Class 540/456 - Two of the cyclos share at least three ring members or a ring member is shared by three of the cyclos (e.g., bridged, peri-fused, etc.)

Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein (a) at least three members of one cyclo
No. of patents: 372
Last issue date: 05/08/2012

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Number	Title	Issue Date
8173801	Processes for the production of polymorphic forms of rifaximin Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means...	05/08/2012
8158781	Polymorphic forms α, β and γ of rifaximin Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means...	04/17/2012
8129521	One pot synthesis of tetrazole derivatives of rapamycin A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled...	03/06/2012
8058426	Phosphorus-containing compounds and uses thereof This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, �...	11/15/2011
8034926	Methods of manufacturing crystalline forms of rapamycin analogs A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic med...	10/11/2011
7923553	Processes for the production of polymorphic forms of rifaximin Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means...	04/12/2011
7872122	Process for making Biolimus A9 A process for making Biolimus A9 comprises reacting sirolimus (or rapamycin) with alkyl benzene sulfonate under the catalyzing of organic base and in the presence of organic solvent to undergo a nucleophilic substitution reaction to obtain the Biolimus A9 with high ...	01/18/2011
7851620	Methods for preparing diazonamides This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further eluci...	12/14/2010
7820812	Methods of manufacturing crystalline forms of rapamycin analogs A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic med...	10/26/2010
7812155	Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chroma...	10/12/2010
7709634	Amorphous form of rifaximin and processes for its preparation A stable amorphous form of rifaximin is disclosed. This form is chemically and polymorphically stable on storage and can be prepared by dissolving rifaximin in a solvent to form a solution, which is precipitated by adding an anti-solvent and isolating of the precipi...	05/04/2010
7678901	Rapamycin analogs containing an antioxidant moiety A rapamycin analog with an antioxidant moiety or a pharmaceutically acceptable salt or prodrug thereof, is an immunomodulatory agent and is useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenos...	03/16/2010
7645876	Processes for producing crystalline macrolides The present invention provides processes for crystallization of macrolides, specifically pimecrolimus and tacrolimus. ...	01/12/2010
7622578	Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate A scalable process for the preparation of a rapamycin 42-ester by reacting a rapamycin 42-ester boronate with a diol and purifying crude rapamycin 42-ester by recrystallization and treatment with a diol is provided. Also provided is a method for isolating and purify...	11/24/2009
7612199	Polymorphic forms α, β, and γ of rifaximin Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means...	11/03/2009
7605257	Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the ...	10/20/2009
7605258	Processes for the synthesis of individual isomers of mono-peg CCI-779 Processes for preparing individual diastereomers of mono-pegylated rapamycin 42 ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) are provided. ...	10/20/2009
7598375	Method of acylating maytansinol with chiral amino acids This invention provides a method for making maytansinoids having a chiral amino acid side chain, such as DM1 and DM4 that are used to treat cancer. According to this method, the side chain may be added with little epimerization of the amino acid chiral center. ...	10/06/2009
7514554	Heteroatoms-containing tricyclic compounds A process for the production of 33-Epi-33-chloro-FR 520 in one step from FR520 wherein protecting groups are avoided. ...	04/07/2009
7442707	CCI-779 polymorph and use thereof The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 polymorph Form II and pharmaceutical compositions including CCI-779 polymorph Form II. ...	10/28/2008
7439252	Ascomycin crystalline forms and preparation thereof The present invention provides novel crystalline forms of ascomycin as well as processes for the preparation thereof and pharmaceutical compositions comprising such crystalline forms of ascomycin. ...	10/21/2008
7432277	Phosphorus-containing macrocycles This invention concerns a new family of phosphorus-containing macrocycles containing various phosphonate- and phosphonate-containing moieties. ...	10/07/2008
7411063	Process for preparation of maytansinol The present invention describes the preparation of maytansinol by methods that minimize processing steps, and reduce solvent volumes, making the process more efficient, and scaleable. This process comprises a step of converting bridged acetals of maytansinol to mayt...	08/12/2008
7393952	Solvent free amorphous rapamycin An improved process for coating implantable medical devices utilizes a number of techniques for improving the stability of therapeutic agents contained within the coating. The stability of the therapeutic agents may be improved by creating substantially solvent-free...	07/01/2008
7390895	Production of polyketides and other natural products The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these...	06/24/2008
7384953	Purification of rapamycin Purified rapamycin and a chemical process for obtaining the purified rapamycin are described. ...	06/10/2008
7375218	Process for preparing macrocyclic HCV protease inhibitors Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: ...	05/20/2008
7375217	Analogs of benzoquinone-containing ansamycins and methods of use thereof The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where...	05/20/2008
7371853	Macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme in involved, ...	05/13/2008
7361647	Analogs of benzoquinone-containing ansamycins and methods of use thereof The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where...	04/22/2008
7345053	Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use The invention describes novel nitrosated and/or nitrosylated rapamycin compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated rapamycin compound, and, optionally, at least one nitric oxide donor compound. The invention also provides...	03/18/2008
7345069	Oxidative activation and episulfonium ion-mediated DNA alkylation-based anticancer The present invention relates to TG-25 and/or analogs thereof and their use of TG-25 in the treatment of cancer. TG-25 inhibits the growth of prostate cells by inhibiting DNA synthesis, more particularly by DNA cleavage. ...	03/18/2008
7338974	Macrocyclic diaminopropanes as beta-secretase inhibitors There is provided a series of novel macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5, n, L, Z, a...	03/04/2008
7332601	CCI-779 derivatives and methods of making same A method of generating synthetic metabolites of CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples. ...	02/19/2008
7320974	Cytoskeletal active compounds, compositions and use The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable...	01/22/2008
7312200	9-ketospinosyn derivatives The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ═N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests. ...	12/25/2007
7303768	Preparation of aqueous clear solution dosage forms with bile acids Compositions for pharmaceutical and other uses comprising clear aqueous solutions of bile acids which do not form any detectable precipitates over selected ranges of pH values of the aqueous solution and methods of making such solutions. The compositions of the inve...	12/04/2007
7300662	Drug/drug delivery systems for the prevention and treatment of vascular disease A drug and drug delivery system may be utilized in the treatment of vascular disease. A local delivery system is coated with rapamycin or other suitable drug, agent or compound and delivered intraluminally for the treatment and prevention of neointimal hyperplasia f...	11/27/2007
7301019	Method for the preparation of maytansinoid esters Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytans...	11/27/2007
7300942	Production of polyketides and other natural products The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these...	11/27/2007

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Class 540/456 - Two of the cyclos share at least three ring members or a ring member is shared by three of the cyclos (e.g., bridged, peri-fused, etc.)