公开(公告)号：US07417170B2

公开(公告)日：2008-08-26

申请号：US11294449

申请日：2005-12-06

Applicant: Wolfgang Hell ,  Markus Kegel ,  Bernhard Akteries ,  Helmut Buschmann ,  Jorg Holenz ,  Harmut Loebermann ,  Detlef Heller ,  Hans-Joachim Drexler ,  Stefan Gladow

Inventor： Wolfgang Hell ,  Markus Kegel ,  Bernhard Akteries ,  Helmut Buschmann ,  Jorg Holenz ,  Harmut Loebermann ,  Detlef Heller ,  Hans-Joachim Drexler ,  Stefan Gladow

IPC: C07C209/70

CPC classification number: C07C209/70 ,  C07C213/08 ,  C07C211/27 ,  C07C211/28 ,  C07C215/54 ,  C07C217/62

Abstract: Methods for the dehydration of substituted 1-amino-3-aryl-butan-3-ol compounds for the preparation of substituted 3-aryl-butyl-amine compounds.

Abstract translation: 用于制备取代的3-芳基 - 丁基胺化合物的取代的1-氨基-3-芳基 - 丁-3-醇化合物脱水的方法。

公开(公告)号：US20070213405A1

公开(公告)日：2007-09-13

申请号：US11646232

申请日：2006-12-28

Applicant: Andreas Fischer ,  Helmut Buschmann ,  Michael Gruss ,  Dagmar Lischke

Inventor： Andreas Fischer ,  Helmut Buschmann ,  Michael Gruss ,  Dagmar Lischke

IPC: A61K31/137 ,  C07C215/28

CPC classification number: C07C213/10 ,  C07B2200/07 ,  C07B2200/13 ,  C07C215/54

Abstract: A novel crystalline form of a (−)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride compound, methods of producing the compound, and related methods of use including treatment methods and pharmaceutical compositions containing the compound.

Abstract translation: （ - ） - （1R，2R）-3-（3-二甲基氨基-1-乙基-2-甲基丙基） - 苯酚盐酸盐化合物的新结晶形式，该化合物的制备方法及相关使用方法，包括处理方法 和含有该化合物的药物组合物。

公开(公告)号：US20070173533A1

公开(公告)日：2007-07-26

申请号：US11698195

申请日：2007-01-26

Applicant: Joerg Holenz ,  Helmut Buschmann ,  Michael Finkam

Inventor： Joerg Holenz ,  Helmut Buschmann ,  Michael Finkam

IPC: A61K31/453 ,  A61K31/452 ,  C07D405/02 ,  C07D409/02 ,  A61K31/445 ,  C07D211/54

CPC classification number: C07D405/06 ,  C07D211/42 ,  C07D409/06

Abstract: Substituted 3-phenylpiperidine compounds corresponding to Formula I in which R1 and R2 have the meanings defined in the specification, methods for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting various conditions, especially pain.

Abstract translation: 对应于式I的取代的3-苯基哌啶化合物，其中R1和R2具有本说明书中定义的含义，制备这些化合物的方法，含有这些化合物的药物组合物，以及这些化合物用于治疗或抑制各种病症，特别是疼痛的用途。

公开(公告)号：US07235693B2

公开(公告)日：2007-06-26

申请号：US10972773

申请日：2004-10-26

Applicant: Helmut Buschmann ,  Wolfgang Hell ,  Markus Kegel

Inventor： Helmut Buschmann ,  Wolfgang Hell ,  Markus Kegel

IPC: C07C211/00

CPC classification number: C07B39/00 ,  C07B2200/07 ,  C07C17/16 ,  C07C213/08 ,  C07C2601/14 ,  C07C217/74

Abstract: The present invention relates to a process for converting a tertiary OH group of an organic compound into a tertiary Cl group of the organic compound by using a solvent selected from the group comprising toluene, o-xylene, m-xylene, p-xylene and mixtures thereof, and thionyl chloride as the chlorinating agent.

Abstract translation: 本发明涉及通过使用选自甲苯，邻二甲苯，间二甲苯，对二甲苯和混合物的溶剂将有机化合物的叔OH基转化为有机化合物的叔C1的方法 和亚硫酰氯作为氯化剂。

公开(公告)号：US20060142321A1

公开(公告)日：2006-06-29

申请号：US11048991

申请日：2005-02-02

Applicant: Antoni Jover ,  Susana Yenes Minguez ,  Jose Mas Prio ,  Luz Romero Alonso ,  Alberto Dordal Zueras ,  Helmut Buschmann

Inventor： Antoni Jover ,  Susana Yenes Minguez ,  Jose Mas Prio ,  Luz Romero Alonso ,  Alberto Dordal Zueras ,  Helmut Buschmann

IPC: C07D471/06 ,  A61K31/473

CPC classification number: C07D221/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  Y10S514/914 ,  Y10S514/923

Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.

Abstract translation: 本发明涉及对5-HT 7受体具有药理活性的化合物，更具体地涉及一些约2,2a，4,5-四氢-1H-3-氮杂 - 苊烯取代的磺酰胺化合物，制备这些化合物的方法， 包括它们的药物组合物，以及其用于治疗和/或预防其中涉及5-HT的疾病如CNS障碍的用途。

公开(公告)号：US20060135787A1

公开(公告)日：2006-06-22

申请号：US11041638

申请日：2005-01-24

Applicant: Antoni Jover ,  Helmut Buschmann ,  Stefan Dahmen ,  Matthias Lormann

Inventor： Antoni Jover ,  Helmut Buschmann ,  Stefan Dahmen ,  Matthias Lormann

IPC: C07D409/02

CPC classification number: C07D409/06

Abstract: A process is described for the preparation of a precursor alcohol of (±)-2-[thienyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethyletanamine and in general for thienylazolylalcoxyethanamines and their enantiomers. The process involves asymmetric addition of a metalated thienyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield the corresponding pharmaceutically active thienylazolylalcoxyethanamines.

Abstract translation: 描述了制备（±）-2- [噻吩基（1-甲基-1H-吡唑-5-基）甲氧基] -N，N-二甲基乙胺的前体醇的方法，通常用于噻吩并噻唑基醛乙氧基胺及其对映异构体。 该方法包括在手性配体的存在下将金属化噻吩试剂不对称加成到吡唑甲醛中以产生手性醇。 手性醇进一步O-烷基化，得到相应的药学活性噻吩并噻唑基乙醇胺。

公开(公告)号：US07064236B2

公开(公告)日：2006-06-20

申请号：US10751585

申请日：2004-01-05

Applicant: Bernd Sundermann ,  Corinna Sundermann ,  Helmut Buschmann ,  Babette-Yvonne Koegel

Inventor： Bernd Sundermann ,  Corinna Sundermann ,  Helmut Buschmann ,  Babette-Yvonne Koegel

IPC: C07C215/42 ,  C07C215/46 ,  C07C215/48 ,  C07C211/01 ,  C07C211/16

CPC classification number: C07C211/28 ,  C07C211/26 ,  C07C211/29 ,  C07C2601/16

Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.

Abstract translation: 本发明涉及取代的1-芳基 - 丁-3-烯胺和1-芳基 - 丁-2-烯胺化合物，其制备方法，含有所述化合物的药物及其在制备药物中的用途。

公开(公告)号：US20060040978A1

公开(公告)日：2006-02-23

申请号：US10920738

申请日：2004-08-18

Applicant: Antoni Torrens Jover ,  Josep Mas Prio ,  Susana Yenes Minguez ,  Monica Garcia Lopez ,  Alberto Dordal Zueras ,  Luz Romero Alonso ,  Helmut Buschmann

Inventor： Antoni Torrens Jover ,  Josep Mas Prio ,  Susana Yenes Minguez ,  Monica Garcia Lopez ,  Alberto Dordal Zueras ,  Luz Romero Alonso ,  Helmut Buschmann

IPC: C07D217/12 ,  A61K31/47 ,  C07D403/02 ,  A61K31/4709

CPC classification number: C07D217/04 ,  C07D401/12

Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.

Abstract translation: 本发明涉及对5-HT7受体具有药理活性的化合物，更具体地说涉及一些四氢异喹啉取代的磺酰胺化合物，这些化合物的制备方法，包含它们的药物组合物及其用于治疗和/ 涉及5-HT的疾病，如CNS疾病。

公开(公告)号：US06998409B2

公开(公告)日：2006-02-14

申请号：US10704200

申请日：2003-11-10

Applicant: Bernd Sundermann ,  Corinna Sundermann ,  Helmut Buschmann ,  Barbara Heller

Inventor： Bernd Sundermann ,  Corinna Sundermann ,  Helmut Buschmann ,  Barbara Heller

IPC: A61K31/4439 ,  C07D401/02

CPC classification number: A61K31/38 ,  A61K31/13 ,  A61K31/132 ,  A61K31/165 ,  A61K31/404 ,  A61K31/425

Abstract: Substituted 2-pyridine cyclohexane-1,4-diamine compounds, a method for their production, pharmaceutical compositions containing them, and the use of such substituted 2-pyridine cyclohexane-1,4-diamine compounds for treating pain and various other medical conditions.

Abstract translation: 取代的2-吡啶环己烷-1,4-二胺化合物，其制备方法，含有它们的药物组合物，以及这些取代的2-吡啶环己烷-1,4-二胺化合物用于治疗疼痛和各种其它医学病症的用途。

公开(公告)号：US20050222135A1

公开(公告)日：2005-10-06

申请号：US10953432

申请日：2004-09-29

Applicant: Helmut Buschmann ,  Bonifacio Gutierrez Silva ,  Joerg Holenz ,  Antonio Farre Gomis

Inventor： Helmut Buschmann ,  Bonifacio Gutierrez Silva ,  Joerg Holenz ,  Antonio Farre Gomis

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/485 ,  A61K31/5517 ,  A61K31/5513 ,  A61K31/445 ,  A61K31/454

CPC classification number: A61K31/4164 ,  A61K31/415 ,  A61K31/485 ,  A61K31/5517 ,  A61K2300/00

Abstract: The present invention relates to an active substance combination comprising at least one substituted carbinol compound and at least one opioid, a medicament comprising said active substance combination, a pharmaceutical formulation comprising said active substance combination and the use of said active substance combination for the manufacture of a medicament.

Abstract translation: 本发明涉及包含至少一种取代的甲醇化合物和至少一种阿片样物质的活性物质组合物，包含所述活性物质组合物的药物，包含所述活性物质组合的药物制剂和所述活性物质组合物用于制备 药物。