公开(公告)号：WO2006100181A3

公开(公告)日：2006-11-30

申请号：PCT/EP2006060589

申请日：2006-03-09

Applicant: HOFFMANN LA ROCHE ,  ABRECHT STEFAN ,  BUBENDORF ANDRE GERARD ,  GOETZOE STEPHAN ,  GRASSMANN OLAF ,  MONTAVON FRANCOIS ,  MOOG REGINA ,  ROHRER FRANZISKA ,  RUF ARMIN ,  SCALONE MICHELANGELO ,  SCHWITTER URS ,  WANG SHAONING

Inventor： ABRECHT STEFAN ,  BUBENDORF ANDRE GERARD ,  GOETZOE STEPHAN ,  GRASSMANN OLAF ,  MONTAVON FRANCOIS ,  MOOG REGINA ,  ROHRER FRANZISKA ,  RUF ARMIN ,  SCALONE MICHELANGELO ,  SCHWITTER URS ,  WANG SHAONING

IPC: C07D413/12 ,  A61K31/422 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D413/12

Abstract: The invention is concerned with (S)-l-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)- ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.

Abstract translation: 本发明涉及该化合物的（S）-1 - {[2-（5-甲基-2-苯基 - 恶唑-4-基）乙基氨基] - 乙酰基} - 吡咯烷-2-甲磺酸酯和结晶多晶型物。 该化合物及其多晶型与先前已知的化合物相比表现出优异的性质，可用作治疗与DPP-IV相关的疾病的药物。

公开(公告)号：PT2240433E

公开(公告)日：2013-04-18

申请号：PT08869959

申请日：2008-12-23

Applicant: HOFFMANN LA ROCHE

Inventor： TRUSSARDI RENE ,  GOLDBACH PIERRE ,  BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  GRASSMANN OLAF ,  SAUER INES

IPC: C07C231/22 ,  C07C233/52

公开(公告)号：PT1597239E

公开(公告)日：2008-10-10

申请号：PT04710031

申请日：2004-02-11

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

公开(公告)号：PL378561A1

公开(公告)日：2006-05-02

申请号：PL37856104

申请日：2004-02-11

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

公开(公告)号：NO20053953L

公开(公告)日：2005-08-31

申请号：NO20053953

申请日：2005-08-25

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

IPC: A61K31/517 ,  A61P35/00 ,  C07D239/94

Abstract: The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

公开(公告)号：PA8555201A1

公开(公告)日：2003-12-10

申请号：PA8555201

申请日：2002-09-25

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  GABEL ROLF-DIETER ,  HENNIG MICHAEL ,  KRIMMER SIEGFRIED ,  NEUGEBAUER GUENTER ,  PREIS WALTER ,  WIRL ALEXANDER

IPC: A61K47/04 ,  A61K9/20 ,  A61K31/403 ,  A61K47/34 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  C07D209/88

Abstract: LA PRESENTE INVENCION SE REFIERE A FORMAS PSEUDOPOLIMORFICAS DE 1-(4-CARBAZOLILOXI)-3-[2-(2-METOXIFENOXI)-ETILAMINO]-2-PROPANOL (CARVEDILOL) O DE FORMAS OPTICAMENTE ACTIVAS O SALES FARMACEUTICAMENTE ACEPTABLES DE LAS MISMAS, PROCEDIMIENTOS PARA LA PREPARACION DE LAS MISMAS Y COMPOSICIONES FARMACEUTICAS QUE LAS CONTENGAN.

公开(公告)号：PL225428B1

公开(公告)日：2017-04-28

申请号：PL37856104

申请日：2004-02-11

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

公开(公告)号：CA2600203C

公开(公告)日：2012-12-04

申请号：CA2600203

申请日：2006-03-09

Applicant: HOFFMANN LA ROCHE

Inventor： ABRECHT STEFAN ,  BUBENDORF ANDRE GERARD ,  GOETZOE STEPHAN ,  GRASSMANN OLAF ,  MONTAVON FRANCOIS ,  MOOG REGINA ,  ROHRER FRANZISKA ,  RUF ARMIN ,  SCALONE MICHELANGELO ,  SCHWITTER URS ,  WANG SHAONING

IPC: C07D413/12 ,  A61K31/422 ,  A61P3/04 ,  A61P3/10

Abstract: The invention is concerned with (S)-l-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.

公开(公告)号：CA2514977C

公开(公告)日：2010-06-22

申请号：CA2514977

申请日：2004-02-11

Applicant: HOFFMANN LA ROCHE

Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

Abstract: The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride and can be used as medicament for the treatment of hyperproliferative disorders.

公开(公告)号：BRPI0609580A2

公开(公告)日：2010-04-20

申请号：BRPI0609580

申请日：2006-03-09

Applicant: HOFFMANN LA ROCHE

Inventor： GRASSMANN OLAF ,  MOOG REGINA ,  RUF ARMIN ,  SCHWITTER URS ,  GOETZOE STEPHAN ,  MONTAVON FRANCOIS ,  ROHRER FRANZISCA ,  SCALONE MICHELANGELO ,  WANG SHAONING ,  ABRECHT STEFAN ,  BUBENDORF ANDRE GERARD

IPC: C07D413/12 ,  A61K31/422 ,  A61P3/04 ,  A61P3/10

Abstract: The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.