公开(公告)号：WO2010003996A1

公开(公告)日：2010-01-14

申请号：PCT/EP2009/058724

申请日：2009-07-09

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  LINK, Paulus A. J. ,  VAN DER HULST, Marcellus M. ,  BIELENBERG, Gerhard-Wilhelm ,  VAN DEN AKKER, Cornelis R.

Inventor： LINK, Paulus A. J. ,  VAN DER HULST, Marcellus M. ,  BIELENBERG, Gerhard-Wilhelm ,  VAN DEN AKKER, Cornelis R.

IPC: A61K9/46 ,  A61K31/4178 ,  A61K31/549 ,  A61P9/04 ,  A61P9/12 ,  A61P13/12

CPC classification number: A61K31/4178 ,  A61K9/0007 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054 ,  A61K31/549 ,  A61K2300/00

Abstract: The disclosed invention relates to a method of treatment of a disorder modulated by blocking angiotensin Il (All) receptors, and particularly selected from the group consisting of hypertension, congestive heart failure, renal failure, and combinations thereof, by administering to a subject in need thereof an effective dose of an eprosartan compound. With reference to the Recommended Effective Daily Dose of 600 mg, calculated on the basis of eprosartan administered in the form of eprosartan mesylate, it has now been found that a lower dose of eprosartan can be administered when the eprosartan compound is eprosartan acid. This dose is in the range of from 410 to 490 mg, most preferably about 450 mg.

Abstract translation: 所公开的发明涉及通过对需要的受试者施用来治疗通过阻断血管紧张素II（全部）受体而调节的病症的方法，特别是选自高血压，充血性心力衰竭，肾衰竭及其组合 其为有效剂量的依普罗沙坦化合物。 参考基于以甲磺酸依普罗沙坦形式施用的依普罗沙坦计算的600mg的推荐有效日剂量现在已经发现，当依普罗沙坦化合物是依普罗沙坦酸时，可以给予较低剂量的依普罗沙坦。 该剂量在410至490mg的范围内，最优选约450mg。

公开(公告)号：WO2008087123A2

公开(公告)日：2008-07-24

申请号：PCT/EP2008/050360

申请日：2008-01-15

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  DE BRUIN, Natasja M.W.J. ,  VAN LOEVEZIJN, Arnold ,  WIJNEN, Johan ,  HERREMANS, Arnoldus H.J. ,  KRUSE, Cornelis G.

Inventor： DE BRUIN, Natasja M.W.J. ,  VAN LOEVEZIJN, Arnold ,  WIJNEN, Johan ,  HERREMANS, Arnoldus H.J. ,  KRUSE, Cornelis G.

IPC: A61K31/404 ,  A61K31/415 ,  A61K31/505 ,  A61P25/30 ,  A61K31/4045 ,  A61K31/496

CPC classification number: A61K31/404 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/496 ,  A61K31/505

Abstract: The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT 6 antagonists. These compounds are useful for the preparation of medicaments for preventing relapse into addiction, in particular relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, into relapse to addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and into relapse to certain addictive behaviors, including gambling.

Abstract translation: 本发明涉及作为5-HT 6拮抗剂的化合物及其药学上可接受的盐的新用途。 这些化合物可用于制备用于预防复发成瘾的药物，特别是复制成滥用物质，包括鸦片剂，致幻剂，吸入剂，苯环利定，苯丙胺，可卡因，大麻，尼古丁和酒精，成瘾成瘾 某些药物，包括镇静剂，安眠药和抗焦虑药物，并复发到某些上瘾行为，包括赌博。

公开(公告)号：WO2008046905A1

公开(公告)日：2008-04-24

申请号：PCT/EP2007/061194

申请日：2007-10-19

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  MÖSCHWITZER, Jan P.

Inventor： MÖSCHWITZER, Jan P.

IPC: A61K9/20 ,  A61K9/50 ,  A61K47/38 ,  A61K47/36 ,  A61K47/34

CPC classification number: A61K9/19 ,  A61K9/2027 ,  A61K9/2077 ,  A61K47/10 ,  A61K47/34

Abstract: The present invention relates to a thermostable solid composition containing nanosized micelles, the micelles containing a poorly soluble chemical substance, such as a biologically active substance, dissolved in an auxiliary material, and the micelles being embedded in a water soluble carrier. The invention further relates to a process for preparing a thermostable solid composition and to a process for preparing pharmaceutical dosage forms comprising the same.

Abstract translation: 本发明涉及含有纳米尺寸胶束的热固性固体组合物，该胶束含有溶于辅助材料中的难溶性化学物质如生物活性物质，并且胶束嵌入水溶性载体中。 本发明还涉及一种制备耐热固体组合物的方法和一种制备包含其的药物剂型的方法。

公开(公告)号：WO2008025780A1

公开(公告)日：2008-03-06

申请号：PCT/EP2007/058957

申请日：2007-08-29

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  WINSEMIUS, Antje, A. ,  VAN DEN BROECK, Pieter, W.A.J. ,  BARBATO, Luigi, M.

Inventor： WINSEMIUS, Antje, A. ,  VAN DEN BROECK, Pieter, W.A.J. ,  BARBATO, Luigi, M.

IPC: A61K31/496 ,  A61P25/18

CPC classification number: A61K31/445 ,  A61K31/00 ,  A61K31/496 ,  A61K33/00 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention is directed to the use of a bifeprunox compound for a titration kit for a titration schedule to facilitate the initiation of the treatment of at least one central nerv ous s ystem condition or disorder by administering a plurality of dosage units of a comprising a compound 7-[4-([1,1'-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)- benzoxazolone (INN bifeprunox).

Abstract translation: 本发明涉及双歧杆菌化合物在滴定试剂盒中的滴定方案在促进至少一种中枢神经系统病症或病症的治疗开始方面的用途，其通过施用多个剂量单位，包括 化合物7- [4 - （[1,1'-联苯] -3-基甲基）-1-哌嗪基] -2（3H） - 苯并恶唑酮（INN bifeprunox）。

公开(公告)号：WO2008003736A1

公开(公告)日：2008-01-10

申请号：PCT/EP2007/056792

申请日：2007-07-05

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  STOIT, Axel ,  COOLEN, Hein K.A.C. ,  VAN DER NEUT, Martina A.W. ,  KRUSE, Cornelis G.

Inventor： STOIT, Axel ,  COOLEN, Hein K.A.C. ,  VAN DER NEUT, Martina A.W. ,  KRUSE, Cornelis G.

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61P25/16 ,  A61P25/28 ,  A61P25/30 ,  A61K31/445 ,  A61K31/40

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

Abstract translation: 本发明涉及具有通式（I）的氮杂吲哚衍生物，其中符号具有说明书中给出的含义。 这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。 本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，特别是其用于给患者施用 在其中涉及烟碱受体和/或多巴胺转运蛋白的病症中的治疗效果，或者可以通过这些受体的操纵来治疗。

公开(公告)号：WO2007144418A1

公开(公告)日：2007-12-21

申请号：PCT/EP2007/055937

申请日：2007-06-15

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  GORISSEN, Henricus R.M.

Inventor： GORISSEN, Henricus R.M.

IPC: A61K9/20 ,  A61K9/48 ,  A61K31/55 ,  A61K45/08

CPC classification number: A61K9/2009 ,  A61K9/485

Abstract: The invention is related to an oral composition of Benzazepin-1-acetic acid derivatives comprising a) said active compound in an amount of between 10 and 65% of the total weight of the formulation; b) at least 10% w/w an alkaline compound or a mixture of alkaline compounds; c) optionally comprises auxiliary materials an amount of between 1% and 45% of the total weight of the formulation. The invention is further related to the above defined oral composition comprising sodium carbonate with a specific particle size and/or surface area as alkaline compound.

Abstract translation: 本发明涉及苯扎氮平-1-乙酸衍生物的口服组合物，其包含a）所述活性化合物的量为制剂总重量的10至65％; b）至少10％w / w的碱性化合物或碱性化合物的混合物; c）任选地包含辅料，其量为制剂总重量的1％至45％。 本发明进一步涉及上述定义的含有特定粒度和/或表面积的碳酸钠作为碱性化合物的口服组合物。

公开(公告)号：WO2006075020A2

公开(公告)日：2006-07-20

申请号：PCT/EP2006/050194

申请日：2006-01-13

Applicant: SOLVAY PHARMACEUTICALS B.V ,  TURSKI, Lechoslaw A. ,  VAN VLIET, Bernard J. ,  REMIE, Rene ,  VAN DER HEIJDEN, Johannes A.m. ,  TULP, Martinus Th.m.

Inventor： TURSKI, Lechoslaw A. ,  VAN VLIET, Bernard J. ,  REMIE, Rene ,  VAN DER HEIJDEN, Johannes A.m. ,  TULP, Martinus Th.m.

IPC: A61K31/551 ,  A61P27/16 ,  A61P43/00

CPC classification number: A61K31/551

Abstract: The invention relates to the use of 8,9-dimethyl-5-phenyl-11 H-1 ,3-dioxolo[4,5-h]-imidazo[1 ,2-c][2,3]benzodiazepine: tautomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of this compound and its tautomers and N-oxides, for the preparation of a pharmaceutical composition for the treatment, amelioration or prevention of dizziness, including vertigo and Meniere's disorder.

Abstract translation: 本发明涉及8,9-二甲基-5-苯基-11H-1,3-二氧杂环戊烯并[4,5-h] - 咪唑并[1,2-c] [2,3]苯并二氮杂：互变异构体和 N-氧化物，以及该化合物及其互变异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物，用于制备用于治疗，改善或预防头晕的药物组合物，包括眩晕和美尼尔氏病。

公开(公告)号：WO2006061376A1

公开(公告)日：2006-06-15

申请号：PCT/EP2005/056505

申请日：2005-12-06

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  FEENSTRA, Roelof W. ,  STOIT, Axel ,  TERPSTRA, Jan-willem ,  PRAS-RAVES, Maria L. ,  MCCREARY, Andrew C. ,  VAN VLIET, Bernard J. ,  HESSELINK, Mayke B. ,  KRUSE, Cornelis G. ,  VAN SCHARRENBURG, Gustaaf J.m.

Inventor： FEENSTRA, Roelof W. ,  STOIT, Axel ,  TERPSTRA, Jan-willem ,  PRAS-RAVES, Maria L. ,  MCCREARY, Andrew C. ,  VAN VLIET, Bernard J. ,  HESSELINK, Mayke B. ,  KRUSE, Cornelis G. ,  VAN SCHARRENBURG, Gustaaf J.m.

IPC: A61K31/423 ,  C07D263/58 ,  C07D413/12 ,  A61P25/00

CPC classification number: C07D263/58 ,  C07D413/12

Abstract: The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D 2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): Z-T-Ar wherein: Z is a fragment of the general formula (2): and wherein the other symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.

Abstract translation: 本发明涉及一组具有双重作用模式的新型芳氧基乙胺衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的部分激动作用。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 所述化合物具有通式（1）：ZT-Ar其中：Z是通式（2）的片段：其中，其它符号具有本说明书中给出的含义及其互变异构体，立体异构体和N-氧化物， 以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物。

公开(公告)号：WO2006051069A3

公开(公告)日：2006-05-18

申请号：PCT/EP2005/055808

申请日：2005-11-08

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  ERASMUS UNIVERSITY MEDICAL CENTER ROTTERDAM ,  DE WIT, Emmie ,  SPRONKEN, Monique I.J. ,  FOUCHIER, Ron A.M. ,  OSTERHAUS, Albert D.M.E.

Inventor： DE WIT, Emmie ,  SPRONKEN, Monique I.J. ,  FOUCHIER, Ron A.M. ,  OSTERHAUS, Albert D.M.E.

IPC: C12N7/04 ,  C12N5/10 ,  A61K39/145 ,  A61K48/00

Abstract: The invention relates to the field of influenza virus and the vaccination against flu. The invention provides a conditionally defective influenza virus particle having seven different influenza nucleic acid segments. The invention also provides a conditionally defective influenza virus particle lacking an influenza nucleic acid segment selected from the group of segments essentially encoding acidic polymerase (PA), the basic polymerase 1 (PB1 ) and the basic polymerase 2 (PB2). In particular, the invention provides defective influenza virus particles having seven different influenza nucleic acid segments and lacking an influenza nucleic acid segment essentially encoding acidic polymerase. Furthermore, the invention provides use of a composition comprising a defective influenza virus particle according to the invention for the production of a pharmaceutical composition directed at generating immunological protection against infection of a subject with an influenza virus, and provides a method for generating immunological protection against infection of a subject with an influenza virus comprising providing a subject in need thereof with a composition comprising such defective influenza virus particle.

公开(公告)号：WO2006027365A1

公开(公告)日：2006-03-16

申请号：PCT/EP2005/054404

申请日：2005-09-07

Applicant: SOLVAY PHARMACEUTICALS B.V. ,  KOCH, Melle ,  DEN HARTOG, Jacobus A.J. ,  KOOMEN, Gerrit-Jan ,  WANNER, Martinus J. ,  FEENSTRA, Roelof W.

Inventor： KOCH, Melle ,  DEN HARTOG, Jacobus A.J. ,  KOOMEN, Gerrit-Jan ,  WANNER, Martinus J. ,  FEENSTRA, Roelof W.

IPC: C07D473/00 ,  C07D473/40 ,  A61K31/52 ,  A61P35/02 ,  A61P29/00

CPC classification number: C07D473/00 ,  C07D473/40

Abstract: The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine -A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

Abstract translation: 本发明涉及2-取代-6-三氟甲基嘌呤衍生物作为选择性腺苷拮抗剂，特别是腺苷-A 3受体拮抗剂，用于制备这些化合物的方法和用于合成所述嘌呤衍生物的新型中间体。 化合物具有通式（1），其中符号具有说明书中给出的含义。