BRPI0516132A - compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica - Google Patents

compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica

Info

Publication number
BRPI0516132A
BRPI0516132A BRPI0516132-0A BRPI0516132A BRPI0516132A BR PI0516132 A BRPI0516132 A BR PI0516132A BR PI0516132 A BRPI0516132 A BR PI0516132A BR PI0516132 A BRPI0516132 A BR PI0516132A
Authority
BR
Brazil
Prior art keywords
aspartic
treating
compounds
ameliorating
composition
Prior art date
Application number
BRPI0516132-0A
Other languages
English (en)
Inventor
John J Baldwin
David A Claremon
Salvacion Cacatian
Alexey V Ishchenko
Zhenrong Xu
Wei Zhao
Colin Tice
Lawrence W Dillard
Jing Yuan
Gerard Mcgeehan
Robert D Simpson
Suresh B Singh
Jean-Pierre Wery
Patrick T Flaherty
Original Assignee
Vitae Pharmaceuticals Inc
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 Vitae Pharmaceuticals Inc filed Critical Vitae Pharmaceuticals Inc
Publication of BRPI0516132A publication Critical patent/BRPI0516132A/pt

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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/40—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/56—Ring systems containing bridged rings
    • C07C2603/58—Ring systems containing bridged rings containing three rings
    • C07C2603/70—Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74—Adamantanes
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • AIDS & HIV (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)

Abstract

COMPOSTOS, COMPOSICAO DESTES, METODO DE ANTAGONIZACAO DE UMA OU MAIS PROTEASES ASPARTICAS E METODO PARA TRATAR OU MELHORAR UM DISTURBIO MEDIADO POR PROTEASE ASPARTICA. Verificou-se, agora, que os diamino alcanos da fórmula I são oralmente ativos e se ligam às proteases aspárticas para inibir sua atividade. Eles são úteis no tratamento ou melhora de doenças associadas aos níveis elevados de atividade da protease aspártica. A invenção também se refere a um método para uso dos compostos da fórmula I na melhora ou tratamento dos distúrbios relacionados à protease aspártica em um indivíduo que dela necessite, compreendendo a administração ao indivíduo de uma quantidade eficaz de um composto da fórmula I.
BRPI0516132-0A 2004-10-07 2005-10-07 compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica BRPI0516132A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61677004P 2004-10-07 2004-10-07
PCT/US2005/036230 WO2006042150A1 (en) 2004-10-07 2005-10-07 Diaminoalkane aspartic protease inhibitors

Publications (1)

Publication Number Publication Date
BRPI0516132A true BRPI0516132A (pt) 2007-12-04

Family

ID=35648206

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0516132-0A BRPI0516132A (pt) 2004-10-07 2005-10-07 compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica

Country Status (14)

Country Link
US (2) US7754737B2 (pt)
EP (1) EP1807078A1 (pt)
JP (2) JP5067968B2 (pt)
KR (1) KR101314277B1 (pt)
CN (1) CN101072561B (pt)
AU (1) AU2005294123C1 (pt)
BR (1) BRPI0516132A (pt)
CA (1) CA2582202A1 (pt)
IL (1) IL182305A0 (pt)
MX (1) MX2007003858A (pt)
NZ (1) NZ554374A (pt)
RU (1) RU2440993C2 (pt)
WO (1) WO2006042150A1 (pt)
ZA (1) ZA200702836B (pt)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0516132A (pt) * 2004-10-07 2007-12-04 Vitae Pharmaceuticals Inc compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica
TWI411607B (zh) 2005-11-14 2013-10-11 Vitae Pharmaceuticals Inc 天門冬胺酸蛋白酶抑制劑
US7790770B2 (en) * 2005-11-23 2010-09-07 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
CA2642685A1 (en) * 2006-02-17 2007-08-30 Gilead Colorado, Inc. Antihypertensive therapy
EP2010488A2 (en) * 2006-04-05 2009-01-07 Vitae Pharmaceuticals, Inc. Renin inhibitors
WO2007117560A2 (en) * 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Piperidine and morpholine renin inhibitors
WO2007117557A2 (en) 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Diaminopropanol renin inhibitors
US20090275581A1 (en) * 2006-04-05 2009-11-05 Baldwin John J Renin inhibitors
TW200815425A (en) * 2006-06-08 2008-04-01 Speedel Experimenta Ag 2,5-disubstituted piperidines
CL2007002689A1 (es) 2006-09-18 2008-04-18 Vitae Pharmaceuticals Inc Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras.
JP2010503682A (ja) * 2006-09-18 2010-02-04 ビテ ファーマシューティカルズ， インコーポレイテッド レニン阻害剤としてのピペリジン誘導体
WO2008124577A1 (en) * 2007-04-05 2008-10-16 Smithkline Beecham Corporation Renin inhibitors
WO2008124582A1 (en) * 2007-04-05 2008-10-16 Smithkline Beecham Corporation Renin inhibitors
WO2008124575A1 (en) * 2007-04-05 2008-10-16 Smithkline Beecham Corporation Renin inhibitors
WO2008156816A2 (en) * 2007-06-20 2008-12-24 Vitae Pharmaceuticals, Inc. Renin inhibitors
US20100168243A1 (en) * 2007-06-20 2010-07-01 Baldwin John J Renin Inhibitors
WO2009096996A1 (en) * 2007-06-20 2009-08-06 Smithkline Beecham Corporation Renin inhibitors
US20100160424A1 (en) * 2007-06-20 2010-06-24 Baldwin John J Renin inhibitors
JP2009173594A (ja) * 2008-01-25 2009-08-06 Sumitomo Chemical Co Ltd アミロイドβタンパク質の蓄積を抑制するための医薬組成物
SG188117A1 (en) 2008-06-19 2013-03-28 Takeda Pharmaceutical Heterocyclic compound and use thereof
WO2009154766A1 (en) * 2008-06-20 2009-12-23 Vitae Pharmaceuticals, Inc. Renin inhibitors and method of use thereof
US20100010228A1 (en) * 2008-06-26 2010-01-14 Vitae Pharmaceuticals, Inc. Process for the asymmetric reduction of 3-benzoylpiperidines
CN102088850A (zh) * 2008-06-26 2011-06-08 生命医药公司 甲基2-((r)-(3-氯苯基)((r)-1-((s)-2-(甲氨基)-3((r)-四氢-2h-吡喃-3-基)丙基氨甲酰基)哌啶-3-基)甲氧基)氨基甲酸乙酯的盐
AR077692A1 (es) 2009-08-06 2011-09-14 Vitae Pharmaceuticals Inc Sales de 2-((r)-(3-clorofenil) ((r)-1-((s) -2-(metilamino)-3-((r)-tetrahidro-2h-piran-3-il) propilcarbamoil) piperidin -3-il) metoxi) etilcarbamato de metilo
US8314250B2 (en) 2009-11-24 2012-11-20 Hoffmann-La Roche Inc. Sultam derivatives
CN102372653A (zh) * 2010-08-10 2012-03-14 江苏恒瑞医药股份有限公司 二苯甲醇类衍生物、其制备方法及其在医药上的应用
WO2012081582A1 (ja) * 2010-12-15 2012-06-21 国立大学法人北海道大学 ジアステレオ選択的にアルコール化合物を製造する方法及びルテニウム化合物
WO2012081585A1 (ja) * 2010-12-15 2012-06-21 国立大学法人北海道大学 光学活性アルコール化合物の製造方法
WO2014042263A1 (ja) * 2012-09-14 2014-03-20 田辺三菱製薬株式会社 新規レニン阻害薬
CN104873482B (zh) * 2015-05-05 2017-12-01 青岛市市立医院 一种抗慢性心力衰竭的药物组合物
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
US11149011B2 (en) 2018-03-20 2021-10-19 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
US12419890B2 (en) 2019-02-27 2025-09-23 Takeda Pharmaceutical Company Limited Administration of sumo-activating enzyme inhibitor and checkpoint inhibitors
ES3074115T3 (es) * 2019-10-07 2026-07-17 De Shaw Res Llc Compuestos heterocíclicos de arilmetileno como bloqueadores de los canales de potasio tipo Shaker Kv1.3
WO2023139581A1 (en) * 2022-01-18 2023-07-27 Bsense Bio Therapeutics Ltd. Modulators of a potassium channel and of trpv1 channel and uses thereof
WO2026015506A1 (en) * 2024-07-11 2026-01-15 Purdue Research Foundation Dual inhibitors for hdac3 and hiv-1 pr

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3071618A (en) * 1956-02-02 1963-01-01 Pfizer & Co C Diquaternary ammonium salts of n, n, n', n'-tetra substituted alkylene diamines
US4136163A (en) * 1971-02-04 1979-01-23 Wilkinson Sword Limited P-menthane carboxamides having a physiological cooling effect
GB1351761A (en) * 1971-02-04 1974-05-01 Wilkinson Sword Ltd Substituted p-menthane carboxamides and compositions containing them
JPS5115098A (ja) 1974-07-26 1976-02-06 Asahi Chemical Ind Akurirukeiseniseihinno shorihoho
US4594343A (en) 1984-10-19 1986-06-10 Shanklin Jr James R 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-α,α-diarylpyrrolidine, piperidine and homopiperidineacetamides and acetonitriles
GB8810067D0 (en) * 1988-04-28 1988-06-02 Ucb Sa Substituted 1-(1h-imidazol-4-yl)alkyl-benzamides
US4908372A (en) 1988-10-13 1990-03-13 Merrell Dow Pharmaceuticals Inc. Antihistaminic piperidinyl benzimidazoles
US5696270A (en) * 1989-05-23 1997-12-09 Abbott Laboratories Intermediate for making retroviral protease inhibiting compounds
DE4018070A1 (de) 1990-06-06 1991-12-12 Bayer Ag Morpholinoharnstoff-derivate
EP0561973A1 (en) 1990-12-14 1993-09-29 Merrell Dow Pharmaceuticals Inc. Antiallergic compounds
DE69330823T2 (de) 1992-02-13 2002-05-02 Merrell Pharmaceuticals Inc., Cincinnati Thiacyclische piperidinylderivate
EP0773921B1 (en) 1994-07-29 1999-12-01 Abbott Laboratories Process for the preparation of a substituted 2.5-diamino-3-hydroxyhexane
US5767144A (en) 1994-08-19 1998-06-16 Abbott Laboratories Endothelin antagonists
US6946481B1 (en) 1994-08-19 2005-09-20 Abbott Laboratories Endothelin antagonists
US6162927A (en) 1994-08-19 2000-12-19 Abbott Laboratories Endothelin antagonists
JP3992291B2 (ja) * 1995-09-28 2007-10-17 アスビオファーマ株式会社 キナゾリン誘導体
CA2291157A1 (en) * 1997-05-29 1998-12-03 Eli Lilly And Company Process for preparing heterocyclic compounds
AU3716499A (en) 1998-04-21 1999-11-08 Aventis Pharma Limited Substituted diamines and their use as cell adhesion inhibitors
US6437146B1 (en) 1998-09-25 2002-08-20 Fujisawa Pharmaceutical Co., Ltd. Oxazole compounds as prostaglandin e2 agonists or antagonists
GB9826540D0 (en) * 1998-12-02 1999-01-27 Darwin Discovery Ltd Process
US6613764B1 (en) 1999-01-06 2003-09-02 The United States Of America As Represented By The Department Of Health And Human Services Aspartic protease inhibitors
JP2000302757A (ja) 1999-04-16 2000-10-31 Shiseido Co Ltd Ｎ−置換ピペリジン誘導体
OA12323A (en) * 2000-03-21 2006-05-15 Smithkline Beecham Corp Protease inhibitors.
US6900329B2 (en) 2001-03-21 2005-05-31 Schering Corporation MCH antagonists and their use in the treatment of obesity
AU2002320490B2 (en) 2001-07-11 2008-10-02 Elan Pharmaceuticals, Inc. N-(3-amino-2-hydroxy-propyl) substituted alkylamide compounds
AR039555A1 (es) * 2001-11-08 2005-02-23 Upjohn Co Derivados n,n'-sustituidos de 1,3-diamino-2-hidroxipropano
TW200408645A (en) 2002-04-26 2004-06-01 Gilead Sciences Inc Non nucleoside reverse transcriptase inhibitors
WO2004002483A1 (en) 2002-06-27 2004-01-08 Actelion Pharmaceuticals Ltd Substituted 3- and 4- aminomethylpiperidines for use as beta-secretase in the treatment of alzheimer’s disease
US7557137B2 (en) * 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
AU2003273310A1 (en) 2002-09-10 2004-04-30 Pharmacia And Upjohn Substituted aminoethers for the treatment of alzheimer's disease
AU2004290499C1 (en) 2003-11-03 2011-02-24 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
CA2548388A1 (en) * 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
US20070093492A1 (en) 2004-03-09 2007-04-26 Weir-Torn Jiaang Pyrrolidine derivatives
CA2576971A1 (en) 2004-08-20 2006-03-02 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
BRPI0516132A (pt) * 2004-10-07 2007-12-04 Vitae Pharmaceuticals Inc compostos, composição destes, método de antagonização de uma ou mais proteases aspárticas e método para tratar ou melhorar um distúrbio mediado por protease aspártica
EP1882684B1 (en) 2005-05-19 2014-12-10 Astellas Pharma Inc. Pyrrolidine derivative or salt thereof
TWI411607B (zh) 2005-11-14 2013-10-11 Vitae Pharmaceuticals Inc 天門冬胺酸蛋白酶抑制劑
WO2007117560A2 (en) * 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Piperidine and morpholine renin inhibitors
WO2007117557A2 (en) 2006-04-05 2007-10-18 Vitae Pharmaceuticals, Inc. Diaminopropanol renin inhibitors
JP2010503682A (ja) 2006-09-18 2010-02-04 ビテ ファーマシューティカルズ， インコーポレイテッド レニン阻害剤としてのピペリジン誘導体
CL2007002689A1 (es) * 2006-09-18 2008-04-18 Vitae Pharmaceuticals Inc Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras.
US20100160424A1 (en) * 2007-06-20 2010-06-24 Baldwin John J Renin inhibitors
WO2009096996A1 (en) 2007-06-20 2009-08-06 Smithkline Beecham Corporation Renin inhibitors
US7773441B2 (en) * 2008-06-18 2010-08-10 Micron Technology, Inc. Memory malfunction prediction system and method
WO2009154766A1 (en) 2008-06-20 2009-12-23 Vitae Pharmaceuticals, Inc. Renin inhibitors and method of use thereof
CN102088850A (zh) 2008-06-26 2011-06-08 生命医药公司 甲基2-((r)-(3-氯苯基)((r)-1-((s)-2-(甲氨基)-3((r)-四氢-2h-吡喃-3-基)丙基氨甲酰基)哌啶-3-基)甲氧基)氨基甲酸乙酯的盐
AR077692A1 (es) 2009-08-06 2011-09-14 Vitae Pharmaceuticals Inc Sales de 2-((r)-(3-clorofenil) ((r)-1-((s) -2-(metilamino)-3-((r)-tetrahidro-2h-piran-3-il) propilcarbamoil) piperidin -3-il) metoxi) etilcarbamato de metilo

Also Published As

Publication number Publication date
US8455521B2 (en) 2013-06-04
JP2008515916A (ja) 2008-05-15
KR20070084040A (ko) 2007-08-24
WO2006042150A1 (en) 2006-04-20
MX2007003858A (es) 2007-12-11
WO2006042150A8 (en) 2007-05-24
AU2005294123C1 (en) 2010-01-21
NZ554374A (en) 2010-11-26
RU2007116725A (ru) 2008-11-20
US20090018103A1 (en) 2009-01-15
IL182305A0 (en) 2007-07-24
CA2582202A1 (en) 2006-04-20
ZA200702836B (en) 2010-06-30
JP5067968B2 (ja) 2012-11-07
KR101314277B1 (ko) 2013-10-02
AU2005294123B2 (en) 2009-07-02
AU2005294123A1 (en) 2006-04-20
US7754737B2 (en) 2010-07-13
EP1807078A1 (en) 2007-07-18
CN101072561B (zh) 2011-05-11
US20110105506A1 (en) 2011-05-05
CN101072561A (zh) 2007-11-14
JP2012180371A (ja) 2012-09-20
RU2440993C2 (ru) 2012-01-27

Similar Documents

Publication Publication Date Title
EP4570320A3 (en) Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
Aroui et al. Naringin inhibits the invasion and migration of human glioblastoma cell via downregulation of MMP-2 and MMP-9 expression and inactivation of p38 signaling pathway
MX2024008539A (es) Compuestos bifuncionales para degradar la tirosina cinasa de bruton (btk) mediante la trayectoria de ubiquitina proteosoma.
DK1902141T3 (da) ADAMTS 13-holdige sammensætninger med thrombolytisk virkning
NO20091700L (no) Florizinanaloger som inhibitorer av glukose-ko-transporter 2
BRPI0307351B8 (pt) composto, composição farmacêutica, uso de um composto, e, processo para preparar um composto
BRPI0417376A (pt) compostos, processo para a manufatura dos mesmos, composições farmacêuticas que os compreendem, método para o tratamento e/ou profilaxia de enfermidades que estão associadas com a modulação de receptores de cb1 e sua utilização
BRPI0407993B8 (pt) compostos inibidores de p38 e composições farmacêuticas compreendendo os mesmos
NO20064347L (no) Substituerte 1,2,3,4-tetrahydroisokinolinderivater
NO20060328L (no) Kombinasjon av mGluR2-antagonist og ACHE-inhibitor for behandiing av akutt og/eller kronisk neurologiske forstyrrelser
DE60236541D1 (de) Inhibitoren von 11-beta-hydroxysteroiddehydrogenase typ 1
DK1296972T3 (da) Arylmethylamin-derivater til anvendelse som tryptaseinhibitorer
BRPI0412893A (pt) composto, composição farmacêutica, uso de um composto, e, métodos de prevenção, tratamento ou melhora de doenças ou condições inflamatórias, ou doenças ou condições oftálmicas, de tratamento ou melhora de cáncer e para a produção de um composto
BR0314353A (pt) Compostos, composições farmacêuticas, uso de um ou mais compostos em combinação com outros compostos farmacologicamente ativos, e, método para tratar um paciente que sofre de um distúrbio
BRPI0514133A (pt) compostos de fórmula i, processo para a sua fabricação, composições farmacêuticas, método para o tratamento e/ou profilaxia de doença que são mediadas por inibidores de cetp e uso dos compostos de fórmula i
WO2006042150A8 (en) Diaminoalkane aspartic protease inhibitors
UY27993A1 (es) Derivados de 4-pirrolidino-fenil-bencil eter
CY1108900T1 (el) Πολυθειωμενα γλυκοζιδια και αλατα αυτων
BRPI0416287A (pt) compostos, processo para a manufatura dos mesmos, composições farmacêuticas que os compreendem, método para o tratamento e/ou prevenção de enfermidades que são moduladas por inibidores de accß e sua utilização
NO20062923L (no) Nye benzofuranderivater som kan anvendes i forebygging eller behandling av 5-HT6 reseptorrelatert forstyrrelse
DK1789398T3 (da) 2-amino-quinazolin derivater anvendelige som inhibitorer af B-sekretase (BACE)
BRPI0508051A (pt) derivados de heteroarilaminopirazol utilizáveis para o tratamento de diabetes
BR0316723A (pt) Derivados de anilinopirazol úteis para o tratamento de diabetes
BRPI0508254A (pt) métodos e composições para o tratamento ou prevenção de distúrbios psiquiátricos com inibidores de cox-2 sozinhos e em combinação com agentes antidepressivos
MA29278B1 (fr) Composition pharmaceutique comprenant un derive de l'indolylmaleimide

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 10A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2326 DE 04-08-2015 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.