# US 2008/0188501 A1 · Dipeptidyl peptidase inhibitors > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2008/0188501 A1 - Document ID: US20080188501A1 - Status: Published application - Kind: A1 - Application number: 11/929,737 - Filed: 2007-10-30 - Published: 2008-08-07 - Earliest claimed: 2004-03-15 - Assignees: Takeda Pharmaceutical Company Limited - Inventors: Jun Feng; Stephen L. Gwaltney; Jeffrey A. Stafford; Zhiyuan Zhang; Bruce J. Elder; Paul K. Isbester; Grant J. Palmer; Jonathon S. Salsbury; Luckner G. Ulysse - Web page: https://patentgrep.com/patent/US20080188501A1 ## CPC - C07D 403/04: directly linked by a ring-member-to-ring-member bond - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 5/02: of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin - A61P 7/06: Antianaemics - A61P 13/08: of the prostate - A61P 13/12: of the kidneys - A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis - A61P 15/16: Masculine contraceptives - A61P 15/18: Feminine contraceptives - A61P 17/06: Antipsoriatics - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 19/10: for osteoporosis - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 31/18: for HIV - A61P 35/00: Antineoplastic agents - A61P 35/04: specific for metastasis - A61P 37/02: Immunomodulators - A61P 37/04: Immunostimulants - A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection - A61P 39/02: Antidotes - C07D 239/545: with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms - C07D 401/04: directly linked by a ring-member-to-ring-member bond - C07D 401/14: containing three or more hetero rings - C07D 403/12: linked by a chain containing hetero atoms as chain links - C07D 409/14: containing three or more hetero rings - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein. ## Claims ### Claim 1 A compound having the formula wherein the compound is in crystalline form. ### Claim 2 (depends on 1) A compound according to claim 1, wherein the compound is in the same crystalline form as is formed when the compound is crystallized from methanol. ### Claim 3 A method comprising: crystallizing a compound having the formula wherein a solvent in which the crystallization is performed is methanol. ### Claim 4 A pharmaceutical composition comprising: a compound having the formula wherein the compound is in crystalline form; and one or more pharmaceutical carriers. ### Claim 5 (depends on 4) A pharmaceutical composition according to claim 4, wherein the compound is in the same crystalline form as is formed when the compound is crystallized from methanol. ### Claim 6 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is a pill or capsule adapted for oral administration. ### Claim 7 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is in an oral dosage form selected from the group consisting of pills, tablets, capsules, emulsions, suspensions, wafers, sprinkles, chewing gum, powders, granules, and troches. ### Claim 8 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is in a parenteral dosage form selected from the group consisting of solutions, suspensions, emulsions, and solid forms suitable for suspension or emulsification prior to injection, and for implantable devices. ### Claim 9 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is adapted for topical or transdermal administration. ### Claim 10 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is in a topical or transdermal dosage form selected from the group consisting of solutions, suspensions, emulsions, creams, gels, ointments, lotions, tinctures, pastes, foams, aerosols, irritations, sprays, suppositories, bandages, and dermal patches. ### Claim 11 (depends on 4) A pharmaceutical composition according to claim 4, wherein the pharmaceutical composition is in a pulmonary dosage form selected from the group consisting of powders and aerosols. ### Claim 12 A kit comprising: a pharmaceutical composition comprising a compound having the formula wherein the compound is in crystalline form, and one or more pharmaceutical carriers; and instructions which comprise one or more forms of information selected from the group consisting of indicating a disease state for which the pharmaceutical composition is to be administered, storage information for the pharmaceutical composition, dosing information and instructions regarding how to administer the composition. ### Claim 13 (depends on 12) A kit according to claim 12, wherein the kit comprises the pharmaceutical composition in a multiple dose form. ### Claim 14 An article of manufacture comprising: a pharmaceutical composition comprising a compound having the formula wherein the compound is in crystalline form, and one or more pharmaceutical carriers; and packaging materials. ### Claim 15 (depends on 14) An article of manufacture according to claim 14, wherein the packaging material comprises a container for housing the pharmaceutical composition. ### Claim 16 (depends on 14) An article of manufacture according to claim 14, wherein the container comprises a label indicating one or more members of the group consisting of a disease state for which the composition is to be administered, storage information, dosing information and/or instructions regarding how to administer the composition. ### Claim 17 (depends on 14) An article of manufacture according to claim 14, wherein the pharmaceutical composition is in a multiple dose form.