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Dopamine D1 receptor agonist compounds (Fri, 19 Dec 2003)
Patent 513552 2,3,4,5-tetrahydro-1H-3-benzazepines of formula (I) that are useful as therapeutic agents that selectively interact positively with postsynaptic dopamine D1 receptors in the striatum, directly or in-directly (termed dopamine D1 agonists) and are particularly valuable as anti-Parkinsonian agents are disclosed, wherein: R1 is hydrogen, halogen, C1-C4 alkyl, or CF3; R2 is hydrogen, methyl, or lower alkenyl of 3-5 carbon atoms; R3 and R4 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring; and R5 is hydrogen or R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R3 is hydrogen; R6 is hydrogen, halogen, CF3, CN, NO2 or NH2; R7 is hydrogen, halogen, CF3, CN, NO2 or NH2. The specific combination of substituents: R1 = H, R2 = H and R4 and R5 together forming a cyclohexane ring is excluded, namely 1-(5,6,7,8-tetrahydronaphthalen-2-yl)-2,3,4,5-tetrahydro-1H-benzol[d]azepine-7,8-diol...
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PROCESSES FOR THE DIASTEREOSELECTIVE SYNTHESIS OF NUCLEOSIDES (Wed, 27 Apr 1994)
This process for the preparation of optically active cis-nucleosides and analogues and derivatives thereof of formula (I): wherein R1 is hydrogen or acyl; R2 is a desired purine or pyrimidene base or an analogue or derivative thereof; W is S, S=O, or SO2, O, NZ, or CH2; X is O, S=O, or SO2 , NZ, CH2, CHF, CH, CHN3, or CHOH; Y is O, S, CH2, CH, CHF, or CHOH; and Z is hydrogen, hydroxyl, alkyl or acyl; provided that W is not O, S, S=O or SO2 when Y is CH2 and X is O, S, S=O or SO2; comprises the step of glycosylating the desired purine or pyrimidine base or analogue or derivative thereof with a single enantiomer of the compound of formula (II) wherein R3 is a substituted carbonyl or carbonyl derivative; and L is a leaving group, using a Lewis acid of the formula (III): R5R6R7R8Si wherein R5, R6 and R7 are independently selected from the group consisting of hydrogen; C1-20 alkyl optionally substituted by fluoro, bromo, chloro, iodo, C1-6 alkoxy or C6-20 aryloxy; C7-20 aralkyl optionally substituted by halogen, C1-20 alkyl or C1-20 alkoxy; C6-20 aryl optionally substituted by fluoro, bromo, chloro, iodo, C1-20 alkyl or C1-20 alkoxy; trialkylsilyl; fluoro; bromo; chloro and iodo; and R8 is selected from the group consisting of fluoro; bromo; chloro; iodo; C1-20 sulphonate esters, optionally substituted by fluoro, bromo, chloro or iodo; C1-20 alkyl esters optionally substituted by fluoro, bromo, chloro or iodo; polyvalent halides; trisubstituted silyl groups of the general formula (R5)(R6)(R7)Si (wherein R5, R6, and R7 are as defined above); saturated or unsaturated selenenyl C6-20 aryl; substituted or unsubstituted C6-20 arylsulphenyl; substituted or unsubstituted C6-20 alkoxyalkyl; and trialkylsiloxy...
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PROCESSES FOR THE DIASTEREOSELECTIVE SYNTHESIS OF NUCLEOSIDES (Tue, 28 Mar 1995)
This diastereoselective process produces optically active cis-nucleosides and nucleoside analogues and derivatives of formula (I) where W is S, S=O, SO2, or O; X is S, S=O, SO2, or O; R1 is hydrogen or acyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof; the process comprising the step of glycosylating the purine or pyrimidine base with an intermediate of formula wherein R3 is a substituted carbonyl or carbonyl derivative; and L is a leaving group, using a Lewis acid of the formula SiR5R6R7R8 where R5, R6 and R7 and independently selected from C1-20 alkyl, C7-20 aralkyl, C6-20 aryl (each optionally substituted by F, Br, Cl, I, C1-6 alkoxy, or C6-20 aryloxy), H, trialkylsilyl, F, Br, Cl, and I; and R8 is selected from the group consisting of fluoro; bromo; chloro; iodo; C1-20 sulphonate esters, optionally substituted by fluoro, bromo, chloro or iodo; C1-20 alkyl esters optionally substituted by fluoro, bromo, chloro or iodo; polyvalent halides; trisubstituted silyl groups of the general formula (R5) (R6) (R7)Si (wherein R5, R6, and R7 are as defined above); saturated or unsaturated selenenyl C6-20 aryl; substituted or unsubstituted C6-20 arylsulphenyl; substituted or unsubstituted C6-20 alkoxyalkyl; and trialkylsiloxy...
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Methods of treating ophthalmic diseases using NPR-B agonists (Thu, 26 Dec 2013)
Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.
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Active agent delivery systems and methods for protecting and administering active agents (Thu, 22 Nov 2001)
A composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide (Figure 1).
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ACTIVE AGENT DELIVERY SYSTEMS COMPRISING POLYPEPTIDES FOR ORAL ADMINISTRATION (Sun, 20 Jan 2008)

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Active agent delivery systems and methods for protecting and administering active agents (Wed, 22 Jul 2009)
A composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide.
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Amphetamine Prodrugs (Thu, 13 Mar 2014)
The present invention relates to amphetamine prodrugs which provide colonic release of amphetamine.
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NPR-B agonists (Thu, 26 Dec 2013)
Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.
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Active agent delivery systems and methods for protecting and administering active agents (Thu, 31 Jul 2003)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents (Figure 1) and methods for administering conjugated active agent compositions.
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Active agent delivery systems and methods for protecting and administering active agents (Thu, 04 Jun 2009)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods or administering conjugated active agent compositions.
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Active agent delivery systems and methods for protecting and administering active agents (Thu, 04 Oct 2007)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
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Delivery system and methods for protecting and administering dextroamphetamine (Wed, 04 May 2011)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
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Active agent delivery sytems and methods for protecting and administering active agents (Wed, 29 Dec 2010)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
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Prodrugs of guanfacine (Thu, 21 Mar 2013)
Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.
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Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances (Thu, 06 Nov 2008)
The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time dependent manner (sustained release) by way of serum enzymes.
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ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS (Thu, 10 Dec 2009)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
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Delivery system and methods for protecting and administering dextroamphetamine (Wed, 04 May 2011)
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.
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CONJUGATES COMPRISING CONTROLLED SUBSTANCES COVALENTLY BOUND TO PEPTIDES OR AMINO ACIDS AND COMPOSITIONS COMPRISING SAME (Sun, 18 Dec 2005)

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Sustained release pharmaceutical compounds to prevent abuse of controlled substances (Thu, 14 Apr 2005)
The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time-dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time-dependent manner (sustained release) by way of serum enzymes.
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