Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/24
A61K-031/21
C07D-401/04
C07D-401/00
C07D-207/00
C07D-333/36
C07D-333/00
C07D-307/02
C07D-307/00
C07D-271/00
출원번호
US-0508131
(2006-08-21)
등록번호
US-7300956
(2007-11-27)
발명자
/ 주소
Gallop,Mark A.
Yao,Fenmei
Ludwikow,Maria J.
Phan,Thu
Peng,Ge
출원인 / 주소
Xenoport, Inc.
대리인 / 주소
Dorsey & Whitney LLP
인용정보
피인용 횟수 :
11인용 특허 :
38
초록▼
The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs
The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (짹)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
대표청구항▼
What is claimed is: 1. A compound of Formula (I): or pharmaceutically acceptable salts, hydrates or solvates thereof, wherein: R1 is selected from the group consisting of acyl, substituted acyl, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, subst
What is claimed is: 1. A compound of Formula (I): or pharmaceutically acceptable salts, hydrates or solvates thereof, wherein: R1 is selected from the group consisting of acyl, substituted acyl, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl and substituted heteroarylalkyl; R2 and R3 are independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkoxycarbonyl, substituted alkoxycarbonyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl and substituted heteroarylalkyl or optionally, R2 and R3 together with the carbon atom to which they are bonded form a cycloalkyl, substituted cycloalkyl, cycloheteroalkyl or substituted cycloheteroalkyl ring; R4 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, aryldialkylsilyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl or trialkylsilyl; and R5 is selected from the group consisting of substituted aryl, heteroaryl and substituted heteroaryl. 2. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable vehicle. 3. The composition of claim 2, comprising an oral dosage form. 4. The composition of claim 3, wherein the oral dosage form is a sustained release oral dosage form. 5. The composition of claim 4, wherein the dosage form is adapted to be swallowed by a patient in order to introduce the dosage form into an intestinal lumen of the patient; the dosage form further being adapted to release the compound of claim 1 gradually into the intestinal lumen of the patient over a period of hours after said swallowing, the gradual release causing the compound of claim 1 to be cleaved after said swallowing to provide a therapeutic concentration the compound of claim 1 in the plasma of the patient. 6. The composition of claim 5 wherein the period of hours comprises at least about 6 hours. 7. The composition of claim 5, wherein the period of hours comprises at least about 8 hours. 8. The composition of claim 5, wherein the period of hours comprises at least about 12 hours.
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이 특허에 인용된 특허 (38)
Alexander Jose (Lawrence KS), (Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs.
Urquhart John (Palo Alto CA) Theeuwes Felix (Los Altos CA), Delivery system comprising means for shielding a multiplicity of reservoirs in selected environment of use.
Ayer Atul D. (Palo Alto CA) Swanson David R. (Palo Alto CA) Kuczynski Anthony L. (Palo Alto CA), Dosage form for treating cardiovascular diseases comprising isradipine.
Grosswald Ralph R. (Fairfield IA) Anderson Jeffory B. (Springville UT) Andrew Clair S. (Provo UT), Method for the manufacture of pharmaceutical cellulose capsules.
Nabil Farah FR; Philippe Barthelemy FR; Joseph Joachim FR, Process for the manufacture of pharmaceutical composition with modified release of active principle comprising the matrix.
Wildervanck Alexander Franciscus,ZAX ; Caira Mino Rodolfo,ZAX ; Scott Janet Lesley,ZAX ; Nassimbeni Liugi Renzo,ZAX ; Clauss Rainer,ZAX ; Easter Barratt Robert Dixon,ZAX, Process for the optical resolution of 3-(p-chlorophenyl)-glutaramide.
Kreutner William (West Caldwell NJ) Bolser Donald (Bedminster NJ) Chapman Richard (Somerville NJ) Aziz Sultan (Woodcliff Lake NJ), Use of GABA-B selective agonists as anti-tussive agents.
Yao, Fenmei; Gallop, Mark A.; Barrett, Ronald W.; Virsik, Peter A., Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use.
Yao, Fenmei; Gallop, Mark A.; Barrett, Ronald W.; Virsik, Peter A., Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use.
Gallop, Mark A.; Yao, Fenmei; Ludwikow, Maria J.; Peng, Ge; Raillard, Stephen P., Enantiomerically resolving acyloxyalkyl thiocarbonates used in synthesizing acyloxyalkyl carbamate prodrugs.
Yao, Fenmei; Gallop, Mark A.; Barrett, Ronald W.; Virsik, Peter A., Mesophasic forms of (3S)-aminomethyl-5-methyl-hexanoic acid prodrugs and methods of use.
Edgren, David E.; Kidney, David J.; Pargaonkar, Nikhil; Kim, Derrick K.; Yoder, Gorm; Karaborni, Sarni, Sustained release oral dosage forms of an R-baclofen prodrug.
Wun, Aetna W.; Wustrow, David J., Use of (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl) butanoic acid for treating urinary incontinence.
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