US2006281821A1PendingUtilityA1

Retinoid replacements and opsin agonists and methods for the use thereof

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Assignee: PALCZEWSKI KRZYSZTOFPriority: Mar 14, 2003Filed: Mar 15, 2004Published: Dec 14, 2006
Est. expiryMar 14, 2023(expired)· nominal 20-yr term from priority
Inventors:Krzysztof PalczewskiDavid Saperstein
A61K 31/435A61K 9/0048A61K 31/07A61K 31/11A61P 27/02A61K 31/695A61P 27/10A61K 31/382A61K 38/1709
65
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Claims

Abstract

Compositions of and methods for using synthetic retinoids as retinoid replacements and opsin agonists are provided.

Claims

exact text as granted — not AI-modified
1 . A method of restoring photoreceptor function in a vertebrate eye, comprising administering to the vertebrate having an endogenous deficiency an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms a functional opsin/synthetic retinoid complex.  
     
     
         2 . The method of  claim 1 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         3 . The method of  claim 1 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         4 . The method of  claim 1 , wherein the endogenous retinoid deficiency is associated with Age-Related Macular Degeneration, Leber Congenital Amaurosis, Retinitis Punctata Albesciens, Congenital Stationary Night Blindness or Fundus Albipunctatus.  
     
     
         5 . The method of  claim 1 , wherein the synthetic retinoid is locally administered to the eye.  
     
     
         6 . The method of  claim 5 , wherein the synthetic retinoid is locally administered by eye drops, intraocular injection or periocular injection.  
     
     
         7 . The method of  claim 1 , wherein the synthetic retinoid is orally administered to the vertebrate.  
     
     
         8 . A method of sparing the requirement for endogenous retinoid in a vertebrate eye, comprising: 
 administering to the eye a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms a functional opsin/synthetic retinoid complex.    
     
     
         9 . The method of  claim 8 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         10 . The method of  claim 8 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         11 . The method of  claim 8 , wherein the endogenous retinoid is 11-cis-retinal.  
     
     
         12 . A method of ameliorating loss of photoreceptor function in a vertebrate eye, comprising: 
 prophylactically administering an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle to the vertebrate eye, wherein the synthetic binds to opsin protein to form a functional opsin/synthetic retinoid complex.    
     
     
         13 . The method of  claim 12 , wherein the synthetic retinoid is orally administered to a vertebrate comprising the eye.  
     
     
         14 . The method of  claim 12 , wherein the synthetic retinoid is locally administered to the vertebrate eye.  
     
     
         15 . The method of  claim 12 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         16 . The method of  claim 12 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         17 . A method of selecting a treatment for a subject having diminished visual capacity, comprising: 
 determining whether the subject has a deficient endogenous retinoid level, as compared with a standard subject; and    administering to the subject an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the subject's eye.    
     
     
         18 . The method of  claim 17 , wherein the subject has Leber Congenital Amaurosis, Retinitis Punctata Albesciens, Congenital Stationary Night Blindness, Fundus Albipunctatus or Age-Related Macular Degeneration.  
     
     
         19 . The method of  claim 17 , wherein the endogenous retinoid is 11-cis-retinal.  
     
     
         20 . The method of  claim 17 , wherein the synthetic retinoid is orally administered to a vertebrate comprising the eye.  
     
     
         21 . The method of  claim 17 , wherein the synthetic retinoid is locally administered to the vertebrate eye.  
     
     
         22 . The method of  claim 17 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         23 . The method of  claim 17 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         24 . An ophthalmologic composition comprising a synthetic retinoid in a pharmaceutically acceptable vehicle.  
     
     
         25 . The composition of  claim 24 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         26 . The composition of  claim 24 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         27 . The composition of  claim 24 , wherein the ophthalmologic composition comprises eye drops, an intraocular injectable solution or a periocular injectable solution.  
     
     
         28 . An oral dosage form comprising an opsin-binding synthetic retinoid in a pharmaceutically acceptable vehicle.  
     
     
         29 . The composition of  claim 28 , wherein the opsin-binding synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         30 . The composition of  claim 28 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         31 . A method of treating Leber Congenital Amaurosis in a vertebrate subject, comprising: 
 administering to the subject an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms a functional opsin/synthetic retinoid complex.    
     
     
         32 . The method of  claim 31 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         33 . The method of  claim 31 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         34 . The method of  claim 31 , wherein the synthetic retinoid is locally administered to the eye.  
     
     
         35 . The method of  claim 34 , wherein the synthetic retinoid is locally administered by eye drops, intraocular injection or periocular injection.  
     
     
         36 . The method of  claim 31 , wherein the synthetic retinoid is orally administered to the subject.  
     
     
         37 . A method of treating Retinitis Punctata Albesciens, Congenital Stationary Night Blindness or Fundus Albipunctatus in a vertebrate subject, comprising: 
 administering to the subject an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms a functional opsin/synthetic retinoid complex.    
     
     
         38 . The method of  claim 37 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         39 . The method of  claim 37 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         40 . The method of  claim 37 , wherein the synthetic retinoid is locally administered to the eye.  
     
     
         41 . The method of  claim 40 , wherein the synthetic retinoid is locally administered by eye drops, intraocular injection or periocular injection.  
     
     
         42 . The method of  claim 37 , wherein the synthetic retinoid is orally administered to the subject.  
     
     
         43 . A method of treating Age-Related Macular Degeneration in a vertebrate subject, comprising: 
 administering to the subject an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms an opsin/synthetic retinoid complex.    
     
     
         44 . The method of  claim 43 , wherein the synthetic retinoid binds to free opsin in the eye.  
     
     
         45 . The method of  claim 43 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         46 . The method of  claim 43 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         47 . The method of  claim 43 , wherein the synthetic retinoid is locally administered to the eye.  
     
     
         48 . The method of  claim 47 , wherein the synthetic retinoid is locally administered by eye drops, intraocular injection or periocular injection.  
     
     
         49 . The method of  claim 43 , wherein the synthetic retinoid is orally administered to the subject.  
     
     
         50 . A method of treating or preventing loss of night vision or contrast sensitivity in an aging vertebrate subject, comprising: 
 administering to the subject an effective amount of a synthetic retinoid in a pharmaceutically acceptable vehicle, wherein the synthetic retinoid binds to opsin in the vertebrate eye and forms an opsin/synthetic retinoid complex.    
     
     
         51 . The method of  claim 50 , wherein the synthetic retinoid binds to free opsin in the eye.  
     
     
         52 . The method of  claim 50 , wherein the synthetic retinoid comprises a synthetic retinoid of formula I, II, III, IV, V, VI, VII, VIII, IX, X, XI, XII or XIII.  
     
     
         53 . The method of  claim 50 , wherein the synthetic retinoid is 9-cis-retinal.  
     
     
         54 . The method of  claim 50 , wherein the synthetic retinoid is locally administered to the eye.  
     
     
         55 . The method of  claim 54 , wherein the synthetic retinoid is locally administered by eye drops, intraocular injection or periocular injection.  
     
     
         56 . The method of  claim 50 , wherein the synthetic retinoid is orally administered to the subject.  
     
     
         57 . The method of  claim 50 , wherein the synthetic retinoid is administered prophylactically to the subject.  
     
     
         58 . The method of  claim 50 , wherein the subject is a human.

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