| Patent Number |
Title Of Patent |
Date Issued |
| 6583134 |
Aza- indolyl derivatives for treating obesity |
June 24, 2003 |
| Novel compounds of formula (I): ##STR1##wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4, n, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are usefu |
| 6548694 |
N-(4-carbamimidoyl-phenyl)-glycine derivatives |
April 15, 2003 |
| N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: ##STR1##wherein X and R.sup.1 to R.sup.5 are as defined herein, and includes hydrates or solvates and/or physiologically acceptable salts thereof and/or physiologically acceptable esters thereof. |
| 6544985 |
Dihydro-benzo [b][1,4]diazepin-2-one derivatives |
April 8, 2003 |
| This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula ##STR1##wherein R.sup.1, R.sup.2, R.sup.3, X and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation, th |
| 6541638 |
Pyrrolidine derivatives |
April 1, 2003 |
| The present invention relates to pyrrolidine derivatives and dimeric forms and/or pharmaceutically acceptable esters, and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treati |
| 6534539 |
Pharmaceutical composition and method for treatment of dyspepsia |
March 18, 2003 |
| The present invention relates to compositions containing lipase inhibitors, e.g. orlistat, and the use of such compositions for treating, reducing or preventing functional dyspepsiaafter ingestion of meals, especially of fat containing or fat rich meals. |
| 6531612 |
Nitrile derivatives that inhibit cathepsin K |
March 11, 2003 |
| Compounds of the formula: ##STR1##wherein R.sup.1 to R.sup.7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, o |
| 6531472 |
Tetralone derivatives |
March 11, 2003 |
| The present invention provides compounds of formula I ##STR1##and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatme |
| 6528543 |
Urea derivatives |
March 4, 2003 |
| Glucokinase activating compounds of the formula ##STR1##wherein R.sup.1 and R.sup.2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sul |
| 6521754 |
Benzothiazole derivatives with activity as adenosine receptor ligands |
February 18, 2003 |
| The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor. |
| 6515124 |
Dehydroamino acids |
February 4, 2003 |
| Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis. |
| 6489479 |
Process for the preparation of mixed anhydrides |
December 3, 2002 |
| The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture |
| 6479666 |
Phenyl-keto-imidazolidine thioamide derivatives |
November 12, 2002 |
| It has been discovered that compounds of the formula: ##STR1##and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory disease |
| 6440995 |
Quinolin-4-yl derivatives |
August 27, 2002 |
| Phenyl substituted quinolin 4-yl derivatives and pharmaceutical compositions with activity as NMDA-receptor subtype selective blockers. The compounds of the invention modulate neuronal activity and plasticity. |
| 6440959 |
Pyrazolobenzodiazepines |
August 27, 2002 |
| Disclosed are novel pyrazolobenzodiazepines having the formula ##STR1##and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds |
| 6437171 |
Process for preparing 1,2-diamino compounds |
August 20, 2002 |
| The invention provides a multistep process for preparing 1,2-diamino compounds of formula ##STR1##wherein R.sup.1, R.sup.1', R.sup.2, R.sup.2', R.sup.3 and R.sup.4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxides of |
| 6423728 |
Heterocyclic thioamide derivatives |
July 23, 2002 |
| It has been discovered that compounds of the formula: ##STR1##and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are usefull in treating inflammation associated with chronic inflammatory diseas |
| 6420600 |
Phenylalaninol derivatives |
July 16, 2002 |
| It has been discovered that compounds of the formula: ##STR1##and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, are more readily absorbed and more bioavailable than the corresponding carboxylic acids from which they are derived, both o |
| 6403579 |
Pharmaceutical compositions containing carvedilol and hydrochlorothiazide |
June 11, 2002 |
| A pharmaceutical combination preparation for the treatment of cardiac and cardiovascular disorders, such as hypertension, angina pectoris, cardiac insufficiency and illnesses associated therewith, contains the active substances carvedilol, or a pharmaceutically acceptable salt thereof, a |
| 6391873 |
Imidazodiazepine derivative |
May 21, 2002 |
| The present invention relates to compound 7-Chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihy dro-imidazo[1,5-a][1,4]benzodiazepin-6-one (I) ##STR1##and to the use of the compound of formula I for the manufacture of medicaments to be used as anxiolytic and/or an |
| 6388088 |
Tetrazolyl-phenyl acetamide glucokinase activators |
May 14, 2002 |
| Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes. |
| 6352717 |
Process for encapsulating shear sensitive fill masses into capsules and capsules containing shea |
March 5, 2002 |
| The present invention provides a process for encapsulating a shear sensitive fill mass which contains a pharmaceutical active agent or nutrient, characterized in that said fill mass is heated and subsequently cooled, prior to the encapsulation. The invention also provides capsules co |
| 6326397 |
Retinoid antagonists and use thereof |
December 4, 2001 |
| The present invention relates to novel retinoid antagonists of the formula I ##STR1##wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R.sup.1 is lower alkyl and R.sup.2 is hydrogen; and, when the dotted bond is h |
| 6320054 |
Thiazole derivatives |
November 20, 2001 |
| Compounds of the formula: ##STR1##as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cel |
| 6316633 |
Process for manufacture of chiral succinic acid derivatives |
November 13, 2001 |
| The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) ##STR1##wherein R.sup.1 is (C.sub.1 -C.sub.6) alkyl or benzyl, and the novel intermediates used therein. |
| 6307056 |
4-aryloxindoles |
October 23, 2001 |
| Disclosed are 4-aryloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheu |
| 6303790 |
Process for the preparation of pyridine derivatives |
October 16, 2001 |
| A process is described for preparing certain 4-alkyl- or 4-aryl-pyridine derivatives. |
| 6294688 |
Process useful to produce vitamin D analogs |
September 25, 2001 |
| A stereospecific method for accomplishing the below reaction: ##STR1##results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then |
| 6294668 |
Vinylpyrrolidinone cephalosporin derivatives |
September 25, 2001 |
| The present invention relates to cephalosporin derivatives of the general formula ##STR1##whereR.sup.1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at leas |
| 6291694 |
Process and intermediates useful to produce vitamin D analogs |
September 18, 2001 |
| A stereospecific method for accomplishing the below reaction: ##STR1##results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then |
| 6274734 |
Process for making pyrimidine derivatives |
August 14, 2001 |
| The present invention provides a process for the manufacture of pyrimidines of formula I: ##STR1##whereinR.sup.1, R.sup.2, R.sup.3 each independently represent hydrogen, C.sub.1-7 -alkyl, or C.sub.1-7 -alkoxy,A signifies--CN,a carbanionic R.sup.4 -alkynyl residue, in which R.sup.4 is hyd |
| 6268499 |
Process and intermediates for preparation of substituted piperidine-epoxides |
July 31, 2001 |
| The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof ##STR1##comprisingepoxidation of a compound of formula 2 or a salt thereof ##STR2##wherein A, R.sup.1 and R.sup.2 are as herein defined. These compounds a |
| 6262089 |
D-proline derivatives |
July 17, 2001 |
| New compounds have the formula: ##STR1##wherein R, R.sup.1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes |
| 6255501 |
Process for preparing antiosteoporotic agents |
July 3, 2001 |
| Methods for preparing antiosteoportic agents are disclosed. Compounds useful in the methods are also disclosed. |
| 6248901 |
Heterocyclic vinyl ethers |
June 19, 2001 |
| The compounds of the formula ##STR1##whereinR signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower |
| 6242601 |
Heterocyclic sulfamides |
June 5, 2001 |
| The compounds of formula (I) ##STR1##wherein R.sup.1, R.sup.2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysf |
| 6229011 |
N-aroylphenylalanine derivative VCAM-1 inhibitors |
May 8, 2001 |
| Compounds of the formula: ##STR1##are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4. |
| 6225117 |
Antibodies against human IL-12 |
May 1, 2001 |
| The present invention relates to novel p75 heterodimer specific anti-human IL-12 antibodies that are characterized by a higher potency and greater efficacy in neutralizing human IL-12 bioactivity than known heterodimer specific IL-12 monoclonal antibodies. The heterodimer specific antibo |
| 6222039 |
Process for the preparation of chiral lactones |
April 24, 2001 |
| The present invention relates to a process for the preparation of compounds of formula I ##STR1##wherein R.sup.1 and R.sup.2 are as defined in the specification as well as to the novel intermediates obtained by said process. |
| 6211166 |
5'-deoxy-cytidine derivative administration to treat solid tumors |
April 3, 2001 |
| Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1##wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straigh |
| 6197995 |
Process for manufacture of chiral succinic acid derivatives |
March 6, 2001 |
| The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) ##STR1##wherein R.sup.1 is (C.sub.1 -C.sub.6) alkyl or benzyl, and the novel intermediates used therein. |
| 6194410 |
Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
February 27, 2001 |
| The present invention is concerned with pyrazolopyrimidines and pyrazolotriazines of the general formula ##STR1##and their pharmaceutically acceptable salts.Surprisingly, these compounds evidence selective affinity to 5HT-6 receptors. They are accordingly suitable for use in the treatmen |
| 6184422 |
Cyclohexanediol derivatives |
February 6, 2001 |
| Compounds of formula I ##STR1##whereinX is C.dbd.CH.sub.2 or CH.sub.2 ;Y and Z are independently of each other hydrogen, fluorine or hydroxy;A is --C.tbd.C--, --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --,R.sup.1 and R.sup.2 are independently of each other alkyl or perfluoroalkyl; andR.sup.3 is |
| 6174881 |
Hydroxymethylimidazodiazepines and their esters |
January 16, 2001 |
| The invention is concerned with hydroxymethyl-imidazodiazepines and their esters of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances. |
| 6156894 |
Process for manufacturing .alpha..sub. 1L-adrenoceptor antagonists |
December 5, 2000 |
| A process is useful for making compounds of the formula: wherein R is hydro, methyl, or fluoro.Valuable intermediates in this process include: ##STR1## wherein R is hydro, methyl, or fluoro, and L is a leaving group. |
| 6153624 |
Pyrrolidine and piperidine derivatives and treatment of neurodegenerative disorders |
November 28, 2000 |
| The present invention relates to the use of pyrrolidine and piperidine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are, independently from each other, hydrogen, lower alkoxy, hydroxy, halogen, --CONH.sub.2 or --C(O)O-lower alkyl; or taken together are |
| 6153605 |
Arylsecocholadiene derivatives |
November 28, 2000 |
| Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperpara |
| 6150350 |
Antimicrobial compositions |
November 21, 2000 |
| The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the comp |
| 6147108 |
Method for treating type II diabetes mellitus |
November 14, 2000 |
| A method for treating or preventing type II diabetes mellitus comprising administering an effective amount of a gastrointestinal lipase inhibitor, such as, tetrahydrolipstatin. |
| 6130354 |
Process for the preparation of shikimic acid and its derivatives |
October 10, 2000 |
| The present invention discloses a process for the preparation of shikimic acid or its derivatives from quinic acid or its derivatives by dehydration with Vilsmeier reagent. The present invention further discloses intermediates produced by this process and their use in the synthesis of |
| 6100282 |
Thiazole derivatives |
August 8, 2000 |
| Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and c |
