公开(公告)号：EP0886637A1

公开(公告)日：1998-12-30

申请号：EP96903604

申请日：1996-02-01

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： WETTERAU JOHN R II ,  SHARP DARU YOUNG ,  GREGG RICHARD E ,  BILLER SCOTT A ,  DICKSON JOHN A ,  LAWRENCE R MICHAEL ,  MAGNIN DAVID R ,  POSS MICHAEL A ,  ROBL JEFFREY A ,  SULSKY RICHARD B ,  TINO JOSEPH A ,  LAWSON JOHN E ,  HOLAVA HENRY M ,  PARTYKA RICHARD A

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  C07D401/06 ,  C07D405/04 ,  C07D409/04

CPC classification number: C07D401/04 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  G01N2800/044

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure (a, b, c or d) wherein R1 to R6, Q, and X are as defined herein.

公开(公告)号：EP1024804A4

公开(公告)日：2001-03-21

申请号：EP98918680

申请日：1998-04-23

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： GREGG RICHARD E ,  WETTERAU JOHN R II

IPC: A61K31/07 ,  A61K31/12 ,  A61K31/355 ,  A61K31/4184 ,  A61K31/4462 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/495 ,  A61K31/59 ,  A61K45/06 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P43/00 ,  A61K31/075 ,  A61K31/34 ,  A61K31/445 ,  A61K31/50 ,  A61P9/00

CPC classification number: A61K45/06 ,  A61K31/07 ,  A61K31/12 ,  A61K31/20 ,  A61K31/355 ,  A61K31/59

Abstract: A pharmaceutical combination formed of an MTP inhibitor and a fat soluble vitamin such as Vitamins E, A, K and/or D, and optionally another cholesterol lowering drug, is provided which is employed in a method for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting or treating atherosclerosis, pancreatitis, hyperglycemia and/or obesity.

公开(公告)号：EP1014791A4

公开(公告)日：2001-03-21

申请号：EP97933435

申请日：1997-07-14

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： GREGG RICHARD E ,  POULEUR HUBERT G ,  WETTERAU JOHN R II

IPC: A61K31/22 ,  A61K31/351 ,  A61K31/38 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K45/06 ,  A61P3/06 ,  A01N43/16 ,  A01N43/18 ,  A01N43/40 ,  A61K31/35 ,  A61P9/00

CPC classification number: A61K45/06 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/365 ,  A61K31/40 ,  A61K31/405 ,  A61K31/455 ,  A61K31/60 ,  A61K31/70 ,  A61K31/785 ,  Y10S514/824

Abstract: A method is provided for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting atherosclerosis by administering to a patient an MTP inhibitor, in combination with a cholesterol lowering drug, such as pravastatin.

公开(公告)号：AT283851T

公开(公告)日：2004-12-15

申请号：AT96903604

申请日：1996-02-01

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： WETTERAU JOHN R II ,  SHARP DARU YOUNG ,  GREGG RICHARD E ,  BILLER SCOTT A ,  DICKSON JOHN A ,  LAWRENCE R MICHAEL ,  MAGNIN DAVID R ,  POSS MICHAEL A ,  ROBL JEFFREY A ,  SULSKY RICHARD B ,  TINO JOSEPH A ,  LAWSON JOHN E ,  HOLAVA HENRY M ,  PARTYKA RICHARD A

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  C07D401/06 ,  C07D405/04 ,  C07D409/04

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure defined herein.

公开(公告)号：UY24165A1

公开(公告)日：2001-07-31

申请号：UY24165

申请日：1996-02-13

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： ROBL JEFFEREY A ,  PARTYKA RICHARD A ,  HOLAVA HENRY M ,  LAWSON JOHN E ,  TINO JOSEPH A ,  SULSKY RICHARD B ,  POSS MICHAEL A ,  MAGNIN DAVID R ,  LAWRENCE R MICHAEL ,  DICKSON JOHN ,  BILLER SCOTT A ,  GREGG RICHARD E ,  SHARP DARU YOUNG ,  II JOHN R WETTERAU

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12

Abstract: Compuestos que presentan la estructura representada en la figura 1, y sales farmacéuticamente aceptables del mismo, donde: R1 es un grupo de tipo flurenilo de estructura representada en la figura 2; Q es carbonilo o sulfito; R6 es hidrógeno o alquilo de C1-C4 o un alquenilo de C1-C4, que puede estar eventualmente sustituido. Ejemplos no limitantes de compuestos según la invención: 9-[3-[4-(2,3-dihidro-1-oxo-1H-isoindol-2-il)-1-piperidinil]propil]-N-propil-9H-fluoren-9-carboxamida; monoclorhidrato de 2,3-dihidro-2-[1-[4-oxo-4-(9-propil-9H-fluoren-9-ul)]butil]-4-piperidin]-1H-isoindol-1-ona. Estos compuestos inhiben la proteína de transferencia de triglicéridos del microsoma y, por consiguiente, son útiles para disminuir los lípidos séricos y para el tratamiento de la arterosclerosis y enfermedades relacionadas con ella.

公开(公告)号：ZA975950B

公开(公告)日：1999-01-04

申请号：ZA975950

申请日：1997-07-03

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： GREGG RICHARD E ,  POULEUR HUBERT G ,  WETTERAU JOHN R II

IPC: A61K31/22 ,  A61K31/351 ,  A61K31/38 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K45/06 ,  A61P3/06 ,  A61K

Abstract: A method is provided for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting atherosclerosis by administering to a patient an MTP inhibitor, in combination with a cholesterol lowering drug, such as pravastatin.

公开(公告)号：ZA9705950B

公开(公告)日：1999-01-04

申请号：ZA9705950

申请日：1997-07-03

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： GREGG RICHARD E ,  POULEUR HUBERT G ,  WETTERAU JOHN R II

IPC: A61K31/22 ,  A61K31/351 ,  A61K31/38 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K45/06 ,  A61P3/06 ,  A61K

CPC classification number: A61K45/06 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/365 ,  A61K31/40 ,  A61K31/405 ,  A61K31/455 ,  A61K31/60 ,  A61K31/70 ,  A61K31/785 ,  Y10S514/824

Abstract: A method is provided for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting atherosclerosis by administering to a patient an MTP inhibitor, in combination with a cholesterol lowering drug, such as pravastatin.

公开(公告)号：CA2286341A1

公开(公告)日：1998-11-12

申请号：CA2286341

申请日：1998-04-23

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： WETTERAU JOHN R II ,  GREGG RICHARD E

IPC: A61K31/07 ,  A61K31/12 ,  A61K31/355 ,  A61K31/4184 ,  A61K31/4462 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/495 ,  A61K31/59 ,  A61K45/06 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P43/00 ,  A61K31/075 ,  A61K31/34 ,  A61K31/445 ,  A61K31/50

Abstract: A pharmaceutical combination formed of an MTP inhibitor and a fat soluble vitamin such as Vitamins E, A, K and/or D, and optionally another cholesterol lowering drug, is provided which is employed in a method for lowering serum lipids, cholesterol and/or triglycerides and thereby inhibiting or treating atherosclerosis, pancreatitis, hyperglycemia and/or obesity.

公开(公告)号：LV11951A

公开(公告)日：1998-01-20

申请号：LV970171

申请日：1997-09-19

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： WETTERAU JOHN R ,  SHARP DARU YOUNG ,  GREGG RICHARD E ,  BILLER SCOTT A ,  DICKSON JOHN A ,  LAWRENCE MICHAEL R ,  MAGNIN DAVID R ,  POSS MICHAEL A ,  ROBL JEFFREY A ,  SULSKY RICHARD B ,  TINO JOSEPH A ,  LAWSON JOHN E ,  HOLAVA HENRY M ,  PARTYKA RICHARD A

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  C07D401/06 ,  C07D405/04 ,  C07D409/04

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure defined herein.

公开(公告)号：CA2213466A1

公开(公告)日：1996-08-29

申请号：CA2213466

申请日：1996-02-01

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： HOLAVA HENRY M ,  LAWSON JOHN E ,  BILLER SCOTT A ,  WETTERAU JOHN R II ,  GREGG RICHARD E ,  SULSKY RICHARD B ,  TINO JOSEPH A ,  PARTYKA RICHARD A ,  POSS MICHAEL A ,  SHARP DARU YOUNG ,  DICKSON JOHN K ,  MAGNIN DAVID R ,  LAWRENCE R MICHAEL ,  ROBL JEFFREY A

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/52 ,  A61K31/535 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D211/00 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/98 ,  C07D215/38 ,  C07D217/00 ,  C07D217/22 ,  C07D221/16 ,  C07D241/04 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D419/12 ,  C07D473/00 ,  A61K31/435 ,  A61K31/53 ,  A61K31/55

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure (a, b, c or d) wherein R1 to R6, Q, and X are as defined herein.