cyclohexyl sulphones as gamma-secretase inhibitors
WO2004112699A2 (en) 2003-06-12 2004-12-29 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2475189C (en) 2003-07-17 2009-10-06 At&T Corp. Method and apparatus for window matching in delta compressors
KR100536215B1 (ko) 2003-08-05 2005-12-12 삼성에스디아이 주식회사 플라즈마 디스플레이 패널
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
US7307085B2 (en) 2003-08-13 2007-12-11 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2005017190A2 (en) 2003-08-15 2005-02-24 Merck & Co., Inc. Mitotic kinesin inhibitors
JP4773961B2 (ja) 2003-08-15 2011-09-14 メルク・シャープ・エンド・ドーム・コーポレイション 有糸分裂キネシン阻害薬
JP2007502773A (ja) 2003-08-15 2007-02-15 メルク エンド カムパニー インコーポレーテッド 有糸分裂キネシン阻害薬
PE20050730A1 (es) 2003-08-15 2005-09-20 Merck & Co Inc Derivados de 2,5-dihidropirrol 2,2-disustituidos como inhibidores de quinesinas mitoticas
US7514459B2 (en) 2003-09-24 2009-04-07 Merck Sharp & Dohme Ltd. Gamma-secretase inhibitors
US7294640B2 (en) 2004-02-06 2007-11-13 Merck & Co., Inc. Mitotic kinesin inhibitors
CA2561311A1 (en) 2004-04-09 2005-10-27 Merck & Co., Inc. Inhibitors of akt activity
EP1737861A4 (en) 2004-04-09 2010-04-28 Merck Sharp & Dohme INHIBITORS OF AKT ACTIVITY
WO2006091395A2 (en) 2005-02-14 2006-08-31 Merck & Co., Inc. Inhibitors of akt activity
JP2008535915A (ja) 2005-04-12 2008-09-04 メルク エンド カムパニー インコーポレーテッド Akt活性の阻害剤
MX2007015578A (es) 2005-06-10 2008-03-06 Merck & Co Inc Inhibidores de la actividad akt.
JP5537034B2 (ja) 2005-12-23 2014-07-02 ナノストリング テクノロジーズ,インコーポレーテッド ナノレポーターならびにその作製方法および使用方法
PE20080695A1 (es) * 2006-04-27 2008-06-28 Banyu Pharma Co Ltd Derivados de dihidropirazolopirimidinona como inhibidores de quinasa weel
JP5411847B2 (ja) * 2007-04-25 2014-02-12 Msd株式会社 Weelキナーゼインヒビターとしてのジヒドロピラゾロピリミジノン誘導体の多形
KR20100024932A (ko) 2007-06-15 2010-03-08 반유 세이야꾸 가부시끼가이샤 비사이클로아닐린 유도체
ES2430053T3 (es) 2008-06-12 2013-11-18 Merck Sharp & Dohme Corp. Procedimiento para producir derivados de bicicloanilina
DK2477628T3 (en) * 2009-09-15 2014-11-24 Merck Sharp & Dohme Preparation of crystalline hemihydratformer of dihydropyrazolopyrimidinon
RU2627841C2 (ru) * 2010-11-16 2017-08-14 Эррэй Биофарма Инк. Комбинация ингибиторов чекпойнт-киназы 1 и ингибиторов киназы wee 1
US9345705B2 (en) * 2011-09-15 2016-05-24 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer

Similar Documents

Publication Publication Date Title
JP2016500110A5 (ja)
RU2015125575A (ru) Композиции и способы для лечения злокачественной опухоли
JP2014144959A5 (ja)
Hu et al. The plasma lncRNA acting as fingerprint in non-small-cell lung cancer
Gao et al. Long non-coding RNA UCA1 may be a novel diagnostic and predictive biomarker in plasma for early gastric cancer
WO2014140933A8 (en) Method for the prognosis and treatment of cancer metastasis
WO2016094330A3 (en) Methods and machine learning systems for predicting the liklihood or risk of having cancer
JP2014529405A5 (ja)
JP2017503481A5 (ja)
Li et al. Identification of circulating MicroRNAs as novel potential biomarkers for hepatocellular carcinoma detection: a systematic review and meta-analysis
GB2552267A (en) Detection and treatment of disease exhibiting disease cell heterogeneity and systems and methods for communicating test results
WO2016046640A3 (en) Methods for predicting drug responsiveness
BR112015018213A8 (pt) métodos para determinar a síndrome da angústia respiratória aguda (ards) e para monitorar o desenvolvimento desta e kit para diagnóstico".
JP2016507233A5 (ja)
JP2018509934A5 (ja)
RU2014112350A (ru) Способ детекции нуклеосом, содержащих нуклеотиды
JP2009538607A5 (ja)
RU2018101257A (ru) Способ детекции нуклеосом, содержащих гистоновые варианты
JP2016118568A5 (ja)
WO2014184679A3 (en) Method for the prognosis and treatment of renal cell carcinoma metastasis
JP2013503617A5 (ja)
JP2015526074A5 (ja)
WO2017025617A8 (en) Method for the quantification of faecalibacterium prausnitzii phylogroup i and/or phylogroup ii members and the use thereof as biomarkers
RU2016107954A (ru) Способы идентификации и прогнозирования риска сердечно-сосудистого события или заболевания, или смертельного исхода, способы оценки тяжести и мониторинга сердечно-сосудистого события или заболевания, способ мониторинга эффективности терапии
WO2015077382A3 (en) Combined cytology and molecular testing for early detection of esophageal adenocarcinoma