| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 341 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM | PCT/US2008086254 | 2008-12-10 | WO2009076454A2 | 2009-06-18 | VELICELEBI GONUL; STAUDERMAN KENNETH A; KING FRANK; PEI YAZHONG; WHITTEN JEFFREY P |
| Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | ||||||
| 342 | COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM | PCT/US2008073392 | 2008-08-15 | WO2009035818A8 | 2009-05-14 | VELICELEBI GONUL; STAUDERMAN KENNETH A; PLEYNET DAVID P M; CHENG SONG; WHITTEN JEFFREY P |
| Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store -operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity. | ||||||
| 343 | COMPOUNDS THAT ARE AGONISTS OF MUSCARINIC RECEPTORS AND THAT MAY BE EFFECTIVE IN TREATING PAIN, ALZHEIMER'S DISEASE AND/OR SCHIZOPHRENIA | PCT/SE2007000409 | 2007-04-27 | WO2007126362A8 | 2008-10-30 | CHENG YUN-XING; LUO XUEHONG; TOMASZEWSKI MIROSLAW |
| Compounds of Formulae I, or pharmaceutically acceptable salts thereof: [Chemical formula should be inserted here. Please see paper copy] I wherein X, R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain. | ||||||
| 344 | INHIBITORS OF PLASMA KALLIKREIN | PCT/US2007074761 | 2007-07-30 | WO2008016883A3 | 2008-04-03 | SINHA SUKANTO; CHILCOTE TAMIE JO |
| The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment. | ||||||
| 345 | LABELLED ANALOGUES OF HALOBENZAMIDES AS RADIOPHARMACEUTICALS | PCT/IB2007052992 | 2007-07-27 | WO2008012782A2 | 2008-01-31 | MADELMONT JEAN-CLAUDE; CHEZAL JEAN-MICHEL |
| The present invention relates to the use of a compound of formula (I): in which R1 represents a radionuclide, Ar represents an aromatic nucleus, m is an integer varying from 2 to 4, R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or an aryl group chosen from a phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl group, and their addition salts with pharmaceutically acceptable acids, in the preparation of a radiopharmaceutical composition intended for the diagnosis and/or treatment of melanoma. | ||||||
| 346 | COMPOSITIONS AND THEIR USE AS ANTI-TUMOR AGENTS | PCT/US2005037307 | 2005-10-18 | WO2006044826A2 | 2006-04-27 | WARD JOHN; JAIN RAMA; JAMES DONALD; VERHEIJ HERMAN J; SCHULTZ JAN C C |
| The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | ||||||
| 347 | ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS | PCT/EP0351021 | 2003-12-16 | WO2004056745A3 | 2004-11-11 | LINDERS JOANNES THEODORUS MARI; WILLEMSENS GUSTAAF HENRI MARIA; GILISSEN RONALDUS ARNODUS HEND; BUYCK CHRISTOPHE FRANCIS ROBER; VANHOOF GRETA CONSTANTIA PETER; VAN DER VEKEN LOUIS JOZEF ELIS; JAROSKOVA LIBUSE |
| The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R<1> and R<2 >each independently represents hydrogen C1-4alkyl, NR<9>R<10>, C1-4alkyloxy; or R<1> and R<2> taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R<1> or R<2> may be absent to form an unsaturated bond; R<3> represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R<3> represents a monovalent radical having one of the following formulae, wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het<1> or Ar<2> wherein said C3-8cycloalkyl, Het<1> or Ar<2> are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR<5>R<6>, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het<2> and NR<7>R<8>, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R<5> and R<6> each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R<1> and R<8> each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or Cl-4alkyloxycarbonyl; L represents C1-4alkyl; Het<1> represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het<2> represents piperidinyl, pyrrolidinyl or morpholinyl; Ar<2> represents phenyl, naphtyl or indenyl. | ||||||
| 348 | NOVEL HETEROCYCLIC AMIDE DERIVATIVES AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS | PCT/US0204917 | 2002-02-15 | WO02066469A3 | 2003-03-13 | HENDRIX JAMES A; STRUPCZEWSKI JOSEPH T; BORDEAU KENNETH J; URMANN MATTHIAS; SHUTSKE GREGORY; HEMMERLE HORST; JURCAK JOHN G; GILL HARPAL; WEIBERTH FRANZ JR; NIEDUZAK THADDEUS; JACKSON SHARON A; ZHAO XU-YANG; MUELLER PAUL J |
| The invention relates to heterocyclic substituted amide derivatives of formula (I) that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors. | ||||||
| 349 | SERINE PROTEASE INHIBITORS | PCT/GB0002291 | 2000-06-13 | WO0077027A3 | 2001-05-25 | LIEBESCHUETZ JOHN WALTER; YOUNG STEPHEN CLINTON; LIVELY SARAH ELIZABETH; HARRISON MARTIN JAMES; WASZKOWYCZ BOHDAN; MORGAN PHILLIP JOHN |
| Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease (especially tryptase) inhibitors useful as antiinflammatory agents. | ||||||
| 350 | HERBICIDES CONTAINING 3-AMINOBENZO(B)THIOPHENES AS AN ANTIDOTE | PCT/EP9201798 | 1992-08-07 | WO9304057A3 | 1993-07-22 | HAGEN HELMUT; NILZ GERHARD; ROETSCH THOMAS; WALTER HELMUT; LANDES ANDREAS |
| Disclosed are herbicides containing at least one 3-aminobenzo[b]thiophene (I) with an antagonistic action (in which R1 = -COX or -COOX; X = H, halogen, optionally substituted amino, optionally substituted C¿1?-C10 alkyl, optionally sustituted C1-C8 alkenyl, optionally substituted C3-C10 cycloalkyl, optionally substituted C3-C10 cycloalkenyl, a 5/6-membered heterocyclic aromatic, optionally substituted phenyl or optionally substituted naphthyl; R?2 and R3¿ = H, CN, NO¿2?, SH, halogen, optionally substituted amino, optionally substituted C1-C10 alkyl, optionally substituted C1-C6 alkoxy, optionally substituted C2-C8 alkenyl, optionally substituted C3-C10 cycloalkyl, optionally substituted C3-C10 cycloalkenyl, optionally substituted phenyl, optionally substituted naphthyl or a 5/6-membered heterocyclic aromatic; R?4 to R7¿ = H, optionally substituted C¿1?-C10 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C3-C10 cycloalkyl, optionally substituted C3-C10 cycloalkenyl, an optionally substituted 5/6-membered heterocyclic aromatic, optionally substituted phenyl or optionally substituted naphthyl or R?4 + R5¿ and/or R6 + R7 form, together with the N-atom to which they are bound, a 5- to 7-membered ring), plus the basic salts of those compounds of formula (I) which carry at least one carboxyl, hydroxythiocarbonyl or sulphonic acid group and the acid salts of those compounds of formula (I) which contain a basic nitrogen atom, and at least one herbicidal substance selected (A) from the group comprising the cyclohexenone derivatives or (B) from the group comprising the 4-(hetero)aryloxyphenoxyacetic acid derivatives. | ||||||
| 351 | FUNCTIONALIZED BENZAMIDE DERIVATIVES AS ANTIVIRAL AGENTS AGAINST HBV INFECTION | PCT/US2013073319 | 2013-12-05 | WO2014089296A3 | 2014-08-07 | XU XIAODONG; BLOCK TIMOTHY M; GUO JU-TAO; DU YANMING |
| Novel functionalized benzamide derivatives are provided. Also provided are pharmaceutical compositions comprising therapeutically effective amounts of functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection, in combination with at least one pharmaceutically acceptable excipient. Functionalized benzamide derivatives of the invention include N-aryl-substituted 1-naphthamide and 2-naphthamide derivatives. | ||||||
| 352 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS | PCT/US2009066211 | 2009-12-01 | WO2010065512A3 | 2010-07-29 | JIANG JUN; KOWALCZYK-PRZEWLOKA TERESA; SCHWEIZER STEFAN M; XIA ZHI-QIANG; CHEN SHOUJUN; BORELLA CHRISTOPHER; SUN LIJUN |
| The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included. | ||||||
| 353 | METHODS OF INHIBITING THE FORMATION OF AMYLOID-ß DIFFUSABLE LIGANDS USING A ACYLHYDRAZIDE COMPOUNDS | PCT/US2008069878 | 2008-07-11 | WO2009009768A8 | 2010-01-28 | LOOK GARY CHARLES; SCHULTZ LAURI; POLOZOV ALEXANDRE MIKHAYLOVICH; BHAGAT NIKHIL; WANG JIAN; ZEMBOWER DAVID E; GOURE WILLIAM F; PRAY TODD; KRAFFT GRANT A |
| Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ß1-42 oligomers from amyloid ß1-42 monomers using acylhydrazidecompounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ß1-42 oligomers using acylhydrazidecompounds. | ||||||
| 354 | ACETYL COENZYME A CARBOXYLASE INHIBITORS | PCT/US2008057933 | 2008-03-21 | WO2008121592A3 | 2009-04-09 | CHANG EDCON; MCNEILL MATTHEW H |
| The present invention relates to acetyl coenzyme-A carboxylase ("ACC") inhibiting compounds of the Formula (I), wherein the variables are as defined herein. In particular, the present invention relates to ACC1 and/or ACC2 inhibitors, compositions of matter, kits and articles of manufacture comprising these compounds, methods for inhibiting ACC1 and/or ACC2, and methods of making the inhibitors. | ||||||
| 355 | NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS | PCT/EP2008053087 | 2008-03-14 | WO2008113760A2 | 2008-09-25 | WAGNER HOLGER; LANGKOPF ELKE; ECKHARDT MATTHIAS; STREICHER RUEDIGER; SCHOELCH CORINNA; SCHULER-METZ ANNETTE; PAUTSCH ALEXANDER |
| The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions. | ||||||
| 356 | COMPOUNDS FOR MODULATING INTEGRIN CD11B/CD18 | PCT/US2007025878 | 2007-12-18 | WO2008082537A3 | 2008-08-28 | GUPTA VINEET; AMIN ARNAOUT M |
| The application describes an assay for the identification of small molecule modulators of integrin CDl lb/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency. | ||||||
| 357 | 2 -AMINOTHIOPHENE COMPOUNDS AS FUNGICIDES | PCT/GB2004004429 | 2004-10-19 | WO2005044008A3 | 2008-01-03 | SELLES PATRICE; WAILES JEFFREY STEVEN; WHITTINGHAM WILLIAM GUY; CLARKE ERIC DANIEL |
| A method of combating phytopathogenic diseases on plants and harvested food crops which comprises applying to a plant, to the seed of a plant, to the locus of the plant or seed or to a harvested food crop a fungicidally effective amount of a compound of the general formula (1), and fungicidals compositions containing these compounds. | ||||||
| 358 | COMPOSITION AND SYNTHESIS OF NEW REAGENTS FOR INHIBITION OF HIV REPLICATION | PCT/US2006039228 | 2006-10-06 | WO2007044565A2 | 2007-04-19 | RANA TARIQ M |
| The present invention provides compounds and compositions for inhibiting Vif and methods for treating viral infection, e.g., HIV infection. | ||||||
| 359 | ACYCLIC 1,4-DIAMINES AND USES THEREOF | PCT/US2006035156 | 2006-09-08 | WO2007030761A2 | 2007-03-15 | JEONG JAE U; MARQUIS ROBERT W |
| This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain acyclic diamines, which are agonists of TRPV4 channel receptors. | ||||||
| 360 | ARYL ALKYL ACID DERIVATIVES FOR AND USE THEREOF | PCT/US2006015194 | 2006-04-18 | WO2006113919A3 | 2006-11-30 | SMITH ROGER; LOWE DEREK; COISH PHILIP; CAMPBELL ANN-MARIE; WANG GAN; PATEL MANOJ; BONDAR GEORGIY |
| This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases. | ||||||
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