AR083610A1 - COMPUESTOS TRICICLICOS COMO INHIBIDORES DE PROSTAGLANDINA E SINTASA-1 MICROSOMICA (mPGES-1) - Google Patents

COMPUESTOS TRICICLICOS COMO INHIBIDORES DE PROSTAGLANDINA E SINTASA-1 MICROSOMICA (mPGES-1)

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Publication number
AR083610A1
AR083610A1 ARP110104018A ARP110104018A AR083610A1 AR 083610 A1 AR083610 A1 AR 083610A1 AR P110104018 A ARP110104018 A AR P110104018A AR P110104018 A ARP110104018 A AR P110104018A AR 083610 A1 AR083610 A1 AR 083610A1
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AR
Argentina
Prior art keywords
substituted
unsubstituted
alkyl
hydrogen
different
Prior art date
Application number
ARP110104018A
Other languages
English (en)
Inventor
Laxmikant Atmaram Gharat
Nagarajan Muthukaman
Lakshminarayana Narayana
Neelima Khairatkar-Joshi
Vidya Ganapati Kattige
Original Assignee
Glenmark Pharmaceuticals Sa
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Publication date
Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of AR083610A1 publication Critical patent/AR083610A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biotechnology (AREA)

Abstract

Composición farmacéutica y uso para el tratamiento del dolor, asma, osteoartritis y enfermedades neurodegenerativas, entre otras.Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde, A es fenilo o piridinilo; Y se selecciona entre -CR3R4-, y -NR4-; L es una unión o se selecciona entre -(CH2)- y -C(O)-; R2 se selecciona entre C(O)ORa, C(O)NRaRb y un heterociclo sustituido o no sustituido seleccionado entre morfolinilo, oxazolinilo, oxazolidinilo, oxadiazolilo, tiazolinilo y tiazolidinilo; R3 y R4, que pueden ser iguales o diferentes, se seleccionan en forma independiente entre hidrógeno y alquilo C1-4; R5 y R6, que pueden ser iguales o diferentes, se seleccionan en forma independiente entre hidrógeno, alquilo C1-4 y cicloalquilo C3-6; en cada caso R8, que puede ser el mismo o distinto, se selecciona en forma independiente entre halógeno, nitro, ciano, hidroxilo, alquilo sustituido o no sustituido y haloalquilo sustituido o no sustituido; en cada caso, Ra y Rb que pueden ser iguales o diferentes, se seleccionan en forma independiente entre hidrógeno, alquilo sustituido o no sustituido, haloalquilo sustituido o no sustituido, haloalcoxi sustituido o no sustituido, alcoxialquilo sustituido o no sustituido, hidroxialquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heterociclo sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, -(CH2)pNRxRy, y -(CH2)pCHRxRy; o Ra y Rb junto con el átomo al cual están unidos, pueden formar un anillo; sustituido o no sustituido; el anillo puede contener opcionalmente uno o más heteroátomos seleccionados entre O, N o S; en cada caso, Rx y Ry, que pueden ser iguales o diferentes, se seleccionan en forma independiente entre hidrógeno, alquilo C1-4, arilo sustituido o no sustituido y arilalquilo sustituido o no sustituido; Rz se selecciona entre hidrógeno, alquilo C1-4, y alcoxialquilo sustituido o no sustituido; la línea punteada [- -] en el anillo representa un enlace opcional; con la condición de que cuando la línea punteada [- -] en el anillo representa una unión, luego R4 y R5 están ambos ausentes; ‘m’ es un entero entre 0 y 5, ambos inclusive; y ‘p’ es un entero entre 0 y 6, ambos inclusive.
ARP110104018A 2010-10-29 2011-10-28 COMPUESTOS TRICICLICOS COMO INHIBIDORES DE PROSTAGLANDINA E SINTASA-1 MICROSOMICA (mPGES-1) AR083610A1 (es)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
IN3009MU2010 2010-10-29
US41640010P 2010-11-23 2010-11-23
IN9MU2011 2011-01-03
US201161436674P 2011-01-27 2011-01-27
IN1121MU2011 2011-04-01
US201161479463P 2011-04-27 2011-04-27
IN1632MU2011 2011-06-02
US201161498758P 2011-06-20 2011-06-20
IN2099MU2011 2011-07-25
US201161523970P 2011-08-16 2011-08-16

Publications (1)

Publication Number Publication Date
AR083610A1 true AR083610A1 (es) 2013-03-06

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ARP110104018A AR083610A1 (es) 2010-10-29 2011-10-28 COMPUESTOS TRICICLICOS COMO INHIBIDORES DE PROSTAGLANDINA E SINTASA-1 MICROSOMICA (mPGES-1)

Country Status (4)

Country Link
US (1) US8519149B2 (es)
AR (1) AR083610A1 (es)
TW (1) TW201305178A (es)
WO (1) WO2012055995A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR084174A1 (es) 2010-12-21 2013-04-24 Lilly Co Eli Compuestos de imidazol-2-benzamida utiles para el tratamiento de osteoartritis y una composicion farmaceutica
US9006257B2 (en) * 2012-02-09 2015-04-14 Glenmark Pharmaceuticals S.A. Bicyclic compounds as mPGES-1 inhibitors
WO2013153535A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲mPGES-1抑制劑之三唑酮化合物
CA2903431C (en) 2013-03-14 2022-12-06 Kalyra Pharmaceuticals, Inc. Bicyclopentane analgesic compounds
WO2014167444A1 (en) 2013-04-08 2014-10-16 Glenmark Pharmaceuticals S.A. SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
WO2015059618A1 (en) 2013-10-22 2015-04-30 Glenmark Pharmaceuticals S.A. SUBSTITUTED PYRIMIDINE COMPOUNDS AS mPGES-1 INHIBITORS
CN105814013A (zh) 2013-12-12 2016-07-27 卡利拉制药公司 双环烷基化合物及合成
US10654812B2 (en) 2014-03-07 2020-05-19 Recurium Ip Holdings Llc Propellane derivates and synthesis
SI3174535T1 (sl) 2014-08-01 2019-06-28 Glenmark Pharmaceuticals S.A. Formulacija nanodelcev, obsegajoča MPGES-1 inhibitor
US10308609B2 (en) 2014-09-17 2019-06-04 Zeno Royalties & Milestones, LLC Bicyclic compounds
US10653681B2 (en) 2016-03-16 2020-05-19 Recurium Ip Holdings, Llc Analgesic compounds
WO2017160926A1 (en) * 2016-03-16 2017-09-21 Kalyra Pharmaceuticals, Inc. Analgesic compounds
WO2018213140A1 (en) 2017-05-15 2018-11-22 Zeno Royalties & Milestones, LLC Analgesic compounds
AU2018371153B2 (en) 2017-11-22 2023-07-13 Khondrion Ip B.V. Compounds as mPGES-1 inhibitors
HRP20230243T1 (hr) 2018-06-07 2023-04-14 Idorsia Pharmaceuticals Ltd Alkoksi supstituirani derivati piridinila kao antagonisti receptora lpa1 i njihova uporaba u liječenju fibroze
AR119162A1 (es) 2019-06-18 2021-12-01 Idorsia Pharmaceuticals Ltd Derivados de piridin-3-ilo
WO2024029819A1 (ko) * 2022-08-01 2024-02-08 경희대학교 산학협력단 벤즈이미다졸 유도체 또는 이의 약학적으로 허용되는 염을 함유하는 약학적 조성물 및 이의 제조방법

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050124638A1 (en) * 2003-12-08 2005-06-09 Swayze Eric E. Benzimidazoles and analogs thereof as antivirals
JP5086809B2 (ja) 2004-12-17 2012-11-28 メルク カナダ インコーポレイテッド mPGES−1阻害剤としての2−(フェニルまたはヘテロ環式)−1H−フェナントロ[9,10−d]イミダゾール
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones

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US20120108583A1 (en) 2012-05-03
TW201305178A (zh) 2013-02-01
US8519149B2 (en) 2013-08-27
WO2012055995A1 (en) 2012-05-03

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