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)
  • 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 (index.php)
JP (1) JPS56167643A (index.php)
AT (1) ATE14423T1 (index.php)
DE (1) DE3171467D1 (index.php)
DK (1) DK156717C (index.php)
ES (1) ES8207508A1 (index.php)
GR (1) GR74496B (index.php)
IE (1) IE53001B1 (index.php)
PT (1) PT72878B (index.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
US6107291A (en) * 1997-12-19 2000-08-22 Amgen Inc. Azepine or larger medium ring derivatives 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
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
AU2003247425B2 (en) 2002-05-22 2007-03-08 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
US7144888B2 (en) 2002-08-08 2006-12-05 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
CN103420877B (zh) 2006-03-29 2015-08-12 诺瓦提斯公司 基于异羟肟酸酯的选择性mmp抑制剂
EP2037928B1 (en) 2006-06-26 2012-01-11 Amgen Inc. Methods for treating atherosclerosis
CA2656535C (en) 2006-07-14 2011-08-23 Amgen Inc. Alkyne-substituted pyridone compounds and methods of use
PL2049517T3 (pl) 2006-07-20 2014-06-30 Novartis Ag Pochodne amino-piperydyny jako inhibitory CETP
CA2658462C (en) 2006-07-20 2011-09-27 Amgen Inc. 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
MX2009009968A (es) 2007-03-23 2009-10-08 Amgen Inc Compuestos heterociclicos y sus usos.
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
PT2229356E (pt) 2007-12-03 2012-01-20 Novartis Ag Derivados de 4-benzilamino-pirrolidina 1,2-dissubstituídos como inibidores de cetp úteis para o tratamento de doenças tais como hiperlipidemia ou arteriosclerose
WO2009118292A1 (en) 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
WO2010077992A1 (en) 2008-12-17 2010-07-08 Amgen Inc. Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
WO2010085968A1 (en) 2008-12-30 2010-08-05 European Molecular Biology Laboratory (Embl) Toluidine sulfonamides and their use as hif-inhibitors
WO2010075869A1 (en) 2008-12-30 2010-07-08 European Molecular Biology Laboratory (Embl) Toluidine sulfonamides and their use
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
CN102803217B (zh) 2009-05-15 2015-06-17 诺华股份有限公司 作为醛固酮合酶抑制剂的芳基吡啶
ES2582395T3 (es) 2009-05-28 2016-09-12 Novartis Ag Derivados aminobutíricos sustituidos como inhibidores de neprilisina
AR076707A1 (es) 2009-05-28 2011-06-29 Novartis Ag Derivados amino-propionicos sustituidos como inhibidores de neprilisina
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
MX2011013901A (es) 2009-06-25 2012-05-08 Amgen Inc Derivados de 4h-pirido [1,2-a] pirimidin-4-ona como inhibidores de pi3k.
BR112012000660A2 (pt) 2009-06-25 2016-11-16 Amgen Inc compostos heterociclos e seus usos
TW201111362A (en) 2009-06-25 2011-04-01 Amgen Inc Heterocyclic compounds and their uses
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
WO2011023677A1 (en) 2009-08-26 2011-03-03 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
ES2730086T3 (es) 2009-09-03 2019-11-08 Allergan Inc Compuestos como moduladores de tirosina cinasa
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
WO2011026911A1 (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
BR112012008147A2 (pt) 2009-09-04 2016-03-01 Novartis Ag compostos heteroarílicos como inibidores da quinase
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.
ES2551002T3 (es) 2009-11-17 2015-11-13 Novartis Ag Derivados de aril-piridina como inhibidores de la aldosterona sintasa
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
CA2784566A1 (en) 2009-12-18 2011-06-23 Amgen Inc. Heterocyclic compounds and their uses
JP2013515033A (ja) 2009-12-21 2013-05-02 ノバルティス アーゲー オレキシン受容体アンタゴニストとしてのジアザ−スピロ[5.5]ウンデカン類
EP2516437B1 (en) 2009-12-21 2014-01-29 Novartis AG Disubstituted heteroaryl-fused pyridines
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
WO2011092290A1 (en) 2010-02-01 2011-08-04 Novartis Ag 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
US8791100B2 (en) 2010-02-02 2014-07-29 Novartis Ag Aryl benzylamine compounds
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
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
CA2799020A1 (en) 2010-05-13 2011-11-17 Jennifer R. Allen Heteroaryloxycarbocyclyl compounds as pde10 inhibitors
JP5702855B2 (ja) 2010-05-13 2015-04-15 アムジエン・インコーポレーテツド Pde10阻害剤として有用な窒素複素環化合物
MX2012013127A (es) 2010-05-13 2012-11-30 Amgen Inc Compuestos heteroariloxiheterociclilo como inhibidores pde10.
CA2800578A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Nitrogen-heterocyclic compounds as phosphodiesterase 10 inhibitors
EP2582681A1 (en) 2010-06-17 2013-04-24 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
AU2011271462A1 (en) 2010-06-30 2013-01-10 Amgen Inc. Nitrogen containing heterocyclic compounds as PIK3 -delta inhibitors
US8686137B2 (en) 2010-06-30 2014-04-01 Amgen Inc. Heterocyclic compounds and their uses
WO2012003283A1 (en) 2010-06-30 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
WO2012003274A1 (en) 2010-07-01 2012-01-05 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
MX2012014996A (es) 2010-07-01 2013-03-21 Amgen Inc Compuestos heterociclicos y su uso como inhibidores de la actividad pi3k.
CA2803624A1 (en) 2010-07-02 2012-01-05 Jason A. Duquette Heterocyclic compounds and their use as inhibitors of pi3k activity
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
NZ598137A (en) 2010-07-13 2014-06-27 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
CN103097385B (zh) 2010-07-14 2016-08-03 诺华股份有限公司 Ip受体激动剂杂环化合物
MA34462B1 (fr) 2010-07-22 2013-08-01 Novartis Ag Composes de thiophene 2,3,5- trisubstitues et leurs utilisations
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
RS54544B1 (sr) 2010-09-13 2016-06-30 Novartis Ag Triazin-oksadiazoli
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
TWI541244B (zh) 2010-09-20 2016-07-11 福倫製藥股份有限公司 咪唑三酮化合物
US20120101110A1 (en) 2010-10-26 2012-04-26 Sangamesh Badiger Diaza-spiro[5.5]undecanes
US20140031355A1 (en) 2010-11-04 2014-01-30 Amgen Inc. Heterocyclic compounds and their uses
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
US8993631B2 (en) 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8765768B2 (en) 2010-11-17 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
EP2649065A1 (en) 2010-12-09 2013-10-16 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
US20140039007A1 (en) 2010-12-20 2014-02-06 David C. Tully Compositions and methods for modulating farnesoid x receptors
CN103370315A (zh) 2010-12-20 2013-10-23 Irm责任有限公司 用于调控法尼醇x受体的组合物和方法
MX2013007261A (es) 2010-12-23 2013-11-04 Amgen Inc Compuestos heterociclicos y sus usos.
MX347391B (es) 2011-01-04 2017-04-25 Novartis Ag Compuestos de indol o análogos de los mismos útiles para el tratamiento de degeneración macular relacionada con la edad (amd).
BR112013017988A2 (pt) 2011-01-13 2019-09-24 Novartis Ag inibidores de bace-2 para o tratamento de distúrbios metabólicos
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
WO2012101066A1 (en) 2011-01-28 2012-08-02 Novartis Ag Pyridine biaryl amine compounds and their uses
WO2012101063A1 (en) 2011-01-28 2012-08-02 Novartis Ag N-acyl pyridine biaryl compounds and their uses
GB201103578D0 (en) 2011-03-02 2011-04-13 Sabrepharm Ltd Dipyridinium derivatives
MX2013010771A (es) 2011-03-22 2014-01-31 Amgen Inc Compuestos de azoles como inhibidores.
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
AP2013007331A0 (en) 2011-06-24 2013-12-31 Amgen Inc TRPM8 antagonists and their use in treatments
WO2012177896A1 (en) 2011-06-24 2012-12-27 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
JP2014530851A (ja) 2011-10-21 2014-11-20 ノバルティスアーゲー Pi3kモジュレータとしてのキナゾリン誘導体
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
WO2013105061A1 (en) 2012-01-13 2013-07-18 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
EP2802585A1 (en) 2012-01-13 2014-11-19 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
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
EP2828262A4 (en) 2012-03-19 2015-09-23 Forum Pharmaceuticals Inc IMIDAZOTRIAZINONVERBINDUNGEN
WO2013152150A1 (en) 2012-04-04 2013-10-10 Amgen Inc. Heterocyclic compounds and their uses
WO2013164802A1 (en) 2012-05-04 2013-11-07 Novartis Ag Complement pathway modulators and uses thereof
US20150152083A1 (en) 2012-06-06 2015-06-04 Irm Llc, A Delaware Limited Liability Company Compounds and Compositions for Modulating EGFR Activity
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
UY34858A (es) 2012-06-14 2013-11-29 Amgen Inc Compuestos de azetidina y piperidina útiles como inhibidores de pde10
WO2013192345A1 (en) 2012-06-20 2013-12-27 Novartis Ag Complement pathway modulators and uses thereof
US9815819B2 (en) 2012-06-28 2017-11-14 Novartis Ag Complement pathway modulators and uses thereof
ES2712190T3 (es) 2012-06-28 2019-05-09 Novartis Ag Moduladores de la vía del complemento y sus usos
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
ES2644700T3 (es) 2012-06-28 2017-11-30 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la ruta del complemento
CN104619698B (zh) 2012-06-28 2016-08-31 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
MX2014015738A (es) 2012-06-28 2015-08-06 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la senda del complemento.
JP6238980B2 (ja) 2012-07-12 2017-11-29 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
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
WO2014041125A1 (en) 2012-09-13 2014-03-20 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents
US9604981B2 (en) 2013-02-13 2017-03-28 Novartis Ag IP receptor agonist heterocyclic compounds
KR20150119109A (ko) 2013-02-14 2015-10-23 노파르티스 아게 Nep (중성 엔도펩티다제) 억제제로서의 치환된 비스페닐 부타노익 포스폰산 유도체
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
ES2770128T3 (es) 2015-04-30 2020-06-30 Recordati Ag Derivados de pirazol tricíclicos condensados útiles para modular los receptores farnesoide x
WO2017031105A1 (en) 2015-08-19 2017-02-23 Selten Pharma, 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
US10729684B2 (en) 2015-12-18 2020-08-04 Amgen Inc. Alkynyl dihydroquinoline sulfonamide compounds
PE20181328A1 (es) 2015-12-18 2018-08-20 Amgen Inc Compuestos de dihidroquinolinsulfonamida de alquilo
HUE057337T2 (hu) 2017-02-10 2022-05-28 Novartis Ag 1-(4-amino-5-bróm-6-(1H-pirazol-1-il)pirimidin-2-il)-1H-pirazol-4-ol és alkalmazása rák kezelésében
CA3067075A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Bicyclic heteroaromatic amide compounds for use in therapy
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
CA3067070A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Bicyclic heteroaromatic urea or carbamate compounds for use in therapy
WO2018229193A1 (en) 2017-06-14 2018-12-20 European Molecular Biology Laboratory Benzofuran amides and heteroaromatic analogues thereof for use in therapy
CN111699181A (zh) 2018-02-06 2020-09-22 海德堡大学 Fap抑制剂
WO2019154859A1 (en) 2018-02-06 2019-08-15 Universität 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
MX419368B (es) 2018-12-20 2025-01-14 Amgen Inc Heteroarilamidas utiles como inhibidores de kif18a
MX2021007104A (es) 2018-12-20 2021-08-11 Amgen Inc Inhibidores de kif18a.
JP7407196B2 (ja) 2018-12-20 2023-12-28 アムジエン・インコーポレーテツド Kif18a阻害剤
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
CA3147276A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
US12435058B2 (en) 2019-08-02 2025-10-07 Amgen Inc. KIF18A inhibitors
WO2021026101A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
US20220289724A1 (en) 2019-08-02 2022-09-15 Amgen Inc. Kif18a inhibitors
CA3159906A1 (en) 2019-11-05 2021-05-14 Helmholtz-Zentrum Fur Infektionsforschung Gmbh Bivalent leca inhibitors targeting biofilm formation of pseudomonas aeruginosa
CA3163585A1 (en) 2020-01-22 2021-07-29 Benevolentai Bio Limited Pharmaceutical compositions and their uses
BR112022013161A2 (pt) 2020-01-22 2022-10-18 Benevolentai Bio Ltd Composições farmacêuticas tópicas compreendendo compostos de imidazo[1,2-b]piridazina
TW202203919A (zh) 2020-04-14 2022-02-01 美商安進公司 用於治療贅生性疾病之kif18a抑制劑
WO2021234181A1 (en) 2020-05-22 2021-11-25 Universität Heidelberg Use of fap inhibitor in a method of diagnosis
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
WO2021252822A1 (en) 2020-06-10 2021-12-16 Amgen Inc. Heteroalkyl dihydroquinoline sulfonamide compounds
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
WO2022133288A1 (en) 2020-12-17 2022-06-23 Trustees Of Tufts College Fap-activated radiotheranostics, and uses related thereto
JP2024541991A (ja) 2021-10-29 2024-11-13 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 新規アロステリック結合部位に結合するウイルスヘリカーゼ阻害剤
WO2023161427A1 (en) 2022-02-24 2023-08-31 Eisbach Bio Gmbh Viral combination therapy
CA3250274A1 (en) 2022-05-02 2023-11-09 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
WO2025012460A1 (en) 2023-07-12 2025-01-16 HMNC Holding GmbH Deuterated 1,3 dihydro -2h-indole-2-one derivatives
TW202525787A (zh) 2023-09-12 2025-07-01 大陸商上海先通生物科技有限公司 前列腺特異性膜抗原之抑制劑及其用途
WO2025055942A1 (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
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
FI55181C (fi) * 1970-09-09 1979-06-11 Ciba Geigy Ag Foerfarande foer framstaellning av nya farmaceutiskt effektiva fenylacethydroxamsyror
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
JPS56167643A (en) 1981-12-23
DK156717B (da) 1989-09-25
IE810899L (en) 1981-10-24
EP0039051A3 (en) 1982-05-26
ATE14423T1 (de) 1985-08-15
EP0039051B1 (en) 1985-07-24
JPH04982B2 (index.php) 1992-01-09
EP0039051A2 (en) 1981-11-04
DK182081A (da) 1981-10-25
DE3171467D1 (en) 1985-08-29
DK156717C (da) 1990-02-19
PT72878A (en) 1981-05-01
ES501573A0 (es) 1982-09-16
ES8207508A1 (es) 1982-09-16
GR74496B (index.php) 1984-06-28
IE53001B1 (en) 1988-05-11

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.
ATE54450T1 (de) Thiazolylessigsaeure-derivate und verfahren zu deren herstellung.
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