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| Number | Title | Issue Date |
| 7872135 | Method for introducing a 1,2-double bond into 3-oxo-4-azasteroid compounds A process for preparing 17β-substituted 4-azaandrost-1-en-3-one compounds of the general formula (I): or a pharmaceutically approved salt thereof, where R is hydroxyl, optionally substituted, line... | 01/18/2011 |
| 7550593 | Process for the preparation of finasteride Form I A process of preparing finasteride Form (I), which process comprises dissolving finasteride in a solvent, replacing the solvent partially or substantially completely with a nonsolvent and thereafter isolating finasteride Form (I). There is also provided finasteride ... | 06/23/2009 |
| 7531658 | Process for the preparation of 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones The present invention relates to a process for producing 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones of formula 1, including Finasteride and Dutasteride. ... | 05/12/2009 |
| 7501515 | Polymorphic form of 17-β-(N-ter. butyl carbamoyl)-4-aza-5-α-androst-1-en-3-one The present invention relates to a novel polymorphic form of 17-β-(N-ter.butyl carbamoyl)-4-aza-5-α-androst-1-en-3-one (Finasteride) of the Formula (I) and processes for preparing the form. ... | 03/10/2009 |
| 7410977 | Fluorinated 4-azasteroids as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorat... | 08/12/2008 |
| 7365202 | Polymorphs of an androgen receptor modulator Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorat... | 04/29/2008 |
| 7351698 | Androgen receptor modulators and methods of use thereof Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patien... | 04/01/2008 |
| 7329750 | 17-Acetamido-4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uteru... | 02/12/2008 |
| 7312229 | 21-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the ute... | 12/25/2007 |
| 7301026 | Process for making fluorinated 4-azasteroid derivatives The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivi... | 11/27/2007 |
| 7276513 | Steroidal compounds for inhibiting steroid sulphatase There is provided a compound of formula XII, wherein G is H or a substituent, and wherein R1 is a sulphamate group. ... | 10/02/2007 |
| 7217720 | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uteru... | 05/15/2007 |
| 7186838 | Fluorinated 4-azasteroid derivatives as androgen receptor modulators Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uteru... | 03/06/2007 |
| 7186728 | Methylene-4-azasteroids 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl ... | 03/06/2007 |
| 7164022 | Process for the preparation of pure Finasteride The present invention relates to an improved process for the preparation of pure Finasteride of Formula I, which comprises converting dihydrofinasteride to finasteride through novel protected dihydrofinasteride a... | 01/16/2007 |
| 7098218 | Steroidal compounds for inhibiting steroid sulphatase There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulph... | 08/29/2006 |
| 7084274 | Method for the selective preparation of 3-oxo-4-aza-5α-androstane compound This invention relates to a method for selectively preparing the 3-oxo-4-aza-5¥á-androstane compound which is used as an intermediate of finasteride by heating 3-oxo-4-aza-5-androstene in a mixture of formic acid and an alkanediol in the presence of zinc. ... | 08/01/2006 |
| 7057045 | Process for obtaining 17β-(substituted)-3-oxo-Δ-4-azasteroids and intermediates The 17β-(substituted)-3-oxo-Δ1,2-4-azasteroids (I), wherein R1 is C1–C4 alkyl, OR2, wherein R2 is a C1–C4 alkyl radical, or NR3R4, wherein R3 | 06/06/2006 |
| 7038050 | Method for the preparation of highly pure 1-androstene derivatives A method for preparing a 1-androstene derivative which comprises reacting a 2-iodo-androstane derivative with an oxidizing agent while maintaining the pH of the reaction mixture at a specific range gives the 1-androstene derivative with high purity and yield. ... | 05/02/2006 |
| 7022854 | Forms of dutasteride and methods for preparation thereof A crystalline Form II of 17β-N-[2,5-bis (trifluoromethyl)phenyl]carbamoyl-4-aza-5-α-androst-1-en-3-one (dutasteride) is provided. The preferred crystalline Form II of dutasteride has an X-ray powder diffraction pattern, expressed in terms of d-spacing (in ° A), w... | 04/04/2006 |
| RE39056 | 4-Azasteroids for treatment of hyperandrogenic conditions Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula... | 04/04/2006 |
| 6930214 | Process for producing 2,5-bis(trifluoromethyl)nitrobenzene A process to produce 2,5-bis(trifluoromethyl)nitrobenzene in a high yield from an industrially easily available material by using a substance with which the reaction operation is simple and handling is easy, with a small number of steps under moderate reaction condi... | 08/16/2005 |
| 6794508 | Process An improved process for preparing steriods, such as 3-oxo-4-azasteroids, is described. Compounds of this type are known to be useful in the preparation of compounds having 5a-reductase inhibitor activity. The process comprises the hydrogenation of the corresponding ... | 09/21/2004 |
| 6762302 | Process for dehydrogenation of azaandrostane compounds The invention relates to a process for the production of compounds of general formula (I), wherein R1 is a —NH-tert-butyl group or a 4-methyl-piperidino group, by bioconversion of compounds of general formula (II), wherein R1 is as described ... | 07/13/2004 |
| 6677453 | Production of polymorphic forms I and II of finasteride by complexation with group I or II metal salts Polymorphic Form (I) finasteride is prepared by first forming a substantially insoluble complex of finasteride and a Group (I) or Group (II) metal salt, such as lithium bromide, and then dissociating the complex by dissolving away the salt component with ... | 01/13/2004 |
| 6645974 | Androgen receptor modulators and methods for use thereof Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor ... | 11/11/2003 |
| 6593319 | Fusidic acid derivatives Novel 17,20-dihydrofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.... | 07/15/2003 |
| 6509466 | Process for obtaining 17 ଲ-(N-tert-butylcarbamoyl)-3-one-4-aza-steroids 17ଲ-(N-tert-butylcarbamoyl)-3-one-4-aza-steroids (I) can be obtained by a process which comprises the reaction of 17ଲ-(alkoxycarbonyl)-3-one-4-aza-steroid with lithium tert-butylamide in an organic solvent. Some compounds of formula (I), for e... | 01/21/2003 |
| 6506765 | Apomorphine derivatives and methods for their use Apomorphine derivative compounds; pharmaceutically active compositions of apomorphine derivative compounds; and the use of apomorphine derivative compounds in methods for treating sexual dysfunction or for enhancing apomorphine effectiveness for patients ... | 01/14/2003 |
| 6444683 | 17-azolyl steroids useful as androgen synthesis inhibitors Androgen synthesis inhibitors, as well as methods for the use of the same to reduce plasma levels of testosterone and/or dyhydrotestosterone, and to treat prostate cancer and benign prostatic hypertrophy, are disclosed.... | 09/03/2002 |
| 6365597 | 4-aza steroids The invention related to 4-aza-17ଲ-(cyclopropoxy)-androst-5-androstan-3-one, 4-aza-17ଲ-(cyclopropylamino)-androst-4-en-3-one and related compounds and to compositions incorporating these compounds, as well as the inhibition of C | 04/02/2002 |
| 6352997 | Method of improving in-vitro fertilization The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: ##STR1## to the subjec... | 03/05/2002 |
| 6342633 | O-benzyl oxime ether derivatives and their use as pesticides Compounds of the formula I ##STR1## in which Y is hydrogen, C1 -C4 alkyl, C1 -C4 alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) ##STR2## R1 ... | 01/29/2002 |
| 6284887 | Process for preparing carboxamido-4-azasteroids A process for producing a compound of formula (I): ##STR1## wherein the dotted lines - - - independently represent a single or double bond and R, R1, R2 and R3 are each hydrogen or an organic radical, comprises treating th... | 09/04/2001 |
| 6262265 | Non-hydrolyzable analogs of heroin metabolites suitable for use in immunoassay Novel chemical analogs are disclosed for the essential heroin metabolite 6-O-acetyl morphine (6MAM). The analogs optionally can be made to contain protein reactive groups, and can be used to form protein conjugates, fluorescently labeled compounds, and so... | 07/17/2001 |
| 6211240 | O-benzyl oxime ether derivatives and their use as pesticides Compounds of the formula I ##STR1## in which Y is hydrogen, C1 -C4 alkyl, C1 -C4 alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) ##STR2## R1 ... | 04/03/2001 |
| 6207396 | Immunoassay reagents and methods for determination of LSD and LSD metabolites To improve the detection of LSD in biological samples, antibodies are raised to LSD conjugated to a protein carrier, preferably through the indole ring. Selected antibodies are matched with an immunoassay reagent in which the LSD is conjugated in the same... | 03/27/2001 |
| 6204273 | 16-substituted-4-aza-androstane 5--reductase isozyme 1 inhibitors Compounds of the Formula I ##STR1## are inhibitors of the 5-reductase 1 isozyme, and are useful alone, or in combination with a 5-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, fe... | 03/20/2001 |
| 6187925 | Intermediates and process for the synthesis of azasteroids The novel process of this invention involves the stereoselective synthesis of certain 16-substituted 4-aza-5-androst-1-en-3-ones, and the useful intermediates obtained therein.... | 02/13/2001 |
| 6180794 | Process for the preparation of 1,2-dihydroquinolines A method for preparing 1,2-dihydroquinolines that is more flexible than the Skraup reaction is provided. The method comprises treating an ortho-alkenyl aniline with a ketone in the presence of a Lewis acid. Novel intermediates and products of this method ... | 01/30/2001 |
