Robert T Mcdowell

US Patent:

6339082, Jan 15, 2002

Filed:

Jun 29, 2000

Appl. No.:

09/509327

Inventors:

Denis Carniato - Cagnes sur Mer, FR
Thomas R. Gadek - Oakland CA
Jean-Francois Gourvest - Claye-Souilly, FR
Jochen Knolle - Kriftel, DE
Robert S. McDowell - San Francisco CA
Anurschirwan Peyman - Kelkheim, DE

Assignee:

Aventis Pharma S.A.
Genetech, Inc.

International Classification:

C07D23352

US Classification:

514218, 514272, 514275, 514303, 514392, 514393, 514395, 514398, 514510, 514569, 514616, 514621, 514632, 514634, 540492, 540553, 544317, 544332, 546118, 5483074, 5483027, 5483215, 560 61, 562461, 564155, 564169, 564251

Abstract:

A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification and its salts with non-toxic pharmaceutically acceptable acids and bases useful for treating loss of bone matrix.

US Patent:

6344439, Feb 5, 2002

Filed:

Jul 26, 2000

Appl. No.:

09/626302

Inventors:

Kazuyuki Kitamura - Saitama, JP
Osamu Komiyama - Tokyo, JP
Mizuho Inazu - Saitama, JP
Roland Baron - Paris, FR
Thomas R. Gadek - Oakland CA
Jochen Knolle - Kriftel, DE
Hans-Ulrich Stilz - Frankfurt am Main, DE
Volkmar Wehner - Sandberg, DE
Robert S. McDowell - San Francisco CA

Assignee:

Aventis Pharma S.A. - Puteaux

International Classification:

A61K 3800

US Classification:

514 2, 514 12, 514 21, 514 16, 514 17, 514 18, 530300, 530329, 530330, 530331

Abstract:

The object is to provide a promoting agent for bone formation, a therapeutic method for bone formation and a process for preparing a promoting agent for bone formation. A promoting agent for bone formation which comprises at least one of kistrin, echstatin, a peptide or polypeptide containing the amino acid sequence ArgGlyAsp in the molecule such as a peptide represented by Gly-Arg-Gly-Asp-Ser or a compound represented by the following general formula (IX) and so on, as well as a biologically acceptable salt thereof wherein R represents âN(R ) (R represents a hydrogen atom or a C -C alkyl group), R represents a hydrogen atom or a C -C alkyl group, R represents a hydrogen atom, a C -C alkyl group and so on, R represents OH, NH and so on, Y represents âNHâ, âOâ or a direct bond, a represents 1-3, b represents 1 or 2, c represents 0 or 1 and d represents 0 or 1.

US Patent:

6387895, May 14, 2002

Filed:

Feb 6, 2001

Appl. No.:

09/777011

Inventors:

Volkmar Wehner - Sandberg, DE
Hans Ulrich Stilz - Frankfurt, DE
Anuschirwan Peyman - Kelkheim, DE
Jochen Knolle - Kriftel, DE
Jean-Marie Ruxer - Issy Ies Moulineaux, FR
Denis Carniato - Marcoussis, FR
Jean-Michel Lefrancois - Livry Gargan, FR
Thomas Richard Gadek - Oakland CA
Robert McDowell - San Francisco CA

Assignee:

Hoechst Aktiengesellschaft - Frankfurt am Main
Genentech, Inc. - San Francisco CA

International Classification:

A61K 31551

US Classification:

514220, 540497

Abstract:

The present invention relates to compounds of the formula I in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

US Patent:

6399620, Jun 4, 2002

Filed:

Jun 29, 2000

Appl. No.:

09/606080

Inventors:

Volkmar Wehner - Sandberg, DE
Jochen Knolle - Kriftel, DE
Hans Ulrich Stilz - Frankfurt, DE
Jean-Francois Gourvest - Biberonne, FR
Denis Carniato - Clamart, FR
Thomas Richard Gadek - Oakland CA
Robert McDowell - San Francisco CA
Robert Maurice Pitti - El Cerrito CA
Sarah Catherine Bodary - San Bruno CA

Assignee:

Aventis Pharma S.A. - Frankfurt

International Classification:

A61K 31505

US Classification:

514256, 514 86, 514183, 514241, 514242, 514245, 514269, 514272, 514274, 514275, 544179, 544182, 544198, 544209, 544212, 544215, 544216, 544217, 544218, 544219, 544238, 544243, 544294, 544295, 544296, 544297, 544310, 544312, 544315, 544316, 544318, 544321, 544330, 544331, 544332, 544319, 544333, 544335

Abstract:

There are described cycloalkyl derivatives of the formula (I) in which R , Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.

US Patent:

6459001, Oct 1, 2002

Filed:

Jan 25, 2001

Appl. No.:

09/769018

Inventors:

Serge Bernard - Le Plessis Belleville, FR
Denis Carniato - Marcoussis, FR
Jean-Francois Gourvest - Claye-Souilly, FR
Jean-Georges Teutsch - Pantin, FR
Jochen Knolle - Kriftel, DE
Hans-Ulrich Stilz - Frankfurt am Main, DE
Volkmar Wehner - Sandberg, DE
Sarah C. Bodary - San Bruno CA
Thomas R. Gadek - Oakland CA
Robert S. McDowell - San Francisco CA
Robert M. Pitti - El Cerrito CA

Assignee:

Aventis Pharma S.A.
Genetech

International Classification:

C07C25182

US Classification:

568326, 560 34, 562439, 564 20, 564 21, 564 36, 564 81, 564163

Abstract:

The subject of the invention is the products of formula (I): in which R , R , R , R , R and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

US Patent:

6482821, Nov 19, 2002

Filed:

Feb 8, 2001

Appl. No.:

09/778755

Inventors:

Volkmar Wehner - Sandberg, DE
Hans Ulrich Stilz - Frankfurt, DE
Anuschirwan Peyman - Kelkheim, DE
Karlheinz Scheunemann - Liederbach, DE
Jean-Marie Ruxer - Issy les Moulineaux, FR
Denis Carniato - Marcoussis, FR
Jean-Michel Lefrancois - Livry Gargan, FR
Thomas Richard Gadek - Oakland CA
Robert McDowell - San Francisco CA

Assignee:

Hoechst Aktiengellschaft - Frankfurt am Main
Genentech, Inc. - South Sanm Francisco CA

International Classification:

A01N 4362

US Classification:

514219, 540494, 540497, 514221

Abstract:

Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I, in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

US Patent:

6492356, Dec 10, 2002

Filed:

Nov 2, 2000

Appl. No.:

09/581915

Inventors:

Anuschirwan Peyman - Kelkheim, DE
Jochen Knolle - San Francisco CA
Gerhard Breipohl - Frankfurt, DE
Karl-Heinz Scheunemann - Liederbach, DE
Denis Carniato - Marcoussis, FR
Jean-Francois Gourvest - Claye Souilly, FR
Thomas Gadek - Oakland CA
Robert McDowell - San Francisco CA
Sarah Catherine Bodary - San Bruno CA
Robert Andrew Cuthbertson - North Fitzroy, AU
Napoleane Ferrara - San Francisco CA

Assignee:

Aventis Pharma Deutschland GmbH - Frankfurt am Main
Genentech, Inc. - South San Francisco CA

International Classification:

A61K 3155

US Classification:

514218, 514275, 514398, 514399, 540470, 544297, 544330, 544335, 5483315, 5483471, 5483481

Abstract:

The present invention relates to acylguanidine derivatives of formula (I) in which R , R , R , R , R , A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.

US Patent:

6525022, Feb 25, 2003

Filed:

Sep 16, 1998

Appl. No.:

09/154390

Inventors:

David G. Lowe - Brisbane CA
Brian C. Cunningham - Piedmont CA
David Oare - Belmont CA
Robert S. McDowell - San Francisco CA
John P. Burnier - Pacifica CA

Assignee:

Genentech, Inc. - South San Francisco CA

International Classification:

A61K 3812

US Classification:

514 11, 514 12, 530317, 530324, 530327, 435 691

Abstract:

Human receptor selective atrial natriuretic factor variants containing various substitutions, especially G16R, show equal potency and binding affinity for the human A-receptor but have decreased affinity for the human clearance or C-receptor. These ANF variants have natriuretic, diuretic and vasorelaxant activity but have increased metabolic stability, making them suitable for treating congestive heart failure, acute kidney failure and renal hypertension.