HUP0000288A2 - Azetidinone derivatives as inhibitors of the enzymatic activity of psa, intermediates, process for their preparation and pharmaceutical compositions thereof - Google Patents

Azetidinone derivatives as inhibitors of the enzymatic activity of psa, intermediates, process for their preparation and pharmaceutical compositions thereof

Info

Publication number
HUP0000288A2
HUP0000288A2 HU0000288A HUP0000288A HUP0000288A2 HU P0000288 A2 HUP0000288 A2 HU P0000288A2 HU 0000288 A HU0000288 A HU 0000288A HU P0000288 A HUP0000288 A HU P0000288A HU P0000288 A2 HUP0000288 A2 HU P0000288A2
Authority
HU
Hungary
Prior art keywords
azetidinone derivatives
psa
enzymatic activity
prostate
intermediates
Prior art date
Application number
HU0000288A
Other languages
Hungarian (hu)
Inventor
Benjamin A. Anderson
Gerald W. Becker
James A. Carty
Nancy K. Harn
Lowell D. Hatfield
Blake L. Neubauer
John R. Rizzo
Tony Y. Zhang
Original Assignee
Eli Lilly And Co.
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 Eli Lilly And Co. filed Critical Eli Lilly And Co.
Publication of HUP0000288A2 publication Critical patent/HUP0000288A2/en
Publication of HUP0000288A3 publication Critical patent/HUP0000288A3/en

Links

Classifications

    • 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
    • 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
    • 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

Ajelen találmány tárgya (I) általános képletű új azetidinonszármazékok- ahol a képletben R1 jelentése adott esetben szubsztituált aril- vagyaralkilcsoport vagy heterociklusos csoport, R2 jelentése alkenil-,aril- vagy heterociklusos csoport, és R3 jelentése heterogyűrű,észterezett karboxilcsoport vagy egy tiokarbamoilcsoport -, bizonyosközbenső termékek és a fenti azetidinonszármazékok előállításieljárásai, valamint a vegyületeket tartalmazó gyógyszerkészítmények.Ajelen találmány szerinti azetidinonszármazékok alkalmasakprosztataspecifikus antigén (Prostate-Specific Antigen, PSA)enzimatikus aktivitásának gátlására, valamint prosztatarák (Pca), aPca áttételei, jóindulatú prosztatanagyobbodás (BPH) és mellrák (Bc)kezelésére. ÓThe subject of the present invention is new azetidinone derivatives of formula (I) - where R1 in the formula is an optionally substituted aryl or alkyl group or a heterocyclic group, R2 is an alkenyl, aryl or heterocyclic group, and R3 is a heteroring, an esterified carboxyl group or a thiocarbamoyl group -, certain intermediates products and the production processes of the above azetidinone derivatives, as well as pharmaceutical preparations containing the compounds. The azetidinone derivatives according to the present invention are suitable for inhibiting the enzymatic activity of prostate-specific antigen (Prostate-Specific Antigen, PSA), as well as prostate cancer (Pca), metastases of aPca, benign prostatic hyperplasia (BPH) and breast cancer (Bc) for treatment. HE

HU0000288A 1996-12-13 1997-12-09 Azetidinone derivatives as inhibitors of the enzymatic activity of psa, intermediates, process for their preparation and pharmaceutical compositions thereof HUP0000288A3 (en)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US3317996P 1996-12-13 1996-12-13
US4054397P 1997-03-13 1997-03-13
US4053997P 1997-03-13 1997-03-13
US4403297P 1997-03-13 1997-03-13
US4036297P 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

Publications (2)

Publication Number Publication Date
HUP0000288A2 true HUP0000288A2 (en) 2001-01-29
HUP0000288A3 HUP0000288A3 (en) 2001-04-28

Family

ID=27580753

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0000288A HUP0000288A3 (en) 1996-12-13 1997-12-09 Azetidinone derivatives as inhibitors of the enzymatic activity of psa, intermediates, process for their preparation and pharmaceutical compositions thereof

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
JP4361273B2 (en) 2001-02-27 2009-11-11 アメリカ合衆国 Thalidomide analogs as potential angiogenesis inhibitors
CN100560131C (en) 2001-10-22 2009-11-18 斯克里普斯研究学院 Antibody targeting compounds
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
US7713983B2 (en) 2003-03-03 2010-05-11 Vertex Pharmaceuticals Incorporated Quinazolines useful as modulators of ion channels
WO2004080391A2 (en) 2003-03-10 2004-09-23 Optimer Pharmaceuticals, Inc. Novel antibacterial agents
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
US7973057B2 (en) 2003-09-17 2011-07-05 The United States Of America As Represented By The Department Of Health And Human Services Thalidomide analogs
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
US9453042B2 (en) 2007-10-25 2016-09-27 Cempra Pharmaceuticals, Inc. Process for the preparation of macrolide antibacterial agents
WO2010048600A1 (en) 2008-10-24 2010-04-29 Cempra Pharmaceuticals, Inc. Methods for treating resistant diseases using triazole containing macrolides
US9937194B1 (en) 2009-06-12 2018-04-10 Cempra Pharmaceuticals, Inc. Compounds and methods for treating inflammatory diseases
WO2011032052A1 (en) 2009-09-10 2011-03-17 Cempra Pharmaceuticals, Inc. Methods for treating malaria, tuberculosis and mac diseases
ES2662350T3 (en) * 2010-07-01 2018-04-06 Azevan Pharmaceuticals, Inc. Procedures for the treatment of posttraumatic stress disorder
WO2012034058A1 (en) 2010-09-10 2012-03-15 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
RU2658050C2 (en) 2012-03-27 2018-06-19 Семпра Фармасьютикалз, Инк. Parenteral formulations for administering macrolide antibiotics
AU2014239959A1 (en) 2013-03-14 2015-10-01 Cempra Pharmaceuticals, Inc. Methods for treating respiratory diseases and formulations therefor
US9751908B2 (en) 2013-03-15 2017-09-05 Cempra Pharmaceuticals, Inc. Convergent processes for preparing macrolide antibacterial agents
CN111295373A (en) 2017-09-15 2020-06-16 阿泽凡药物公司 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
EP0944594A1 (en) 1999-09-29
WO1998025895A1 (en) 1998-06-18
CA2274958A1 (en) 1998-06-18
JP2002514197A (en) 2002-05-14
AU5597098A (en) 1998-07-03
EP0944594A4 (en) 2000-05-03
KR20000069431A (en) 2000-11-25
IL130300A0 (en) 2000-06-01
BR9714394A (en) 2000-05-16
HUP0000288A3 (en) 2001-04-28

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