OA12909A - Beta-lactamase inhibitor prodrug. - Google Patents

Beta-lactamase inhibitor prodrug. Download PDF

Info

Publication number: OA12909A
Authority: OA; OAPI
Prior art keywords: prodrug; beta; heptane; oxo; thia
Prior art date: 2002-08-23

Application number

OA1200500051A

Other languages

English (en)

Inventor

Anthony Marfat

Dale Gordon Mcleod

Original Assignee

Pfizer Prod 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.)

2002-08-23

Filing date

2003-08-11

Publication date

2006-10-13

2003-08-11 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2006-10-13 Publication of OA12909A publication Critical patent/OA12909A/en

Links

239000000651 prodrug Substances 0.000 title claims abstract description 171
229940002612 prodrug Drugs 0.000 title claims abstract description 171
239000003781 beta lactamase inhibitor Substances 0.000 title description 14
229940126813 beta-lactamase inhibitor Drugs 0.000 title description 14
229940126085 β‑Lactamase Inhibitor Drugs 0.000 title description 11
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239000002132 β-lactam antibiotic Substances 0.000 claims abstract description 32
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208000035143 Bacterial infection Diseases 0.000 claims abstract description 7
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LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims description 54
NNYHKYDYHWSHKQ-UHFFFAOYSA-N 4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid Chemical compound OC(=O)C1CSC2CCN12 NNYHKYDYHWSHKQ-UHFFFAOYSA-N 0.000 claims description 37
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ABVRVIZBZKUTMK-JSYANWSFSA-M potassium clavulanate Chemical compound [K+].[O-]C(=O)[C@H]1C(=C/CO)/O[C@@H]2CC(=O)N21 ABVRVIZBZKUTMK-JSYANWSFSA-M 0.000 description 1
BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical group CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
238000000746 purification Methods 0.000 description 1
150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
238000010791 quenching Methods 0.000 description 1
VMXUWOKSQNHOCA-UKTHLTGXSA-N ranitidine Chemical compound [O-][N+](=O)\C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-UKTHLTGXSA-N 0.000 description 1
230000001105 regulatory effect Effects 0.000 description 1
208000023504 respiratory system disease Diseases 0.000 description 1
230000000717 retained effect Effects 0.000 description 1
230000000979 retarding effect Effects 0.000 description 1
IOVGROKTTNBUGK-SJCJKPOMSA-N ritodrine Chemical compound N([C@@H](C)[C@H](O)C=1C=CC(O)=CC=1)CCC1=CC=C(O)C=C1 IOVGROKTTNBUGK-SJCJKPOMSA-N 0.000 description 1
238000005070 sampling Methods 0.000 description 1
229920006395 saturated elastomer Polymers 0.000 description 1
DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 description 1
239000012056 semi-solid material Substances 0.000 description 1
239000000377 silicon dioxide Substances 0.000 description 1
206010040872 skin infection Diseases 0.000 description 1
210000000813 small intestine Anatomy 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
239000007909 solid dosage form Substances 0.000 description 1
239000011877 solvent mixture Substances 0.000 description 1
238000002798 spectrophotometry method Methods 0.000 description 1
238000001228 spectrum Methods 0.000 description 1
238000012453 sprague-dawley rat model Methods 0.000 description 1
239000007921 spray Substances 0.000 description 1
239000008107 starch Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
238000003860 storage Methods 0.000 description 1
239000001384 succinic acid Substances 0.000 description 1
229960005137 succinic acid Drugs 0.000 description 1
235000011044 succinic acid Nutrition 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000004094 surface-active agent Substances 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
230000002194 synthesizing effect Effects 0.000 description 1
LPQZKKCYTLCDGQ-WEDXCCLWSA-N tazobactam Chemical compound C([C@]1(C)S([C@H]2N(C(C2)=O)[C@H]1C(O)=O)(=O)=O)N1C=CN=N1 LPQZKKCYTLCDGQ-WEDXCCLWSA-N 0.000 description 1
229960003865 tazobactam Drugs 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
DBGVGMSCBYYSLD-UHFFFAOYSA-N tributylstannane Chemical compound CCCC[SnH](CCCC)CCCC DBGVGMSCBYYSLD-UHFFFAOYSA-N 0.000 description 1
210000001635 urinary tract Anatomy 0.000 description 1
230000035899 viability Effects 0.000 description 1
238000003260 vortexing Methods 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1
229920001285 xanthan gum Polymers 0.000 description 1
239000011592 zinc chloride Substances 0.000 description 1
235000005074 zinc chloride Nutrition 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- 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
- 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
- A61P31/04—Antibacterial agents
- 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
- C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D499/21—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a nitrogen atom directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D499/44—Compounds with an amino radical acylated by carboxylic acids, attached in position 6
- C07D499/48—Compounds with an amino radical acylated by carboxylic acids, attached in position 6 with a carbon chain, substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, attached to the carboxamido radical

Landscapes

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

OA1200500051A 2002-08-23 2003-08-11 Beta-lactamase inhibitor prodrug. OA12909A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US40564002P	2002-08-23	2002-08-23

Publications (1)

Publication Number	Publication Date
OA12909A true OA12909A (en)	2006-10-13

Family

ID=31946909

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200500051A OA12909A (en)	2002-08-23	2003-08-11	Beta-lactamase inhibitor prodrug.

Country Status (31)

Country	Link
US (1)	US7091197B2 (de)
EP (1)	EP1534717B1 (de)
JP (1)	JP2005539037A (de)
KR (1)	KR20050037583A (de)
CN (1)	CN1688589A (de)
AP (1)	AP2005003231A0 (de)
AR (1)	AR041028A1 (de)
AT (1)	ATE349452T1 (de)
AU (1)	AU2003250489A1 (de)
BR (1)	BR0313683A (de)
CA (1)	CA2494953A1 (de)
DE (1)	DE60310733D1 (de)
EA (1)	EA007540B1 (de)
EC (1)	ECSP055625A (de)
GT (1)	GT200300179A (de)
HR (1)	HRP20050162A2 (de)
IL (1)	IL166719A0 (de)
IS (1)	IS7693A (de)
MA (1)	MA27387A1 (de)
MX (1)	MXPA05001446A (de)
NO (1)	NO20051497L (de)
NZ (1)	NZ538340A (de)
OA (1)	OA12909A (de)
PA (1)	PA8579701A1 (de)
PE (1)	PE20040899A1 (de)
PL (1)	PL375988A1 (de)
TN (1)	TNSN05054A1 (de)
TW (1)	TWI250162B (de)
UY (1)	UY27947A1 (de)
WO (1)	WO2004018484A1 (de)
ZA (1)	ZA200501513B (de)

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JP2006526612A (ja) *	2003-06-05	2006-11-24	ファイザー・プロダクツ・インク	ベータ−ラクタマーゼ阻害剤・プロドラッグ
US20060105941A1 (en) *	2004-11-12	2006-05-18	Allergan, Inc.	Mixed antibiotic codrugs
EP1913378A1 (de) *	2005-07-29	2008-04-23	Sigma-Aldrich Production GmbH	Ionisierungsadditive enthaltende lc/ms-blends
WO2010118968A1 (en)	2009-04-16	2010-10-21	Nicox S.A.	No-donor aspirin derivatives
WO2013056163A1 (en)	2011-10-14	2013-04-18	The Regents Of The University Of California	Beta-lactamase inhibitors
EP2800568A4 (de)	2012-01-06	2015-06-10	Univ South Florida	Zusammensetzungen, verwendungsverfahren dafür und behandlungsverfahren damit
CN109422765B (zh) *	2017-09-05	2020-08-28	香港理工大学深圳研究院	C类β-内酰胺酶抑制剂及其制备方法和应用

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IE34011B1 (en) *	1969-03-13	1975-01-08	Leo Pharm Prod Ltd	New penicillin esters
IE34019B1 (en) *	1969-03-18	1975-01-08	Leo Pharm Prod Ltd	New semi-synthetic penicillin esters
GB1267936A (en)	1969-05-28	1972-03-22	Beecham Group Ltd	DERIVATIVES OF alpha-AMINOPENICILLINS
US3957764A (en) *	1969-11-11	1976-05-18	Lovens Kemiske Fabrik Produktionsaktieselskab	6-aminopenicillanic acid derivatives
US3862181A (en) *	1970-10-28	1975-01-21	Squibb & Sons Inc	Process for preparing cephalosporins
GB1315566A (en)	1970-11-06	1973-05-02	Leo Pharm Prod Ltd	Penicillanic acid derivatives
CA996929A (en)	1971-04-05	1976-09-14	Kohzi Nakano	Acyloxyalkyl ester derivatives of penicillin
GB1433131A (en) *	1972-03-13	1976-04-22	Astra Laekemedel Ab	Penicillins
GB1426717A (en)	1972-03-13	1976-03-03	Astra Laekemedel Ab	Penicillins
US4397783A (en) *	1979-03-05	1983-08-09	Pfizer Inc.	Process for converting 6,6-disubstituted penicillanic acid derivatives to the 6-β-congeners
DE2927004A1 (de) *	1979-07-04	1981-05-27	Bayer Ag, 5090 Leverkusen	Penicillansaeure-1,1-dioxide, ihre herstellung und ihre verwendung als arzneimittel als arzneimittel
US4287181A (en) *	1979-10-22	1981-09-01	Pfizer Inc.	Derivatives of 6β-hydroxyalkylpenicillanic acids as β-lactamase inhibitors
US4432970A (en) *	1979-11-23	1984-02-21	Pfizer Inc.	6-beta-Halopenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
GB2076812A (en) *	1980-05-22	1981-12-09	Ciba Geigy Ag	Penam-dioxide compounds, processes for their manufacture, and their use
JPS5849387A (ja)	1981-09-17	1983-03-23	Sankyo Co Ltd	７−メトキシセフアロスポリン化合物およびその製法
EP0076066B1 (de) *	1981-09-22	1986-11-26	Kureha Kagaku Kogyo Kabushiki Kaisha	Penicillin-Derivate
US4406887A (en) *	1981-10-13	1983-09-27	Bristol-Myers Company	Method for treating resistant bacteria including anaerobes
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DE3901405A1 (de)	1989-01-19	1990-07-26	Hoechst Ag	Cephalosporinderivate und verfahren zu ihrer herstellung
JPH03206038A (ja)	1990-01-08	1991-09-09	Yoshitomi Pharmaceut Ind Ltd	抗菌剤
GB9001405D0 (en) *	1990-01-22	1990-03-21	Leo Pharm Prod Ltd	New intermediates,their production and use
GB9208492D0 (en) *	1992-04-16	1992-06-03	Glaxo Spa	Heterocyclic compounds
JP2006526612A (ja) *	2003-06-05	2006-11-24	ファイザー・プロダクツ・インク	ベータ−ラクタマーゼ阻害剤・プロドラッグ

2003
- 2003-08-06 PA PA20038579701A patent/PA8579701A1/es unknown
- 2003-08-11 AP AP2005003231A patent/AP2005003231A0/xx unknown
- 2003-08-11 PL PL03375988A patent/PL375988A1/xx unknown
- 2003-08-11 EP EP03792574A patent/EP1534717B1/de not_active Expired - Lifetime
- 2003-08-11 CA CA002494953A patent/CA2494953A1/en not_active Abandoned
- 2003-08-11 JP JP2004530453A patent/JP2005539037A/ja not_active Abandoned
- 2003-08-11 EA EA200500398A patent/EA007540B1/ru unknown
- 2003-08-11 NZ NZ538340A patent/NZ538340A/en unknown
- 2003-08-11 AT AT03792574T patent/ATE349452T1/de not_active IP Right Cessation
- 2003-08-11 BR BR0313683-3A patent/BR0313683A/pt not_active IP Right Cessation
- 2003-08-11 WO PCT/IB2003/003582 patent/WO2004018484A1/en not_active Ceased
- 2003-08-11 HR HR20050162A patent/HRP20050162A2/xx not_active Application Discontinuation
- 2003-08-11 MX MXPA05001446A patent/MXPA05001446A/es unknown
- 2003-08-11 KR KR1020057002983A patent/KR20050037583A/ko not_active Abandoned
- 2003-08-11 OA OA1200500051A patent/OA12909A/en unknown
- 2003-08-11 AU AU2003250489A patent/AU2003250489A1/en not_active Abandoned
- 2003-08-11 CN CNA038243164A patent/CN1688589A/zh active Pending
- 2003-08-11 DE DE60310733T patent/DE60310733D1/de not_active Expired - Lifetime
- 2003-08-19 PE PE2003000840A patent/PE20040899A1/es not_active Application Discontinuation
- 2003-08-21 AR ARP030103023A patent/AR041028A1/es unknown
- 2003-08-21 UY UY27947A patent/UY27947A1/es not_active Application Discontinuation
- 2003-08-22 TW TW092123156A patent/TWI250162B/zh not_active IP Right Cessation
- 2003-08-22 GT GT200300179A patent/GT200300179A/es unknown
- 2003-08-25 US US10/648,408 patent/US7091197B2/en not_active Expired - Fee Related
2005
- 2005-02-07 IL IL16671905A patent/IL166719A0/xx unknown
- 2005-02-10 IS IS7693A patent/IS7693A/is unknown
- 2005-02-21 ZA ZA200501513A patent/ZA200501513B/en unknown
- 2005-02-23 MA MA28119A patent/MA27387A1/fr unknown
- 2005-02-23 TN TNP2005000054A patent/TNSN05054A1/fr unknown
- 2005-02-23 EC EC2005005625A patent/ECSP055625A/es unknown
- 2005-03-21 NO NO20051497A patent/NO20051497L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
EP1534717B1 (de)	2006-12-27
JP2005539037A (ja)	2005-12-22
PE20040899A1 (es)	2004-12-28
CA2494953A1 (en)	2004-03-04
NO20051497D0 (no)	2005-03-21
ECSP055625A (es)	2005-04-18
EA007540B1 (ru)	2006-10-27
AU2003250489A1 (en)	2004-03-11
HRP20050162A2 (en)	2005-06-30
MA27387A1 (fr)	2005-06-01
TWI250162B (en)	2006-03-01
AP2005003231A0 (en)	2005-03-31
UY27947A1 (es)	2004-03-31
MXPA05001446A (es)	2005-06-06
PL375988A1 (en)	2005-12-12
BR0313683A (pt)	2005-06-21
EA200500398A1 (ru)	2005-08-25
IS7693A (is)	2005-02-10
AR041028A1 (es)	2005-04-27
NZ538340A (en)	2006-10-27
IL166719A0 (en)	2006-01-15
ZA200501513B (en)	2006-09-27
GT200300179A (es)	2004-05-18
WO2004018484A1 (en)	2004-03-04
TW200417548A (en)	2004-09-16
TNSN05054A1 (fr)	2007-05-14
CN1688589A (zh)	2005-10-26
PA8579701A1 (es)	2005-05-24
ATE349452T1 (de)	2007-01-15
KR20050037583A (ko)	2005-04-22
DE60310733D1 (de)	2007-02-08
US20040110740A1 (en)	2004-06-10
US7091197B2 (en)	2006-08-15
EP1534717A1 (de)	2005-06-01
NO20051497L (no)	2005-03-21

Publication	Publication Date	Title
US4098897A (en)	1978-07-04	Anti bacterial agents
KR20140052927A (ko)	2014-05-07	화합물 및 그의 용도
US4918068A (en)	1990-04-17	Cephem compounds
OA12909A (en)	2006-10-13	Beta-lactamase inhibitor prodrug.
NO802686L (no)	1978-10-24	Fremgangsmaate for fremstilling av en ester av et klavulansyreamin
JPS60202889A (ja)	1985-10-14	β‐ラクタマーゼ阻害剤としての６‐（アミノアシルオキシメチル）ペニシラン酸１，１‐ジオキシド誘導体
US9115131B2 (en)	2015-08-25	Nitrogen containing compounds and their use
HU207522B (en)	1993-04-28	Process for producing esters of antibacterial cepheme-derivatives and pharmaceutical compositions containing them
DE69625910T2 (de)	2003-11-06	Penamsulfone als beta-laktamase inhibitoren
US20050004093A1 (en)	2005-01-06	Beta-lactamase inhibitor prodrug
JPH05508625A (ja)	1993-12-02	新規なセファロスポリン化合物およびその製法
US20150322087A1 (en)	2015-11-12	Cephalosporin derivatives and methods of use
CN115304594B (zh)	2023-02-14	磺酰脲环取代的化合物的盐型及其晶型
KR830001902B1 (ko)	1983-09-19	폐니실란산유도체의 제조방법
JPS6360991A (ja)	1988-03-17	（５ｒ，６ｓ，８ｒ）−６−（１−ヒドロキシエチル）−２−（３ｒ−ピロリジン−２−オン−３−イル）チオペネム−３−カルボン酸
JPH0314586A (ja)	1991-01-23	セフェム化合物及びその製造法
HK1079520A (en)	2006-04-07	Beta-lactamase inhibitor prodrug
KR20020085180A (ko)	2002-11-16	신규 세팔로스포린계 항생제 및 이의 제조 방법
JPWO1996005205A1 (ja)	1996-12-24	新規セフェム誘導体
KR20030071311A (ko)	2003-09-03	신규 세팔로스포린 화합물 및 그의 제조방법
JP2005509039A (ja)	2005-04-07	Ｃ−３がｓ／ｏおよびｓ／ｎである新規なセファロスポリンのホルムアルデヒドアセタール誘導体およびその抗生物質としての使用
JPH09176091A (ja)	1997-07-08	新規化合物ｆ−１２４３６類