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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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 (show.php)
JP (1) JPS56167643A (show.php)
AT (1) ATE14423T1 (show.php)
DE (1) DE3171467D1 (show.php)
DK (1) DK156717C (show.php)
ES (1) ES501573A0 (show.php)
GR (1) GR74496B (show.php)
IE (1) IE53001B1 (show.php)
PT (1) PT72878B (show.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
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
ATE493987T1 (de) 2002-05-22 2011-01-15 Amgen Inc Aminopyrimidin-derivate zur verwendung als vanilloid-rezeptor-liganden zur behandlung von schmerzen
US6908935B2 (en) 2002-05-23 2005-06-21 Amgen Inc. Calcium receptor modulating agents
US7176322B2 (en) 2002-05-23 2007-02-13 Amgen Inc. Calcium receptor modulating agents
NZ537952A (en) 2002-08-08 2008-04-30 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
MX2008012387A (es) 2006-03-29 2008-10-09 Novartis Ag Inhibidores selectivos de mmp basados en hidroxamato.
ES2376396T3 (es) 2006-06-26 2012-03-13 Amgen Inc. Método para tratar aterosclerosis.
ES2426780T3 (es) 2006-07-14 2013-10-25 Amgen Inc. Compuestos de piridona sustituidos con alquino y métodos de uso
MX2009000646A (es) 2006-07-20 2009-01-29 Novartis Ag Derivados de amino-piperidina como inhibidores de la proteina de transferencia de colesteril-ester (cetp).
EP2057133B1 (en) 2006-07-20 2014-08-20 Amgen Inc. Di-amino-substituted heterocyclic compounds and methods of use
ATE469144T1 (de) 2006-07-20 2010-06-15 Amgen Inc Substituierte pyridonverbindungen und anwendungsverfahren
CA2681136C (en) 2007-03-23 2012-05-22 Amgen Inc. Heterocyclic compounds and their uses
CA2704633C (en) 2007-11-05 2015-10-20 Novartis Ag 4-benzylamino-1-carboxyacyl-piperidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
CN101878199B (zh) 2007-12-03 2013-09-18 诺瓦提斯公司 用于治疗例如高血脂或动脉硬化疾病的作为cetp抑制剂的1，2-二取代的-4-苄基氨基-吡咯烷衍生物
BRPI0908603A2 (pt) 2008-03-24 2020-08-18 Novartis Ag inibidores de metaloprotease de matriz com base em arilsulfonamida.
CA2746307C (en) 2008-12-17 2013-11-19 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
CA2761859A1 (en) 2009-05-15 2010-11-18 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
CN102448928B (zh) 2009-05-28 2014-10-01 诺华股份有限公司 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物
ES2602826T3 (es) 2009-05-28 2017-02-22 Novartis Ag Derivados aminobutíricos sustituidos como inhibidores de neprilisina
EA201270013A1 (ru) 2009-06-25 2012-06-29 Амген Инк. Гетероциклические соединения и их применение
CA2765823A1 (en) 2009-06-25 2010-12-29 Amgen Inc. Tricyclic heterocyclic compounds as mediators of p13k activity
EP2445902A2 (en) 2009-06-25 2012-05-02 Amgen, Inc Heterocyclic compounds and their uses as inhibitors of pi3k activity
JP2012531435A (ja) 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド ＰＩ３Ｋ阻害剤としての４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オン誘導体
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
CA2771936A1 (en) 2009-08-26 2011-03-03 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
US9340555B2 (en) 2009-09-03 2016-05-17 Allergan, Inc. Compounds as tyrosine kinase modulators
MX2012002596A (es) 2009-09-03 2012-07-03 Allergan Inc Compuestos como moduladores de tirosina cinasas.
CN102498107A (zh) 2009-09-04 2012-06-13 诺瓦提斯公司 作为激酶抑制剂的杂芳基化合物
EP2473499A1 (en) 2009-09-04 2012-07-11 Novartis AG Bipyridines useful for the treatment of proliferative diseases
CN102482265A (zh) 2009-09-04 2012-05-30 诺瓦提斯公司 用于治疗增殖性疾病的吡嗪基吡啶化合物
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.
EP2501678B1 (en) 2009-11-17 2015-09-23 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
CN102762567A (zh) 2009-12-21 2012-10-31 诺瓦提斯公司 作为食欲肽受体拮抗剂的二氮杂-螺[5.5]十一烷类
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
CN102762572A (zh) 2010-02-01 2012-10-31 诺瓦提斯公司 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
US8835444B2 (en) 2010-02-02 2014-09-16 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
AU2011253143A1 (en) 2010-05-13 2012-12-06 Amgen Inc. Nitrogen- heterocyclic compounds as phosphodiesterase 10 inhibitors
US8497265B2 (en) 2010-05-13 2013-07-30 Amgen Inc. Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors
NZ603876A (en) 2010-05-13 2015-02-27 Amgen Inc Nitrogen heterocyclic compounds useful as pde10 inhibitors
JP2013526537A (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ールオキシカルボシクリル化合物
EP2582681A1 (en) 2010-06-17 2013-04-24 Novartis AG Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
JP2013528635A (ja) 2010-06-17 2013-07-11 ノバルティス アーゲー ビフェニル置換１，３−ジヒドロ−ベンゾイミダゾール−２−イリデンアミン誘導体
UY33469A (es) 2010-06-29 2012-01-31 Irm Llc Y Novartis Ag Composiciones y metodos para modular la via de señalizacion de wnt
AU2011272862A1 (en) 2010-06-30 2013-01-10 Amgen Inc. Heterocyclic compounds and their use as inhibitors of PI3K activity
WO2012003264A1 (en) 2010-06-30 2012-01-05 Amgen Inc. Nitrogen containing heterocyclic compounds as pik3 -delta inhibitors
CA2803619A1 (en) 2010-06-30 2012-01-05 Amgen Inc. Heterocycle compounds and their uses
MX2012014996A (es) 2010-07-01 2013-03-21 Amgen Inc Compuestos heterociclicos y su uso como inhibidores de la actividad pi3k.
EP2588467A1 (en) 2010-07-01 2013-05-08 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
EP2588469A1 (en) 2010-07-02 2013-05-08 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
RS53096B (sr) 2010-07-13 2014-06-30 Novartis Ag Derivati oksazina i njihova upotreba u lečenju neuroloških oboljenja
AU2011278279C1 (en) 2010-07-14 2014-11-27 Novartis Ag IP receptor agonist heterocyclic compounds
CN103025728B (zh) 2010-07-22 2015-11-25 诺华股份有限公司 2,3,5-三取代的噻吩化合物及其用途
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
NZ608116A (en) 2010-09-13 2014-05-30 Novartis Ag Triazine-oxadiazoles
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
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
CA2816144A1 (en) 2010-11-17 2012-05-24 Amgen Inc. Quinoline derivatives as pik3 inhibitors
EP2649065A1 (en) 2010-12-09 2013-10-16 Amgen Inc. Bicyclic compounds as pim inhibitors
US20130261108A1 (en) 2010-12-20 2013-10-03 Irm Llc Compositions and methods for modulating farnesoid x receptors
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
JP2014500319A (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
JP2014501261A (ja) 2010-12-23 2014-01-20 アムジエン・インコーポレーテツド 複素環化合物およびそれらの使用
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)
MX2013008192A (es) 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
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
WO2012129338A1 (en) 2011-03-22 2012-09-27 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
EP2691392A1 (en) 2011-03-31 2014-02-05 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
WO2012148775A1 (en) 2011-04-29 2012-11-01 Amgen Inc. Bicyclic pyridazine compounds as pim inhibitors
CA2839703A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
PH12013502611A1 (en) 2011-06-24 2014-04-28 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
US20150005311A1 (en) 2012-01-13 2015-01-01 Novartis Ag IP receptor agonist heterocyclic compounds
TW201335160A (zh) 2012-01-13 2013-09-01 Novartis Ag Ｉｐ受體激動劑之雜環化合物
EP2802585A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of 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
US20140378463A1 (en) 2012-01-13 2014-12-25 Novartis Ag IP receptor agonist heterocyclic compounds
WO2013130660A1 (en) 2012-02-28 2013-09-06 Amgen Inc. Amides as pim inhibitors
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
HK1206726A1 (en) 2012-03-19 2016-01-15 Ironwood Pharmaceuticals, Inc. Imidazotriazinone compounds
CA2869413A1 (en) 2012-04-04 2013-10-10 Amgen Inc. Heterocyclic compounds and their uses
EA027113B1 (ru) 2012-05-04 2017-06-30 Новартис Аг Регуляторы пути комплемента и их применение
JP2015518895A (ja) 2012-06-06 2015-07-06 アイアールエム・リミテッド・ライアビリティ・カンパニーＩｒｍ，Ｌｌｃ Ｅｇｆｒ活性を調節するための化合物および組成物
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
US9452990B2 (en) 2012-06-20 2016-09-27 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
US9388199B2 (en) 2012-06-28 2016-07-12 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
EA201590118A1 (ru) 2012-06-28 2015-04-30 Новартис Аг Производные пирролидина и их применение в качестве модуляторов пути активации комплемента
US9468661B2 (en) 2012-06-28 2016-10-18 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
WO2014002051A2 (en) 2012-06-28 2014-01-03 Novartis Ag Complement pathway modulators and uses thereof
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
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
WO2014041125A1 (en) 2012-09-13 2014-03-20 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents
EP2956455B1 (en) 2013-02-13 2017-05-17 Novartis AG Ip receptor agonist heterocyclic compounds
SG11201506018PA (en) 2013-02-14 2015-08-28 Novartis Ag Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors
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
AU2016236187B2 (en) 2015-03-24 2020-05-21 Helmholtz-Zentrum Fur Infektionsforschung Gmbh Inhibitors of Pseudomonas aeruginosa LecB
JP6691552B2 (ja) 2015-04-30 2020-04-28 ノバルティス アーゲー ファルネソイドｘ受容体をモジュレートするのに有用である縮合三環式ピラゾール誘導体
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
JP6985271B2 (ja) 2015-12-18 2021-12-22 アムジエン・インコーポレーテツド アルキニルジヒドロキノリンスルホンアミド化合物
US10383866B2 (en) 2015-12-18 2019-08-20 Amgen Inc. Alkyl dihydroquinoline sulfonamide compounds
AU2018217963B2 (en) 2017-02-10 2020-11-19 Novartis Ag 1-(4-amino-5-bromo-6-(1 H-pyrazol-1-yl)pyrimidin-2-yl)-1 H-pyrazol-4-ol and use thereof in the treatment of cancer
US20210147405A1 (en) 2017-06-14 2021-05-20 European Molecular Biology Laboratory Bicyclic heteroaromatic urea or carbamate compounds for use in therapy
JP2020523379A (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アミドおよびそれらの複素芳香族アナログ
US20200216435A1 (en) 2017-06-14 2020-07-09 European Molecular Biology Laboratory Bicyclic heteroaromatic amide 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
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
EP3898616B1 (en) 2018-12-20 2024-10-02 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
EP3898592B1 (en) 2018-12-20 2024-10-09 Amgen Inc. Heteroaryl amides useful as kif18a inhibitors
US11236069B2 (en) 2018-12-20 2022-02-01 Amgen Inc. KIF18A inhibitors
MA54550A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
CN114269731A (zh) 2019-08-02 2022-04-01 美国安进公司 Kif18a抑制剂
WO2021026099A1 (en) 2019-08-02 2021-02-11 Amgen Inc. Kif18a inhibitors
JP7756070B2 (ja) 2019-08-02 2025-10-17 アムジエン・インコーポレーテツド Ｋｉｆ１８ａ阻害剤としてのピリジン誘導体
EP4007752B1 (en) 2019-08-02 2025-09-24 Amgen Inc. Kif18a inhibitors
CN114901362A (zh) 2019-11-05 2022-08-12 赫姆霍尔兹传染病研究中心有限责任公司 针对铜绿假单胞菌生物膜形成的二价leca抑制剂
MX2022008930A (es) 2020-01-22 2022-10-18 Benevolentai Bio Ltd Composiciones farmaceuticas y sus usos.
KR20220130164A (ko) 2020-01-22 2022-09-26 베네볼런트에이아이 바이오 리미티드 이미다조[1,2-b]피리다진 화합물을 포함하는 국소 약제학적 조성물
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
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
ES3023366T3 (en) 2020-06-10 2025-05-30 Amgen Inc Heteroalkyl dihydroquinoline sulfonamide compounds
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
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
EP4262878A1 (en) 2020-12-17 2023-10-25 Trustees Of Tufts College Fap-activated radiotheranostics, and uses related thereto
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
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
WO2023213833A1 (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
TW202535405A (zh) 2023-10-25 2025-09-16 德商艾斯巴赫生物有限公司 用於藉由增強數類已核准藥物的作用以治療癌症之alc1抑制劑
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
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
ATE14423T1 (de) 1985-08-15
JPS56167643A (en) 1981-12-23
EP0039051A3 (en) 1982-05-26
DK156717C (da) 1990-02-19
DK156717B (da) 1989-09-25
EP0039051A2 (en) 1981-11-04
ES8207508A1 (es) 1982-09-16
PT72878A (en) 1981-05-01
DE3171467D1 (en) 1985-08-29
IE53001B1 (en) 1988-05-11
JPH04982B2 (show.php) 1992-01-09
ES501573A0 (es) 1982-09-16
EP0039051B1 (en) 1985-07-24
DK182081A (da) 1981-10-25
IE810899L (en) 1981-10-24
GR74496B (show.php) 1984-06-28

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
ATE25974T1 (de) Acyl-substituierte derivate von 1,2,3,4tetrahydroisochinolin-3-carboxysaeuren, ihre salze, diese enthaltende arzneimittel und verfahren zu ihrer herstellung.
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