Abstract: Described are new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and Form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.

Abstract: The present invention pertains, at least in part, to novel substituted etracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

Abstract: Topical minocycline compositions with reduced fluorescence are provided. In some instances, the compositions include an amount of a minocycline active agent associated with porous calcium particles. Also provided are methods of using the compositions, e.g., in the treatment of acne.

Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.

Abstract: Provided are a Tigecycline crystalline hydrate, and a preparation method therefor and use thereof. The crystalline hydrate has high stability for storage, and is used for the manufacture of a medicament for treating or preventing the infection of respiratory system, hepatobiliary system, facial features, urogenital system, bone and joint, skin and soft tissue and endocarditis, septicemia, meningitis caused by susceptible strains of Gram-positive or Gram-negative bacteria, anaerobic bacteria, chlamydia, and mycoplasma in human or animal.

Abstract: Methods for the synthesis and purification of 9-amino alkyl tetracycline compounds are described.

Abstract: Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.

Abstract: The invention in one embodiment is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to a composition comprising the compound of formula I or a pharmaceutically acceptable salt, and methods of treating the indications listed herein.

Abstract: The present invention relates to crystalline form C of Tigecycline dihydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline form C of Tigecycline dihydrochloride as an intermediate for the preparation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form C of Tigecycline dihydrochloride in an effective amount and to the use of crystalline form C of Tigecycline dihydrochloride as an anti-infective medicament.

Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.

Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

Abstract: 11a,12-dehydrotetracycline compounds are described.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Crystalline solid forms of tigecycline, Form I, Form II, Form III, Form IV, and Form V, compositions comprising these crystalline solid forms, and processes for preparing these crystalline solid forms are described herein.

Abstract: The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II and Form III, of minocycline base are provided. These are characterised by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallisation from the mixture.

Abstract: The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant activity in tetracycline responsive states. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the invention, a substituted tetracycline compound may be prepared by combining a reactive tetracycline-based precursor compound such as an arene tetracycline diazonium salt, and a reactive organic substituent precursor, e.g., alkenes, substituted alkenes, vinyl monomers, aromatics and heteroaromatics, in the presence of a transition metal catalyst, such as palladium chloride, under conditions such that a tetracycline compound substituted with the organic substituent is formed.

Abstract: Cancer stem cells exhibit different metabolic profiles from other cancer cells, such that they do not readily respond to treatment using conventional chemotherapeutic agents. Studies disclosed herein now demonstrate that the glycylcycline antibiotic tigecycline (a tetracycline derivative) exhibits anti-cancer activity, including activity against cancer stem cells. This anti-neoplastic activity appears to be due to inhibition of mitochondrial protein synthesis in the cancer cells. In preferred embodiments, the cancer to be treated is a hematological cancer, such as leukemia, lymphoma or myeloma.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.

Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention relates to a process for the reaction of a compound with hydrogen wherein the reaction is conducted using a hydrogen-containing gas comprising up to about 10 vol. % hydrogen and at least about 90 vol. % of an inert gas and wherein the compound to be reacted with hydrogen is provided in a liquid phase. The process of the present invention is particularly suitable for hydrogenation and hydrogenolysis reactions.

Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form II and Form III, of minocycline base are provided. These are characterized by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallization from the mixture.

Abstract: The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament.

Abstract: The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

Abstract: Described herein are compounds (including medical foods, pharmaceutical compositions, methods of compounding them), methods and systems for the diagnosis and/or treatment of prodromal schizophrenia. For example, described herein are methods of treating a developmentally-based neuropsychiatric disorder (schizophrenia) that includes first determining if a subject is at risk for such a disorder by examining phenotypical, serological immune markers and genotypical biomarkers. The biomarkers may be used to tailor the dose to be delivered by the medial food or pharmaceutical composition. Also described are compounds for treating prodromal (rather than full-blown) schizophrenia.

Abstract: The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.

Abstract: The present invention provides processes for the preparation of crystalline forms of Tigecycline.

Abstract: The present invention provides crystalline forms of Tigecycline, and methods of for preparation of crystalline forms and amorphous.

Abstract: Efficient method for preparing the enone intermediate (VII) used in the synthesis of tetracyclines derivatives. In particular, the invention provides a synthesis which allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

Abstract: 11a,12-dehydrotetracycline compounds are described.

Abstract: The present invention provides a process for isolating tigecycline which process comprises the step of spray drying a solution of tigecycline in a solvent. Preferably the solvent is water or an organic solvent. In another aspect, there is provided tigecycline obtainable by spray drying, particularly in amorphous form. In particular, the invention provides tigecycline obtainable by spray drying according to the process of the invention.

Abstract: The present invention relates to crystalline form C of Tigecycline dihydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline form C of Tigecycline dihydrochloride as an intermediate for the preparation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form C of Tigecycline dihydrochloride in an effective amount and to the use of crystalline form C of Tigecycline dihydrochloride as an anti-infective medicament.

Abstract: A compound of formula (I):

Abstract: The present invention relates to substituted tetracycline compounds and related methods for increasing the antifungal activity of an antifungal agent. The methods include administering to a subject an effective amount of a substituted tetracycline compound in combination with an antifungal agent such that the subject is treated for the fungal associated disorder.

Abstract: The present invention relates to the new crystalline solid form XI of Tigecycline and a process of preparing the same. Form XI of Tigecycline is particularly suitable for the isolation of Tigecycline in the last step of the synthesis of Tigecycline. Further the present invention relates to a process of preparing amorphous Tigecycline by spray drying form XI or another crystalline form of Tigecycline.

Abstract: The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.

Abstract: The present invention relates to crystalline forms A and B of Tigecycline hydrochloride and to methods for the preparation of the same. Furthermore the present invention relates to the use of crystalline forms A and B of Tigecycline hydrochloride as intermediates for the formulation of an anti-infective medicament. Moreover the present invention relates to pharmaceutical compositions comprising crystalline form A of Tigecycline hydrochloride in an effective amount and to the use of crystalline form A of Tigecycline hydrochloride as anti-infective medicament.

Abstract: Methods and compositions for treating Cryptosporidium parvum related disorders in a mammal are discussed. Several novel tetracycline compounds useful for treating Cryptosporidium parvum related disorders are also included.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Dendrimer-based compositions and methods are provided, that are useful for administering pharmaceutical compositions to target cells and tissues for treatment of ocular diseases including macular degeneration, diabetic retinopathy, and retinitis pigmentosa.

Abstract: The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.

Abstract: Substituted tetracycline compounds, methods of synthesis, and methods of use are discussed. Tetracyclines useful for treating tetracycline related disorders are also discussed. Intermediates useful for synthesizing other tetracycline compounds are also included.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.

Abstract: The present invention pertains to novel 3, 10, and/or 12a-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: The present invention relates to the novel crystalline form X of Tigecycline and to processes of preparing the same. Furthermore the present invention relates to the use of crystalline form X of Tigecycline as an intermediate for the preparation of an anti-infective medicament.