L-Threonine derivatives of high therapeutic index
AssigneeSignature R&D Holdings, LLC
InventorV. Ravi Chandran
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Abstract
The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
Claims8
A L-Threonine ester of a drug wherein the drug is Abacavir, Acarbose, Acetylsalicyclic acid, Acebutolol, Adefovir, Albuterol, Amphotericin B, Amprenavir, Atenolol, Atorvastatin, Atropine, Baclofen, Benazeprilat, Betaxolol, Bicalutamide, Biotin, Biperiden, Bisoprolol, Bitolterol, Buprenorphine, Butorphanol, Captopril, Carbidopa, Carnitine, Carteolol, Carvedilol, Cefditoren, Cerivastatin, Chloramphenicol, Clopidogrel Acid, Clorazepic Acid, Cyclosporine, Cytarabine, Danazol, Dextroamphetamine, Didanosine, Digoxin, Divalproex, Docetaxel, Dyphylline, Enalaprilat, Ephedrine, Eplerenone, Eprosartan, Esmolol, Estramustine, Ethambutol, Ethchlorvynol, Etoposide, Ezetimibe, Fenofibrate, Fenoprofen, Fexofenadine, Fluticasone, Fluvastatin, Folic Acid, Fosinoprilat, Fulvestrant, Gabapentin, Ganciclovir, Goserelin, Hydroxychloroquine, Hydroxyzine, Hyoscyamine, Ibuprofen, Ibutilide, Indinavir, Ipratropium, Irinotecan, Isosorbide, Ketoprofen, Ketorolac, Labetalol, Lamivudine, Lansoprazole, Latanoprost Acid, Leuprolide, Levobunolol, Levodopa, Levorphanol, Liothyronine, Lisinopril, Lopinavir, Lovastatin, Medroxyprogesterone, Mefloquine, Megestrol, Metaproterenol, Methohexital, Methotrexate, Methylphenidate, Methylprednisolone, Metoprolol, Miglitol, Moexiprilat, Mometasone, Montelukast, Nadolol, Nalbuphine, Naproxen, Nateglinide, Nelfinavir, Niacin, Norgestimate, Octreotide, Ofloxacin, Olmesartan, Paclitaxel, Pantothenic Acid, Penbutolol, Penicillamine, Pentazocine, Perindoprilat, Phenylephrine, Phenylpropanolamine, Pimecrolimus, Pindolol, Pirbuterol, Pravastatin, Propafenone, Propranolol, Pseudoephedrine, Quinaprilat, Quinidine, Quinine, Ramiprilat, Repaglinide, Ribavirin, Ritonavir, Rosuvastatin, Salmeterol, Simavastatin, Sirolimus, Sotalol, Tacrolimus, Tazorotene, Telmesartan, Tenofovir, Terbutaline, Thyroxine, Tiagabine, Timolol, Tirofiban, Tramadol, Trandolaprilat, Treprostinil, Triamcinolone, Troglitazone, Unoprostone, Valproic acid, Valsartan, Venlafaxine, Vidarabine, Warfarin, Zalcitabine, or Zidovudine.
A method of facilitating the separation of a racemic mixture of a drug containing a carboxy or hydroxyl group into its separate stereoisomers which comprises reacting said drug with L-Threonine or acylating derivative thereof under conditions effective to form an ester linkage between said drug and L-Threonine or acylating derivative and separating the stereoisomer thus formed, said drug being Abacavir, Acarbose, Acebutolol, Albuterol, Amphotericin B, Amprenavir, Atenolol, Atorvastatin, Atropine, Baclofen, Benazeprilat, Betaxolol, Bicalutamide, Biotin, Biperiden, Bisoprolol, Bitolterol, Buprenorphine, Butorphanol, Captopril, Carbidopa, Carnitine, Carteolol, Carvedilol, Cefditoren, Cerivastatin, Chloramphenicol, Clopidogrel Acid, Clorazepic Acid, Cyclosporine, Cytarabine, Danazol, Dextroamphetamine, Didanosine, Digoxin, Divalproex, Docetaxel, Dyphylline, Enalaprilat, Ephedrine, Eplerenone, Eprosartan, Esmolol, Estramustine, Ethambutol, Ethchlorvynol, Etoposide, Ezetimibe, Fenoprofen, Fexofenadine, Fluticasone, Fluvastatin, Folic Acid, Fosinoprilat, Fulvestrant, Gabapentin, Goserelin, Hydroxychloroquine, Hydroxyzine, Hyoscyamine, Ibuprofen, Ibutilide, Indinavir, Ipratropium, Irinotecan, Isosorbide, Ketoprofen, Ketorolac, Labetalol, Lamivudine, Latanoprost Acid, Leuprolide, Levobunolol, Levodopa, Levorphanol, Liothyronine, Lisinopril, Lopinavir, Lovastatin, Medroxyprogesterone, Mefloquine, Megestrol, Metaproterenol, Methohexital, Methotrexate, Methylphenidate, Methylprednisolone, Metoprolol, Miglitol, Moexiprilat, Mometasone, Montelukast, Nadolol, Nalbuphine, Naproxen, Nateglinide, Nelfinavir, Norgestimate, Octreotide, Ofloxacin, Paclitaxel, Pantothenic Acid, Penbutolol, Penicillamine, Pentazocine, Perindoprilat, Phenylephrine, Phenylpropanolamine, Pimecrolimus, Pindolol, Pirbuterol, Pravastatin, Propafenone, Propranolol, Pseudoephedrine, Quinaprilat, Quinidine, Quinine, Ramiprilat, Repaglinide, Ribavirin, Ritonavir, Rosuvastatin, Salmeterol, Simavastatin, Sirolimus, Sotalol, Tacrolimus, Telmesartan, Tenofovir, Terbutaline, Thyroxine, Tiagabine, Timolol, Tirofiban, Tramadol, Trandolaprilat, Treprostinil, Triamcinolone, Troglitazone, Unoprostone, Valsartan, Venlafaxine, Vidarabine, Warfarin, Zalcitabine, or Zidovudine.
Dependencies are inferred from the claim text.