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JP4638225B2 |
The present invention provides a process of catalyzing a click chemistry ligation reaction between a first reactant having a terminal alkyne moiety and second reactant having an azide moiety for forming a product having a triazole moiety...
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JP4629030B2 |
The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
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JP4613366B2 |
The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: -X 1 -(CH 2 ) m -Q...
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JP4606408B2 |
The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory dise...
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JP4601297B2 |
Sterol derivatives (I) are new. Sterol derivatives of formula (I) are new. T1, T2 = H or Me, Me being in alpha- or beta-configuration; T4 = H, Me or Et; T3 = H or beta-Me; dotted line = optional additional 5(6) or 6(7) bond; Z = H or OH ...
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JP4598953B2 |
Compounds of formula (I)in which the radicals are as defined in the specification and claims, and physiologically tolerated and physiologically functional derivatives thereof and processes for their preparation are described. The compoun...
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JP2010538072A |
This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
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JP4564108B2 |
Deoxynojirimycin derivatives containing a large hydrophobic moiety, such as cholesterol or adamantame-methanol, linked through a spacer, such as pentamethylene, to the nitrogen atom of deoxynojirimycin, and salts thereof, inhibit glucosy...
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JP4563578B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP4545929B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP4545930B2 |
The invention is directed to 17 beta -nitro-11 beta -arylsteroids of formula I: wherein R1, R6, R7, R12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment o...
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JP2010193809A |
To provide a method for producing a feeding center-suppressing substance.The method for producing the feeding center-suppressing substance comprises a step of fermenting a caralluma fruit and caffeine with lactobacillus. The feeding cent...
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JP4541166B2 |
Methods and compositions for interacting with the GABAA receptor complex to induce sleep in humans using certain 5 3 alpha -hydroxy-5-reduced steroid derivatives.
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JP4530851B2 |
The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents a...
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JP4509380B2 |
A process for the preparation of a compound of the formulawherein the substituents are defined as in the specification.
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JP4507024B2 |
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JP4495456B2 |
There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents -C(-O)-aryl or -C(-O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the alpha or beta configuration) or methylene; R4 and R5...
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JP4486363B2 |
The invention relates to substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, of general formula (I), wherein R1 represents C7-C22 alkyl, C2-C4 alkyl that is substituted by C4-C20 alkoxy, C6-C10 aryl, C6-C10 aryloxy or C4-C12-alkoxy-C2-...
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JP4476480B2 |
A compound selected from the group consisting of a compound of the formulawherein the substituents are defined as set forth in the specification which compounds are useful for the treatment of osteoporosis.
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JP4470197B2 |
Amphoteric sterol derivatives, and liposomes containing these derivatives are new. The amphoteric sterol derivatives have an isoelectric point of 4.5-8.5 and are compounds of formula (I): Amphoter-Y-spacer-X-sterol (I) X and Y : linking ...
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JP4474101B2 |
The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.
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JP2010095528A |
To provide a non-thermally reversible photochromic compound.The invention relates to a photochromic compound which may be thermally reversible or non-thermally reversible, and the like. The invention also relates to a photochromic dichro...
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JP4436041B2 |
According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.
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JP2010031062A |
To provide a method and medicinal composition for treating disorders involving a ceramide-mediated signaling transmission system, for example, those selected from the group consisting of Gaucher disease, Tay-Sachs disease, Sandhoff disea...
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JP2010024238A |
To provide an enzyme inhibitor strongly inhibiting 17-hydroxylase/C17,20-lyase and 5-reductase, blocking all androgen synthesis, and useful in treatment of prostatic cancer and benign prostatic hypertrophy, based on defects associated wi...
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JP2010501575A |
Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17α-hydroxylase/C17,20-lyase inhibitor, such as abiraterone acetate (i.e., 3β-acetoxy-17-(3-...
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JP2009256388A |
To provide a new hybrid drug for cancer treatment and for releasing the drug by setting a target on cancer cells.Provided is a hybrid drug for cancer treatment, having a targeting moiety specifically bonding with proteins, receptors and ...
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JP4357597B2 |
The invention relates to a method of preparing a compound of the general formula fac-ÄM(CO)3(OH2)3Ü<+> wherein M is Mn, <99m>Tc, <186>Re or <188>Re, by reacting a metal in the permetallate form with carbon monoxide and a reducing agent...
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JP4338306B2 |
The invention relates to the steroidal saponin compounds for the propylaxis or treatment dementia, the new steroidal saponin compounds and the pharmaceutical composition containing the same.
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JP4335820B2 |
17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives (I), having a 7alpha -side-chain, are new. 17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives of formula (I), their acid addition salts and esters are new. [Ima...
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JP4324249B2 |
This invention describes the new 17alpha-fluoroalkyl steroids of general formula I as well as their physiologically compatible salts with bases. The new compounds have an extraordinary strong antigestagenic action and are suitable for th...
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JP4308824B2 |
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 ...
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JP4297994B2 |
6-Hydroxy and 6-oxo-androstane derivatives having the general formula (I): wherein the symbol @ represents a single or a double bond and A, R<1> and R<2> have the meanings given in the description; a pharmaceutical composition comprising...
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JP2009143963A |
To provide a pharmaceutical composition for treating tumor, using hedgehog/smoothened signals for inhibiting apoptosis of tumor cells.The pharmaceutical composition contains a sufficient amount of cyclopamine, its pharmaceutically accept...
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JP2009522383A |
The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
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JP2009102413A |
To provide a method for administering a glucocorticoid receptor antagonist to a patient receiving AP regimen for a long term.The present invention generally pertains to the field of psychiatry. In particular, the present invention pertai...
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JP2009517425A |
Sulfonamide prodrugs (I) are new. Sulfonamide prodrugs of fromula (I) are new Drug-OCO-X-SO 2NH 2 (I) X : optionally substituted heteroaromatic group or alkyl-heteroaromatic group; Drug : pharmaceutical able to form a carboxylate ester t...
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JP2009515828A |
The disclosure provides androsterone derivatives. The derivatives of the disclosure are useful in the treatment of androgen- and estrogen-associated diseases and disorders, including breast cancer.
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JP2008542419A |
The present invention relates to a pharmaceutical composition, comprising 3±-hydroxy-3²-methoxymethyl-21-(1'-imidazolyl)-5a-pregnan-
20-one or a pharmaceutically-acceptable salt or solvate thereof, and one or more pharmaceutically-acce...
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JP4184986B2 |
The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, ...
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JP2008266348A |
To provide a caspase inhibitor which is an effective inhibitor of apoptosis and IL-1 secretion.The caspase inhibitor is represented by formula (I) (wherein Z is oxygen or sulfur; R1 is hydrogen, -CHN2, -R, -CH2OR, -CH2SR or -CH2Y; Y is a...
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JP4145350B2 |
The invention relates to a 3 alpha -hydroxy, 17-(un)substituted derivatives of the androstane series and 3 alpha -hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at the recently identif...
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JP2008517993A |
The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure VIII: L represents the chain of the substructure IX or XIII: -X 1 -(CH...
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JP4089181B2 |
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JP4085601B2 |
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JP4066272B2 |
Methods, compositions and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
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JP4065399B2 |
Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals
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JP2008506675A |
The present invention relates to the use of a compound of formula (I) in the manufacture of a pharmaceuticals composition for cell death by photo activation therapy and the use of the compounds in the prevention and/or treatment of cancer.
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JP4039683B2 |
A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may ...
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JP2007537131A |
Pharmaceutical compositions for and methods of preventing infection or treating an individual who has been identified as being infected with a Flavivirus, Pestivirus, picornovirus or coronavirus such as HCV, GB virus B, JEV, WNV, CSFV, B...
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