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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/12Heterocyclic 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
    • C07D295/125Heterocyclic 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
    • C07D295/13Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/26Radicals 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
    • C07D209/281-(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)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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 (ref)
JP (1) JPS56167643A (ref)
AT (1) ATE14423T1 (ref)
DE (1) DE3171467D1 (ref)
DK (1) DK156717C (ref)
ES (1) ES501573A0 (ref)
GR (1) GR74496B (ref)
IE (1) IE53001B1 (ref)
PT (1) PT72878B (ref)

Families Citing this family (196)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
US6410729B1 (en) 1996-12-05 2002-06-25 Amgen Inc. Substituted pyrimidine compounds and methods of use
US6096753A (en) * 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone 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
US6107291A (en) * 1997-12-19 2000-08-22 Amgen Inc. Azepine or larger medium ring derivatives and methods of use
US6335329B1 (en) 1997-12-19 2002-01-01 Amgen Inc. Carboxylic acid substituted heterocycles, derivatives thereof 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
WO2003099284A1 (en) 2002-05-22 2003-12-04 Amgen Inc. Amino-pyridine, -pyridine and pyridazine derivatives for use as vanilloid receptor ligands for the treatment of pain
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
BR0313255A (pt) 2002-08-08 2005-07-12 Amgen Inc Composto, composição farmacêutica, uso de um composto e métodos de fabricar um medicamento e de preparar um composto
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
BRPI0709677A2 (pt) 2006-03-29 2011-07-19 Novartis Ag inibidores seletivos das mmp à base de hidroxamato
EP2452683A3 (en) 2006-06-26 2012-08-22 Amgen Inc. Methods for treating atherosclerosis
ES2426780T3 (es) 2006-07-14 2013-10-25 Amgen Inc. Compuestos de piridona sustituidos con alquino y métodos de uso
CA2657258A1 (en) 2006-07-20 2008-01-24 Novartis Ag Amino-piperidine derivatives as cetp inhibitors
ES2344760T3 (es) 2006-07-20 2010-09-06 Amgen Inc. Compuestos de piridona sustituidos y metodo de uso.
WO2008011110A2 (en) 2006-07-20 2008-01-24 Amgen Inc. Di-amino-substituted heterocyclic compounds and methods of use
EA017389B1 (ru) 2007-03-23 2012-12-28 Амген Инк. Гетероциклические соединения и их применение
EP2463282B1 (en) 2007-11-05 2013-08-07 Novartis AG 4-Benzylamino-1-carboxyacyl-piperidine derivatives as CETP inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
MX2010006063A (es) 2007-12-03 2010-07-01 Novartis Ag Derivados de 4-bencil-amino-pirrolidina 1,2-disustituida como inhibidores de la proteina de transferencia de colesteril-ester (cetp) utiles para el tratamiento de las enfermedades tales como hiperlipidemia o arterioesclerosis.
WO2009118292A1 (en) 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
ES2397934T3 (es) 2008-12-17 2013-03-12 Amgen Inc. Compuestos de aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10
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
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
HRP20140371T1 (hr) 2009-05-15 2014-05-23 Novartis Ag Arilpiridini kao inhibitori sinteze aldosterona
EP2435402B1 (en) 2009-05-28 2016-04-13 Novartis AG Substituted aminobutyric derivatives as neprilysin inhibitors
CN103896796B (zh) 2009-05-28 2016-04-27 诺华股份有限公司 作为脑啡肽酶抑制剂的取代的氨基丙酸衍生物
EP2445902A2 (en) 2009-06-25 2012-05-02 Amgen, Inc Heterocyclic compounds and their uses as inhibitors of pi3k activity
CN102625799A (zh) 2009-06-25 2012-08-01 安姆根有限公司 杂环化合物及其用途
EA201270013A1 (ru) 2009-06-25 2012-06-29 Амген Инк. Гетероциклические соединения и их применение
WO2010151735A2 (en) 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
WO2011023677A1 (en) 2009-08-26 2011-03-03 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
IN2012DN02493A (ref) 2009-09-03 2015-08-28 Allergan Inc
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
CA2771568A1 (en) 2009-09-04 2011-03-10 Novartis Ag Heteroaryl compounds as kinase inhibitors
US20120165306A1 (en) 2009-09-04 2012-06-28 Barsanti Paul A Pyrazinylpyridines useful for the treatment of proliferative diseases
WO2011026911A1 (en) 2009-09-04 2011-03-10 Novartis Ag Bipyridines useful for the treatment of proliferative diseases
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.
US8519134B2 (en) 2009-11-17 2013-08-27 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
ES2472446T3 (es) 2009-11-30 2014-07-01 Novartis Ag Derivados de imidazol como inhibidores de aldosterona sintasa
WO2011073316A1 (en) 2009-12-18 2011-06-23 Novartis Ag 4-aryl-butane-1,3-diamides
US8633313B2 (en) 2009-12-18 2014-01-21 Amgen Inc. Heterocyclic compounds and their uses
EP2516437B1 (en) 2009-12-21 2014-01-29 Novartis AG Disubstituted heteroaryl-fused pyridines
ES2459496T3 (es) 2009-12-21 2014-05-09 Novartis Ag Diaza-espiro[5.5]undecanos como antagonistas del receptor de orexina
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
WO2011092290A1 (en) 2010-02-01 2011-08-04 Novartis Ag Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists
EP2531490B1 (en) 2010-02-02 2014-10-15 Novartis AG Cyclohexyl amide derivatives as crf receptor antagonists
US8791100B2 (en) 2010-02-02 2014-07-29 Novartis Ag Aryl benzylamine compounds
UY33226A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
AR082453A1 (es) 2010-04-21 2012-12-12 Novartis Ag Compuestos de furopiridina, composiciones farmaceuticas que los contienen y usos de los mismos
MA34300B1 (fr) 2010-05-13 2013-06-01 Amgen Inc Composés azotés hétérocycliques convenant comme inhibiteurs de la pde10
AU2011253058A1 (en) 2010-05-13 2012-12-06 Amgen Inc. Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
CA2798325A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
US8946230B2 (en) 2010-05-13 2015-02-03 Amgen Inc. Aryl- and heteroaryl- nitrogen-heterocyclic compounds as PDE10 inhibitors
CN102947274A (zh) 2010-06-17 2013-02-27 诺瓦提斯公司 联苯基取代的1,3-二氢-苯并咪唑-2-亚基胺衍生物
WO2011157793A1 (en) 2010-06-17 2011-12-22 Novartis Ag Piperidinyl 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
US20130079342A1 (en) 2010-06-30 2013-03-28 Paul John Dransfield Heterocyclic compounds and their uses
AU2011272857A1 (en) 2010-06-30 2013-01-10 Amgen Inc. Quinolines as P13K inhibitors
AU2011272862A1 (en) 2010-06-30 2013-01-10 Amgen Inc. Heterocyclic compounds and their use as inhibitors of PI3K activity
EP2588468B1 (en) 2010-07-01 2014-03-26 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
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
JP2013533884A (ja) 2010-07-02 2013-08-29 アムジエン・インコーポレーテツド Pi3k活性阻害剤としての複素環化合物およびそれらの使用
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
PH12012500361A1 (en) 2010-07-13 2012-01-19 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
EP2593452B1 (en) 2010-07-14 2017-01-18 Novartis AG Ip receptor agonist heterocyclic compounds
EP2595983A1 (en) 2010-07-22 2013-05-29 Novartis AG 2,3,5-trisubstituted thiophene compounds and uses thereof
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
CN103221408A (zh) 2010-09-13 2013-07-24 诺瓦提斯公司 三嗪-*二唑类化合物
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
RU2603140C2 (ru) 2010-09-20 2016-11-20 Айронвуд Фармасьютикалз, Инк. Соединения имидазотриазинона
US20120101110A1 (en) 2010-10-26 2012-04-26 Sangamesh Badiger Diaza-spiro[5.5]undecanes
EP2635565A1 (en) 2010-11-04 2013-09-11 Amgen Inc. 5 -cyano-4, 6 -diaminopyrimidine or 6 -aminopurine derivatives as pi3k- delta inhibitors
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
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
EP2640715A1 (en) 2010-11-17 2013-09-25 Amgen Inc. Quinoline derivatives as pik3 inhibitors
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
EP2655368A1 (en) 2010-12-20 2013-10-30 Irm Llc Compositions and methods for modulating farnesoid x receptors
WO2012087521A1 (en) 2010-12-20 2012-06-28 Irm Llc Compositions and methods for modulating farnesoid x receptors
MX2013007261A (es) 2010-12-23 2013-11-04 Amgen Inc Compuestos heterociclicos y sus usos.
EP2661433B1 (en) 2011-01-04 2017-08-16 Novartis AG Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
MX2013008192A (es) 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
WO2012101063A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyridine biaryl compounds and their uses
WO2012101066A1 (en) 2011-01-28 2012-08-02 Novartis Ag Pyridine biaryl amine compounds and their uses
WO2012101065A2 (en) 2011-01-28 2012-08-02 Novartis Ag Pyrimidine 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
EP2688886A1 (en) 2011-03-22 2014-01-29 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
CA2831356A1 (en) 2011-03-31 2012-10-04 Emblem Technology Transfer Gmbh Imidazo [1,2-a]pyridine_compounds for use in therapy
WO2012130314A1 (en) 2011-03-31 2012-10-04 Elara Pharmaceuticals Gmbh Composition comprising docetaxel
WO2012138648A1 (en) 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
JP2014516941A (ja) 2011-04-29 2014-07-17 アムジェン インコーポレイテッド Pim阻害剤としての二環式ピリダジン化合物
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
US8710043B2 (en) 2011-06-24 2014-04-29 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
WO2013057711A1 (en) 2011-10-21 2013-04-25 Novartis Ag Quinazoline derivatives as pi3k modulators
WO2013105058A1 (en) 2012-01-13 2013-07-18 Novartis Ag 7,8- dihydropyrido [3, 4 - b] pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802583A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
US9115129B2 (en) 2012-01-13 2015-08-25 Novartis Ag Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
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
AR089698A1 (es) 2012-01-13 2014-09-10 Novartis Ag Compuestos heterociclicos antagonistas del receptor ip
US9394297B2 (en) 2012-02-28 2016-07-19 Amgen Inc. Amides as pim inhibitors
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
EP2828262A4 (en) 2012-03-19 2015-09-23 Forum Pharmaceuticals Inc IMIDAZOTRIAZINONVERBINDUNGEN
HUE028762T2 (en) 2012-04-04 2016-12-28 Amgen Inc Heterocyclic compounds and their applications
EP2855456B1 (en) 2012-05-04 2017-03-29 Novartis AG Complement pathway modulators and uses thereof
CN104520291A (zh) 2012-06-06 2015-04-15 Irm责任有限公司 用于调节egfr活性的化合物和组合物
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
AR091436A1 (es) 2012-06-14 2015-02-04 Amgen Inc Compuestos de azetidina y piperidina utiles como inhibidores de pde10
JP6163205B2 (ja) 2012-06-20 2017-07-12 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
ES2644700T3 (es) 2012-06-28 2017-11-30 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la ruta del complemento
CN104379579B (zh) 2012-06-28 2017-03-08 诺华股份有限公司 吡咯烷衍生物及其作为补体途径调节剂的用途
WO2014002054A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
JP6214647B2 (ja) 2012-06-28 2017-10-18 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
EP2867222A1 (en) 2012-06-28 2015-05-06 Novartis AG Pyrrolidine derivatives and their use as complement pathway modulators
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
WO2014009833A2 (en) 2012-07-12 2014-01-16 Novartis Ag Complement pathway modulators and uses thereof
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
ES2637719T3 (es) 2013-02-13 2017-10-16 Novartis Ag Compuestos heterocíclicos agonistas del receptor IP
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
EP3030902B1 (en) 2013-08-07 2019-09-25 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
AU2016236187B2 (en) 2015-03-24 2020-05-21 Helmholtz-Zentrum Fur Infektionsforschung Gmbh Inhibitors of Pseudomonas aeruginosa LecB
CN107531721B (zh) 2015-04-30 2020-07-17 诺华股份有限公司 用于调节法尼醇x受体的稠合的三环吡唑衍生物
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
MX378012B (es) 2015-12-18 2025-03-10 Amgen Inc Compuestos de alquinil dihidroquinolina sulfonamida.
CN108602804B (zh) 2015-12-18 2025-05-02 美国安进公司 烷基二氢喹啉磺酰胺化合物
DK3579874T3 (da) 2017-02-10 2021-10-11 Novartis Ag 1-(4-amino-5-brom-6-(1h-pyrazol-1-yl)pyrimidin-2-yl)-1h-pyrazol-4-ol og anvendelse deraf til behandling af cancer
JP2020523363A (ja) 2017-06-14 2020-08-06 ヨーロピアン モレキュラー バイオロジー ラボラトリーEuropean Molecular Biology Laboratory 治療への使用のための二環式複素芳香族アミド化合物
JP2020523391A (ja) 2017-06-14 2020-08-06 ヨーロピアン モレキュラー バイオロジー ラボラトリーEuropean Molecular Biology Laboratory 治療への使用のためのベンゾフラン尿素またはカルバメートおよびそれらの複素芳香族アナログ
EP3638664A1 (en) 2017-06-14 2020-04-22 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
CA3067070A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Bicyclic heteroaromatic urea or carbamate compounds for use in therapy
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität Heidelberg Fap inhibitor
SG11202007180QA (en) 2018-02-06 2020-08-28 Univ Heidelberg Fap inhibitor
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
EP3898616B1 (en) 2018-12-20 2024-10-02 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
WO2020132651A1 (en) 2018-12-20 2020-06-25 Amgen Inc. Kif18a inhibitors
JP7676308B2 (ja) 2018-12-20 2025-05-14 アムジエン・インコーポレーテツド Kif18a阻害剤として有用なヘテロアリールアミド
TWI844602B (zh) 2018-12-20 2024-06-11 美商安進公司 Kif18a抑制劑
US12540129B2 (en) 2019-08-02 2026-02-03 Amgen Inc. KIF18A inhibitors
WO2021026099A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
AU2020326627B2 (en) 2019-08-02 2026-01-29 Amgen Inc. KIF18A inhibitors
EP4007756B1 (en) 2019-08-02 2025-12-24 Amgen Inc. Kif18a inhibitors
AU2020379206A1 (en) 2019-11-05 2022-05-05 Centre National De La Recherche Scientifique Direction De La Politique Industrielle Bivalent LecA inhibitors targeting biofilm formation of
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
WO2021148807A1 (en) 2020-01-22 2021-07-29 Benevolentai Bio Limited Pharmaceutical compositions and their uses
JP2023521802A (ja) 2020-04-14 2023-05-25 アムジエン・インコーポレーテツド 新生物疾患の処置のためのkif18a阻害剤
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.
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
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
US20240025849A1 (en) 2020-08-26 2024-01-25 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
TW202241516A (zh) 2020-12-17 2022-11-01 美商杜夫特學院信託管理公司 經fap活化之放射性治療診斷(radiotheranostics),與其相關用途
CA3234157A1 (en) 2021-10-29 2023-05-04 William M. MENZER Inhibitors of viral helicases binding to a novel allosteric binding site
TW202348228A (zh) 2022-02-24 2023-12-16 德商艾斯巴赫生物有限公司 病毒組合療法
JP2025515110A (ja) 2022-05-02 2025-05-13 アイスバッハ・バイオ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング Alc1阻害剤の使用およびparpiとの相乗作用
WO2024022332A1 (en) 2022-07-26 2024-02-01 Shanghai Sinotau Biotech. Co., Ltd Fap inhibitors
WO2025012460A1 (en) 2023-07-12 2025-01-16 HMNC Holding GmbH Deuterated 1,3 dihydro -2h-indole-2-one derivatives
CN121773094A (zh) 2023-09-12 2026-03-31 上海先通生物科技有限公司 前列腺特异性膜抗原的抑制剂和其用途
WO2025055943A1 (en) 2023-09-12 2025-03-20 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
AU2024366320A1 (en) 2023-10-25 2026-04-16 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
NL175382C (nl) * 1970-09-09 1984-11-01 Ciba Geigy Werkwijze ter bereiding van antiflogistisch, analgetisch of antipyretisch werkzame farmaceutische preparaten, alsmede werkwijze ter bereiding van voor gebruik bij die werkwijze geschikte o-anilinofenylaceetamidederivaten.
US4206220A (en) * 1978-07-13 1980-06-03 Interx Research Corporation Prodrugs for the improved delivery of non-steroidal anti-inflammatory agents

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ES501573A0 (es) 1982-09-16
ATE14423T1 (de) 1985-08-15
DK156717B (da) 1989-09-25
EP0039051A3 (en) 1982-05-26
EP0039051B1 (en) 1985-07-24
JPS56167643A (en) 1981-12-23
DK156717C (da) 1990-02-19
IE53001B1 (en) 1988-05-11
PT72878A (en) 1981-05-01
EP0039051A2 (en) 1981-11-04
JPH04982B2 (ref) 1992-01-09

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