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

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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
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Prior art keywords
ylamino
benzothiazol
methyl
carboxylic acid
amide
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CA2789950A
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English (en)
French (fr)
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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
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vTv Therapeutics LLC
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vTv Therapeutics LLC
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Publication of CA2789950A1 publication Critical patent/CA2789950A1/en
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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

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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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

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ID=62839064

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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 (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
EA201290808A1 (ru) 2010-02-18 2013-03-29 ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Замещенные конденсированные производные имидазола, фармацевтические композиции и способы их применения
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
KR102301867B1 (ko) * 2013-12-18 2021-09-15 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 Nrf2 조절제
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
KR20210129034A (ko) * 2019-01-18 2021-10-27 브이티브이 테라퓨틱스 엘엘씨 치환된 융합 이미다졸 유도체 및 겸상 적혈구 질환과 관련 합병증을 치료하는 방법
TW202104211A (zh) * 2019-04-12 2021-02-01 美商米突倍基公司 Hmox1誘導劑
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
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
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
CN1251579A (zh) 1997-04-07 2000-04-26 Axys药物公司 治疗与丝氨酸蛋白酶－特别是类胰蛋白酶－活性有关的疾病的化合物与组合物
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
JP2002521375A (ja) 1998-07-23 2002-07-16 アストラゼネカ アクチエボラーク 化合物
DE19853487A1 (de) 1998-11-19 2000-05-25 Fumapharm Ag Muri Verwendung von Dialkylfumaraten
BR0012450B1 (pt) 1999-06-23 2011-08-23 benzimidazóis substituìdos.
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
MXPA04012863A (es) * 2002-06-21 2005-03-31 Univ Pittsburgh Uso farmaceutico de oxido nitrico, heme oxigenasa-1 y productos de degradacion de heme.
KR101116627B1 (ko) 2002-06-27 2012-10-09 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
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
WO2005103716A2 (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
CN101084209A (zh) 2004-12-21 2007-12-05 德福根有限公司 具有Kv4离子通道活性的化合物
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
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
US7820821B2 (en) * 2006-02-10 2010-10-26 Transtech Pharma, Inc. Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
CA2641767A1 (en) 2006-02-14 2007-08-23 Neurosearch A/S Novel diazabicycloalkane derivatives and their medical use
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
PT2653873T (pt) 2007-02-08 2022-07-26 Biogen Ma Inc Composições e utilizações para o tratamento de esclerose múltipla
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
CA2727528A1 (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
RU2010106878A (ru) 2007-07-31 2011-09-10 Шеринг Корпорейшн (US) Комбинация антимитотического агента и ингибитора аврора киназы как средство для лечения рака
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
WO2009126635A1 (en) 2008-04-09 2009-10-15 Abbott Laboratories 2-amino-benzothiazole derivates useful as inhibitors of rock kinases
CA2721060A1 (en) 2008-04-09 2009-10-15 Infinity Pharmaceuticals, Inc. Inhibitors of fatty acid amide hydrolase
EP2279197B1 (en) 2008-04-18 2014-11-05 Reata Pharmaceuticals, Inc. Antioxidant inflammation modulators: oleanolic acid derivatives with saturation in the c-ring
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
KR20110039558A (ko) 2008-07-18 2011-04-19 사노피-아벤티스 신규 트리아졸로(4,3-ａ)피리딘 유도체, 그의 제조 방법, 의약으로서의 그의 용도, 제약 조성물, 및 특히 ｍｅｔ 억제제로서의 신규 용도
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
AR072518A1 (es) 2008-07-18 2010-09-01 Sanofi Aventis Derivados de imidazo [1,2-a]piridina, su procedimiento de preparacion, composiciones farmaceuticas y su utilizacion particularmente como inhibidores de met."
US8394969B2 (en) 2008-09-26 2013-03-12 Merck Sharp & Dohme Corp. Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
PE20120124A1 (es) 2008-12-03 2012-03-17 Presidio Pharmaceuticals Inc Derivados 2-pirrolidin-3-il-1h-imidazol, como inhibidores de la proteina no estructural 5a del virus de la heptitis c
EP2401273A1 (en) 2009-02-27 2012-01-04 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
EA201290808A1 (ru) 2010-02-18 2013-03-29 ХАЙ ПОЙНТ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Замещенные конденсированные производные имидазола, фармацевтические композиции и способы их применения
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
US9655905B2 (en) 2011-09-14 2017-05-23 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
US9944669B2 (en) 2014-03-21 2018-04-17 Universite Paris Est Creteil Val De Marne Fumarate-CO-releasing molecule hybrids, their use in the treatment of inflammatory or cardiovascular diseases and their process of preparation
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
KR20210129034A (ko) 2019-01-18 2021-10-27 브이티브이 테라퓨틱스 엘엘씨 치환된 융합 이미다졸 유도체 및 겸상 적혈구 질환과 관련 합병증을 치료하는 방법
TW202104211A (zh) 2019-04-12 2021-02-01 美商米突倍基公司 Hmox1誘導劑
US20230093476A1 (en) 2020-02-05 2023-03-23 Vtv Therapeutics Llc Substituted fused imidazole derivatives and methods of treating refractive ocular disorders

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