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公开(公告)号：EP1045908A2
公开(公告)日：2000-10-25
申请号：EP99902140.5
申请日：1999-01-08
申请人： SMITHKLINE BEECHAM CORPORATION , SMITHKLINE BEECHAM PLC , Smithkline BeechamLaboratoires Pharmaceutiques
发明人： CULP, Jeffrey, S. , MCNULTY, Dean, E. , ELLIS, Catherine, E. , DOUGLAS, Stephen, A.,B202 La Maison Apartments , WILLETTE, Robert, N. , AIYAR, Nambi, V. , ARNOLD, Anne, Romanic , KHANDOUDI, Nassirah , GOUT, Bernard , AL-BARAZANJI, Kamal
IPC分类号： C12N15/16 , C07K14/575 , C07K16/26 , A61K48/00 , A61K38/22 , C12Q1/68 , G01N33/68 , C12N15/11
CPC分类号： G01N33/74 , A61K38/00 , A61K48/00 , A61K2039/51 , C07K14/57509 , G01N33/6893
摘要： Human Urotensin II polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing Human Urotensin II polypeptides and polynucleotides in therapy, and diagnostic assays for such.
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2.发明公开USE OF A GLUCOSE UPTAKE ENHANCER FOR REDUCING POST-ISCHEMIC INJURY OF THE HEART 有权放大器葡萄糖记录的使用，减少POST缺血性损伤HERTZ
公开(公告)号：EP1098638A1
公开(公告)日：2001-05-16
申请号：EP99934911.1
申请日：1999-07-21
发明人： BRIL, Antoine Michel A.,SmithK. Beecham Lab. Ph. , BUCKINGHAM, Robin Edwin,SmithK. Beecham Pharmac. , KHANDOUDI, Nassirah,SmithKline Beecham Lab. Phar.
IPC分类号： A61K31/00 , A61K31/425 , A61K31/44
CPC分类号： A61K31/4439 , A61K31/00 , A61K31/426 , A61K31/427
摘要： A method for reducing post-ischaemic injury of the heart and/or improving the functional recovery of the heart following myocardial ischaemia which method comprises administration of an effective, non-toxic amount of a glucose uptake enhancer to a human or non-human mammal in need thereof.
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3.发明公开POLYMORPHIC N-[3-[[2-(3,4-DIMETHOXYPHENYL)ETHYL]AMINO]PROPYL]- 4-NITRO BENZAMIDE HYDROCHLORIDE 审中-公开（3,4-二甲氧基苯基）乙基氨基丙基-4-硝基苯甲酸氢氯化物
公开(公告)号：EP1218334A1
公开(公告)日：2002-07-03
申请号：EP00964535.9
申请日：2000-10-06
IPC分类号： C07C233/78 , A61K31/165 , A61P9/10 , A61P9/06
CPC分类号： C07C233/78
摘要： A polymorphic form of N-[3-[[2-(3,4-dimeth0xyphenyl)ethyl]amino]propyl]-4-nitro benzamide hydrochloride, a process for preparing such a compound and the use of such a compound in medicine.
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4.发明公开QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 AND NK-2 RECEPTOR ANTAGONISTS 审中-公开喹啉-4-甲酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：EP1131295A1
公开(公告)日：2001-09-12
申请号：EP99961001.7
申请日：1999-11-19
发明人： FARINA, C.,SmithKline Beecham S.p.A. , GIARDINA, G.,SmithKline Beecham S.p.A. , GRUGNI, M,SmithKline Beecham S.p.A. , MORVAN, M.,SmithKline Beecham Lab. Pharm. , NADLER, G M.M.G.,SmithKlineBeecham Lab.Pharm. , RAVEGLIA, Luca, Francesco
IPC分类号： C07D215/52 , A61K31/47 , C07D401/06 , C07D471/10 , C07D401/12 , C07D401/14 , C07D487/04 , C07D491/10 , C07D487/10 , C07D413/10 , C07D417/12
CPC分类号： C07D401/06 , C07D215/52 , C07D401/12 , C07D401/14 , C07D413/10 , C07D417/12 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/10
摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, R1 represents hydrogen or up to three optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety -(CH2)n-NY1Y2 wherein n is an integrer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6- alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl)amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl, R5 represents hydrogen or halogen; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.
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5.发明公开HUMAN RECEPTOR GPR14, AND A METHOD OF FINDING AGONIST AND ANTAGONIST TO HUMAN AND RAT GPR14 审中-公开人类受体GPR14和方法用于搜索激动剂和拮抗剂人和大鼠GPR14受体
公开(公告)号：EP1056844A1
公开(公告)日：2000-12-06
申请号：EP99903409.3
申请日：1999-01-27
申请人： SMITHKLINE BEECHAM CORPORATION , SMITHKLINE BEECHAM PLC , Smithkline BeechamLaboratoires Pharmaceutiques
发明人： DOUGLAS, Stephen, A.,B202 La Maison Apartments , WILLETTE, Robert, N. , AIYAR, Nambi, V. , ARNOLD, Anne, Romanic , KHANDOUDI, Nassirah , GOUT, Bernard , AL-BARAZANJI, Kamal , AMES, Robert, S. , FOLEY, James, J. , SARAU, Henry, M. , CHAMBERS, Jon , SHABON, Usman , BERGSMA, Derk, J.
CPC分类号： C07K14/705 , A61K38/00 , A61K48/00 , C07K14/723
摘要： Human GPR14 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing Human GPR14 polypeptides and polynucleotides in the design of protocols for the treatment of ischemic coronary artery disease (angina and myocardial infarction); atherosclerosis; metabolic diseases (e.g. diabetes); CHF/myocardial dysfunction; arrhythmias; restenosis; hypertension; hypotension; pulmonary disease (hypertension, COPD, asthma); fibrotic vasculopathies (diabetes, SLE, AS, Reynaud's); cerebrovascular events (e.g. hemnorrhagic and ischemic stroke); neurogenic inflammation/migraine; hematopoietic disorders; ARDS; cancer; autoimmune diseases (e.g. HIV-1 and -2 infection and AIDS); gastrointestinal and genitourinary disturbances (e.g. ulcers); endocrine disorders; fibroproliferative disorders (e.g. psoriasis); inflammatory disease (e.g. RA, Crohn's, IBS); benign prostatic hypertrophy; renal failure and glomerulopathies; disease states, both cardiovascular and non-cardiovascular, which are characterized by excessive vasoconstriction, myocardial dysfunction and/or aberrant fibroproliferative/inflammatory responses; psychotic and neurological disorders, including anxiety, schizophrenia, manic depression, delirium, dementia, severe mental retardation, Parkinson's disease, and dyskinesias, infections such as bacterial, fungal, protozoan and viral infections; pain; eating disorders, such as obesity, anorexia, and bulimia; asthma; urinary retention; oteoporosis; allergies; Huntington's disease or Gilles de la Tourette's syndrome, among others and diagnostic assays for such conditions.
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公开(公告)号：EP1042316A1
公开(公告)日：2000-10-11
申请号：EP98966951.0
申请日：1998-12-17
IPC分类号： C07D401/12 , A61K31/40 , C07D209/18
CPC分类号： C07D401/12 , C07D209/18
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents -CO-NRsRt wherein Rs and Rt each independently represents hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or alkylsulphonyl and arylsulphonyl; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.
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公开(公告)号：EP1131294A1
公开(公告)日：2001-09-12
申请号：EP99959340.3
申请日：1999-11-22
发明人： FARINA, CarloSmithKline Beecham S.p.A. , GIARDINA, GiuseppeSmithKline Beecham S.p.A. , GRUGNI, MarioSmithKline Beecham S.p.A. , NADLER, Guy M. M. G.SmithKline Beecham Lab. Phar. , RAVEGLIA, Luca FrancescoSmithKline Beecham S.p.A.
IPC分类号： C07D215/52 , A61K31/4725 , C07D401/06 , A61K31/4709 , A61P25/00 , A61P11/00 , A61K31/47
CPC分类号： C07D401/06 , C07D215/52 , C07D401/14
摘要： A compound, or a solvate or a salt thereof, of formula (I), wherein R is linear or branched alkyl; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety -(CH2)n-NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 or Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or alkyl or R4 and R together with the carbon atom to which they are attached form an optionally substituted C3-12 cycloalkyl group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds as NK-2 or NK-3 receptor ligands.
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8.发明公开USE OF A GLUCOSE UPTAKE ENHANCER FOR REDUCING APOPTOSIS 有权使用放大器葡萄糖RECORD罗格列酮，以减少缺血诱导的凋亡内皮细胞和神经细胞的胰腺β细胞
公开(公告)号：EP1098639A1
公开(公告)日：2001-05-16
申请号：EP99934914.5
申请日：1999-07-21
发明人： BRIL, Antoine, M. A.-SmithKline Beecham Lab. Pharm , BUCKINGHAM, Robin, Edwin-SmithKline Beecham Pharma , KHANDOUDI, Nassirah-SmithKline Beecham Laboratoire
IPC分类号： A61K31/00 , A61K31/425 , A61K31/44
CPC分类号： A61K31/00
摘要： A method for reducing or preventing apoptosis of differentiated cells selected from the list consisting of cardiac myocytes, pancreatic beta cells, endothelial cells and neuronal cells in the human or non-human mammal, which method comprises administration, including acute administration, of an effective, non-toxic amount of a glucose uptake enhancer to a human or non-human mammal in need thereof.
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公开(公告)号：EP1062241A1
公开(公告)日：2000-12-27
申请号：EP99915583.1
申请日：1999-03-11
发明人： CALMELS, Thierry Paul Gérard,SmithKline Beecham , SOUCHET, Michel Louis,SmithKline Beecham Labor. , MATHIAS, Stephen Lee,SmithKline Beecham
CPC分类号： C07K14/4747 , A61K38/00 , C07K2319/00
摘要： SBhfaf1 polypeptides and polynucleotides and methods for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing SBhfaf1 polypeptides and polynucleotides in therapy, and diagnostic assays for such.
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公开(公告)号：EP0975342A1
公开(公告)日：2000-02-02
申请号：EP98912303.9
申请日：1998-02-10
申请人： SMITHKLINE BEECHAMLABORATOIRES PHARMACEUTIQUES , Smithkline Beecham S.A. , SMITHKLINE BEECHAM CORPORATION
发明人： MENTION, Jacky Andre Gustave,SmithKline Beecham , SANROMA BORDALLO Jose Luis,SmithKline Beecham SA. , STORM, Kevin,SmithKline Beecham Pharmaceuticals
CPC分类号： A61K9/5084 , A61K9/0007 , A61K9/0095 , A61K9/2077 , A61K31/43 , A61K2300/00
摘要： Novel co-amoxiclav formulations are described, having reduced weight compared to existing formulations, as well as formulations comprising amoxycillin and potassium clavulanate in a ratio of 8:1 and formulations prepared from granulates of amoxycillin and granulates of amoxycillin and clavulanate.
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