PT72878B - Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents - Google Patents

Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents

Info

Publication number
PT72878B
PT72878B PT72878A PT7287881A PT72878B PT 72878 B PT72878 B PT 72878B PT 72878 A PT72878 A PT 72878A PT 7287881 A PT7287881 A PT 7287881A PT 72878 B PT72878 B PT 72878B
Authority
PT
Portugal
Prior art keywords
inflammatory agents
steroidal anti
drugs
chem
topical
Prior art date
Application number
PT72878A
Other languages
English (en)
Portuguese (pt)
Other versions
PT72878A (en
Inventor
Kenneth B Sloan
Roy Little
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PT72878A publication Critical patent/PT72878A/pt
Publication of PT72878B publication Critical patent/PT72878B/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
    • C07D209/28—1-(4-Chlorobenzoyl)-2-methyl-indolyl-3-acetic acid, substituted in position 5 by an oxygen or nitrogen atom; Esters thereof

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PT72878A 1980-04-24 1981-04-16 Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents PT72878B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14352080A 1980-04-24 1980-04-24

Publications (2)

Publication Number Publication Date
PT72878A PT72878A (en) 1981-05-01
PT72878B true PT72878B (en) 1983-03-29

Family

ID=22504442

Family Applications (1)

Application Number Title Priority Date Filing Date
PT72878A PT72878B (en) 1980-04-24 1981-04-16 Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents

Country Status (9)

Country Link
EP (1) EP0039051B1 (member.php)
JP (1) JPS56167643A (member.php)
AT (1) ATE14423T1 (member.php)
DE (1) DE3171467D1 (member.php)
DK (1) DK156717C (member.php)
ES (1) ES8207508A1 (member.php)
GR (1) GR74496B (member.php)
IE (1) IE53001B1 (member.php)
PT (1) PT72878B (member.php)

Families Citing this family (196)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5112868A (en) * 1988-05-19 1992-05-12 Warner-Lambert Company Hydroxamate derivatives of selected nonsteroidal antiinflammatory acyl residues having cyclooxygenase and 5-lipoxygenase inhibition
US4943587A (en) * 1988-05-19 1990-07-24 Warner-Lambert Company Hydroxamate derivatives of selected nonsteroidal antiinflammatory acyl residues and their use for cyclooxygenase and 5-lipoxygenase inhibition
US5068251A (en) * 1988-12-16 1991-11-26 Abbott Laboratories Lipoxygenase inhibiting compounds
US5212189A (en) * 1991-12-17 1993-05-18 Warner-Lambert Company Thiadiazole or oxadiazole analogs of fenamic acids containing substituted hydroxamate side chains as antiinflammatory agents
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6410729B1 (en) 1996-12-05 2002-06-25 Amgen Inc. Substituted pyrimidine compounds and methods of use
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6174901B1 (en) 1998-12-18 2001-01-16 Amgen Inc. Substituted pyridine and pyridazine compounds and methods of use
US6335329B1 (en) 1997-12-19 2002-01-01 Amgen Inc. Carboxylic acid substituted heterocycles, derivatives thereof and methods of use
US6107291A (en) * 1997-12-19 2000-08-22 Amgen Inc. Azepine or larger medium ring derivatives and methods of use
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
US6514964B1 (en) 1999-09-27 2003-02-04 Amgen Inc. Fused cycloheptane and fused azacycloheptane compounds and their methods of use
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
US6429223B1 (en) * 2000-06-23 2002-08-06 Medinox, Inc. Modified forms of pharmacologically active agents and uses therefor
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
PL375552A1 (en) 2002-05-22 2005-11-28 Amgen Inc. Vanilloid receptor ligands and their medical applications
US7176322B2 (en) 2002-05-23 2007-02-13 Amgen Inc. Calcium receptor modulating agents
US6908935B2 (en) 2002-05-23 2005-06-21 Amgen Inc. Calcium receptor modulating agents
AU2003264047B2 (en) 2002-08-08 2008-06-26 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
US7582631B2 (en) 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
US7429616B2 (en) 2005-07-15 2008-09-30 Board Of Regents, University Of Texas System Synthesis and complete stereochemical assignment of psymberin/irciniastatin for use as antitumor compounds
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
EP2001838B1 (en) 2006-03-29 2014-03-12 Novartis AG Selective hydroxamate based mmp inhibitors
ATE540681T1 (de) 2006-06-26 2012-01-15 Amgen Inc Verfahren zur behandlung von atherosklerose
CA2656535C (en) 2006-07-14 2011-08-23 Amgen Inc. Alkyne-substituted pyridone compounds and methods of use
WO2008011110A2 (en) 2006-07-20 2008-01-24 Amgen Inc. Di-amino-substituted heterocyclic compounds and methods of use
ES2344760T3 (es) 2006-07-20 2010-09-06 Amgen Inc. Compuestos de piridona sustituidos y metodo de uso.
US20090286790A1 (en) 2006-07-20 2009-11-19 Hidetomo Imase Organic compounds
HUE028954T2 (en) 2007-03-23 2017-01-30 Amgen Inc Heterocyclic compounds and their use
EA022912B1 (ru) 2007-11-05 2016-03-31 Новартис Аг Производные 4-бензиламино-1-карбоксиацилпиперидина как ингибиторы бпхэ (белка-переносчика холестерилового эфира), применимые для лечения заболеваний, таких как гиперлипидемия или артериосклероз
US8759365B2 (en) 2007-12-03 2014-06-24 Novartis Ag Organic compounds
EA020114B1 (ru) 2008-03-24 2014-08-29 Новартис Аг Производные арилсульфонамида в качестве ингибиторов матриксной металлопротеазы
US8637500B2 (en) 2008-12-17 2014-01-28 Amgen Inc. Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
WO2010075869A1 (en) 2008-12-30 2010-07-08 European Molecular Biology Laboratory (Embl) Toluidine sulfonamides and their use
WO2010085968A1 (en) 2008-12-30 2010-08-05 European Molecular Biology Laboratory (Embl) Toluidine sulfonamides and their use as hif-inhibitors
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
BRPI1010600A2 (pt) 2009-05-15 2016-03-15 Novartis Ag aril piridina como inibidores de aldosterona sintase
CA2763565A1 (en) 2009-05-28 2010-12-02 Novartis Ag Substituted aminobutyric derivatives as neprilysin inhibitors
PL2435409T3 (pl) 2009-05-28 2015-01-30 Novartis Ag Podstawione pochodne aminopropionowe jako inhibitory neprylizyny
JP2012531438A (ja) 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド 複素環式化合物およびその使用
MX2011013901A (es) 2009-06-25 2012-05-08 Amgen Inc Derivados de 4h-pirido [1,2-a] pirimidin-4-ona como inhibidores de pi3k.
EP2445900B1 (en) 2009-06-25 2016-03-02 Amgen, Inc Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases
JP2012531436A (ja) 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド 複素環式化合物およびそれらのｐｉ３ｋ活性阻害剤としての使用
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US20120149661A1 (en) 2009-08-26 2012-06-14 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
MX2012002591A (es) 2009-09-03 2012-04-02 Allergan Inc Compuestos como moduladores de tirosina cinasas.
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
CA2771563A1 (en) 2009-09-04 2011-03-10 Novartis Ag Bipyridines useful for the treatment of proliferative diseases
US20120165306A1 (en) 2009-09-04 2012-06-28 Barsanti Paul A Pyrazinylpyridines useful for the treatment of proliferative diseases
WO2011026917A1 (en) 2009-09-04 2011-03-10 Novartis Ag Heteroaryl compounds as kinase inhibitors
AR078770A1 (es) 2009-10-27 2011-11-30 Elara Pharmaceuticals Gmbh Derivados de dihidrobenzo oxacinas y tiazinas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades inflamatorias e hiperproliferativas.
WO2011061168A1 (en) 2009-11-17 2011-05-26 Novartis Ag Aryl-pyridine derivatives as aldosterone synthase inhibitors
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
WO2011064376A1 (en) 2009-11-30 2011-06-03 Novartis Ag Imidazole derivatives as aldosterone synthase inhibitors
WO2011075628A1 (en) 2009-12-18 2011-06-23 Amgen Inc. Heterocyclic compounds and their uses
WO2011073316A1 (en) 2009-12-18 2011-06-23 Novartis Ag 4-aryl-butane-1,3-diamides
TW201132642A (en) 2009-12-21 2011-10-01 Novartis Ag Diaza-spiro[5.5]undecanes
ES2460915T3 (es) 2009-12-21 2014-05-16 Novartis Ag Piridinas fusionadas con heteroarilo disustituido
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
US20120295942A1 (en) 2010-02-01 2012-11-22 Nicholas James Devereux Pyrazolo[5,1b]oxazole Derivatives as CRF-1 Receptor Antagonists
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
WO2011095450A1 (en) 2010-02-02 2011-08-11 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
US8791100B2 (en) 2010-02-02 2014-07-29 Novartis Ag Aryl benzylamine compounds
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
UY33226A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
US8324239B2 (en) 2010-04-21 2012-12-04 Novartis Ag Furopyridine compounds and uses thereof
JP2013526524A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Ｐｄｅ１０阻害剤としてのアリールおよびヘテロアリール窒素ヘテロ環式化合物
JP2013526546A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Ｐｄｅ１０阻害剤としてのヘテロアリ−ルオキシヘテロシクリル化合物
MA34300B1 (fr) 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
EP2569306A1 (en) 2010-05-13 2013-03-20 Amgen Inc. Heteroaryloxycarbocyclyl compounds as pde10 inhibitors
US20130085161A1 (en) 2010-06-17 2013-04-04 Novartis Ag Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
EP2582680A1 (en) 2010-06-17 2013-04-24 Novartis AG Biphenyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
UY33469A (es) 2010-06-29 2012-01-31 Irm Llc Y Novartis Ag Composiciones y metodos para modular la via de señalizacion de wnt
CA2803358A1 (en) 2010-06-30 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
EP2588473A1 (en) 2010-06-30 2013-05-08 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
WO2012003278A1 (en) 2010-06-30 2012-01-05 Amgen Inc. Quinolines as p13k inhibitors
JP2013530236A (ja) 2010-07-01 2013-07-25 アムジエン・インコーポレーテツド Ｐｉ３ｋ活性の阻害剤としての複素環式化合物およびその用途
JP2013530238A (ja) 2010-07-01 2013-07-25 アムジエン・インコーポレーテツド Ｐｉ３ｋ活性の阻害剤としての複素環化合物及びその使用
WO2012003271A1 (en) 2010-07-02 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
BR112012004154A2 (pt) 2010-07-13 2017-05-30 Novartis Ag "derivados de oxazina e seu uso no tratamento de distúrbios neurológicos"
DK2593452T3 (en) 2010-07-14 2017-04-24 Novartis Ag Heterocyclic compounds as IP receptor agonists
MX2013000906A (es) 2010-07-22 2013-02-27 Novartis Ag Compuestos de tiofeno 2, 3, 5-trisustituidos y usos de los mismos.
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
DK2616465T3 (da) 2010-09-13 2016-02-01 Novartis Ag Triazin-oxadiazoler
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
EP3181566A1 (en) 2010-09-20 2017-06-21 Ironwood Pharmaceuticals, Inc. Imidazotriazinone compounds
US20120101110A1 (en) 2010-10-26 2012-04-26 Sangamesh Badiger Diaza-spiro[5.5]undecanes
AU2011323243A1 (en) 2010-11-04 2013-05-23 Amgen Inc. Heterocyclic compounds and their uses
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8993631B2 (en) 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
MX2013005567A (es) 2010-11-17 2013-10-30 Amgen Inc Derivados de quinolina como inhibidores de pik3.
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
WO2012087521A1 (en) 2010-12-20 2012-06-28 Irm Llc Compositions and methods for modulating farnesoid x receptors
JP2014500318A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー ファルネソイドｘ受容体を調節するための組成物および方法
WO2012087784A1 (en) 2010-12-23 2012-06-28 Amgen Inc. Heterocyclic compounds and their uses
WO2012093101A1 (en) 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
JP2014505689A (ja) 2011-01-13 2014-03-06 ノバルティス アーゲー 代謝障害の処置用ｂａｃｅ−２阻害剤
WO2012101063A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyridine biaryl compounds and their uses
WO2012101065A2 (en) 2011-01-28 2012-08-02 Novartis Ag Pyrimidine biaryl amine compounds and their uses
WO2012101066A1 (en) 2011-01-28 2012-08-02 Novartis Ag Pyridine biaryl amine compounds and their uses
WO2012101064A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyrimidine biaryl compounds as protein kinase inhibitors
GB201103578D0 (en) 2011-03-02 2011-04-13 Sabrepharm Ltd Dipyridinium derivatives
AU2012230890A1 (en) 2011-03-22 2013-09-26 Amgen Inc. Azole compounds as Pim inhibitors
WO2012130306A1 (en) 2011-03-30 2012-10-04 Elara Pharmaceuticals Gmbh Bicyclic 2,3-dihyrdobenzazine compounds for use in therapy
WO2012130314A1 (en) 2011-03-31 2012-10-04 Elara Pharmaceuticals Gmbh Composition comprising docetaxel
WO2012130322A1 (en) 2011-03-31 2012-10-04 Elara Pharmaceuticals Gmbh Imidazo [1,2-a]pyridine compounds for use in therapy
WO2012138648A1 (en) 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
WO2012148775A1 (en) 2011-04-29 2012-11-01 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
CA2839699A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
AU2012272898A1 (en) 2011-06-24 2013-04-11 Amgen Inc. TRPM8 antagonists and their use in treatments
US8846656B2 (en) 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
CN103987699A (zh) 2011-10-21 2014-08-13 诺华股份有限公司 作为pi3k调节剂的喹唑啉衍生物
WO2013105065A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pah and related disorders
US20150005311A1 (en) 2012-01-13 2015-01-01 Novartis Ag IP receptor agonist heterocyclic compounds
EP2802581A1 (en) 2012-01-13 2014-11-19 Novartis AG 7,8- dihydropyrido [3, 4 - b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802582A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused dihydropyrido [2,3 -b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
WO2013105057A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused pyrroles as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
TW201348226A (zh) 2012-02-28 2013-12-01 Amgen Inc 作為ｐｉｍ抑制劑之醯胺
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
WO2013142269A1 (en) 2012-03-19 2013-09-26 Envivo Pharmaceuticals, Inc. Imidazotriazinone compounds
RS54716B1 (sr) 2012-04-04 2016-08-31 Amgen Inc. Heterociklična jedinjenja i njihova primena
CA2872000A1 (en) 2012-05-04 2013-11-07 Novartis Ag Complement pathway modulators and uses thereof
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
WO2013184766A1 (en) 2012-06-06 2013-12-12 Irm Llc Compounds and compositions for modulating egfr activity
UY34858A (es) 2012-06-14 2013-11-29 Amgen Inc Compuestos de azetidina y piperidina útiles como inhibidores de pde10
ES2584702T3 (es) 2012-06-20 2016-09-28 Novartis Ag Moduladores de ruta del complemento y usos de los mismos
WO2014002054A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6209605B2 (ja) 2012-06-28 2017-10-04 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
WO2014002058A2 (en) 2012-06-28 2014-01-03 Novartis Ag Complement pathway modulators and uses thereof
WO2014002051A2 (en) 2012-06-28 2014-01-03 Novartis Ag Complement pathway modulators and uses thereof
ES2648962T3 (es) 2012-06-28 2018-01-09 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la vía del complemento
EP2867222A1 (en) 2012-06-28 2015-05-06 Novartis AG Pyrrolidine derivatives and their use as complement pathway modulators
EA201590200A1 (ru) 2012-07-12 2015-08-31 Новартис Аг Модуляторы пути активации комплемента и их применение
WO2014022752A1 (en) 2012-08-03 2014-02-06 Amgen Inc. Macrocycles as pim inhibitors
WO2014023329A1 (en) 2012-08-06 2014-02-13 Life And Brain Gmbh Niclosamide and its derivatives for use in the treatment of solid tumors
EP2895462A1 (en) 2012-09-13 2015-07-22 Baden-Württemberg Stiftung gGmbH Specific inhibitors of protein p21 as therapeutic agents
WO2014125413A1 (en) 2013-02-13 2014-08-21 Novartis Ag Ip receptor agonist heterocyclic compounds
CU24330B1 (es) 2013-02-14 2018-03-13 Novartis Ag Derivados del ácido 4-((1,1) bifenil-4-il)-3-(3-fosfonopropanamido) butanoico, activos como inhibidores de nep (endopeptidasa neutral)
US20150018376A1 (en) 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
WO2015019286A1 (en) 2013-08-07 2015-02-12 Friedrich Miescher Institute For Biomedical Research New screening method for the treatment friedreich's ataxia
EP2924026A1 (en) 2014-03-28 2015-09-30 Novartis Tiergesundheit AG Aminosulfonylmethylcyclohexanes as JAK inhibitors
WO2016088082A1 (en) 2014-12-05 2016-06-09 Novartis Ag Amidomethyl-biaryl derivatives complement factor d inhibitors and uses thereof
CN107531686B (zh) 2015-03-24 2021-07-09 亥姆霍兹感染研究中心有限责任公司 铜绿假单胞菌LecB的抑制剂
US10351576B2 (en) 2015-04-30 2019-07-16 Novartis Ag Fused tricyclic pyrazole derivatives useful for farnesoid X receptors
EP4066822A1 (en) 2015-08-19 2022-10-05 Vivus, Inc. Pharmaceutical formulations
CN105418480B (zh) * 2015-11-16 2019-05-10 青岛大学 2-(1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1氢-吲哚-3-基)-n-羟基乙酰胺的制备和应用
MA44066A (fr) 2015-12-18 2018-10-24 Amgen Inc Composés sulfonamides de dihydroquinoline d'alcynyle
US10383866B2 (en) 2015-12-18 2019-08-20 Amgen Inc. Alkyl dihydroquinoline sulfonamide compounds
CN110290808B (zh) 2017-02-10 2023-07-11 诺华股份有限公司 1-(4-氨基-5-溴-6-(1h-吡唑-1-基)嘧啶-2-基)-1h-吡唑-4-醇及其在治疗癌症中的用途
CN111032653A (zh) 2017-06-14 2020-04-17 欧洲分子生物学实验室 用于疗法的双环杂芳族酰胺化合物
AU2018285833A1 (en) 2017-06-14 2020-01-02 European Molecular Biology Laboratory Bicyclic heteroaromatic urea or carbamate compounds for use in therapy
CA3067080A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Benzofuran ureas or carbamates and heteroaromatic analogues thereof for use in therapy
CA3067086A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
JP2021512949A (ja) 2018-02-06 2021-05-20 ウニベルジテート ハイデルベルク Ｆａｐ阻害物質
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
GB201811825D0 (en) 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
GB201813791D0 (en) 2018-08-23 2018-10-10 Benevolental Bio Ltd Organic compounds
ES2997190T3 (en) 2018-12-20 2025-02-14 Amgen Inc Heteroaryl amides useful as kif18a inhibitors
CA3123227A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
CA3123042A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
AU2019403486B2 (en) 2018-12-20 2025-04-24 Amgen Inc. KIF18A inhibitors
CN114391012B (zh) 2019-08-02 2025-10-31 美国安进公司 作为kif18a抑制剂的吡啶衍生物
CA3147451A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
CN114401953A (zh) 2019-08-02 2022-04-26 美国安进公司 Kif18a抑制剂
US20220289724A1 (en) 2019-08-02 2022-09-15 Amgen Inc. Kif18a inhibitors
US20220402960A1 (en) 2019-11-05 2022-12-22 Helmholtz-Zentrum für Infektionsforschung GmbH Bivalent leca inhibitors targeting biofilm formation of pseudomonas aeruginosa
CN115297863A (zh) 2020-01-22 2022-11-04 博善人工智能生物科技有限公司 包含咪唑并[1,2-b]哒嗪化合物的表面药物组合物
MX2022008930A (es) 2020-01-22 2022-10-18 Benevolentai Bio Ltd Composiciones farmaceuticas y sus usos.
WO2021211549A1 (en) 2020-04-14 2021-10-21 Amgen Inc. Kif18a inhibitors for treatment of neoplastic diseases
WO2021234181A1 (en) 2020-05-22 2021-11-25 Universität Heidelberg Use of fap inhibitor in a method of diagnosis
MX2022015857A (es) 2020-06-10 2023-01-24 Amgen Inc Compuestos de dihidroquinolin sulfonamida de heteroalquilo.
JP2021195367A (ja) 2020-06-10 2021-12-27 アムジエン・インコーポレーテツド シクロプロピルジヒドロキノリンスルホンアミド化合物
JP7739051B2 (ja) 2020-06-10 2025-09-16 アムジエン・インコーポレーテツド シクロブチルジヒドロキノリンスルホンアミド化合物
EP4204087A1 (en) 2020-08-26 2023-07-05 Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft Inhibitors of no production
TW202237095A (zh) 2020-12-03 2022-10-01 德商艾斯巴赫生物有限公司 Ａｌｃ１抑制劑及與ｐａｒｐｉ之協同性
KR20230121800A (ko) 2020-12-17 2023-08-21 트러스티즈 오브 터프츠 칼리지 Fap-활성화된 래디오테라노스틱스, 및 이와 관련된용도
CN118891042A (zh) 2021-10-29 2024-11-01 艾斯巴赫生物有限公司 与新型变构结合位点结合的病毒解旋酶抑制剂
WO2023161427A1 (en) 2022-02-24 2023-08-31 Eisbach Bio Gmbh Viral combination therapy
EP4518862A1 (en) 2022-05-02 2025-03-12 Eisbach Bio GmbH Use of alc1 inhibitors and synergy with parpi
WO2024022332A1 (en) 2022-07-26 2024-02-01 Shanghai Sinotau Biotech. Co., Ltd Fap inhibitors
TW202517632A (zh) 2023-07-12 2025-05-01 德商Ｈｍｎｃ控股有限公司 氘代1,3二氫-2h-吲哚-2-酮衍生物
WO2025055942A1 (en) 2023-09-12 2025-03-20 Shanghai Sinotau Biotech. Co., Ltd Inhibitors of prostate specific membrane antigen and use thereof
EP4590664A1 (en) 2023-09-12 2025-07-30 Shanghai Sinotau Biotech. Co., Ltd Inhibitors of prostate specific membrane antigen and use thereof
WO2025088087A1 (en) 2023-10-25 2025-05-01 Eisbach Bio Gmbh A pyrido-thieno-pyrimidin derivative as alc1 inhibitor for use in the treatment of homologous recombination deficiency (hrd) cancers
WO2025088175A1 (en) 2023-10-25 2025-05-01 Eisbach Bio Gmbh Alc1 inhibitors for use in treating cancer by potentiating the effects of several classes of approved cancer drugs
WO2025093706A1 (en) 2023-10-31 2025-05-08 Eisbach Bio Gmbh Alc1 inhibitors alc1i-1 and alc1i-2 for use in treating pancreatic cancer by potentiating the effect of irinotecan
WO2025252850A1 (en) 2024-06-06 2025-12-11 Helmholtz-Zentrum für Infektionsforschung GmbH Thiourea based derivatives are novel antimicrobials against a. baumannii

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1081993A (en) * 1963-04-17 1967-09-06 Ici Ltd Difluoramino compounds
US3336194A (en) * 1963-04-30 1967-08-15 Merck & Co Inc Indolyl acid amides
US3417096A (en) * 1965-07-01 1968-12-17 Bristol Myers Co Certain 5(1-benzoyl-3-indolylmethyl) tetrazoles
IT1036004B (it) * 1968-05-21 1979-10-30 Abc Ist Biolog Chem Spa Acidt 3 indolil adetoidrossamici
NO134946C (member.php) * 1970-09-09 1977-01-12 Ciba Geigy Ag
US4206220A (en) * 1978-07-13 1980-06-03 Interx Research Corporation Prodrugs for the improved delivery of non-steroidal anti-inflammatory agents

Also Published As

Publication number Publication date
EP0039051A3 (en) 1982-05-26
EP0039051B1 (en) 1985-07-24
DE3171467D1 (en) 1985-08-29
ES501573A0 (es) 1982-09-16
IE53001B1 (en) 1988-05-11
JPS56167643A (en) 1981-12-23
DK156717B (da) 1989-09-25
ATE14423T1 (de) 1985-08-15
EP0039051A2 (en) 1981-11-04
ES8207508A1 (es) 1982-09-16
PT72878A (en) 1981-05-01
DK182081A (da) 1981-10-25
IE810899L (en) 1981-10-24
JPH04982B2 (member.php) 1992-01-09
GR74496B (member.php) 1984-06-28
DK156717C (da) 1990-02-19

Similar Documents

Publication Publication Date Title
PT72878B (en) Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
SG15689G (en) Substituted acyl derivatives of 1,2,3,4-tetrahydroiso-quinoline-3-carboxylic acids,salts thereof,pharmaceutical compositions containing the derivatives or salts,and the production of the same
HU9300759D0 (en) Method for producing triazolo-pyridine derivatives and pharmaceutical preparatives containing said compounds as active substance
ES8103093A1 (es) Un procedimiento para preparar derivados de oxapenem
PH24176A (en) New bicyclic compounds,process for preparation thereof and pharmaceutical composition comprising the same
ATE19773T1 (de) Nitroaliphatische verbindungen, verfahren zu deren herstellung und deren verwendung.
GB1513742A (en) 6-aryl-2,3,6,7-tetrahydro-5h-pyrrolo(1,2-a)imidazole derivatives processes for their manufacture and compositions containing them
HU910748D0 (en) New substituted amine compounds and process for producing them
IE780901L (en) Tetrazolyl-piperidinyl amides
ES8200689A1 (es) Un procedimiento para la produccion de analogos de cefalosporina.
MA18964A1 (fr) 2-aminoalkyl-5-pyridinols,procede pour leur preparation,compositions pharmaceutiques contenant ces composes et leurs utilisations therapeutiques
DE3063105D1 (en) Clavulanic acid derivatives, process for their preparation and pharmaceutical compositions containing them
JPS5767599A (en) Preparation of 5-beta-choleic acid derivative

Legal Events

Date Code Title Description
MM3A Annulment or lapse

Free format text: LAPSE DUE TO NON-PAYMENT OF FEES

Effective date: 19940930