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BR9714394A - Inhibitors of psa enzyme activity - Google Patents

Inhibitors of psa enzyme activity

Info

Publication number
BR9714394A
BR9714394A BR9714394-4A BR9714394A BR9714394A BR 9714394 A BR9714394 A BR 9714394A BR 9714394 A BR9714394 A BR 9714394A BR 9714394 A BR9714394 A BR 9714394A
Authority
BR
Brazil
Prior art keywords
psa
pca
inhibitors
relates
enzyme activity
Prior art date
Application number
BR9714394-4A
Other languages
Portuguese (pt)
Inventor
Benjamin A Anderson
Gerald W Becker
James A Caty
Nancy K Harn
Lowell D Hatfield
Blake L Neubauer
Jonh R Rizzo
Tony Y Zhang
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of BR9714394A publication Critical patent/BR9714394A/en

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Patente de Invenção:<B>"INIBIDORES DA ATIVIDADE ENZIMáTICA DE PSA"<D>. A presente invenção refere-se a novos compostos de azeitidinona, a certos intermediários e processos para a preparação desses compostos de azetidinona, e a formulações contendo os mesmos. A presente invenção também se refere ao uso dessas azetidinonas como inibidores da atividade enzimática de Antígeno Específico para a Próstata (PSA), bem como para o tratamento de câncer prostático (Pca), metástase de Pca, hiperplasia prostática benigna (BPH) e câncer de mama (Bc). Um outro aspecto da invenção refere-se a métodos inventivos para o tratamento de Pca, metástase de Pca, BPH e Bc por administração de qualquer composto inibidor de PSA.Invention Patent: <B> "PSA ENZYMATIC ACTIVITY INHIBITORS" <D>. The present invention relates to new compounds of azeitidinone, to certain intermediates and processes for the preparation of these azetidinone compounds, and to formulations containing them. The present invention also relates to the use of these azetidinones as inhibitors of the enzyme activity of Prostate Specific Antigen (PSA), as well as for the treatment of prostate cancer (Pca), Pca metastasis, benign prostatic hyperplasia (BPH) and cancer of the prostate. breast (Bc). Another aspect of the invention relates to inventive methods for the treatment of Pca, Pca metastasis, BPH and Bc by administering any PSA inhibiting compound.

BR9714394-4A 1996-12-13 1997-12-09 Inhibitors of psa enzyme activity BR9714394A (en)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US3317996P 1996-12-13 1996-12-13
US4036297P 1997-03-13 1997-03-13
US4403297P 1997-03-13 1997-03-13
US4054397P 1997-03-13 1997-03-13
US4053997P 1997-03-13 1997-03-13
US4080597P 1997-03-18 1997-03-18
US4080497P 1997-03-18 1997-03-18
US4705497P 1997-05-19 1997-05-19
US4705597P 1997-05-19 1997-05-19
US5072197P 1997-06-25 1997-06-25
PCT/US1997/022573 WO1998025895A1 (en) 1996-12-13 1997-12-09 Inhibitors of the enzymatic activity of psa

Publications (1)

Publication Number Publication Date
BR9714394A true BR9714394A (en) 2000-05-16

Family

ID=27580753

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9714394-4A BR9714394A (en) 1996-12-13 1997-12-09 Inhibitors of psa enzyme activity

Country Status (9)

Country Link
EP (1) EP0944594A4 (en)
JP (1) JP2002514197A (en)
KR (1) KR20000069431A (en)
AU (1) AU5597098A (en)
BR (1) BR9714394A (en)
CA (1) CA2274958A1 (en)
HU (1) HUP0000288A3 (en)
IL (1) IL130300A0 (en)
WO (1) WO1998025895A1 (en)

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US6335324B1 (en) 1998-06-25 2002-01-01 Bristol-Myers Squibb Co. Beta lactam compounds and their use as inhibitors of tryptase
EP1389203B8 (en) 2001-02-27 2010-03-10 The Governement of the United States of America, represented by The Secretary Department of Health and Human services Analogs of thalidomide as angiogenesis inhibitors
WO2003059251A2 (en) 2001-10-22 2003-07-24 The Scripps Research Institute Antibody targeting compounds
US7713983B2 (en) 2003-03-03 2010-05-11 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels
CL2004000409A1 (en) 2003-03-03 2005-01-07 Vertex Pharma COMPOUNDS DERIVED FROM 2- (REPLACED CILO) -1- (AMINO OR REPLACED OXI) -CHINAZOLINE, INHIBITORS OF IONIC SODIUM AND CALCIUM VOLTAGE DEPENDENTS; PHARMACEUTICAL COMPOSITION; AND USE OF THE COMPOUND IN THE TREATMENT OF ACUTE PAIN, CHRONIC, NEU
CA2801100A1 (en) 2003-03-10 2004-09-23 Optimer Pharmaceuticals, Inc. Macrolides and processes for their preparation
WO2005016326A2 (en) * 2003-07-11 2005-02-24 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Analogs of thalidomide as potential angiogenesis inhibitors
US8952895B2 (en) 2011-06-03 2015-02-10 Apple Inc. Motion-based device operations
CA2538864C (en) 2003-09-17 2013-05-07 The Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services Thalidomide analogs as tnf-alpha modulators
WO2005063704A1 (en) * 2003-12-25 2005-07-14 Ono Pharmaceutical Co., Ltd. Azetidine ring compounds and drugs comprising the same
US7928107B2 (en) 2004-09-02 2011-04-19 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels
US8283354B2 (en) 2004-09-02 2012-10-09 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels
AU2008316830B2 (en) 2007-10-25 2016-03-17 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
CN102245195B (en) 2008-10-24 2016-01-13 森普拉制药公司 Biodefense using triazole-containing macrolides
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
CN102724874B (en) 2009-09-10 2018-06-01 森普拉制药公司 Methods of treating malaria, tuberculosis and MAC disease
CN107007596A (en) * 2010-07-01 2017-08-04 阿泽凡药物公司 Method for treating posttraumatic stress disorder
US9815863B2 (en) 2010-09-10 2017-11-14 Cempra Pharmaceuticals, Inc. Hydrogen bond forming fluoro ketolides for treating diseases
US8927725B2 (en) 2011-12-02 2015-01-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Thio compounds
KR20140139083A (en) 2012-03-27 2014-12-04 셈프라 파마슈티컬스, 인크. Parenteral formulations for administering macrolide antibiotics
CA2905975A1 (en) 2013-03-14 2014-09-25 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
JP6675973B2 (en) 2013-03-15 2020-04-08 センプラ ファーマシューティカルズ，インコーポレイテッド Focused method for preparing macrolide antimicrobial agents
JP2020534274A (en) 2017-09-15 2020-11-26 アゼヴァン ファーマシューティカルズ，インコーポレイテッド Compositions and Methods for Treating Brain Injury

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA94128B (en) * 1993-02-01 1994-08-19 Univ New York State Res Found Process for the preparation of taxane derivatives and betalactam intermediates therefor

Also Published As

Publication number Publication date
KR20000069431A (en) 2000-11-25
IL130300A0 (en) 2000-06-01
EP0944594A4 (en) 2000-05-03
AU5597098A (en) 1998-07-03
EP0944594A1 (en) 1999-09-29
HUP0000288A2 (en) 2001-01-29
WO1998025895A1 (en) 1998-06-18
HUP0000288A3 (en) 2001-04-28
JP2002514197A (en) 2002-05-14
CA2274958A1 (en) 1998-06-18

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Legal Events

Date Code Title Description
FA10 Dismissal: dismissal - article 33 of industrial property law
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]