公开(公告)号：WO2006077024A3

公开(公告)日：2006-09-08

申请号：PCT/EP2006000125

申请日：2006-01-10

Applicant: HOFFMANN LA ROCHE ,  NETTEKOVEN MATTHIAS HEINRICH ,  PLANCHER JEAN-MARC ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

Inventor： NETTEKOVEN MATTHIAS HEINRICH ,  PLANCHER JEAN-MARC ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

IPC: C07D209/40 ,  A61K31/404 ,  A61P3/04

CPC classification number: C07D401/14 ,  C07D401/12

Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， >和m如说明书和权利要求书中所定义，及其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗和/或预防与H3受体调节相关的疾病。

公开(公告)号：WO2007020213A3

公开(公告)日：2007-04-12

申请号：PCT/EP2006065167

申请日：2006-08-09

Applicant: HOFFMANN LA ROCHE ,  NETTEKOVEN MATTHIAS HEINRICH ,  ROCHE OLIVIER

Inventor： NETTEKOVEN MATTHIAS HEINRICH ,  ROCHE OLIVIER

IPC: C07D417/04 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4436 ,  A61K31/455 ,  A61P3/04 ,  A61P25/00 ,  C07D417/14

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined in the description and claims. It further relates to pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及其中R 1，R 2和R 3的式（I）化合物如说明书和权利要求中所定义。 它还涉及其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

公开(公告)号：WO0248124A2

公开(公告)日：2002-06-20

申请号：PCT/EP0114343

申请日：2001-12-06

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  DAVIDSON JAMES EDWARD PAUL ,  DAWSON CLAIRE ELIZABETH ,  GEORGE ASHLEY ROGER ,  MANSELL HOWARD LANGHAM ,  MATTEI PATRIZIO ,  MIZRAHI JACQUES ,  NETTEKOVEN MATTHIAS HEINRICH ,  PRATT ROBERT MARK ,  ROFFEY JONATHAN RICHARD ANTHON ,  ROEVER STEPHAN ,  SPECKLIN JEAN-LUC ,  STALDER HENRI ,  WILKINSON KERRY

IPC: C07D295/20 ,  A61K31/365 ,  A61K31/495 ,  A61K31/496 ,  A61P1/04 ,  A61P1/14 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P15/10 ,  A61P17/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P43/00 ,  C07D207/32 ,  C07D207/325 ,  C07D213/30 ,  C07D213/64 ,  C07D213/643 ,  C07D233/86 ,  C07D241/04 ,  C07D261/08 ,  C07D277/24 ,  C07D285/14 ,  C07D295/205 ,  C07D295/21 ,  C07D307/12 ,  C07D307/42 ,  C07D333/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

CPC classification number: C07D207/325 ,  C07D213/30 ,  C07D213/64 ,  C07D213/643 ,  C07D261/08 ,  C07D277/24 ,  C07D285/14 ,  C07D295/205 ,  C07D295/21 ,  C07D307/12 ,  C07D307/42 ,  C07D333/16 ,  C07D413/04

Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R to 4 , A , A m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

Abstract translation: 本发明涉及式（I）化合物及其可药用的盐，溶剂合物和酯，其中R 1至4 4，A 1，A 2 m和n具有重要性 它们可以以用于治疗或预防中枢神经系统疾病，心血管疾病，胃肠道疾病，糖尿病，肥胖症和睡眠呼吸暂停的药学制剂的形式使用。

公开(公告)号：WO2007131907A2

公开(公告)日：2007-11-22

申请号：PCT/EP2007054415

申请日：2007-05-08

Applicant: HOFFMANN LA ROCHE ,  NETTEKOVEN MATTHIAS HEINRICH ,  ROCHE OLIVIER

Inventor： NETTEKOVEN MATTHIAS HEINRICH ,  ROCHE OLIVIER

IPC: C07D209/40 ,  A61K31/404 ,  A61P3/04

CPC classification number: C07D403/06

Abstract: The present invention relates to compounds of formula (1) wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式（1）的化合物，其中R 1至R 4如在说明书和权利要求书中所定义，及其药学上可接受的盐。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

公开(公告)号：WO0220488A3

公开(公告)日：2002-05-16

申请号：PCT/EP0110014

申请日：2001-08-30

Applicant: HOFFMANN LA ROCHE

Inventor： BREU VOLKER ,  DAUTZENBERG FRANK ,  GUERRY PHILIPPE ,  NETTEKOVEN MATTHIAS HEINRICH ,  PFLIEGER PHILIPPE

IPC: C07D239/94 ,  A61K31/365 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/00 ,  A61P1/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P13/12 ,  A61P19/02 ,  A61P43/00 ,  C07D215/00 ,  C07D215/42 ,  C07D239/84 ,  C07D401/04 ,  C07D409/04 ,  A61K31/4706

CPC classification number: C07D401/04 ,  C07D215/42 ,  C07D239/84 ,  C07D409/04

Abstract: Compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R , R , R , R , A and A have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Abstract translation: 式（I）化合物及其可药用的盐，溶剂合物和酯，其中R 1，R 2，R 3，R 4，A 1和A 2具有 权利要求1中给出的意义可以以用于治疗或预防关节炎，心血管疾病，糖尿病，肾衰竭，进食障碍和肥胖的药物制剂的形式使用。

公开(公告)号：WO0117999A3

公开(公告)日：2001-12-06

申请号：PCT/EP0008372

申请日：2000-08-28

Applicant: HOFFMANN LA ROCHE

Inventor： HUBER TROTTMANN GERDA ,  HUNKELER WALTER ,  JAKOB-ROETNE ROLAND ,  KILPATRICK GAVIN JOHN ,  NETTEKOVEN MATTHIAS HEINRICH ,  RIEMER CLAUS

IPC: C07D213/73 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04

Abstract: The invention relates to compounds of formula (I) wherein R is a 5 or 6 membered heteroaryl group, optionally substituted and optionally linked to the pyrazole ring via an alkylene or alkenyle group, or is phenyl, optionally substituted or is -O(CH2)nphenyl, benzofuryl, indolyl or benzothiophenyl, or is -S-lower alkyl; R and R are independently from each other hydrogen, cyano or -S(O)2-phenyl; R is hydrogen, halogen or is heteroaryl or phenyl, optionally substituted -NR'R" or -O-phenyl, or is -benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl; R is -NR2, n is 0-4 and their pharmaceutically acceptable salts. These compounds are adenosine receptor ligands.

Abstract translation: 本发明涉及式（I）化合物，其中R 1是5或6元杂芳基，任选被取代并任选地通过亚烷基或烯基连接到吡唑环上，或者是苯基，任选被取代或是-O （CH 2）n苯基，苯并呋喃基，吲哚基或苯并噻吩基，或是-S-低级烷基; R 2和R 4彼此独立地为氢，氰基或-S（O）2 - 苯基; R 3是氢，卤素或是杂芳基或苯基，任选取代的-NR'R“或-O-苯基，或是 - 苯并[1,3]二氧杂环戊烯基，-1H-吲哚-5-基，萘基，苯并呋喃 -2-基，1,3,4,9-四氢-b-咔啉-2-基，哌啶-1-基，吡咯烷-1-基，哌嗪-4-基 - 甲基或吗啉基; R 5是 -NR2，n为0-4及其药学上可接受的盐，这些化合物是腺苷受体配体。

公开(公告)号：ME00116B

公开(公告)日：2010-10-10

申请号：MEP27708

申请日：2004-08-02

Applicant: HOFFMANN LA ROCHE

Inventor： PINARD EMMANUEL ,  JOLIDON SYNESE ,  NARQUIZIAN ROBERT ,  NETTEKOVEN MATTHIAS HEINRICH ,  NORCROSS ROGER DAVID ,  STALDER HENRI

IPC: C07D213/85 ,  A61P25/28 ,  C07D239/42 ,  C07D241/20 ,  C07D251/42 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D295/192 ,  C07D309/12

Abstract: Pronalazak se odnosi na jedinjenja formule (I) pri čemu su supstituentu opisani u patentnom zahtevu l. Jedinjenja mogu da se koriste u tretmanu bolesti baziranih na inhibitoru pojave glicina, kao što su psihoze, bol, neurodegenerativna disfunkcija u pamćenju i učenju, šizofrenija, demencija i druge bolesti u kojima su pogoršani kognitivni procesi, kao što su oboljenja smanjene pažnje ili Alchajmerova bolest.

公开(公告)号：MEP27708A

公开(公告)日：2010-06-10

申请号：MEP27708

申请日：2004-08-02

Applicant: HOFFMANN LA ROCHE

Inventor： JOLIDON SYNESE ,  NARQUIZIAN ROBERT ,  NETTEKOVEN MATTHIAS HEINRICH ,  NORCROSS ROGER DAVID ,  PINARD EMMANUEL ,  STALDER HENRI

IPC: A61P25/28 ,  C07D213/85 ,  C07D239/42 ,  C07D241/20 ,  C07D251/42 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D295/192 ,  C07D309/12

Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

公开(公告)号：AU2004263306B2

公开(公告)日：2010-04-22

申请号：AU2004263306

申请日：2004-08-02

Applicant: HOFFMANN LA ROCHE

Inventor： NETTEKOVEN MATTHIAS HEINRICH ,  STALDER HENRI ,  NARQUIZIAN ROBERT ,  NORCROSS ROGER DAVID ,  PINARD EMMANUEL ,  JOLIDON SYNESE

IPC: A61P25/28 ,  C07D213/85 ,  C07D239/42 ,  C07D241/20 ,  C07D251/42 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D295/192 ,  C07D309/12

Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

公开(公告)号：MY139941A

公开(公告)日：2009-11-30

申请号：MYPI20052800

申请日：2005-06-20

Applicant: HOFFMANN LA ROCHE

Inventor： MCARTHUR SILVIA GATTI ,  HERTEL CORNELIA ,  NETTEKOVEN MATTHIAS HEINRICH ,  PLANCHER JEAN-MARC ,  RAAB SUSANNE ,  ROCHE OLIVIER ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  SCHULER FRANZ

IPC: A61K31/4439 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: THE PRESENT INVENTION RELATES TO COMPOUNDS FORMULA &Igr; WHEREIN X, R¹, R², R³, R⁴ AND R⁵ ARE AS DEFINED IN THE DESCRIPTION AND CLAIMS, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, TO THE PREPARATION OF SUCH COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. THE COMPOUNDS ARE USEFUL FOR THE TREATMENT AND/OR PREVENTION OF DISEASES WHICH ARE ASSOCIATED WITH THE MODULATION OF H3 RECEPTORS.