ES2175137T3 - Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de laproteina farnesil-transferasa. - Google Patents

Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de laproteina farnesil-transferasa.

Info

Publication number
ES2175137T3
ES2175137T3 ES96934727T ES96934727T ES2175137T3 ES 2175137 T3 ES2175137 T3 ES 2175137T3 ES 96934727 T ES96934727 T ES 96934727T ES 96934727 T ES96934727 T ES 96934727T ES 2175137 T3 ES2175137 T3 ES 2175137T3
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Spain
Prior art keywords
rent
hydrogen
halo
amino
farnesil
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 - Lifetime
Application number
ES96934727T
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English (en)
Inventor
Marc Gaston Venet
Patrick Rene Angibaud
Philippe Muller
Gerard Charles Sanz
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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Publication of ES2175137T3 publication Critical patent/ES2175137T3/es
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Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

LA INVENCION SE REFIERE A NUEVOS COMPUESTOS DE FORMULA (I), DONDE LA LINEA DISCONTINUA REPRESENTA UN ENLACE OPCIONAL; X ES OXIGENO O AZUFRE; R1 ES HIDROGENO, ALQUILO C1 C12 , AR1 , AR2 ALQUILO C1-C6 , QU INOLINIL ALQUILO C1-C6 , PIRIDIL ALQUILO C1-C6 , HIDROXI ALQUILO C1-C6 , ALQUILOXI C1-C6 ALQUILO C1-C6 , MONO-O DI(ALQUILO C1-C6) AMINO ALQUILO C1-C6 O UN RADICAL DE FORMULA-ALK 1-S(O) 2-R9 ; RSUP,2 , R3 Y R16 , CADA UNO INDEPENDIENTEMENTE, SON HIDROGENO, HIDROXILO, HALO, CIANO, ALQUILO C1-C6 , ALQUILOXI C1-C6 , HIDROXI ALQUILOXI C1 C6 , ALQUILOXI C1-C6 ALQUILOXI C1 C6 , AMINO ALQUILOXI C1-C6 , MONO- O DI-(ALQUIL C1-C6 AMINO ALQUILOXI C1-C6 , AR1 , AR2 ALQUILO C1-C6 , AR2 OXI, AR2 ALQUILOXI C1-C6 , HIDROXICARBONIL ALQUILOXICARBONIL C1-C6 , TRIHALOMETILO, TRIHALOMETOXI, ALQUENILO C2-C6 ; R4 Y R5 SON CADA UNO IND EPENDIENTEMENTE HIDROGENO, HALO, AR1 , ALQUILO C1 C6 , HIDROXI ALQUILO C1-C6 , ALQUILOXI CSUB ,1-C6 ALQUILO C1-C6 , ALQUILOXI C1-C6 , ALQUILTIO C1-C6 , AMINO, HIDROXICARBONILO, ALQUILOXICARBONILO C1-C6 , ALQUIL C1-C6 S(O) ALQUILO C1-C6 O ALQUILO C1-C6 S(O) 2 ALQUILO C1 C6 ; R6 Y R7 SON CADA UNO INDEPENDIENTEMENTE HIDROGENO, HALO, CIANO, ALQUILO C1-C6 , 4, 4 DIMETIL-OXAZOLILO, ALQUILOXI C1-C6 O AR2 OXI; R8 ES HIDROGENO, ALQUILO C1-C6 , CIANO, HIDROXICARBONILO, ALQUILOXICARBONILO C1-C6 , ALQUILCARBONILO C1-C6 ALQUILO C1-C6 , CIANO ALQUILO C1-C6 , ALQUILOXICARBONILO C1 C6 ALQUILO C1-C6 , CARBOXI ALQUILO C1 C6 , HIDROXI ALQUIL C1-C6 AMINO ALQUILO C1-C6 , MONO- O DI(ALQUIL C1-C6 )AMINO ALQUILO C1-C6, IMIDAZOLILO, HALO ALQUILO C1 C6 , ALQUILOXI CSU B,1-C6 ALQUILO C1 C6 , AMINOCARBONIL ALQUILO C1-C6 O UN RADICAL DE FORMULA-O-R10 ,-S-R10 ,-N R11 R12 ; R17 ES HIDROGENO, HALO, CIANO, ALQUILO C1-C6 , ALQUILOXICARBONI LO C1-C6 , AR1 ; R18 ES HIDROGENO, ALQUILO C1-C6 , ALQUILOXI C1-C6 O HALO; R19 ES HIDROGENO O ALQUILO C1-C6 . DICHOS COMPUESTOS PRESENTAN ACTIVIDAD INHIBIDORA DE LA FARNESIL TRANSFERASA. SE DESCRIBE ASIMISMO SU PREPARACION, COMPOSICIONES QUE LOS CONTIENEN Y SU UTILIZACION COMO MEDICAMENTO.
ES96934727T 1995-12-08 1996-10-16 Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de laproteina farnesil-transferasa. Expired - Lifetime ES2175137T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP95203427 1995-12-08

Publications (1)

Publication Number Publication Date
ES2175137T3 true ES2175137T3 (es) 2002-11-16

Family

ID=8220926

Family Applications (2)

Application Number Title Priority Date Filing Date
ES96934727T Expired - Lifetime ES2175137T3 (es) 1995-12-08 1996-10-16 Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de laproteina farnesil-transferasa.
ES01202750T Expired - Lifetime ES2260156T3 (es) 1995-12-08 1996-10-16 Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de la proteina farnesil-transferasa.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES01202750T Expired - Lifetime ES2260156T3 (es) 1995-12-08 1996-10-16 Derivados de (imidazol-5-il)metil-2-quinolinona como inhibidores de la proteina farnesil-transferasa.

Country Status (36)

Country Link
US (3) US6037350A (es)
EP (2) EP1162201B1 (es)
JP (1) JP3257559B2 (es)
KR (1) KR100272676B1 (es)
CN (1) CN1101392C (es)
AP (1) AP1108A (es)
AR (1) AR004992A1 (es)
AT (2) ATE321757T1 (es)
AU (1) AU711142B2 (es)
BG (1) BG62615B1 (es)
BR (1) BR9610745A (es)
CA (1) CA2231105C (es)
CY (1) CY2289B1 (es)
CZ (1) CZ293296B6 (es)
DE (2) DE69620445T2 (es)
DK (2) DK1162201T3 (es)
EA (1) EA000710B1 (es)
EE (1) EE03484B1 (es)
ES (2) ES2175137T3 (es)
HK (2) HK1012188A1 (es)
HR (1) HRP960576B1 (es)
HU (1) HU221227B1 (es)
IL (1) IL123568A (es)
MX (1) MX9802068A (es)
MY (1) MY114444A (es)
NO (1) NO314036B1 (es)
NZ (1) NZ320244A (es)
PL (1) PL184171B1 (es)
PT (2) PT865440E (es)
SI (2) SI1162201T1 (es)
SK (1) SK283335B6 (es)
TR (1) TR199800825T2 (es)
TW (1) TW494101B (es)
UA (1) UA57717C2 (es)
WO (1) WO1997021701A1 (es)
ZA (1) ZA9610254B (es)

Families Citing this family (225)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
DE69807222T2 (de) 1997-06-02 2003-04-17 Janssen Pharmaceutica Nv (imidazol-5-yl)methyl-2-quinolinone derivativen als inhibitoren von proliferation der glatten muskelzellen
US20030114503A1 (en) * 1997-06-16 2003-06-19 Pfizer Inc. Farnesyl transferase inhibitors in combination with HMG CoA reductase inhibitors for the treatment of cancer
DK1097150T3 (da) * 1998-06-16 2004-07-26 Sod Conseils Rech Applic Imidazolylderivater
US6420555B1 (en) 1998-06-16 2002-07-16 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Imidazolyl derivatives
TR200003882T2 (tr) * 1998-07-06 2001-06-21 Janssen Pharmaceutica N.V. Artropatilerin tedavisi için farnesil protein transferaz inhibitörleri.
EA003877B1 (ru) * 1998-07-06 2003-10-30 Янссен Фармацевтика Н.В. Ингибиторы фарнезилпротеинтрансферазы, обладающие in vivo радиосенсибилизирующими свойствами
FR2780892B1 (fr) * 1998-07-08 2001-08-17 Sod Conseils Rech Applic Utilisation d'inhibiteurs de prenyltransferases pour preparer un medicament destine a traiter les pathologies qui resultent de la fixation membranaire de la proteine g heterotrimerique
OA11645A (en) * 1998-08-27 2004-11-16 Pfizer Prod Inc Alkynyl-substituted quinolin-2-one derivatives useful as anticancer agents.
CA2341739C (en) 1998-08-27 2005-07-12 Pfizer Products Inc. Quinolin-2-one derivatives useful as anticancer agents
AU2478500A (en) 1998-12-08 2000-06-26 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
WO2000034437A2 (en) 1998-12-08 2000-06-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
EE04962B1 (et) * 1998-12-23 2008-02-15 Janssen Pharmaceutica N.V. Kinoliini ühend, seda sisaldav farmatseutiline kompositsioon, ühendi kasutamine ravimina ning meetod ühendi ja kompositsiooni valmistamiseks
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
DE60020812T2 (de) 1999-02-11 2006-05-04 Pfizer Products Inc., Groton Heteroaryl-substituierte chinolin-2-on derivate verwendbar als antikrebsmittel
US6143766A (en) * 1999-04-16 2000-11-07 Warner-Lambert Company Benzopyranone and quinolone inhibitors of ras farnesyl transferase
EP1420015A1 (en) * 1999-06-11 2004-05-19 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. Imidazolyl derivatives
FR2796943A1 (fr) * 1999-07-30 2001-02-02 Aventis Pharma Sa Derives de benzoxazinnes, leur procede de preparation et leur utilisation en therapeutique
RU2298417C2 (ru) * 1999-11-09 2007-05-10 Сосьете Де Консей Де Решерш Э Д`Аппликасьон Сьентифик (С.К.Р.А.С.) Продукт, включающий ингибитор трансдукции сигналов гетеротримерных протеинов g в комбинации с другим цитостатическим средством, для терапевтического применения при лечении рака
ATE259365T1 (de) * 1999-11-30 2004-02-15 Pfizer Prod Inc Chinolinderivate verwendbar zur hemmung der farnesyl-protein transferase
HN2000000266A (es) * 2000-01-21 2001-05-21 Pfizer Prod Inc Compuesto anticanceroso y metodo de separacion de enantiomeros util para sintetizar dicho compuesto.
SI1255537T1 (sl) * 2000-02-04 2006-10-31 Janssen Pharmaceutica Nv Inhibitorji farnezil protein transferaze za zdravljenje raka dojk
US6838467B2 (en) 2000-02-24 2005-01-04 Janssen Pharmaceutica N. V. Dosing regimen
JP2003525246A (ja) * 2000-02-29 2003-08-26 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 白金化合物とのファルネシルタンパク質トランスフェラーゼ阻害剤の組み合わせ剤
CA2397446A1 (en) * 2000-02-29 2001-09-07 Janssen Pharmaceutica Inc. Combinations of a farnesyl protein transferase inhibitor with nitrogen mustard or nitrosourea alkylating agents
JP2003525236A (ja) * 2000-02-29 2003-08-26 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ビンカアルカロイドとのファルネシルタンパク質トランスフェラーゼ阻害剤の組み合わせ剤
US20030212008A1 (en) * 2000-02-29 2003-11-13 Palmer Peter Albert Farnesyl protein transferase inhibitor combinations with further anti-cancer agents
JP2003525252A (ja) * 2000-02-29 2003-08-26 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Her2抗体とのファルネシルタンパク質トランスフェラーゼ阻害剤組み合わせ剤
AU2001239275A1 (en) * 2000-02-29 2001-09-12 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor podophyllotoxin derivatives
WO2001064199A2 (en) * 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with taxane compounds
WO2001064197A2 (en) * 2000-02-29 2001-09-07 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives
CA2397240A1 (en) * 2000-02-29 2001-09-07 Peter Albert Palmer Farnesyl protein transferase inhibitor combinations with camptothecin compounds
AU2001256166A1 (en) * 2000-02-29 2001-09-12 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations with anti-tumor nucleoside derivatives
AU2001252147A1 (en) * 2000-02-29 2001-09-12 Janssen Pharmaceutica N.V. Farnesyl protein transferase inhibitor combinations
US6844357B2 (en) * 2000-05-01 2005-01-18 Pfizer Inc. Substituted quinolin-2-one derivatives useful as antiproliferative agents
JO2361B1 (en) 2000-06-22 2006-12-12 جانسين فارماسيوتيكا ان. في Enaniumer 1,2-anylated quinoline inhibitor for the transporter - farnesyl
AU2001293835A1 (en) 2000-09-25 2002-04-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives
AU2001293826A1 (en) 2000-09-25 2002-04-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors
AU2001293829A1 (en) * 2000-09-25 2002-04-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6-((substituted phenyl)methyl)-quinoline and quinazoline derivatives
JP4974438B2 (ja) 2000-09-25 2012-07-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ファルネシルトランスフェラーゼを阻害する6−ヘテロシクリルメチルキノリンおよびキナゾリン誘導体
ATE434615T1 (de) 2000-11-21 2009-07-15 Janssen Pharmaceutica Nv Farnesyltransferase hemmende benzoheterocyclische derivate
US20040044032A1 (en) * 2000-11-28 2004-03-04 End David William Farnesyl protein transfer inhibitors for the treatment of inflammatory bowel disease
JP2004516287A (ja) * 2000-12-19 2004-06-03 ファイザー・プロダクツ・インク 6−[(4−クロロ−フェニル)−ヒドロキシ−(3−メチル−3h−イミダゾール−4−イル)−メチル]−4−(3−エチニル−フェニル)−1−メチル−1h−キノリン−2−オン,2,3−ジヒドロキシブタン二酸塩の結晶形および製造方法
ES2263684T3 (es) * 2000-12-27 2006-12-16 Janssen Pharmaceutica N.V. Derivados de 4-heterociclil-quinolina y -quinazolina que inhiben la farnesil transferasa.
DE60117847T2 (de) * 2000-12-27 2006-11-16 Janssen Pharmaceutica N.V. Farnesyltransferase hemmende, in der 4-stellung substituierte chinolin- und chinazolinderivate
WO2002056884A2 (en) * 2001-01-22 2002-07-25 Schering Corporation Treatment of malaria with farnesyl protein transferase inhibitors
DE60230017D1 (de) * 2001-02-15 2009-01-08 Janssen Pharmaceutica Nv Farnesyl-protein-transferase hemmer in kombination mit antiöstrogenen
DE60202755T2 (de) * 2001-03-12 2006-03-30 Janssen Pharmaceutica N.V. Verfahren zur herstellung von imidazolverbindungen
US20020151563A1 (en) * 2001-03-29 2002-10-17 Pfizer Inc. Farnesyl transferase inhibitors in combination with HMG CoA reductase inhibitors for the inhibition of abnormal cell growth
US6706699B2 (en) * 2001-06-21 2004-03-16 Ariad Pharmaceuticals, Inc. Quinolines and uses thereof
WO2003000266A1 (en) * 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel quinolines and uses thereof
US6740757B2 (en) 2001-08-29 2004-05-25 Pfizer Inc Enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3h-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1h-quinolin-2-one and salts thereof, useful in the treatment of cancer
US20030134846A1 (en) * 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
US7408063B2 (en) 2001-12-19 2008-08-05 Janssen Pharmaceutica, N.V. 1,8-annelated quinoline derivatives substituted with carbon-linked triazoles as farnesyl transferase inhibitors
CA2478813C (en) * 2002-03-22 2011-10-18 Janssen Pharmaceutica N.V. Benzylimidazolyl substituted 2-quinoline and quinazoline derivatives for use as farnesyl transferase inhibitors
AU2003229688B2 (en) 2002-04-15 2009-07-30 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting tricyclic quinazoline derivatives substituted with carbon-linked imidazoles or triazoles
US7132100B2 (en) 2002-06-14 2006-11-07 Medimmune, Inc. Stabilized liquid anti-RSV antibody formulations
US7425618B2 (en) 2002-06-14 2008-09-16 Medimmune, Inc. Stabilized anti-respiratory syncytial virus (RSV) antibody formulations
US20030125268A1 (en) * 2002-08-28 2003-07-03 Rybak Mary Ellen Margaret Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives
US20040265315A1 (en) * 2002-09-05 2004-12-30 Christine Dingivan Methods of preventing or treating T cell malignancies by administering CD2 antagonists
US7563810B2 (en) 2002-11-06 2009-07-21 Celgene Corporation Methods of using 3-(4-amino-1-oxo-1,3-dihydroisoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myeloproliferative diseases
US8034831B2 (en) * 2002-11-06 2011-10-11 Celgene Corporation Methods for the treatment and management of myeloproliferative diseases using 4-(amino)-2-(2,6-Dioxo(3-piperidyl)-isoindoline-1,3-dione in combination with other therapies
KR20120035234A (ko) 2003-04-11 2012-04-13 메디뮨 엘엘씨 재조합 il?9 항체 및 그의 용도
US20050003422A1 (en) 2003-07-01 2005-01-06 Mitch Reponi Methods for assessing and treating cancer
EP1660087A2 (en) * 2003-07-22 2006-05-31 Janssen Pharmaceutica N.V. Quinolinone derivatives as inhibitors of c-fms kinase
CA2536238C (en) 2003-08-18 2015-04-07 Medimmune, Inc. Humanization of antibodies
US20060228350A1 (en) * 2003-08-18 2006-10-12 Medimmune, Inc. Framework-shuffling of antibodies
JP4794445B2 (ja) * 2003-09-23 2011-10-19 メルク・シャープ・エンド・ドーム・コーポレイション キノリンカリウムチャネル阻害剤
WO2005089515A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
US20050272068A1 (en) * 2004-03-18 2005-12-08 The Brigham And Women's Hospital, Inc. UCH-L1 expression and cancer therapy
US20070293539A1 (en) * 2004-03-18 2007-12-20 Lansbury Peter T Methods for the treatment of synucleinopathies
EP1732549A4 (en) * 2004-03-18 2009-11-11 Brigham & Womens Hospital METHOD FOR THE TREATMENT OF SYNUCLEINOPATHIES
WO2005089502A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
WO2005089504A2 (en) * 2004-03-18 2005-09-29 The Brigham And Women's Hospital, Inc. Methods for the treatment of synucleinopathies
US7572916B2 (en) 2004-05-03 2009-08-11 Janssen Pharmaceutica Nv Diastereoselective synthesis process with 6-bromo-4-(3-chlorophenyl)-2-methoxy-quinoline
CN100567292C (zh) 2004-05-03 2009-12-09 詹森药业有限公司 制备咪唑化合物的非对映选择性合成方法
US7524961B2 (en) 2004-05-03 2009-04-28 Janssen Pharmaceutica, N.V. Diastereoselective addition of lithiated N-methylimidazole on sulfinimines
EP1765313A2 (en) 2004-06-24 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Compounds for immunopotentiation
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
CA2585717A1 (en) 2004-10-27 2006-05-04 Medimmune Inc. Modulation of antibody specificity by tailoring the affinity to cognate antigens
PT1815247E (pt) 2004-11-05 2013-04-23 Janssen Pharmaceutica Nv Uso terapêutico de inibidores de farnesiltransferase e métodos para monitorizar a eficácia do mesmo
US20060194821A1 (en) * 2005-02-18 2006-08-31 The Brigham And Women's Hospital, Inc. Compounds inhibiting the aggregation of superoxide dismutase-1
AU2006227377B2 (en) 2005-03-18 2013-01-31 Medimmune, Llc Framework-shuffling of antibodies
WO2006123182A2 (en) 2005-05-17 2006-11-23 Merck Sharp & Dohme Limited Cyclohexyl sulphones for treatment of cancer
US20060281769A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using thienopyrimidine and thienopyridine kinase modulators
US20070004660A1 (en) * 2005-06-10 2007-01-04 Baumann Christian A Synergistic Modulation of Flt3 Kinase Using Alkylquinolines and Alkylquinazolines
US20060281755A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using aminopyrimidines kinase modulators
US20060281788A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
KR20080025174A (ko) 2005-06-23 2008-03-19 메디뮨 인코포레이티드 응집 및 단편화 프로파일이 최적화된 항체 제제
JP5225092B2 (ja) * 2005-10-14 2013-07-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ チピファルニブの新規iv調合物
WO2007075923A2 (en) 2005-12-23 2007-07-05 Link Medicine Corporation Treatment of synucleinopathies
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
TWI417095B (zh) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-二取代之3-氰基-吡啶酮衍生物及其作為mGluR2-受體之正向異位性調節劑之用途
AR060358A1 (es) 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
AU2007240437B2 (en) 2006-04-20 2012-12-06 Janssen Pharmaceutica N.V. Heterocyclic compounds as inhibitors of c-fms kinase
BRPI0710548B8 (pt) 2006-04-20 2021-05-25 Janssen Pharmaceutica Nv inibidores de c-fms cinase, composição farmacêutica e forma de dosagem farmacêutica
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
MX2009002151A (es) 2006-08-28 2009-07-03 Kirin Pharma Kk Anticuerpos monoclonales humanos especificos para light humano antagonistas.
EP2083831B1 (en) 2006-09-22 2013-12-25 Merck Sharp & Dohme Corp. 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
EP2336120B1 (en) 2007-01-10 2014-07-16 MSD Italia S.r.l. Combinations containing amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
JP5330274B2 (ja) 2007-03-01 2013-10-30 ノバルティス アーゲー Pimキナーゼ阻害剤およびその使用方法
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
EP2077859A4 (en) 2007-03-30 2010-11-24 Medimmune Llc ANTIBODY FORMULATION
JO2959B1 (en) 2007-05-14 2016-03-15 جانسين فارماسوتيكا ان. في Mono-hydrochloric salts for histone dacetylase inhibitor
AU2008254425A1 (en) 2007-05-21 2008-11-27 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
DK2160386T3 (da) * 2007-05-23 2012-08-27 Allergan Inc Terapeutiske ((phenyl)imidazolyl)methylquinolinylforbindelser
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
EA019085B1 (ru) 2007-09-14 2014-01-30 Янссен Фармасьютикалз, Инк. 1',3-двузамещенные 4-(арил-х-фенил)-1н-пиридин-2-оны
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
JO3240B1 (ar) 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
BRPI0818810A2 (pt) 2007-10-31 2014-10-29 Medimmune Llc Esqueletos d polipeptídeo recombinante e multimérico, molécula de ácido n ucleico isolado, vetor de expressão, célula hospedeira, biblioteca de exibição de polipeptídeo, coleção de moléculas de ácido nucleico isolado, métodos para obter um esqueleto de polipeptídeo e pelo menos dois esqueletos, para detectar um composto em uma amostra, para capturar um composto em uma amostra, para prevenir, tratar, controlar ou melhorar uma doença, para diagnose ou formação de imagem de uma doença para purificar e produzir um esqueleto, para ensaiar ou detectar a ligação de um esqueleto a um alvo, para usar o esqueleto e para prevenir, tratar, melhora ou controlar câncer, composição estéril, isenta de pirógeno, composição farmacêutica, e, processo escalável.
CA2708281A1 (en) 2007-12-11 2009-08-27 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties
PA8809001A1 (es) 2007-12-20 2009-07-23 Novartis Ag Compuestos organicos
US7932036B1 (en) 2008-03-12 2011-04-26 Veridex, Llc Methods of determining acute myeloid leukemia response to treatment with farnesyltransferase
US8232402B2 (en) * 2008-03-12 2012-07-31 Link Medicine Corporation Quinolinone farnesyl transferase inhibitors for the treatment of synucleinopathies and other indications
WO2010025890A1 (en) 2008-09-02 2010-03-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
BRPI0921113A2 (pt) * 2008-11-13 2016-02-16 Link Medicine Corp tratamento de proteinopatias usando um inibidor de farnesil transferase.
JP2012508768A (ja) * 2008-11-13 2012-04-12 リンク・メディスン・コーポレーション アザキノリノン誘導体及びその使用
US20100331363A1 (en) * 2008-11-13 2010-12-30 Link Medicine Corporation Treatment of mitochondrial disorders using a farnesyl transferase inhibitor
US20110060005A1 (en) * 2008-11-13 2011-03-10 Link Medicine Corporation Treatment of mitochondrial disorders using a farnesyl transferase inhibitor
AU2009319387B2 (en) 2008-11-28 2012-05-10 Addex Pharma S.A. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
US8691825B2 (en) 2009-04-01 2014-04-08 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
CA2760259C (en) 2009-05-12 2018-05-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
JP5634506B2 (ja) 2009-05-12 2014-12-03 ジャンセン ファーマシューティカルズ, インコーポレイテッド 1,2,3−トリアゾロ[4,3−a]ピリジン誘導体ならびに神経障害および精神障害の治療または予防のためのその使用
US8765747B2 (en) 2009-06-12 2014-07-01 Dana-Farber Cancer Institute, Inc. Fused 2-aminothiazole compounds
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
KR101485645B1 (ko) 2009-10-14 2015-01-22 머크 샤프 앤드 돔 코포레이션 p53 활성을 증가시키는 치환된 피페리딘 및 그의 용도
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
KR20130006664A (ko) 2010-03-16 2013-01-17 다나-파버 캔서 인스티튜트 인크. 인다졸 화합물 및 그의 용도
US8999957B2 (en) 2010-06-24 2015-04-07 Merck Sharp & Dohme Corp. Heterocyclic compounds as ERK inhibitors
CN103328971B (zh) 2010-07-28 2016-09-28 维里德克斯有限责任公司 急性髓细胞性白血病应答法尼基转移酶抑制剂治疗的测定方法
AR082418A1 (es) 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
CN107090456B (zh) 2010-08-02 2022-01-18 瑟纳治疗公司 使用短干扰核酸的RNA干扰介导的联蛋白(钙粘蛋白关联蛋白质),β1基因表达的抑制
EP4079856A1 (en) 2010-08-17 2022-10-26 Sirna Therapeutics, Inc. 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
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
EP2615916B1 (en) 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
WO2012058210A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA)
JP5852666B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド 1,2,4−トリアゾロ[4,3−a]ピリジン誘導体およびmGluR2受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
JP5852665B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド 1,2,4−トリアゾロ[4,3−a]ピリジン誘導体およびmGluR2受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
ES2552455T3 (es) 2010-11-08 2015-11-30 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
EP2654748B1 (en) 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
WO2012103165A2 (en) 2011-01-26 2012-08-02 Kolltan Pharmaceuticals, Inc. Anti-kit antibodies and uses thereof
PE20140293A1 (es) 2011-01-31 2014-03-19 Novartis Ag Novedosos derivados heterociclicos
US20140045847A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2771342B1 (en) 2011-10-28 2016-05-18 Novartis AG Purine derivatives and their use in the treatment of disease
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
EP2844261B1 (en) 2012-05-02 2018-10-17 Sirna Therapeutics, Inc. SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS
AU2013263043B2 (en) 2012-05-16 2016-06-16 Novartis Ag Dosage regimen for a PI-3 kinase inhibitor
NZ630363A (en) 2012-07-25 2018-09-28 Celldex Therapeutics Inc Anti-kit antibodies and uses thereof
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
EP2882757B1 (en) 2012-08-07 2016-10-05 Janssen Pharmaceutica, N.V. Process for the preparation of heterocyclic ester derivatives
EP2900241B1 (en) 2012-09-28 2018-08-08 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
SG11201502757QA (en) 2012-10-09 2015-05-28 Igenica Biotherapeutics Inc Anti-c16orf54 antibodies and methods of use thereof
PL2909192T3 (pl) 2012-10-16 2017-09-29 Janssen Pharmaceutica Nv Połączone metylenem modulatory chinolinylowe ROR-GAMMA-T
CN105073729A (zh) 2012-10-16 2015-11-18 詹森药业有限公司 RORγt的苯基连接的喹啉基调节剂
KR20150070348A (ko) 2012-10-16 2015-06-24 얀센 파마슈티카 엔.브이. RoRγt의 헤테로아릴 결합 퀴놀리닐 조절제
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9758522B2 (en) 2012-10-19 2017-09-12 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
SI2925888T1 (en) 2012-11-28 2018-02-28 Merck Sharp & Dohme Corp. Compounds and methods for the treatment of cancer
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
US9540377B2 (en) 2013-01-30 2017-01-10 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as HDM2 inhibitors
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
US10100123B2 (en) 2013-06-06 2018-10-16 Pierre Fabre Medicament Anti-C10orf54 antibodies and uses thereof
KR20160054501A (ko) 2013-08-26 2016-05-16 맵백스 테라퓨틱스, 인코포레이티드 시알릴-루이스 a에 대한 사람 항체 코드화 핵산
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
WO2015057626A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv QUINOLINYL MODULATORS OF RORyT
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
WO2015057629A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv ALKYL LINKED QUINOLINYL MODULATORS OF RORyt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
AU2014337044A1 (en) 2013-10-18 2016-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
TN2016000179A1 (en) 2013-12-06 2017-10-06 Novartis Ag Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor.
LT3096790T (lt) 2014-01-21 2019-10-10 Janssen Pharmaceutica, N.V. Deriniai, apimantys 2 potipio metabotropinio glutamaterginio receptoriaus teigiamus alosterinius moduliatorius arba ortosterinius agonistus, ir jų panaudojimas
WO2015110435A1 (en) 2014-01-21 2015-07-30 Janssen Pharmaceutica Nv Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
GB201403775D0 (en) 2014-03-04 2014-04-16 Kymab Ltd Antibodies, uses & methods
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
US11311519B2 (en) 2014-05-01 2022-04-26 Eiger Biopharmaceuticals, Inc. Treatment of hepatitis delta virus infection
US10076512B2 (en) 2014-05-01 2018-09-18 Eiger Biopharmaceuticals, Inc. Treatment of hepatitis delta virus infection
WO2015187811A2 (en) 2014-06-04 2015-12-10 MabVax Therapeutics, Inc. Human monoclonal antibodies to ganglioside gd2
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
ES2834739T3 (es) 2014-12-11 2021-06-18 Pf Medicament Anticuerpos anti-C10orf54 y utilizaciones de los mismos
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
PL3265123T3 (pl) 2015-03-03 2023-03-13 Kymab Limited Przeciwciała, zastosowania i sposoby
EP3273966B1 (en) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3285768B1 (en) 2015-04-21 2020-12-30 Eiger Biopharmaceuticals, Inc. Pharmaceutical compositions comprising lonafarnib and ritonavir
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
DK3277842T5 (da) 2015-08-17 2020-08-31 Kura Oncology Inc Fremgangsmåder til at behandle kræftpatienter med farnesyl-transferase-inhibitorer
WO2017034877A1 (en) * 2015-08-27 2017-03-02 Janssen Pharmaceutica Nv Chemically modified quinoline and quinolone derivatives useful as cb-1 inverse agonists
WO2017044858A2 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
RU2018119085A (ru) 2015-11-02 2019-12-04 Новартис Аг Схема введения ингибитора фосфатидилинозитол-3-киназы
CN108925136B (zh) 2015-12-02 2022-02-01 斯特赛恩斯公司 特异于糖基化的btla(b和t淋巴细胞衰减因子)的抗体
CN114470194A (zh) 2015-12-02 2022-05-13 斯特库伯株式会社 与btn1a1免疫特异性结合的抗体和分子及其治疗用途
JOP20190055A1 (ar) 2016-09-26 2019-03-24 Merck Sharp & Dohme أجسام مضادة ضد cd27
WO2018060833A1 (en) 2016-09-27 2018-04-05 Novartis Ag Dosage regimen for alpha-isoform selective phosphatidylinositol 3-kinase inhibitor alpelisib
EP3534947A1 (en) 2016-11-03 2019-09-11 Kymab Limited Antibodies, combinations comprising antibodies, biomarkers, uses & methods
KR20190082247A (ko) 2016-11-03 2019-07-09 쿠라 온콜로지, 인크. 파르네실전달효소 억제제를 이용하여 암 환자를 치료하는 방법
US10954210B2 (en) 2016-12-08 2021-03-23 Hangzhou Solipharma Co., Ltd. Crystal form of tipifarnib and preparation method and pharmaceutical composition thereof
CN118267470A (zh) 2017-04-13 2024-07-02 赛罗帕私人有限公司 抗SIRPα抗体
US20200131266A1 (en) 2017-05-31 2020-04-30 Stcube & Co., Inc. Methods of treating cancer using antibodies and molecules that immunospecifically bind to btn1a1
AU2018277838A1 (en) 2017-05-31 2019-12-19 Stcube & Co., Inc. Antibodies and molecules that immunospecifically bind to BTN1A1 and the therapeutic uses thereof
JP2020522562A (ja) 2017-06-06 2020-07-30 ストキューブ アンド シーオー., インコーポレイテッド Btn1a1又はbtn1a1リガンドに結合する抗体及び分子を用いて癌を治療する方法
WO2019073069A1 (en) 2017-10-13 2019-04-18 Boehringer Ingelheim International Gmbh HUMAN ANTIBODIES AGAINST THOMSEN-NEW ANTIGEN (TN)
US10947234B2 (en) 2017-11-08 2021-03-16 Merck Sharp & Dohme Corp. PRMT5 inhibitors
WO2019113269A1 (en) 2017-12-08 2019-06-13 Kura Oncology, Inc. Methods of treating cancer patients with farnesyltransferase inhibitors
WO2019148412A1 (en) 2018-02-01 2019-08-08 Merck Sharp & Dohme Corp. Anti-pd-1/lag3 bispecific antibodies
AU2019270163A1 (en) 2018-05-18 2020-12-03 Kura Oncology, Inc. Synthesis of tipifarnib
MX2021000786A (es) 2018-07-20 2021-06-15 Pf Medicament Receptor para supresor de ig del dominio v de activación de células t (vista).
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
TW202108170A (zh) 2019-03-15 2021-03-01 美商庫拉腫瘤技術股份有限公司 以法呢基轉移酶(farnesyltransferase)抑制劑治療癌症患者之方法
TW202327590A (zh) 2021-11-30 2023-07-16 美商庫拉腫瘤技術股份有限公司 大環化合物及組合物以及其製備及使用方法
WO2023141082A1 (en) * 2022-01-20 2023-07-27 Teva Czech Industries S.R.O. Solid state forms of tipifarnib and process for preparation thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2101115A (en) * 1980-10-23 1983-01-12 Pfizer Ltd Thromboxane synthetase inhibitors
CA2002864C (en) * 1988-11-29 1999-11-16 Eddy J. E. Freyne (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives
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.

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