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WO1999063937A9 |
Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more prot...
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WO/2001/040228A1 |
Carbapenem compounds represented by general formula (I), and pharmacologically acceptable salts thereof, [wherein R?1¿ is acyl derived from an $g(a)-amino acid whose amino group may be substituted with lower alkyl; R?2¿ is hydrogen or ...
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WO/2001/032172A1 |
A novel process for preparing a stabilized, lyophilized carbapenem, antibiotic formulation suitable for intravenous administration to patients in need thereof, wherein the active ingredient is of formula (II). The process entails compoun...
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WO/2001/009135A1 |
An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an...
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WO1999064049A9 |
This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligan...
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WO/2001/002401A1 |
Crystals of compound (I) or pharmacologically acceptable salts thereof, which exhibit an excellent antimicrobial activity and are so excellent in storage stability and handleability as to be put into practical use as antimicrobial agents.
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WO/2001/000624A1 |
A process of synthesizing a carbapenem compound of formula (6) is disclosed wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R?1¿ is independently selected from: H, halo, OH, OP wherein ...
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WO/2000/075143A1 |
Crystals of mono- or tri-hydrates of hydrochlorides of carbapenem compounds useful as antibacterial agents, which are chemically stable and easy to purify; processes for the production of the crystals; and injectable powder preparations ...
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WO1999064033A9 |
This invention relates to novel multibinding compounds that bind to the enzyme phosphodiesterase V (PDE V) and modulate its activity. The compounds of this invention comprise 2-10 PDE V modulator (particularly inhibitor) ligands covalent...
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WO1999064048A9 |
Disclosed are multibinding compounds which inhibit the enzyme HIV reverse transcriptase, an enzyme which catalyzes the conversion of viral RNA to single stranded DNA. The multibinding compounds of this invention containing from 2 to 10 l...
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WO/2000/042041A1 |
Problem: Carbapenem compounds exhibiting excellent antimicrobial activities and peroral absorbability. Means for solving the problem: Carbapenem ester compounds represented by general formula (I), or pharmacologically acceptable derivati...
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WO/2000/034282A1 |
1-Methylcarbapenem compounds represented by general formula (I) or pharmacologically acceptable salts or derivatives thereof, exhibiting excellent antibacterial activities wherein n is 2, 3 or 4; R?1¿ is hydrogen or C¿1?-C¿4? alkyl; n...
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WO1999063988A9 |
Disclosed are multibinding compounds which inhibit nitric oxide synthases (NOSs), enzymes which form nitric oxide and L-citrulline from L-arginine. The multibinding compounds of this invention contain from 2 to 10 ligands covalently atta...
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WO/2000/015640A1 |
Carbapenem compounds represented by general formula (I); pharmacologically acceptable salts of the same; and antibacterial agents containing these compounds or salts as the active ingredient (wherein R is hydrogen or optionally substitut...
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WO1999064047A9 |
Novel compounds are disclosed, useful as antiviral agents.
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WO1999063929A9 |
Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compound...
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WO/2000/012048A2 |
The present invention relates to novel 2-(naphthosultamyl)methyl-carbapenem antibacterial agents or pharmaceutically acceptable salts thereof in combination with other $g(b)-lactams, which are useful in treating and preventing enterococc...
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WO1999064054A9 |
Disclosed are multibinding compounds which inhibit topoisomerases which are essential enzymes in higher encaryotes for DNA replication and repair. The multibinding compounds of this invention containing from 2 to 10 ligands covalently at...
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WO/2000/006581A1 |
Novel compounds having a broad antibacterial activity over gram-positive and gram-negative bacteria, in particular, a potent antibacterial effect on $g(b)-lactamase producing bacteria, MRSA, tolerant $i(Pseudomonas aeruginosa), DRSP, $i(...
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WO/2000/006574A1 |
The compounds of general formula (I) wherein R?1¿ denotes hydrogen, hydroxymethyl or 1-hydroxyethyl, R?2¿ denotes hydrogen or methyl and R?3¿ denotes a pharmaceutically acceptable group which is bonded to the remaining part of the mol...
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WO/2000/002880A1 |
The invention describes an improved process for synthesizing 1-$g(b)-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The synthesis eliminates the use of BU¿3?SnC...
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WO/1999/066928A1 |
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof are disclosed.
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WO/1999/067241A1 |
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof are disclosed.
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WO/1999/067240A1 |
Compounds of formula (I): as well as pharmaceutically acceptable salts thereof are disclosed.
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WO/1999/066927A1 |
Compounds of formula (I), as well as pharmaceutically acceptable salts thereof are disclosed.
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WO/1999/067242A1 |
Compounds of formula (I) as well as pharmaceutically acceptable salts thereof are disclosed.
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WO/1999/065921A1 |
A process of synthesizing a carbapenem compound of formula (6) is disclosed, wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R?1¿ is independently selected from: H, halo, OH, OP wherein...
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WO/1999/064051A1 |
Novel multibinding compounds are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of inhibiting bacterial Type II DNA topoisomerase, thereby modulating the biol...
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WO/1999/063940A2 |
Disclosed are multibinding compounds which inhibit H?+¿/K?+¿-ATPase, an enzyme which is involved in the control of acid secretion in the stomach. The multibinding compounds of this invention containing from 2 to 10 ligands covalently a...
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WO/1999/064037A1 |
Novel multi-binding compounds are disclosed that modulate enzymatic processes. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to an enzyme, enzyme substrate o...
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WO/1999/062878A1 |
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6-membered carbocyclic ring. The compound is further substituted with various substituent groups including at least ...
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WO/1999/062907A1 |
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least ...
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WO/1999/062906A1 |
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleous is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least...
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WO/1999/058536A1 |
Novel $g(b)-lactam compounds represented by general formula (1), wherein R?1¿ represents lower alkyl or hydroxylated lower alkyl; R?2¿ represents H or lower alkyl; X represents O or S; R?3¿ represents H, a metal or a protective group;...
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WO/1999/057121A1 |
Carbapenem compounds represented by general formula (I) wherein R?1¿ represents a modifying group hydrolyzable $i(in vivo); R?2¿ and R?3¿ may be the same or different and each represents lower alkyl; and R represents a group represent...
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WO/1999/052908A1 |
An efficient method for the synthesis of a compound of formula (2) is disclosed which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.
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WO/1999/045010A1 |
A process for the direct crystallization of a compound of formula (I) or a pharmaceutically acceptable salt thereof, is disclosed, wherein R?1¿ and R?2¿ represent H, C¿1-10? alkyl, aryl or heteroaryl, or substituted C¿1-10? alkyl, ar...
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WO/1999/031106A1 |
Compounds represented by general formula (I); a process for producing the same; and utilization thereof as antimicrobial agents and metallo-$g(b)-lactamase inhibitors, wherein R?1¿ represents hydrogen or lower alkyl; R?2¿ represents hy...
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WO/1999/020269A1 |
Carbapenems substituted with a naphthosultam at position 2 and linked through a CH¿2? group are disclosed. Pharmaceutical compositions and methods of treatment are also included. The naphtosultam is substituted with at least one cationi...
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WO/1999/020628A1 |
Compounds of formula (I) are disclosed as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B. The carbapenems of the inventio...
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WO/1999/020627A1 |
Compounds of formula (I) are disclosed as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B. The carbapenems of the inventio...
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WO/1999/020270A1 |
The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least ...
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WO/1999/018954A1 |
Compounds of formula (I), as well as pharmaceutically acceptable salts thereof are disclosed. R?2¿ is H and R?3¿ is C¿1-3? alkyl, or R?2¿ and R?3¿ taken in combination represent C¿1-3? alkylidene. Pharmaceutical compositions and me...
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WO/1999/018078A1 |
A process of synthesizing a carbapenem compound of formula (6), is disclosed using a compound of formula (4'). The intermediate compounds that are described herein are also included in the present invention.
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WO/1999/018107A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a -Z-CH¿2? group. The naphthosultam is further substituted with variou...
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WO/1999/014218A1 |
The present invention relates to carbapenem derivatives represented by formula (I) and a preparation method thereof. The preparation method comprises first preparing the carbapenem intermediate represented by formula (VII) by reacting th...
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WO/1999/014217A1 |
The present invention relates to carbapenem antibacterial agents of formula (I), as well as salts and hydrates thereof. Pharmaceutical compositions and methods of treatment are also included.
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WO/1999/012928A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH¿2?-O- group. The compounds of the invention are repres...
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WO/1999/010348A1 |
Novel crystalline carbapenem intermediate compounds of formula (I) wherein R¿1? represents CH¿3? or H; and P and P' independently represent H or a protecting group; and efficient process for synthesis thereof.
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WO/1999/009032A1 |
The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH¿2? group. The napththosultam is further substituted with various ...
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