US 2014/0275018 A1Published application

Nitrogen containing compounds

AssigneeWockhardt Limited

InventorsMahesh Vithalbhai PATEL, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Snjeev Joshi

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Abstract

Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.

Claims30

Dependent claims

A compound of Formula (I)

or a stereoisomer or a pharmaceutically acceptable salt thereof;
wherein:
R1 is:
(c) hydrogen,
(d) (CO)n—R3, or
(e) COOR4.
n is 0, 1 or 2;
R2 is:
(m) SO3M,
(n) SO2NH2,
(o) PO3M,
(p) CH2COOM,
(q) CF2COOM,
(r) CHFCOOM, or
(s) CF3;
M is hydrogen or a cation;
R3 is:
(a) hydrogen,
(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, NR5CONR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(c) CN,
(d) NR6R7,
(e) CONR6R7,
(f) NHCONR6R7,
(g) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(h) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(i) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(j) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(k) cycloalkyl substituted with C1-C6 alkyl wherein C1-C6 alkyl is further substituted with one or more substituents independently selected from OR5, NR6R7, halogen, CN, or CONR6R7, or
(l) OR8;
R4 is:
(a) hydrogen,
(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(c) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(d) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(e) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7, or
(f) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7;
R5 and R8 are each independently:
(g) hydrogen, or
(h) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, CN, CONR6R7, NR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl;
R6 and R7 are each independently:
(h) hydrogen,
(i) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR5R8, NR5R8, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(j) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(k) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(l) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(m) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8, or
(n) R6 and R7 are joined together to form a four to seven member ring.

44 more elements

Dependencies are inferred from the claim text.

Facts

Application: 14/294,364Filed 3 Jun 2014
Priority: IN 2412/MUM/201127 Aug 2011
Published: 18 Sep 2014
Term ends: Not estimatedThe source records don’t support an estimate.

Classification22 codes

A61K 31/5377
1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/167
Having aromatic rings, e.g. colchicine, atenolol, progabide: having the nitrogen of a carboxamide group directly attached to the aromatic ring,…
A61K 31/407
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: condensed with other…
A61K 31/427
Thiazoles: not condensed and containing further heterocyclic rings

Family

Application14/111,592Continuation · filed 20 Dec 2013
Application14/294,364Continuation
US 2014/0148431 A1Published application
US 8,822,450 B2Related patent
US 8,853,197 B1Related patent
US 2014/0275018 A1This patent

From the US filing history. Foreign family members aren’t listed.

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A compound of Formula (I)

or a stereoisomer or a pharmaceutically acceptable salt thereof;
wherein:
R1 is:
(c) hydrogen,
(d) (CO)n—R3, or
(e) COOR4.
n is 0, 1 or 2;
R2 is:
(m) SO3M,
(n) SO2NH2,
(o) PO3M,
(p) CH2COOM,
(q) CF2COOM,
(r) CHFCOOM, or
(s) CF3;
M is hydrogen or a cation;
R3 is:
(a) hydrogen,
(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, NR5CONR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(c) CN,
(d) NR6R7,
(e) CONR6R7,
(f) NHCONR6R7,
(g) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(h) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(i) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(j) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(k) cycloalkyl substituted with C1-C6 alkyl wherein C1-C6 alkyl is further substituted with one or more substituents independently selected from OR5, NR6R7, halogen, CN, or CONR6R7, or
(l) OR8;
R4 is:
(a) hydrogen,
(b) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR6R7, NR6R7, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(c) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(d) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7,
(e) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7, or
(f) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR6R7, halogen, CN, CONR6R7, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR6R7;
R5 and R8 are each independently:
(g) hydrogen, or
(h) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, CN, CONR6R7, NR6R7, heterocyclyl, heteroaryl, cycloalkyl or aryl;
R6 and R7 are each independently:
(h) hydrogen,
(i) C1-C6 alkyl optionally substituted with one or more substituents independently selected from halogen, OR5, CN, COOR5, CONR5R8, NR5R8, NR5COR8, heterocyclyl, heteroaryl, cycloalkyl or aryl,
(j) aryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(k) heterocyclyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(l) heteroaryl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8,
(m) cycloalkyl optionally substituted with one or more substituents independently selected from C1-C6 alkyl, OR5, NR5R8, halogen, CN, CONR5R8, SO2-alkyl, SO2-aryl, OSO2-alkyl, OSO2-aryl, or NHCONR5R8, or
(n) R6 and R7 are joined together to form a four to seven member ring.

44 more elements

Facts

Application

14/294,364Filed 3 Jun 2014

Priority

IN 2412/MUM/201127 Aug 2011

Published

18 Sep 2014

Term ends

Not estimatedThe source records don’t support an estimate.

Classification22 codes

A61K 31/5377
1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/167
Having aromatic rings, e.g. colchicine, atenolol, progabide: having the nitrogen of a carboxamide group directly attached to the aromatic ring,…
A61K 31/407
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: condensed with other…
A61K 31/427
Thiazoles: not condensed and containing further heterocyclic rings