WO2003049741A1 - Ureas of 2-aminobenzothiazoles as adenosine modulators - Google Patents

Ureas of 2-aminobenzothiazoles as adenosine modulators Download PDF

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Publication number
WO2003049741A1
WO2003049741A1 PCT/EP2002/013761 EP0213761W WO03049741A1 WO 2003049741 A1 WO2003049741 A1 WO 2003049741A1 EP 0213761 W EP0213761 W EP 0213761W WO 03049741 A1 WO03049741 A1 WO 03049741A1
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WO
WIPO (PCT)
Prior art keywords
methoxy
benzothiazol
morpholin
aza
amide
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2002/013761
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English (en)
French (fr)
Inventor
Alexander Flohr
Roland Jakob-Roetne
Roger David Norcross
Claus Riemer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Priority to EP02804578A priority Critical patent/EP1455792B1/en
Priority to KR1020047008868A priority patent/KR100659793B1/ko
Priority to MXPA04005444A priority patent/MXPA04005444A/es
Priority to DE60219682T priority patent/DE60219682T2/de
Priority to CA002469596A priority patent/CA2469596A1/en
Priority to AU2002356626A priority patent/AU2002356626B2/en
Priority to BR0214825-0A priority patent/BR0214825A/pt
Priority to JP2003550790A priority patent/JP4245483B2/ja
Priority to ES02804578T priority patent/ES2283652T3/es
Publication of WO2003049741A1 publication Critical patent/WO2003049741A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/16—Central respiratory analeptics
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/36—Opioid-abuse
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
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    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems

Definitions

  • Preferred compounds ofthe present application for use against diseases, related to the A 2a receptor are compounds of formula I, wherein X is -O-, for example the following compounds:

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  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
PCT/EP2002/013761 2001-12-10 2002-12-05 Ureas of 2-aminobenzothiazoles as adenosine modulators Ceased WO2003049741A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
EP02804578A EP1455792B1 (en) 2001-12-10 2002-12-05 Ureas of 2-aminobenzothiazoles as adenosine modulators
KR1020047008868A KR100659793B1 (ko) 2001-12-10 2002-12-05 아데노신 조절제로서의 2-아미노벤조티아졸의 유레아
MXPA04005444A MXPA04005444A (es) 2001-12-10 2002-12-05 Ureas de 2-aminobenzotiazoles como moduladores de adenosina.
DE60219682T DE60219682T2 (de) 2001-12-10 2002-12-05 Harnstoffe von 1-Aminobenzothiazolen als Adenosin-Modulatoren
CA002469596A CA2469596A1 (en) 2001-12-10 2002-12-05 Ureas of 2-aminobenzothiazoles as adenosine modulators
AU2002356626A AU2002356626B2 (en) 2001-12-10 2002-12-05 Ureas of 2-aminobenzothiazoles as adenosine modulators
BR0214825-0A BR0214825A (pt) 2001-12-10 2002-12-05 Uréias de 2-aminobenzotiazóis como moduladores de adenosina
JP2003550790A JP4245483B2 (ja) 2001-12-10 2002-12-05 アデノシン調節薬としての２−アミノベンゾチアゾールの尿素
ES02804578T ES2283652T3 (es) 2001-12-10 2002-12-05 Ureas de 2-aminobenzotiazoles como modulares de adenosina.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01129228 2001-12-10
EP01129228.1 2001-12-10

Publications (1)

Publication Number Publication Date
WO2003049741A1 true WO2003049741A1 (en) 2003-06-19

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ID=8179478

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/013761 Ceased WO2003049741A1 (en) 2001-12-10 2002-12-05 Ureas of 2-aminobenzothiazoles as adenosine modulators

Country Status (20)

Country Link
US (2) US6727247B2 (https=)
EP (1) EP1455792B1 (https=)
JP (1) JP4245483B2 (https=)
KR (1) KR100659793B1 (https=)
CN (1) CN1602196A (https=)
AR (1) AR037731A1 (https=)
AT (1) ATE359792T1 (https=)
AU (1) AU2002356626B2 (https=)
BR (1) BR0214825A (https=)
CA (1) CA2469596A1 (https=)
DE (1) DE60219682T2 (https=)
ES (1) ES2283652T3 (https=)
GT (1) GT200200266A (https=)
MX (1) MXPA04005444A (https=)
PA (1) PA8559901A1 (https=)
PE (1) PE20030759A1 (https=)
PL (1) PL371063A1 (https=)
RU (1) RU2311905C2 (https=)
TW (1) TW200409628A (https=)
WO (1) WO2003049741A1 (https=)

Cited By (28)

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WO2004105755A1 (en) * 2003-05-30 2004-12-09 F. Hoffmann-La Roche Ag Benzothiazole derivatives and use thereof in the treatment of diseases related to the adenosine a2a receptor
WO2005000842A1 (en) * 2003-05-19 2005-01-06 F. Hoffman-La Roche Ag Benzothiazole derivatives as adenosine receptor ligands
WO2005028484A1 (en) * 2003-09-19 2005-03-31 F. Hoffmann-La Roche Ag Thiazolopyridine derivatives as adenosine receptor ligands
WO2005068463A1 (en) * 2004-01-08 2005-07-28 F. Hoffmann-La Roche Ag Diaza-spiropiperidine derivatives
WO2005116026A1 (en) * 2004-05-24 2005-12-08 F. Hoffmann-La Roche Ag 4-hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide
WO2006008040A1 (en) * 2004-07-22 2006-01-26 F. Hoffmann-La Roche Ag Substituted benzothiazoles
WO2006008041A1 (en) * 2004-07-22 2006-01-26 F. Hoffmann-La Roche Ag Benzothiazole derivatives
US7238808B2 (en) 2005-03-23 2007-07-03 Hoffmann-La Roche Inc. Acetylenyl-pyrazolo-pyrimidine derivatives
WO2007140439A3 (en) * 2006-05-31 2008-01-24 Abbott Lab Compounds as cannabinoid receptor ligands and uses thereof
KR100834179B1 (ko) * 2004-05-24 2008-05-30 에프. 호프만-라 로슈 아게 4-하이드록시-4-메틸-피페리딘-1-카복실산(4-메톡시-7-모폴린-4-일-벤조티아졸-2-일)-아마이드
US7504404B2 (en) 2005-09-27 2009-03-17 Hoffmann-La Roche Inc. Compounds as metabotropic glutamate receptor antagonists
US7714009B2 (en) 2003-10-31 2010-05-11 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
EP2065369A4 (en) * 2006-08-23 2011-12-28 Astellas Pharma Inc UREA CONNECTION OR SALT THEREOF
US8455520B2 (en) 2007-07-17 2013-06-04 Merck Sharp & Dohme Corp. Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
EP1522314B1 (en) * 2002-06-26 2014-03-05 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
US8735434B2 (en) 2007-05-18 2014-05-27 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8835475B2 (en) 2007-04-17 2014-09-16 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8841334B2 (en) 2006-05-31 2014-09-23 Abbvie Inc. Compounds as cannabinoid receptor ligands and uses thereof
WO2014146994A1 (en) * 2013-03-20 2014-09-25 F. Hoffmann-La Roche Ag Urea derivatives and their use as fatty-acid binding protein (fabp) inhibitors
WO2014146995A1 (en) * 2013-03-20 2014-09-25 F. Hoffmann-La Roche Ag Urea derivatives and their use as fatty-acid binding protein (fabp) inhibitors
US8846730B2 (en) 2008-09-08 2014-09-30 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8859596B2 (en) 2008-09-16 2014-10-14 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8865753B2 (en) 2007-03-28 2014-10-21 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8895592B2 (en) 2008-12-16 2014-11-25 Abbvie Inc. Compounds as cannabinoid receptor ligands
US8940745B2 (en) 2010-05-03 2015-01-27 Janssen Pharmaceutica Nv Modulators of fatty acid amide hydrolase
US9169224B2 (en) 2004-12-30 2015-10-27 Janssen Pharmaceutica Nv Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase
US9193713B2 (en) 2007-10-12 2015-11-24 Abbvie Inc. Compounds as cannabinoid receptor ligands
US9226907B2 (en) 2008-02-01 2016-01-05 Abbvie Inc. Extended release hydrocodone acetaminophen and related methods and uses thereof

Families Citing this family (23)

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Publication number Priority date Publication date Assignee Title
AU8181701A (en) * 2000-06-21 2002-01-02 Hoffmann La Roche Benzothiazole derivatives
DE60216830T2 (de) * 2001-02-06 2007-06-14 Pfizer Products Inc., Groton Pharmazeutische Zusammensetzungen zur Behandlung von Störungen des ZNS oder anderen Erkrankungen
US6727247B2 (en) * 2001-12-10 2004-04-27 Hoffman-La Roche Inc. Substituted benzothiazole amide derivatives
NZ543102A (en) * 2003-04-24 2008-12-24 Incyte Corp Aza spiro alkane derivatives as inhibitors of metalloproteases
US7910108B2 (en) * 2006-06-05 2011-03-22 Incyte Corporation Sheddase inhibitors combined with CD30-binding immunotherapeutics for the treatment of CD30 positive diseases
JP2009541354A (ja) * 2006-06-22 2009-11-26 シーブイ・セラピューティクス・インコーポレイテッド 虚血の治療におけるａ２ａアデノシン受容体アゴニストの使用
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DE60219682D1 (de) 2007-05-31
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ATE359792T1 (de) 2007-05-15
AR037731A1 (es) 2004-12-01
CA2469596A1 (en) 2003-06-19
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US20040229893A1 (en) 2004-11-18
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