| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 101 | Process for obtaining compounds derived from tetrahydro-β-carboline | US13984458 | 2012-02-10 | US08829023B2 | 2014-09-09 | Xavier Berzosa Rodríguez; Francisco Marquillas Olondriz |
| The invention relates to a process for obtaining compounds derived from tetrahydro-β-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine. | ||||||
| 102 | Combination antineoplastic therapy | US13319604 | 2010-05-04 | US08716307B2 | 2014-05-06 | Ravi Kumar Amaravadi; Craig B. Thompson |
| The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described. | ||||||
| 103 | Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder | US13444151 | 2012-04-11 | US08716278B1 | 2014-05-06 | Clifford Riley King; Stephen G. D'Ambrosio; David W. Bristol |
| A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic. | ||||||
| 104 | Enediyne compounds, conjugates thereof, and uses and methods therefor | US13764226 | 2013-02-11 | US08709431B2 | 2014-04-29 | Naidu S. Chowdari; Sanjeev Gangwar; Bilal Sufi |
| Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer. | ||||||
| 105 | Synthesis of 4H-benzo[D]pyrrolo[1,2-A]thiazoles and indolizino[6,7-b]indole derivatives and their use as antitumor therapeutic agents | US13549572 | 2012-07-16 | US08703951B2 | 2014-04-22 | Tsann-Long Su; Ting-Chao Chou; Te-Chang Lee |
| The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications. | ||||||
| 106 | Tandem process for preparing N-alkyl morphinans | US13196921 | 2011-08-03 | US08703949B2 | 2014-04-22 | Subo Liao; Peter X. Wang; David W. Berberich; Douglas C. Miller |
| The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis/alkylation reactions for the synthesis of N-alkyl morphinans. | ||||||
| 107 | Method for the enrichment of buprenorphine using chromatographic techniques | US12818230 | 2010-06-18 | US08492547B2 | 2013-07-23 | Enrico A. Antonini |
| The present invention provides processes for the enrichment of buprenorphine in a product. In particular, the present invention provides processes for the enrichment of buprenorphine in a product using chromatographic techniques. | ||||||
| 108 | Process for preparing 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine | US11794584 | 2005-12-18 | US08436176B2 | 2013-05-07 | Hughes Martin; David Ach; Clement Toussaint; Fabrice Dubois |
| The invention provides various processes for preparing 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine. | ||||||
| 109 | Hsp90, buffering and drug resistance | US11175515 | 2005-07-05 | US08343913B1 | 2013-01-01 | Leah Cowen; Susan L. Lindquist |
| A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used. | ||||||
| 110 | Noribogaine in the treatment of pain and drug addiction | US12796249 | 2010-06-08 | US08178524B2 | 2012-05-15 | Deborah C. Mash |
| The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone. | ||||||
| 111 | Substituted diazepine sulfonamides as bombesin receptor subtype-3 modulators | US12517836 | 2007-12-07 | US08153626B2 | 2012-04-10 | Robert K. Baker; Linda L. Chang; Marc Chioda; Harry R. Chobanian; Ying-Duo Gao; Yan Guo; Linus S. Lin; Ping Liu; Ravi P. Nargund; Kathleen M. Rupprecht; Shouwu Miao |
| Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes. | ||||||
| 112 | Compounds | US12469767 | 2009-05-21 | US08097628B2 | 2012-01-17 | Carlos Alemparte-Gallardo; Christopher Barfoot; David Barros-Aguirre; Monica Cacho-Izquierdo; Jose Maria Fiandor Roman; Alan Joseph Hennessy; Neil David Pearson; Modesto Jesus Remuinan-Blanco |
| Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described. | ||||||
| 113 | Fungicide N-cycloalkyl-benzyl-amide derivatives | US12223105 | 2006-11-15 | US08088927B2 | 2012-01-03 | Darren Mansfield; Pierre-Yves Coqueron; Philippe Desbordes; Alain Villier; Marie-Claire Grosjean-Cournoyer; Stéphanie Gary; Stéphane Carbonne; Ralf Dunkel; Arounarith Tuch; Jean-Pierre Vors |
| The present invention relates to N-cycloalkyl-benzyl-amide derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: | ||||||
| 114 | Pharmaceutical formulations comprising an immune response modifier | US12172712 | 2008-07-14 | US07968562B2 | 2011-06-28 | Raymond D. Skwierczynski; Terri F. Busch; Amy L. Gust-Heiting; Mary Fretland; Matthew T. Scholz |
| Pharmaceutical formulations comprising an immune response modifier (IRM) chosen from imidazoquinoline amines, imidazotetrahydroquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, thiazolo-quinolineamines, oxazolo-quinolinamines, thiazolo-pyridinamines, oxazolo-pyridinamines, imidazonaphthyridine amines, tetrahydroimidazonaphthyridine amines, and thiazolonaphthyridine amines; a fatty acid; and a hydrophobic, aprotic component miscible with the fatty acid are useful for the treatment of dermal associated conditions. Novel topical formulations are provided. In one embodiment, the topical formulations are advantageous for treatment of actinic keratosis, postsurgical scars, basal cell carcinoma, atopic dermatitis, and warts. | ||||||
| 115 | Benzo[b]chromeno-naphthyridin-7-one and pyrano[2′,3′:7,8]quino[2,3-b]quinoxalin-7-one compounds | US11047259 | 2005-01-31 | US07741325B2 | 2010-06-22 | Michel Koch; François Tillequin; Sylvie Michel; John Hickman; Alain Pierre; Stéphane Leonce; Bruno Pfeiffer; Pierre Renard |
| A compound selected from those of formula (I): wherein: B1, B2 represent carbon or nitrogen, X, Y, X1 and Y1 represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, trihaloalkyl and NRaRb wherein Ra and Rb are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, alkyl, —OR″a, —NR′aR′b, —O-Ta-OR″a, —NR″a-Ta-NR′aR′b, NR″a—C(O)-TaH, —O—C(O)-TaH, —O-Ta-NRa′Rb′, —NR″a-Ta-OR″a, —NR″a-Ta-CO2R″a and —NR″a—C(O)-Ta-NR′aR′b wherein R′a, R′b, R″a and Ta are as defined in the description, R3, R4 represent hydrogen or alkyl, A represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH—, —C(O)—CH(R8)— or —CH(R8)—C(O)— wherein R5, R6, R7 and R8 are as defined in the description, its isomers, N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer. | ||||||
| 116 | N-(alkoxyalkyl) carbamoyl-substituted 6-phenyl-benzonaphthyridine derivatives and their use as PDE ¾ inhibitors | US10591955 | 2005-03-16 | US07671068B2 | 2010-03-02 | Dieter Flockerzi |
| Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective PDE 3/4 inhibitors. | ||||||
| 117 | Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions | US10865719 | 2004-06-10 | US07566707B2 | 2009-07-28 | Matthias Eckhardt; Norbert Hauel; Elke Langkopf; Frank Himmelsbach; Iris Kauffmann-Hefner; Mohammad Tadayyon; Michael Mark |
| The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV). | ||||||
| 118 | Process for the production of pentostatin aglycone and pentostatin | US10734545 | 2003-12-12 | US07393954B2 | 2008-07-01 | Sourena Nadji; James Smoot; UmaShanker Sampath |
| A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates. | ||||||
| 119 | Substituted tricyclic heterocycles and their uses | US10960550 | 2004-10-07 | US07291733B2 | 2007-11-06 | Charles Lawrence Cywin; Roman Wolfgang Fleck; Eugene Richard Hickey; Weimin Liu; Tina Marie Morwick; John Robert Proudfoot; Denice M. Spero |
| Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds | ||||||
| 120 | Polyketide synthase enzymes and recombinant DNA constructs therefor | US11299244 | 2005-12-09 | USRE39762E1 | 2007-08-07 | Christopher Reeves; Daniel Chu; Chaitan Khosla; Daniel Santi; Kai Wu |
| Polyketide compounds of the formula but not including FK-506, FK-520, 18-hydroxy-FK520 and 18-hydroxy-FK-506. | ||||||
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