公开(公告)号：EP1572954A2

公开(公告)日：2005-09-14

申请号：EP03765717.8

申请日：2003-07-17

申请人： SCHERING CORPORATION

发明人： ALTMANN, Scott, W. ,  MURGOLO, Nicholas, J. ,  WANG, Lu, Quan ,  GRAZIANO, Michael, P.

IPC分类号： C12N1/00

CPC分类号： C07K14/705 ,  A01K2217/075

摘要： The present invention provides rat and mouse NPC1L1 polypeptides and polynucleotides encoding the polypeptides. Also provided are methods for detecting agonists and antagonists of NPC1L1. Inhibitors of NPC1L1 can be used for inhibiting intestinal cholesterol absorption in a subject.

公开(公告)号：EP1680189A2

公开(公告)日：2006-07-19

申请号：EP04800720.7

申请日：2004-11-03

申请人： SCHERING CORPORATION

发明人： GRAZIANO, Michael, P.

IPC分类号： A61P9/00 ,  A61P3/00 ,  A61K45/06 ,  A61K31/397

CPC分类号： A61K45/06 ,  A61K31/397 ,  A61K2300/00

摘要： The present invention provides compositions, therapeutic combinations and methods including: (a) at least one lipid modulating agent; and (b) at least one substituted azetidinone or substituted -lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols or 5α-stanols.

公开(公告)号：EP1965862A2

公开(公告)日：2008-09-10

申请号：EP06847740.5

申请日：2006-12-18

申请人： Schering Corporation

发明人： VAN HEEK, Margaret ,  HWA, Joyce, J. ,  GRAZIANO, Michael, P. ,  LACHOWICZ, Jean, E. ,  KOWALSKI, Timothy, J. ,  VELTRI, Enrico, P. ,  MCCORMICK, Kevin, D. ,  BERLIN, Michael, Y. ,  ASLANIAN, Robert, G.

IPC分类号： A61P3/04 ,  A61P3/10 ,  A61K45/06

CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K2300/00

摘要： The present invention relates to pharmaceutical compositions comprising therapeutic combinations comprising: one or more H3 antagonists/inverse agonists; one or more appetite suppressants selected from the group consisting of CBi antagonists/inverse agonists, sibutramine, phentermine and topiramate; and option one or more HMG-CoA reductase inhibitors. The invention also relates to medicaments and kits comprising the pharmaceutical compositions of the present invention, and methods of treating obesity, obesity related disorders and diabetes using the pharmaceutical compositions of the present invention.

公开(公告)号：EP1701953A1

公开(公告)日：2006-09-20

申请号：EP05705212.8

申请日：2005-01-07

申请人： SCHERING CORPORATION

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WU, Wenxue ,  WANG, Tao ,  CHIU, John, S. ,  BOGDANOWICH-KNIPP, Susan ,  PAVLOVSKY, Anastasia ,  GREENLEE, William, J. ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu ,  CHACKALAMANNIL, Samuel

IPC分类号： C07D405/06 ,  C07D307/00 ,  C07D213/00

CPC分类号： C07D417/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

摘要： A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: Chemical formula should be inserted here as it appears on the abstract in paper form. and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

公开(公告)号：EP1751144B1

公开(公告)日：2008-08-27

申请号：EP05755642.5

申请日：2005-05-25

申请人： Schering Corporation

发明人： CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan ,  CLASBY, Martin, C. ,  GREENLEE, William, J. ,  WANG, Yuguang ,  VELTRI, Enrico, P. ,  WU, Wenxue ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu

IPC分类号： C07D405/08 ,  C07D493/04 ,  A61K31/443 ,  A61K31/4433 ,  A61P9/00 ,  A61P25/28 ,  A61P11/00

CPC分类号： C07D493/04 ,  C07D405/06

摘要： A compound represented by the structural formula (Chemical formula should be inserted here as it appears on abstract in paper form) and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is -O- or -NR6- when the double-dashed line represents a single bond; X is H, -OH or -NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.

公开(公告)号：EP1751144A1

公开(公告)日：2007-02-14

申请号：EP05755642.5

申请日：2005-05-25

申请人： SCHERING CORPORATION

发明人： CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan ,  CLASBY, Martin, C. ,  GREENLEE, William, J. ,  WANG, Yuguang ,  VELTRI, Enrico, P. ,  WU, Wenxue ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu

IPC分类号： C07D405/08 ,  C07D493/04 ,  A61K31/443 ,  A61K31/4433 ,  A61P9/00 ,  A61P25/28 ,  A61P11/00

CPC分类号： C07D493/04 ,  C07D405/06

摘要： A compound represented by the structural formula (Chemical formula should be inserted here as it appears on abstract in paper form) and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is -O- or -NR6- when the double-dashed line represents a single bond; X is H, -OH or -NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.

摘要翻译： 公开了由结构式（化学式应当插入本文作为摘要以纸形式出现）的化合物及其药学上可接受的盐和溶剂，其中：R10和R34所代表的环碳之间的单点划线 连接表示单键或双键; X与Y所连接的碳之间的双点划线表示单键或无键; 当双虚线表示单键时，X是-O-或-NR6-; 当双虚线表示无键时，X是H，-OH或-NHR20; 和其他参数如本文所定义。 还公开了含有所述化合物及其作为凝血酶受体拮抗剂和大麻素受体结合剂的用途的药物组合物和组合。

公开(公告)号：EP1682140A2

公开(公告)日：2006-07-26

申请号：EP04810675.1

申请日：2004-11-09

申请人： SCHERING CORPORATION

发明人： CHACKALAMANNIL, Samuel ,  CLASBY, Martin, C. ,  GREENLEE, William, J. ,  WANG, Yuguang ,  XIA, Yan ,  VELTRI, Enrico, P. ,  CHELLIAH, Mariappan, V. ,  WU, Wenxue ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu

IPC分类号： A61K31/4525 ,  A61K31/343 ,  A61P9/00 ,  A61P29/00 ,  A61P11/00 ,  A61P35/00 ,  A61P25/28 ,  A61P13/12

CPC分类号： A61K31/4525 ,  A61K31/343 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas: or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer's disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.

公开(公告)号：EP1648223A1

公开(公告)日：2006-04-26

申请号：EP03818238.2

申请日：2003-12-16

申请人： SCHERING CORPORATION

发明人： ALTMANN, Scott, W. ,  MURGOLO, Nicholas, J. ,  WANG, Lu, Quan ,  GRAZIANO, Michael, P.

IPC分类号： A01K67/00 ,  A01K67/033

CPC分类号： C07K14/705 ,  A01K67/0276 ,  A01K2217/075 ,  A01K2227/105 ,  A01K2267/0362 ,  A61K49/0008 ,  A61K51/0427 ,  A61K51/0444 ,  A61K51/0493 ,  C12N15/8509

摘要： The present invention provides human, rat and mouse NPC1L1 polypeptides and polynucleotides encoding the polypeptides. Also provided are methods for detecting agonists and antagonists of NPC1L1. Inhibitors of NPC1L1 can be used for inhibiting intestinal cholesterol absorption in a subject.