John G Baran

US Patent:

6342624, Jan 29, 2002

Filed:

Jan 6, 2000

Appl. No.:

09/479280

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL

Assignee:

G. D. Searle Co. - Chicago IL

International Classification:

C07C30300

US Classification:

560 13, 514225, 514315, 514317, 514357, 514365, 514374, 514378, 514400, 514427, 514438, 514471, 514478, 514484, 514485, 514489, 514517, 514588, 514595, 514601, 514608, 514616

Abstract:

Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO wherein X is is selected from oxygen atom and methylene; wherein each of R and R is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R and R are attached may be combined with oxygen to form an N-oxide; wherein R is selected from hydrido, methyl, ethyl and isopropyl; wherein R is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R and R is independently propargyl or a propargyl-containing moiety; wherein R is cyclohexylmethyl; wherein each of R and R is independently selected from hydrido and methyl; wherein each of R and R is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

6403648, Jun 11, 2002

Filed:

Jan 17, 2001

Appl. No.:

09/761907

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL
Barbara B. Chen - Glenview IL

Assignee:

G. D. Searle Co. - Chicago IL

International Classification:

A61K 3116

US Classification:

514616, 564154

Abstract:

Compounds characterized generally as alkylaminoalkyl-terminated -alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R is selected from hydrido, methyl, ethyl and phenyl; wherein R is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R is methyl; wherein R is cyclohexylmethyl; wherein R is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R and R is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6515025, Feb 4, 2003

Filed:

Dec 4, 2000

Appl. No.:

09/729534

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

A61K 31165

US Classification:

514603, 514616

Abstract:

Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to inhibit enzymatic conversion of angiotensinogen to angiotensin I. Such enzymatic inhibition is useful to treat disorders mediated by plasma renin activity. An example of such disorders is hypertension. Compounds of particular interest are those of Formula I. wherein A is selected from CO and SO wherein X is selected from oxygen atom and methylene; wherein each of R and R is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R and R are attached may be combined with oxygen to form an N-oxide; wherein R is selected from hydrido, methyl, ethyl and isopropyl; wherein R is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R is propargyl or a propargyl-containing moiety; wherein R is cyclohexylmethyl; wherein each of R and R is independently selected from hydrido and methyl; wherein R is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R and R is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

6667414, Dec 23, 2003

Filed:

Nov 28, 2001

Appl. No.:

09/996344

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

C07C30300

US Classification:

560 13, 514225, 514315, 514317, 514357, 514365, 514374, 514378, 514400, 514427, 514438, 514471, 514478, 514484, 514485, 514489, 514517, 514588, 514595, 514601, 514608, 514616

Abstract:

Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO wherein X is selected from oxygen atom and methylene; wherein each of R and R is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R and R are attached may be combined with oxygen to form an N-oxide; wherein R is selected from hydrido, methyl, ethyl and isopropyl; wherein R is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R and R is independently propargyl or a propargyl-containing moiety; wherein R is cyclohexylmethyl; wherein each of R and R is independently selected from hydrido and methyl; wherein each of R and R is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

6777572, Aug 17, 2004

Filed:

Nov 28, 2001

Appl. No.:

09/996345

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL

Assignee:

Pharmacia Corporation (of Pfizer Inc.) - Chesterfield MO

International Classification:

C07C30300

US Classification:

560 13, 514225, 514315, 514317, 514357, 514365, 514374, 514378, 514400, 514427, 514438, 514471, 514478, 514484, 514485, 514517, 514588, 514595, 514601, 514608, 514616

Abstract:

Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO wherein X is selected from oxygen atom and methylene; wherein each of R and R is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R and R are attached may be combined with oxygen to form an N-oxide; wherein R is selected from hydrido, methyl, ethyl and isopropyl; wherein R is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R and R is independently propargyl or a propargyl-containing moiety; wherein R is cyclohexylmethyl; wherein each of R and R is independently selected from hydrido and methyl; wherein each of R and R is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

20030130522, Jul 10, 2003

Filed:

Nov 28, 2001

Appl. No.:

09/996343

Inventors:

Gunnar Hanson - Skokie IL, US
John Baran - Winnetka IL, US

International Classification:

C07D213/26
C07C311/30
C07C271/08

US Classification:

546/329000, 548/566000, 548/567000, 558/047000, 558/059000, 560/159000

Abstract:

Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SOwherein X is selected from oxygen atom and methylene; wherein each of Rand Ris a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which Rand Rare attached may be combined with oxygen to form an N-oxide; wherein Ris selected from hydrido, methyl, ethyl and isopropyl; wherein Ris selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of Rand Ris independently propargyl or a propargyl-containing moiety; wherein Ris cyclohexylmethyl; wherein each of Rand Ris independently selected from hydrido and methyl; wherein each of Rand Ris independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

20040220272, Nov 4, 2004

Filed:

May 24, 2004

Appl. No.:

10/852070

Inventors:

Gunnar Hanson - Skokie IL, US
John Baran - Winnetka IL, US

Assignee:

G.D. Searle & Co. - Chicago IL

International Classification:

A61K031/165

US Classification:

514/616000, 564/155000

Abstract:

Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SOwherein X is selected from oxygen atom and methylene; wherein each of Rand Ris a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which Rand Rare attached may be combined with oxygen to form an N-oxide; wherein Ris selected from hydrido, methyl, ethyl and isopropyl; wherein Ris selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of Rand Ris independently propargyl or a propargyl-containing moiety; wherein Ris cyclohexylmethyl; wherein each of Rand Ris independently selected from hydrido and methyl; wherein each of Rand Ris independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

US Patent:

54182492, May 23, 1995

Filed:

Jan 25, 1994

Appl. No.:

8/186356

Inventors:

Gunnar J. Hanson - Skokie IL
John S. Baran - Winnetka IL

Assignee:

G.D. Searle & Co. - Chicago IL

International Classification:

A61K 31425
C07D27704

US Classification:

514369

Abstract:

Non-peptidyl compounds characterized generally as. alpha. -succinamidoacyl aminodiols having a thiazolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.