Claims for Patent: 7,151,114

Summary for Patent: 7,151,114

Title:	Use of substituted 2-phenylbenzimidazoles as medicaments
Abstract:	The present invention relates to the use of a substituted 2-phenylbenzimidazole of formula I ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and m have the meanings given in the claims, for the preparation of a medicament for the treatment or prevention of diseases involving glucagon receptors, as well as new compounds of formula I wherein R.sup.1 is a group of formula ##STR00002##
Inventor(s):	Streicher; Ruediger (Biberach, DE), Mack; Juergen (Biberach, DE), Walter; Rainer (Biberach, DE), Konetzki; Ingo (Warthausen, DE), Trieselmann; Thomas (Warthausen, DE), Austel; Volkhard (Biberach, DE)
Assignee:	Boehringer Ingelheim International GmbH (Ingelheim, DE)
Application Number:	10/744,830
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,151,114
Patent Claims:	1. A compound of formula IA ##STR00053## wherein R.sup.11, R.sup.12 and R.sup.13 each independently of one another denote hydrogen or halogen or C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 haloalkyl or C.sub.1 C.sub.6 haloalkoxy; R.sup.2 denotes optionally substituted C.sub.6 C.sub.10 aryl or an optionally substituted, optionally benzo- or cyclohexano-fused 5- or 6-membered heteroaryl group, wherein the substituents are selected from the group consisting of halogen, C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkylthio, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 haloalkoxy, C.sub.1 C.sub.6 alkanoyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryloxy, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkoxy, C.sub.3 C.sub.8 cycloalkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, piperidyl-C.sub.1 C.sub.6 alkyl, morpholino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkoxy)-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl, dihydroxy-C.sub.1 C.sub.6 alkyl, amino, C.sub.1 C.sub.6 alkylamino, di-(C.sub.1 C.sub.6 alkyl)-amino, C.sub.1 C.sub.6 alkanoylamino, C.sub.1 C.sub.6 alkylsulphonamino, carboxamido, carbox-C.sub.1 C.sub.6 alkylamido, carboxyl-C.sub.1 C.sub.6 alkyl, carboxyl-C.sub.1 C.sub.6 alkoxy, carboxyl, cyano, formyl, hydroxy and nitro, or denotes a carboxamide group of formula --CO--NR.sup.21R.sup.22 , wherein R.sup.21 and R.sup.22 each independently of one another denote hydrogen, C.sub.1 C.sub.6 alkyl, C.sub.2 C.sub.8 alkenyl, C.sub.4 C.sub.12 alkadienyl, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylthio-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkyl, C.sub.5 C.sub.8 cycloalkenyl, C.sub.3 C.sub.8 cycloalkyl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkoxy-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkanoyl-C.sub.1 C.sub.6 alkyl, C.sub.5 C.sub.8 cycloalkenyl-C.sub.1 C.sub.6 alkyl, adamantyl-C.sub.1 C.sub.6 alkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxycarbonylamino-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl; or one of the groups R.sup.21 and R.sup.22 denotes hydrogen or C.sub.1 C.sub.6 alkyl, and the other denotes a group of formula --(CH.sub.2).sub.n--X--Het wherein n denotes 0 or an integer from 1 to 6, X denotes CO or a single bond and if n is other than 0 may also denote O, S or NH, and Het denotes an optionally substituted 5- or 6-membered heterocyclic group; or R.sup.21 and R.sup.22 in each case form, with the enclosed nitrogen atom, an optionally substituted, optionally benzo- or cyclohexano-fused 5- or 6-membered heterocyclic ring, wherein one or two CH.sub.2 groups may be replaced by O, S or NR.sup.23, wherein R.sup.23 denotes hydrogen, C.sub.1 C.sub.6 alkyl or adamantyl-C.sub.1 C.sub.6 alkyl, R.sup.3 denotes a group of formula A--(E).sub.r--Y-- wherein A denotes a tetrazolyl group or a group of formula --COOR.sup.31, wherein R.sup.31 denotes hydrogen or C.sub.1 C.sub.6 alkyl; E denotes a C.sub.1 C.sub.6 alkylenediyl or C.sub.2 C.sub.6 alkenylenediyl group or a C.sub.2 C.sub.6 alkynylenediyl group; and Y denotes O, CO--NH, NH--CO, NH, N(CH.sub.3) or a single bond; and r denotes 0 or 1; R.sup.4 in each case independently of one another represent halogen, C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkylthio, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 haloalkoxy, C.sub.1 C.sub.6 alkanoyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryloxy, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkoxy, C.sub.3 C.sub.8 cycloalkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl or di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl; R.sup.5 denotes a hydrogen atom or R.sup.5 together with the group R.sup.2 forms a group of formula --N.dbd.CH--N.dbd.CR.sup.51--, while R.sup.51 denotes a hydrogen atom or a group of formula --NR.sup.52R.sup.53, wherein R.sup.52 and R.sup.53 each independently of one another denote hydrogen, C.sub.1 C.sub.6 alkyl, C.sub.2 C.sub.8 alkenyl, C.sub.4 C.sub.12 alkadienyl, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylthio-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkyl, C.sub.5 C.sub.8 cycloalkenyl or C.sub.3 C.sub.8 cycloalkyl-C.sub.1 C.sub.6 alkyl; and m denotes 0 or is an integer from 1 to 4. 2. The compound according to claim 1, wherein R.sup.11, R.sup.12 and R.sup.13 each independently of one another denote hydrogen or C.sub.1 C.sub.6 alkyl; R.sup.2 denotes optionally substituted phenyl, naphthyl, quinolinyl, isoquinolinyl or a 5- or 6-membered heteroaryl group selected from the group consisting of imidazolyl, pyrazolyl, furanyl, thiophenyl, thiazolyl, pyridyl, pyrimidyl and pyrazinyl, wherein the substituents are selected from the group consisting of fluorine, chlorine, bromine, C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkylthio, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 haloalkoxy, C.sub.1 C.sub.6 alkanoyl, phenyl, phenoxy, phenyl-C.sub.1 C.sub.6 alkyl, phenyl-C.sub.1 C.sub.6 alkoxy, C.sub.5 C.sub.6 cycloalkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, piperidyl-C.sub.1 C.sub.6 alkyl, morpholino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkoxy)-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl, dihydroxy-C.sub.1 C.sub.6 alkyl, amino, C.sub.1 C.sub.6 alkylamino, di-(C.sub.1 C.sub.6 alkyl)-amino, C.sub.1 C.sub.6 alkanoylamino, C.sub.1 C.sub.6 alkylsulphonylamino, aminocarbonyl, C.sub.1 C.sub.6 carboxy-C.sub.1 C.sub.6 alkyl, carboxy-C.sub.1 C.sub.6 alkoxy, carboxl, cyano, formyl, hydroxy and nitro; or denotes a carboxamide group of formula --CO--NR.sup.21R.sup.22, wherein R.sup.21 denotes hydrogen, C.sub.1 C.sub.6 alkyl, C.sub.2 C.sub.8 alkenyl, C.sub.4 C.sub.12 alkadienyl, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylthio-C.sub.1 C.sub.6 alkyl, phenyl, C.sub.5 C.sub.6 cycloalkyl, C.sub.5 C.sub.6 cycloalkenyl, C.sub.5 C.sup.8 cycloalkyl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkoxy-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkanoyl-C.sub.1 C.sub.3 alkyl, C.sub.5 C.sub.8 cycloalkenyl-C.sub.1 C.sub.3 alkyl, adamantyl-C.sub.1 C.sub.2 alkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxycarbonylamino-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl or denotes phenyl-C.sub.1 C.sub.6 alkyl R.sup.22 denotes hydrogen or C.sub.1 C.sub.3 alkyl, or one of the groups R.sup.21 and R.sup.22 denotes hydrogen or C.sub.1 C.sub.3 alkyl, and the other denotes a group of formula --(CH.sub.2).sub.n--X--Het wherein n denotes an integer from 1 to 4, X denotes CO, O, S, NH or a single bond, and Het denotes an optionally substituted 5- or 6-membered heterocyclic group selected from among imidazolyl, pyrrolidinyl, pyrrolidonyl, morpholino, furanyl, thienyl, pyridyl and pyrimidyl, while the above-mentioned heterocyclic group may be substituted by nitro or di-(C.sub.1 C.sub.6 alkoxy)-phenyl; or R.sup.21 and R.sup.22 in each case form, with the enclosed nitrogen atom, a tetrahydrobenzoazepino, morpholino, piperidyl, benzopiperidyl or cyclohexanopiperidyl group, R.sup.4 in each case independently of one another represent fluorine, chlorine, bromine, C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 haloalkyl, C.sub.1 C.sub.3 alkoxy or C.sub.1 C.sub.3-haloalkoxy, R.sup.5 denotes a hydrogen atom; and m is 0 or an integer from 1 to 2. 3. The compound according to claim 1 or 2, wherein R.sup.11 and R.sup.12 denote methyl, and R.sup.13 denotes isopropyl. 4. The compound according claim 3, wherein R.sup.2 denotes optionally substituted phenyl, naphthyl, quinolinyl, isoquinolinyl, imidazolyl, furanyl, thiophenyl, thiazolyl, pyridyl, pyrimidinyl, pyrazinyl, the substituents being selected from the group consisting of fluorine, chlorine, bromine, C.sub.1 C.sub.3 alkyl, trifluoromethyl, C.sub.1 C.sub.3 alkoxy, C.sub.1 C.sub.3 alkylthio, trifluoromethoxy, difluoromethoxy, C.sub.1 C.sub.3 alkanoyl, phenyl, phenoxy, phenyl-C.sub.1 C.sub.2 alkyl, phenyl-C.sub.1 C.sub.2 alkoxy, cyclohexyl, amino-C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 alkylamino-C.sub.1 C.sub.3 alkyl, di-(C.sub.1 C.sub.3 alkyl)-amino-C.sub.1 C.sub.3 alkyl, piperidyl-C.sub.1 C.sub.3 alkyl, morpholino-C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 alkoxy-C.sub.1 C.sub.3 alkyl, di-(C.sub.1 C.sub.3 alkoxy)-C.sub.1 C.sub.3 cyano-C.sub.1 C.sub.3 alkyl, hydroxy-C.sub.1 C.sub.3 alkyl, dihydroxy-C.sub.1 C.sub.3 alkyl, amino, C.sub.1 C.sub.3 alkylamino, di-(C.sub.1 C.sub.3 alkyl)-amino, C.sub.1 C.sub.3 alkanoylamino, C.sub.1 C.sub.3 alkylsulphonylamino, aminocarbonyl, carboxy-C.sub.1 C.sub.3 alkyl, carboxy-C.sub.1 C.sub.3 alkoxy, carboxyl, cyano, formyl, hydroxy and nitro; or denotes a carboxamide group of formula --CO--NR.sup.21R.sup.22, wherein R.sup.21 denotes hydrogen, C.sub.1 C.sub.3 alkyl, C.sub.2 C.sub.6 alkenyl, C.sub.6 C.sub.12 alkadienyl, 2,2,2-trifluoroethyl, C.sub.1 C.sub.3 alkoxy-C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 alkylthio-C.sub.1 C.sub.3 alkyl, phenyl, cyclohexyl, cyclohexenyl, cyclohexyl-C.sub.1 C.sub.3 alkyl, cyclohexyloxy-C.sub.1 C.sub.3 alkyl, cyclohexanoyl-C.sub.1 C.sub.3 alkyl, cyclohexenyl-C.sub.1 C.sub.3 alkyl, adamantyl-C.sub.1 C.sub.2 alkyl, amino-C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 alkylamino-C.sub.1 C.sub.3 alkyl, di-(C.sub.1 C.sub.3 alkyl)-amino-C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 alkoxycarbonylamino-C.sub.1 C.sub.3 alkyl, cyano-C.sub.1 C.sub.3 alkyl, hydroxy-C.sub.1 C.sub.3 alkyl; or denotes phenyl-C.sub.1 C.sub.6 alkyl; or denotes a group of formula --(CH.sub.2).sub.n--X--Het wherein n denotes an integer from 1 to 4, X denotes CO, O, S, NH or a single bond, and Het denotes imidazolyl, pyrrolidinyl, pyrrolidonyl, morpholino, furanyl, thienyl and pyridyl, which may be substituted by nitro or dimethoxyphenyl; and R.sup.22 denotes hydrogen or methyl, or R.sup.21 and R.sup.22 in each case form, with the enclosed nitrogen atom, a tetrahydrobenzoazepino, morpholino, piperidyl, benzopiperidyl or cyclohexanopiperidyl group, R.sup.4 in each case independently of one another represent fluorine, chlorine, bromine, C.sub.1 C.sub.3 alkyl, C.sub.1 C.sub.3 haloalkyl, C.sub.1 C.sub.3 alkoxy or C.sub.1 C.sub.3-haloalkoxy; R.sup.5 denotes a hydrogen atom; and m is 0 or an integer from 1 to 2. 5. A compound of formula IA1 ##STR00054## wherein R.sup.2 denotes optionally substituted C.sub.6 C.sub.10 aryl or an optionally substituted, optionally benzo- or cyclohexano-fused 5- or 6-membered heteroaryl group, wherein the substituents are selected from the group consisting of halogen, C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkylthio, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 haloalkoxy, C.sub.1 C.sub.6 alkanoyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryloxy, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkoxy, C.sub.3 C.sub.8 cycloalkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, piperidyl-C.sub.1 C.sub.6 alkyl, morpholino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkoxy)-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl, dihydroxy-C.sub.1 C.sub.6 alkyl, amino, C.sub.1 C.sub.6 alkylamino, di-(C.sub.1 C.sub.6 alkyl)-amino, C.sub.1 C.sub.6 alkanoylamino, C.sub.1 C.sub.6 alkylsulphonamino, carboxamido, carbox-C.sub.1 C.sub.6 alkylamido, carboxyl-C.sub.1 C.sub.6 alkyl, carboxyl-C.sub.1 C.sub.6 alkoxy, carboxyl, cyano, formyl, hydroxy and nitro, or denotes a carboxamide group of formula --CO--NR.sup.21R.sup.22, wherein R.sup.21 and R.sup.22 each independently of one another denote hydrogen, C.sub.1 C.sub.6 alkyl, C.sub.2 C.sub.8 alkenyl, C.sub.4 C.sub.12 alkadienyl, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 alkoxy-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylthio-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkyl, C.sub.5 C.sub.8 cycloalkenyl, C.sub.3 C.sub.8 cycloalkyl-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkoxy-C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.8 cycloalkanoyl-C.sub.1 C.sub.6 alkyl, C.sub.5 C.sub.8 cycloalkenyl-C.sub.1 C.sub.6 alkyl, adamantyl-C.sub.1 C.sub.6 alkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl, di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxycarbonylamino-C.sub.1 C.sub.6 alkyl, cyano-C.sub.1 C.sub.6 alkyl, hydroxy-C.sub.1 C.sub.6 alkyl; or one of the groups R.sup.21 and R.sup.22 denotes hydrogen or C.sub.1 C.sub.6 alkyl, and the other denotes a group of formula --(CH.sub.2).sub.n--X--Het wherein n denotes 0 or an integer from 1 to 6, X denotes CO or a single bond and if n is other than 0 may also denote O, S or NH, and Het denotes an optionally substituted 5- or 6-membered heterocyclic group; or R.sup.21 and R.sup.22 in each case form, with the enclosed nitrogen atom, an optionally substituted, optionally benzo- or cyclohexano-fused 5- or 6-membered heterocyclic ring, wherein one or two CH.sub.2 groups may be replaced by O, S or NR.sup.23, wherein R.sup.23 denotes hydrogen, C.sub.1 C.sub.6 alkyl or adamantyl-C.sub.1 C.sub.6 alkyl, R.sup.3 denotes a group of formula A--(E).sub.r--Y-- wherein A denotes a tetrazolyl group or a group of formula --COOR.sup.31, wherein R.sup.31 denotes hydrogen or C.sub.1 C.sub.6 alkyl; E denotes a C.sub.1 C.sub.6 alkylenediyl or C.sub.2 C.sub.6 alkenylenediyl group or a C.sub.2 C.sub.6 alkynylenediyl group; and Y denotes O, CO--NH, NH--CO, NH, N(CH.sub.3) or a single bond; and r denotes 0 or 1, R.sup.4 in each case independently of one another represent halogen, C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkylthio, C.sub.1 C.sub.6 haloalkyl, C.sub.1 C.sub.6 haloalkoxy, C.sub.1 C.sub.6 alkanoyl, C.sub.6 C.sub.10 aryl, C.sub.6 C.sub.10 aryloxy, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkyl, C.sub.6 C.sub.10 aryl-C.sub.1 C.sub.6 alkoxy, C.sub.3 C.sub.8 cycloalkyl, amino-C.sub.1 C.sub.6 alkyl, C.sub.1 C.sub.6 alkylamino-C.sub.1 C.sub.6 alkyl or di-(C.sub.1 C.sub.6 alkyl)-amino-C.sub.1 C.sub.6 alkyl; and m denotes 0 or is and integer from 1 to 4. 6. The compound according to claims 1 or 5, wherein the group R.sup.3 is in the meta or para position in relation to the benzimidazole group. 7. A Pharmaceutical composition comprising a compound according to claim 1 and a pharmacologically acceptable carrier. 8. The Pharmaceutical composition according to claim 7 further comprising an active substance selected from among: acarbose, beraprost, bexarotene, captopril, denileukin, diftitox, etanercept, farglitazar, fidarestat, glibenclamide, glibomuride, gliclazide, glimepiride, glipizide, glucagon, ilomastat, imidapril, insulin, lanreotide, linogliride, lisinopril, metformin, mexiletine, miglitol, minalrestat, mitiglinide, moxonidine, nafagrel, nateglinide, octreotide, orlistat, oxcarbazepine, pegvisomant, pioglitazone, ponalrestat, pramlintide, ramipril, repaglinide, rosiglitazone, sirolimus, sorbinil, tolrestat, troglitazone, voglibose, zenarestat and zopolrestat. 9. A method of treating diabetes mellitus comprising administering to a patient a pharmaceutically effective amount of a compound according to claim 1.

Details for Patent 7,151,114

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Pharmacia & Upjohn Company Llc	SOMAVERT	pegvisomant	For Injection	021106	03/25/2003		2023-01-09
Pharmacia & Upjohn Company Llc	SOMAVERT	pegvisomant	For Injection	021106	07/31/2014		2023-01-09
Eisai, Incorporated	ONTAK	denileukin diftitox	Injection	103767	02/05/1999		2023-01-09
Immunex Corporation	ENBREL	etanercept	For Injection	103795	11/02/1998		2023-01-09
Immunex Corporation	ENBREL	etanercept	For Injection	103795	05/27/1999		2023-01-09