Isidoros Vlattas

7291635, Nov 6, 2007

Apr 2, 2003

10/510026

Gary Mark Coppola - Budd Lake NJ, US
John William Davies - Winchester MA, US
Yu-Chin Li - Edison NJ, US
James Richard Wareing - Stow MA, US
Donald Mark Sperbeck - Berkeley Heights NJ, US
Travis Mathew Stams - Stow MA, US
Sidney Wolf Topiol - Fair Lawn NJ, US
Isidoros Vlattas - Summit NJ, US

Novartis AG - Basel

A61K 31/433
C07D 285/10

514362, 548135

Compounds of the formula.

20040023974, Feb 5, 2004

Apr 2, 2003

10/405728

Gary Coppola - Budd Lake NJ, US
John Davies - Montclair NJ, US
Charles Jewell - Sudbury MA, US
Yu-Chin Li - Edison NJ, US
James Wareing - Randolph NJ, US
Donald Sperbeck - Berkeley Heights NJ, US
Travis Stams - Belle Mead NJ, US
Sidney Topiol - Fair Lawn NJ, US
Isidoros Vlattas - Summit NJ, US

A61K031/501
A61K031/4439
A61K031/435
C07D417/04

514/252050, 514/341000, 514/362000, 544/238000, 546/268700, 548/135000

Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

20080139576, Jun 12, 2008

Sep 24, 2007

11/860034

Gary Mark Coppola - Budd Lake NJ, US
John William Davies - Montclair NJ, US
Charles Francis Jewell - Sudbury MA, US
Yu-Chin Li - Edison NJ, US
James Richard Wareing - Randolph NJ, US
Donald Mark Sperbeck - Berkeley Heights NJ, US
Travis Matthew Stams - Belle Mead NJ, US
Sidney Wolf Topiol - Fair Lawn NJ, US
Isidoros Vlattas - Summit NJ, US

A61K 31/497
C07D 285/10
C07D 403/02
A61K 31/47
A61P 3/00
C07D 215/00
A61K 31/41

51425403, 548134, 514362, 544367, 546153, 514312

Compounds of the formulaprovide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

44605080, Jul 17, 1984

Sep 13, 1982

6/417747

Isidoros Vlattas - Summit NJ

Ciba-Geigy Corporation - Ardsley NY

C07D24304
A61K 31495

2602456

5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e. g. , R. sub. 1, R. sub. 2 and R. sub. 4 are hydrogen, R. sub. 3 is methyl and C. sub. n H. sub. 2n is CH. sub. 2 CH. sub. 2, have neurcleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.

44592329, Jul 10, 1984

Sep 13, 1982

6/417746

Isidoros Vlattas - Summit NJ

Ciba-Geigy Corporation - Ardsley NY

C07D24304
C07D40304
A61K 31495

2602456

5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e. g. , R. sub. 1, R. sub. 2 and R. sub. 4 are hydrogen, R. sub. 3 is methyl and C. sub. n H. sub. 2n is CH. sub. 2 CH. sub. 2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.

40779793, Mar 7, 1978

Feb 4, 1977

5/765577

Isidoros Vlattas - Summit NJ

Ciba-Geigy Corporation - Ardsley NY

C07D33348
A01N 900

2603321

7-[3. alpha. -(3-hydroxy-3-hydrocarbylpropyl, or -1-propenyl, or 1-propynyl)-4-hydroxy-tetrahydro-2. beta. -thienyl]-heptanoic or 5-heptenoic acids, sulfoxides, sulfones, esters or salts thereof are stable, prostaglandin-like acting and antiasthmatic agents.

45004722, Feb 19, 1985

Aug 9, 1982

6/406760

Isidoros Vlattas - Summit NJ

Ciba-Geigy Corporation - Ardsley NY

C07D51307

2602455

5-Diazacycloalkyl-imidazo[2,1-b][1,3,5] benzothiadiazepines, e. g. those of the formula ##STR1## R. sub. 1, R. sub. 2 =H or alkyl R. sub. 4 =H, alkyl or HO--alkyl; R. sub. 5 =H, alkyl, alkoxy, halo or CF. sub. 3 ; p=0 to 2 the N-oxides and salts thereof are neuroleptic agents, lacking extrapyramidal side-effects.

45073112, Mar 26, 1985

Apr 23, 1984

6/602649

Isidoros Vlattas - Summit NJ

Ciba-Geigy Corporation - Ardsley NY

A61K 31415
C07D48704

260239BD

5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e. g. , R. sub. 1, R. sub. 2 and R. sub. 4 are hydrogen, R. sub. 3 is methyl and C. sub. n H. sub. 2n is CH. sub. 2 CH. sub. 2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.