Class 540/543 - Spiro

Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain a spiro ring system.
No. of patents: 187
Last issue date: 03/13/2012

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Number	Title	Issue Date
8133992	Azepinoindole and pyridoindole derivatives as pharmaceutical agents Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of di...	03/13/2012
8022060	Spirocyclic heterocyclic derivatives and methods of their use Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be us...	09/20/2011
7928224	Optically active quaternary ammonium salt having axial asymmetry and process for producing α-amino acid and derivative thereof with the same The present invention provides a compound of the following formula (I) below. This compound (I) can be produced by reacting a 2,2′-dimethylene bromide-1,1′-binaphthyl derivative, which can be produced by a relatively small number of processes, with an easily ava...	04/19/2011
7566779	Optically active quaternary ammonium salt, process for producing the same, and process for producing optically active α-amino acid derivative with the same There are provided (1) an optically active α-amino acid derivative, a stereoselectively useful intermediate for the synthesis of pharmaceutical or agrochemical products, which derivative is an optically active quaternary ammonium salt that, when used as an axially ...	07/28/2009
7419969	HIV integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates us...	09/02/2008
7365062	Nonpeptide substituted spirobenzoazepines as vasopressin antagonists The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, wh...	04/29/2008
7294632	Substituted 8′-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one and 8′-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one derivatives The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. The invention relates also...	11/13/2007
7285546	Cephalotaxanes, their method of preparation and their use in treatment of cancers, leukemias, parasites including those resistant to usual chemotherapeutic agents and as reversal agents The present invention concerns a compound of formula (I) wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or arom...	10/23/2007
7273859	HIV integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates us...	09/25/2007
7238703	Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane NMDA, 5HT, and neuronal nicotinic receptor antagonists Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of tr...	07/03/2007
7238687	Nonpeptide substituted spirobenzoazepines as vasopressin antagonists The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specif...	07/03/2007
7196087	Quinazolinone and benzoxazinone derivatives and uses thereof Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—,...	03/27/2007
7169774	Cephalotaxane derivatives and their processes of preparation and purification The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constit...	01/30/2007
7160912	Heterocyclic compounds having antibacterial activity: process for their preparation and pharmaceutical compositions containing them The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for t...	01/09/2007
7148214	Antihistaminic spiro compounds This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, —A—B—, L, and n hav...	12/12/2006
7122677	NK1 antagonists A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5...	10/17/2006
7091198	2,5-disubstituted pyrimidine derivatives The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of cent...	08/15/2006
7067315	Identification of anti-protozoal agents The present invention provides novel assay systems and methods for monitoring cell invasion by protozoal parasites. The present invention further provides methods of using these assays systems to identify compounds that treat or prevent protozoal infection. The pres...	06/27/2006
6992077	Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates ...	01/31/2006
6953787	5HT2C receptor modulators The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity....	10/11/2005
6919349	Spiro compounds and adhesion molecule inhibitors containing the same as the active ingredient Disclosed are novel spiro derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases. The spiro derivative according to the present invention has the chemical structure, for example, represented by th...	07/19/2005
6916807	Triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as ...	07/12/2005
6908926	Substituted imidazoles, their preparation and use Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compoun...	06/21/2005
6900201	N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G...	05/31/2005
6887867	5H-2,3-benzodiazepine antagonists of excitatory amino acid receptors Substituted benzodiazepine compositions are provided which are active as non-NMDA ionotropic excitatory amino acid (EAA) receptor antagonists. The compounds are generally 7- or 8-mono substituted 5H-2,3-benzodiazepines. The compositions are useful for treating disor...	05/03/2005
6867204	Benzoxazine derivatives and uses thereof Compounds of the formula: or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is —SO2— or —SO2—N(R10)—, Z1 is...	03/15/2005
6858599	Tricyclic compound having spiro union This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which e...	02/22/2005
6812358	Process for making estra-4,9(10)-diene steroids A novel process for making estra-4,9(10)-diene-3,17-dione steroids from readily available 19-nor-androst-4-ene-3-one steroids by a straightforward three-step process. Products of this process are important intermediates in the preparation of biologically active subs...	11/02/2004
6797819	Alkaloids The present invention provides novel alkaloid compounds and collections of these compounds, and provides methods for the synthesis of these compounds using biomimetic synthetic strategies. Additionally, the present invention provides pharmaceutical compositions and ...	09/28/2004
6762177	Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof One aspect of the present invention relates to spirocyclic compounds. Another aspect of the present invention relates to the use of the spirocyclic compounds as ligands for mammalian G-protein-coupled receptors or sigma receptors. The present invention also relates ...	07/13/2004
6706878	Spiroazabicyclic heterocyclic compounds A compound of formula wherein n, m, p, X, Y, W, A, G and D are as defined in the specification, enantiomers thereof, pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, a...	03/16/2004
6703502	Spiroazo bicyclic heterocyclic A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2 ; A is N or C(R2); G is N or C(R3); D is N or C(R4); wit...	03/09/2004
6693101	଱v integrin receptor antagonists The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as ଱v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ଱...	02/17/2004
6677332	Heterocyclic analgesic compounds and methods of use thereof One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-pro...	01/13/2004
6638925	Benzazepine derivatives, medicaments containing the same and their use to prepare medicaments New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) ##STR1## and new compounds of the general formula (III) ##STR2## Drugs, containing compounds of formulas (I) and/or (III), which can be used ...	10/28/2003
6627634	Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them Bicyclic heterocycles of general formula ##STR1## wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorg...	09/30/2003
6579869	Cephalotaxanes: their method of preparation and their use in treatment of cancers, leukemias, parasites, including those resistant to usual chemotherapeutic agents, and as reversal agents The present invention concerns a compound of formula (I) ##STR1## wherein: W represents O or NH, Q represents an unbranched or branched, saturated or unsaturated or aromatic, cyclic or acyclic or heterocyclic hydrocarbon radical containing 1 to 30 carbon ...	06/17/2003
6566357	Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the form...	05/20/2003
6512112	Aminoaryl oxazolidinone N-oxides The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I ##STR1## wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of ...	01/28/2003
6509334	Cyclocarbamate derivatives as progesterone receptor modulators This invention provides compounds of Formula (I): ##STR1## wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 ...	01/21/2003

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Class 540/543 - Spiro