CA2789950C - Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof - Google Patents

Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof Download PDF

Info

Publication number
CA2789950C
CA2789950C CA2789950A CA2789950A CA2789950C CA 2789950 C CA2789950 C CA 2789950C CA 2789950 A CA2789950 A CA 2789950A CA 2789950 A CA2789950 A CA 2789950A CA 2789950 C CA2789950 C CA 2789950C
Authority
CA
Canada
Prior art keywords
ylamino
benzothiazol
methyl
carboxylic acid
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.)
Active
Application number
CA2789950A
Other languages
English (en)
French (fr)
Other versions
CA2789950A1 (en
Inventor
Adnan M. M. Mjalli
Dharma Rao Polisetti
Jareer Nabeel Kassis
Matthew J. Kostura
Otis Clinton Attucks
Robert Carl Andrews
Samuel Victory
Suparna Gupta
Mustafa Guzel
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.)
vTv Therapeutics LLC
Original Assignee
vTv Therapeutics LLC
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 vTv Therapeutics LLC filed Critical vTv Therapeutics LLC
Publication of CA2789950A1 publication Critical patent/CA2789950A1/en
Application granted granted Critical
Publication of CA2789950C publication Critical patent/CA2789950C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/41—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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2789950A 2010-02-18 2011-02-10 Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof Active CA2789950C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US30572410P 2010-02-18 2010-02-18
US61/305,724 2010-02-18
JO47/2011 2011-02-03
JOP20110047 2011-02-03
PCT/US2011/024311 WO2011103018A1 (en) 2010-02-18 2011-02-10 Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof

Publications (2)

Publication Number Publication Date
CA2789950A1 CA2789950A1 (en) 2011-08-25
CA2789950C true CA2789950C (en) 2018-09-04

Family

ID=62839064

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2789950A Active CA2789950C (en) 2010-02-18 2011-02-10 Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof

Country Status (14)

Country Link
US (1) US12091407B2 (https=)
EP (1) EP2536285B1 (https=)
JP (1) JP5814948B2 (https=)
KR (1) KR101837759B1 (https=)
CN (1) CN102762101B (https=)
AU (1) AU2011218316B2 (https=)
CA (1) CA2789950C (https=)
DK (1) DK2536285T3 (https=)
EA (1) EA201290808A1 (https=)
ES (1) ES2679918T3 (https=)
MX (1) MX339243B (https=)
NZ (1) NZ602395A (https=)
SG (1) SG182629A1 (https=)
WO (1) WO2011103018A1 (https=)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8759535B2 (en) 2010-02-18 2014-06-24 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
WO2011103018A1 (en) 2010-02-18 2011-08-25 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
WO2012094580A2 (en) 2011-01-07 2012-07-12 High Point Pharmaceuticals, Llc Compounds that modulate oxidative stress
SG11201604611SA (en) * 2013-12-18 2016-07-28 Glaxosmithkline Ip Dev Ltd Nrf2 regulators
WO2015175845A1 (en) * 2014-05-15 2015-11-19 Peloton Therapeutics, Inc. Benzimidazole derivatives and uses thereof
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
WO2020117886A1 (en) * 2018-12-07 2020-06-11 Vtv Therapeutics Llc Methods of inhibiting osteoclastogenesis and osteoclast activity
CN113557019B (zh) * 2019-01-18 2026-04-10 Vtv治疗有限责任公司 取代的稠和咪唑衍生物和治疗镰状细胞病和相关并发症的方法
WO2020210339A1 (en) 2019-04-12 2020-10-15 Mitobridge, Inc. Hmox1 inducers
US20230093476A1 (en) 2020-02-05 2023-03-23 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating refractive ocular disorders
CN117658832A (zh) * 2022-09-08 2024-03-08 史梦婷 一种n，n-二甲基双氨乙基醚的制备方法

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4356108A (en) 1979-12-20 1982-10-26 The Mead Corporation Encapsulation process
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US5300434A (en) 1987-11-06 1994-04-05 Washington Research Foundation Hybridoma cell line producing an antibody to type-I collagen amino-terminal telopeptide
US4973666A (en) 1987-11-06 1990-11-27 Washington Research Foundation Peptide fragments containing HP and LP cross-links
US5320970A (en) 1987-11-06 1994-06-14 Washington Research Foundation Detection of collagen degradation in vivo
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
EP0639573A1 (de) 1993-08-03 1995-02-22 Hoechst Aktiengesellschaft Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament
FR2716192B1 (fr) 1994-02-17 1996-04-12 Rhone Poulenc Agrochimie Dérivés de 2-imidazoline-5-ones fongicides.
CA2132690A1 (en) * 1994-09-22 1996-03-23 Dean Willis Control and modulation of inflammatory response in humans in need of such control and modulation
US6562854B2 (en) 1994-12-14 2003-05-13 Axys Pharmaceuticals, Inc. Compositions comprising a substituted benzimidazole useful for treating immunomediated inflammatory disorders
JP2001519806A (ja) 1997-04-07 2001-10-23 アクシス ファーマシューティカルズ，インコーポレイティド セリンプロテアーゼ活性、特にトリプターゼ活性に関連する疾病を処理するための化合物及び組成物
WO1999026932A1 (en) 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. By amidino group substituted heterocyclic derivatives and their use as anticoagulants
JP2000038387A (ja) 1998-05-19 2000-02-08 Sankyo Co Ltd 三環性カルバペネム化合物
EP1133484A2 (en) 1998-07-23 2001-09-19 AstraZeneca AB Heterocyclic derivatives and their use as integrin inhibitors
DE19853487A1 (de) 1998-11-19 2000-05-25 Fumapharm Ag Muri Verwendung von Dialkylfumaraten
SI1194425T1 (sl) * 1999-06-23 2005-12-31 Sanofi Aventis Deutschland Substituirani benzimidazoli
US8639009B2 (en) 2000-10-11 2014-01-28 Imatx, Inc. Methods and devices for evaluating and treating a bone condition based on x-ray image analysis
AU2002232439A1 (en) 2000-11-29 2002-06-11 Glaxo Group Limited Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors
SE0101387D0 (sv) 2001-04-20 2001-04-20 Astrazeneca Ab Novel compounds
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
JP2003344971A (ja) 2002-05-24 2003-12-03 Konica Minolta Holdings Inc ハロゲン化銀写真感光材料
WO2004000368A1 (en) * 2002-06-21 2003-12-31 University Of Pittsburgh Of The Commonwealth System Of Higher Education Pharmaceutical use of nitric oxide, heme oxygenase-1 and products of heme degradation
BR0312023A (pt) 2002-06-27 2005-03-22 Novo Nordisk As Composto, composto ativador da glicose cinase, método para evitar a hipoglicemia, uso de um composto, e, composição farmacêutica
SE0203070D0 (en) 2002-10-16 2002-10-16 Astrazeneca Ab Novel compounds
FR2851563B1 (fr) 2003-02-26 2005-04-22 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament
US7531553B2 (en) * 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
CA2562833A1 (en) 2004-04-27 2005-11-03 Galapagos N.V. Methods, agents, and compound screening assays for inducing differentiation of undifferentiated mammalian cells into osteoblasts
GB0412467D0 (en) 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
EP1838690A2 (en) 2004-12-21 2007-10-03 Devgen N.V. Compounds with kv4 ion channel activity
US7429608B2 (en) 2005-01-20 2008-09-30 Amgen Inc. Benzo[d]imidazol analogs as vanilloid receptor ligands and their use in treatments
DE102005003362A1 (de) 2005-01-25 2006-07-27 Wella Aktiengesellschaft Kationische Azacyanin-Farbstoffe enthaltende Färbemittel
US7517893B2 (en) 2005-05-20 2009-04-14 The University Of North Carolina At Chapel Hill Bichalcophenes and their prodrugs as antiprotozoal agents
US20100249175A1 (en) 2005-12-02 2010-09-30 Wilson W David Dicationic compounds which selectively recognize G-quadruplex DNA
CN102633783A (zh) * 2006-02-10 2012-08-15 转化技术制药公司 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
AU2007216531A1 (en) 2006-02-14 2007-08-23 Neurosearch A/S Novel diazabicycloalkane derivatives and their medical use
CA2641673A1 (en) 2006-02-15 2007-08-23 Abbott Laboratories Novel acetyl-coa carboxylase (acc) inhibitors and their use in diabetes, obesity and metabolic syndrome
EP2680006A1 (en) 2007-02-08 2014-01-01 Biogen Idec MA Inc. Treatment for Amyotrophic Lateral Sclerosis
CN103087043A (zh) 2007-03-16 2013-05-08 中国人民解放军军事医学科学院放射与辐射医学研究所 具有抗增殖活性的苯甲酰胺类衍生物及其药用制剂
WO2008153701A1 (en) * 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
WO2008151437A1 (en) * 2007-06-14 2008-12-18 Osta Biotechnologies Heme-oxygenase inhibitors and use of the same in the treatment of cancer and diseases of the central nervous system
KR20100042287A (ko) 2007-07-31 2010-04-23 쉐링 코포레이션 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물
US8088824B2 (en) 2007-08-15 2012-01-03 Reata Pharmaceuticals Inc. Forms of CDDO methyl ester
US20100331368A1 (en) 2007-10-17 2010-12-30 Tidwell Richard R 2,5-diaryl selenophene compounds, aza 2,5-diaryl thiophene compounds, and their prodrugs as antiprotozoal agents
UA103013C2 (uk) 2007-12-06 2013-09-10 Тиботек Фармасьютикелз Амідні сполуки як активатори противірусних препаратів
JP2009149589A (ja) 2007-12-24 2009-07-09 Dnp Fine Chemicals Co Ltd 非対称モノアザメチンシアニンの製造方法
PL2252283T3 (pl) 2008-01-11 2019-09-30 Reata Pharmaceuticals, Inc. Syntetyczne triterpenoidy i sposoby zastosowania w leczeniu choroby
WO2009116074A2 (en) 2008-02-13 2009-09-24 Cadila Healthcare Limited Substituted benzimidazoles as cannabinoid modulator
TW201000107A (en) 2008-04-09 2010-01-01 Infinity Pharmaceuticals Inc Inhibitors of fatty acid amide hydrolase
WO2009126635A1 (en) 2008-04-09 2009-10-15 Abbott Laboratories 2-amino-benzothiazole derivates useful as inhibitors of rock kinases
CN102164941B (zh) 2008-04-18 2015-05-27 里亚塔医药公司 抗氧化剂炎症调节剂:具有饱和c环的齐墩果酸衍生物
US20110039895A1 (en) 2008-04-30 2011-02-17 Glaxo Smith Kline LLC., a corporation Prolyl hydroxylase inhibitors
AR071523A1 (es) 2008-04-30 2010-06-23 Merck Serono Sa Compuestos biciclicos fusionados, un proceso para su preparacion, el compuesto para ser utilizado como medicamento en el tratamiento y profilaxis de enfermedades, una composicion farmaceutica y un conjunto que comprende paquetes separados del compuesto y de un ingrediente activo del medicamento
GB0810981D0 (en) 2008-06-16 2008-07-23 Univ Leuven Kath Novel compounds
KR20110039559A (ko) 2008-07-18 2011-04-19 사노피-아벤티스 신규 이미다조[1,2-ａ]피리딘 유도체, 그의 제조 방법, 의약으로서의 그의 용도, 제약 조성물, 및 특히 ｍｅｔ 억제제로서의 신규 용도
PE20110560A1 (es) 2008-07-18 2011-08-29 Sanofi Aventis NUEVOS DERIVADOS DE TRIAZOLO[4,3-a]PIRIDINA, SU PROCEDIMIENTO DE PREPARACION, SU APLICACION COMO MEDICAMENTOS, COMPOSICIONES FARMACEUTICAS Y NUEVA UTILIZACION PARTICULARMENTE COMO INHIBIDORES DE MET
FR2933982A1 (fr) 2008-07-18 2010-01-22 Sanofi Aventis Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met
CN102361857B (zh) 2008-09-26 2015-09-16 默沙东公司 可用作抗糖尿病剂的环状苯并咪唑衍生物
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
SI2373172T1 (sl) 2008-12-03 2013-12-31 Presidio Pharmaceuticals, Inc. Inhibitorji HCV NS5A
MX2011009033A (es) 2009-02-27 2011-09-15 Vertex Pharma Inhibidores triciclicos de cinasa pirazolopiridina.
WO2011103018A1 (en) 2010-02-18 2011-08-25 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
US8759535B2 (en) 2010-02-18 2014-06-24 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
WO2012094580A2 (en) 2011-01-07 2012-07-12 High Point Pharmaceuticals, Llc Compounds that modulate oxidative stress
WO2013057592A2 (en) 2011-09-14 2013-04-25 King Abdullah University Of Science And Technology Treatment of sickle cell disease
US20130158077A1 (en) 2011-12-19 2013-06-20 Ares Trading S.A. Pharmaceutical compositions
US20140171504A1 (en) 2012-12-14 2014-06-19 Georgia Regents Research Institute, Inc. Methods of Treating Sickle Cell Disease and Related Disorders Using Fumaric Acid Esters
ES2718548T3 (es) 2014-03-21 2019-07-02 Univ Paris Val De Marne Híbridos de molécula de liberación de CO-fumarato, su utilización en el tratamiento de enfermedades inflamatorias o cardiovasculares y su procedimiento de preparación
US10039513B2 (en) 2014-07-21 2018-08-07 Zebra Medical Vision Ltd. Systems and methods for emulating DEXA scores based on CT images
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
WO2020117886A1 (en) 2018-12-07 2020-06-11 Vtv Therapeutics Llc Methods of inhibiting osteoclastogenesis and osteoclast activity
CN113557019B (zh) 2019-01-18 2026-04-10 Vtv治疗有限责任公司 取代的稠和咪唑衍生物和治疗镰状细胞病和相关并发症的方法
WO2020210339A1 (en) 2019-04-12 2020-10-15 Mitobridge, Inc. Hmox1 inducers
US20230093476A1 (en) 2020-02-05 2023-03-23 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating refractive ocular disorders

Also Published As

Publication number Publication date
EA201290808A1 (ru) 2013-03-29
AU2011218316B2 (en) 2015-08-20
JP2013520420A (ja) 2013-06-06
AU2011218316A1 (en) 2012-10-04
WO2011103018A1 (en) 2011-08-25
MX339243B (es) 2016-05-18
CN102762101A (zh) 2012-10-31
EP2536285B1 (en) 2018-04-25
KR20150074221A (ko) 2015-07-02
JP5814948B2 (ja) 2015-11-17
CA2789950A1 (en) 2011-08-25
NZ602395A (en) 2014-05-30
SG182629A1 (en) 2012-08-30
EP2536285A4 (en) 2014-01-22
ES2679918T3 (es) 2018-08-31
US12091407B2 (en) 2024-09-17
EP2536285A1 (en) 2012-12-26
KR101837759B1 (ko) 2018-04-26
DK2536285T3 (en) 2018-07-16
WO2011103018A8 (en) 2011-10-27
MX2012009628A (es) 2012-09-28
US20230312548A1 (en) 2023-10-05
CN102762101B (zh) 2014-09-17

Similar Documents

Publication Publication Date Title
CA2789950C (en) Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
US11649230B2 (en) Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
CA2740583A1 (en) C-met protein kinase inhibitors
KR20170096034A (ko) Cftr 활성을 증가시키는 화합물, 조성물 및 방법
WO2016100578A2 (en) Antimicrobial polymyxins for treatment of bacterial infections
AU2008309378A1 (en) Benzothiazoles as ghrelin receptor modulators
WO2023154466A1 (en) Arylbenzoisoxazole compounds as ip6k and ipmk inhibitors and methods of use thereof
JP2025542258A (ja) Ｎａｍｐｔモジュレーター
JP7787893B2 (ja) Ｎａｍｐｔモジュレーターとして有用なピラゾール誘導体
HK1173335B (en) Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
HK1173335A1 (en) Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
BRPI0714535A2 (pt) composto, pelo menos uma entidade quÍmica, composiÇço farmacÊutica, mÉtodo, formulaÇço farmcÊutica embalda e uso
HK1247918A1 (en) Macrocyclic compounds as irak1/4 inhibitors and uses thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20160210

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 14TH ANNIV.) - STANDARD

Year of fee payment: 14

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250131

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20250131