SG182629A1 - 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
SG182629A1
SG182629A1 SG2012053732A SG2012053732A SG182629A1 SG 182629 A1 SG182629 A1 SG 182629A1 SG 2012053732 A SG2012053732 A SG 2012053732A SG 2012053732 A SG2012053732 A SG 2012053732A SG 182629 A1 SG182629 A1 SG 182629A1
Authority
SG
Singapore
Prior art keywords
methods
substituted fused
fused imidazole
pharmaceutical compositions
imidazole derivatives
Prior art date
Application number
SG2012053732A
Other languages
English (en)
Inventor
Adnan M M Mjalli
Dharma Rao Polisetti
Jareer Nabeel Kassis
Matthew J Kostura
Mustafa Guzel
Otis Clinton Attucks
Robert Carl Andrews
Samuel Victory
Suparna Gupta
Original Assignee
High Point Pharmaceuticals 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 High Point Pharmaceuticals Llc filed Critical High Point Pharmaceuticals Llc
Publication of SG182629A1 publication Critical patent/SG182629A1/en

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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
SG2012053732A 2010-02-18 2011-02-10 Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof SG182629A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30572410P 2010-02-18 2010-02-18
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 (1)

Publication Number Publication Date
SG182629A1 true SG182629A1 (en) 2012-08-30

Family

ID=62839064

Family Applications (1)

Application Number Title Priority Date Filing Date
SG2012053732A SG182629A1 (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 (enExample)
EP (1) EP2536285B1 (enExample)
JP (1) JP5814948B2 (enExample)
KR (1) KR101837759B1 (enExample)
CN (1) CN102762101B (enExample)
AU (1) AU2011218316B2 (enExample)
CA (1) CA2789950C (enExample)
DK (1) DK2536285T3 (enExample)
EA (1) EA201290808A1 (enExample)
ES (1) ES2679918T3 (enExample)
MX (1) MX339243B (enExample)
NZ (1) NZ602395A (enExample)
SG (1) SG182629A1 (enExample)
WO (1) WO2011103018A1 (enExample)

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
SG182629A1 (en) 2010-02-18 2012-08-30 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
CN105829305B (zh) * 2013-12-18 2018-11-30 葛兰素史密斯克莱知识产权发展有限公司 Nrf2调节剂
US10040767B2 (en) 2014-05-15 2018-08-07 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
WO2020150306A1 (en) * 2019-01-18 2020-07-23 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating sickle cell disease and related complications
EP3952990A1 (en) 2019-04-12 2022-02-16 Mitobridge, Inc. Hmox1 inducers
WO2021158466A1 (en) 2020-02-05 2021-08-12 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
US5320970A (en) 1987-11-06 1994-06-14 Washington Research Foundation Detection of collagen degradation in vivo
US4973666A (en) 1987-11-06 1990-11-27 Washington Research Foundation Peptide fragments containing HP and LP cross-links
US5300434A (en) 1987-11-06 1994-04-05 Washington Research Foundation Hybridoma cell line producing an antibody to type-I collagen amino-terminal telopeptide
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
CA2285454A1 (en) 1997-04-07 1998-10-15 Axys Pharmaceuticals Corporation Compounds and compositions for treating diseases associated with serine protease, particularly tryptase, activity
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
WO2000005223A2 (en) 1998-07-23 2000-02-03 Astrazeneca Ab Heterocyclic derivatives and their use as integrin inhibitors
DE19853487A1 (de) 1998-11-19 2000-05-25 Fumapharm Ag Muri Verwendung von Dialkylfumaraten
ES2246240T3 (es) * 1999-06-23 2006-02-16 Sanofi-Aventis Deutschland Gmbh Bencimidazoles sustituidos.
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
EA200500062A1 (ru) * 2002-06-21 2005-06-30 Юниверсити Оф Питтсбург Оф Дзе Коммонвелт Систем Оф Хайер Эдьюкейшн Фармацевтическое применение оксида азота, гемоксигеназы-1 и продуктов деградации гема
EP1531815B1 (en) 2002-06-27 2014-09-24 Novo Nordisk A/S Glucokinase activators
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
EP2214018B1 (en) 2004-04-27 2013-06-26 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
WO2006066879A2 (en) 2004-12-21 2006-06-29 Devgen N.V. Compounds with kv4 ion channel activity
WO2006078907A1 (en) 2005-01-20 2006-07-27 Amgen Inc. 2-substituted benzimidazole derivatives as vanilloid receptor ligands and their use in treatments
DE102005003362A1 (de) 2005-01-25 2006-07-27 Wella Aktiengesellschaft Kationische Azacyanin-Farbstoffe enthaltende Färbemittel
AU2006202040A1 (en) 2005-05-20 2006-12-07 Reto Brun Novel biochalcophenes 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
JP5188988B2 (ja) 2006-02-10 2013-04-24 トランステック ファーマ，インコーポレイティド ベンゾアゾール誘導体、組成物、及びオーロラキナーゼ阻害剤としての使用方法
JP2009526776A (ja) 2006-02-14 2009-07-23 ノイロサーチ アクティーゼルスカブ 新規なジアザビシクロアルカン誘導体及びその医療上の使用
EP1996567B1 (en) 2006-02-15 2013-09-18 AbbVie Inc. Novel acetyl-coa carboxylase (acc) inhibitors and their use in diabetes, obesity and metabolic syndrome
EP2680009A1 (en) 2007-02-08 2014-01-01 Biogen Idec MA Inc. Nrf2 screening assays and related methods and compositions
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
AU2008282885A1 (en) 2007-07-31 2009-02-05 Schering Corporation Anti-mitotic agent and aurora kinase inhibitor combination as anti-cancer treatment
US8088824B2 (en) 2007-08-15 2012-01-03 Reata Pharmaceuticals Inc. Forms of CDDO methyl ester
WO2009051796A2 (en) 2007-10-17 2009-04-23 The University Of North Carolina At Chapel Hill 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
ME03529B (me) 2008-01-11 2020-04-20 Reata Pharmaceuticals Inc Sintetički triterpenoidi i metode njihove upotrebe u tretmanu bolesti
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
US20090258907A1 (en) 2008-04-09 2009-10-15 Abbott Laboratories Compounds useful as inhibitors of rock kinases
MX2010011437A (es) 2008-04-18 2010-12-20 Reata Pharmaceuticals Inc Moduladores antioxidantes de inflamacion: derivados del acido oleanolico con saturacion en el anillo c.
WO2009133127A1 (en) 2008-04-30 2009-11-05 Merck Serono S.A. Fused bicyclic compounds and use thereof as pi3k inhibitors
JP2011519858A (ja) 2008-04-30 2011-07-14 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー プロリルヒドロキシラ−ゼ阻害剤
GB0810981D0 (en) 2008-06-16 2008-07-23 Univ Leuven Kath Novel compounds
MX2011000675A (es) 2008-07-18 2011-04-11 Sanofi Aventis Nuevos derivados de imidazo [1,2-a] piridina, su procedimiento de preparación, su uso como medicamentos, composiciones farmaceuticas y nuevo uso particularmente como inhibidores de met.
US20110263594A1 (en) 2008-07-18 2011-10-27 Sanofi-Aventis Novel triazolo(4,3-a)pyridine derivatives, process for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use, in particular as met inhibitors
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
WO2010036613A1 (en) 2008-09-26 2010-04-01 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
BRPI0922366B8 (pt) 2008-12-03 2021-05-25 Presidio Pharmaceuticals Inc composto, composição farmacêutica e uso de um composto
EP2401273A1 (en) 2009-02-27 2012-01-04 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
US8759535B2 (en) 2010-02-18 2014-06-24 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
SG182629A1 (en) 2010-02-18 2012-08-30 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
JP6564785B2 (ja) 2014-03-21 2019-08-21 ユニベルシテ パリ−エスト クレテイユ ヴァル ド マルヌＵｎｉｖｅｒｓｉｔｅ Ｐａｒｉｓ−Ｅｓｔ Ｃｒｅｔｅｉｌ Ｖａｌ Ｄｅ Ｍａｒｎｅ フマレート−ｃｏ−放出分子ハイブリッド、炎症性疾患又は心血管疾患の治療におけるそれらの使用及びそれらの調製方法
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
WO2020150306A1 (en) 2019-01-18 2020-07-23 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating sickle cell disease and related complications
EP3952990A1 (en) 2019-04-12 2022-02-16 Mitobridge, Inc. Hmox1 inducers
WO2021158466A1 (en) 2020-02-05 2021-08-12 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating refractive ocular disorders

Also Published As

Publication number Publication date
CN102762101A (zh) 2012-10-31
MX2012009628A (es) 2012-09-28
WO2011103018A8 (en) 2011-10-27
KR101837759B1 (ko) 2018-04-26
WO2011103018A1 (en) 2011-08-25
DK2536285T3 (en) 2018-07-16
NZ602395A (en) 2014-05-30
AU2011218316B2 (en) 2015-08-20
ES2679918T3 (es) 2018-08-31
EP2536285A4 (en) 2014-01-22
CA2789950C (en) 2018-09-04
US20230312548A1 (en) 2023-10-05
US12091407B2 (en) 2024-09-17
EP2536285A1 (en) 2012-12-26
CN102762101B (zh) 2014-09-17
EA201290808A1 (ru) 2013-03-29
JP2013520420A (ja) 2013-06-06
EP2536285B1 (en) 2018-04-25
MX339243B (es) 2016-05-18
JP5814948B2 (ja) 2015-11-17
KR20150074221A (ko) 2015-07-02
AU2011218316A1 (en) 2012-10-04
CA2789950A1 (en) 2011-08-25

Similar Documents

Publication Publication Date Title
SG182629A1 (en) Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
MX2013008851A (es) Composiciones y metodos para el tratamiento de inflamacion cronica y enfermedades inflamatorias.
WO2012064973A3 (en) Heterocyclic compounds and uses thereof
SG10201907588XA (en) Androgen Receptor Modulators And Uses Thereof
ZA201206062B (en) Aminotetraline derivatives,pharmaceutical compositions containing them,and their use in therapy
SG194469A1 (en) Tetrahydroquinoline derivatives useful as bromodomain inhibitors
WO2012024620A3 (en) Autotaxin inhibitors and uses thereof
IL224288A (en) Derivatives of converted pyrazolamide, pharmaceutical preparations containing them and their use
HUE037742T2 (hu) Szubsztituált azolok, vírusellenes aktív adalék, gyógyszerészeti készítmény, az elõállításukat célzó eljárás és alkalmazásuk
PL2562172T3 (pl) Pochodne sfelaktonu, ich kompozycje farmaceutyczne, sposoby wytwarzania i zastosowania
IL231050A0 (en) Pyridines are converted in 4,5,6,7 tetrahydro-1hydrogen-pyrazolo[3,4-si], their use as medicine and medical preparations containing them
IL223721A0 (en) Heterocyclic compounds, their preparation and their therapeutic application
IL233238A0 (en) Sulphonylaminopyrrolidinone derivatives, their preparation and therapeutic use
IN2014DN09437A (enExample)
EP2476420B8 (en) Pharmaceutical composition having antimicrobial and fast-healing activity for external administration, process for preparing same
IL228319A (en) Azul carpentry, pharmaceuticals containing them and their use for prevention or treatment of baldness
EP2980103A4 (en) Low molecular weight glycosaminoglycan derivative, pharmaceutical composition thereof, preparation method therefor and use thereof
BR112013009647A2 (pt) derivado de vitamina, composição farmacêutica, agente terapêutico, e, composto
TN2011000352A1 (en) New combination of active ingredients containing a non steroidal anti inflammatory drug and a colchicoside derivative
IL220859A0 (en) Alkyl-heterocycle-carbamate derivatives, their preparation and therapeutic application
ZA201304035B (en) Diarylpyridazinone derivatives,preparation thereof,and use thereof for the treatment of humans
IL220906A0 (en) Transformed histories of compressed imidazole, pharmaceutical preparations containing them and such compounds for use in healing
HK1179257A (en) Heterocyclic compounds, their preparation and their therapeutic application
HK1159603A (en) Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy
HK1179250A (en) Indolizine derivatives, process for the preparation thereof and therapeutic use thereof