US20070259900A1 - Polymorphs - Google Patents

Polymorphs Download PDF

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Publication number
US20070259900A1
US20070259900A1 US11/744,700 US74470007A US2007259900A1 US 20070259900 A1 US20070259900 A1 US 20070259900A1 US 74470007 A US74470007 A US 74470007A US 2007259900 A1 US2007259900 A1 US 2007259900A1
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US
United States
Prior art keywords
methyl
polymorph
butyn
quinazolin
xanthine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
US11/744,700
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English (en)
Inventor
Peter Sieger
Dirk Kemmer
Peter Kohlbauer
Thomas Nicola
Martin Renz
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38335646&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=US20070259900(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of US20070259900A1 publication Critical patent/US20070259900A1/en
Assigned to BOEHRINGER INGELHEIM INTERNATIONAL GMBH reassignment BOEHRINGER INGELHEIM INTERNATIONAL GMBH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: KOHLBAUER, PETER, RENZ, MARTIN, SIEGER, PETER, KEMMER, DIRK, NICOLA, THOMAS
Priority to US13/563,767 priority Critical patent/US20120296091A1/en
Priority to US14/462,654 priority patent/US9266888B2/en
Priority to US14/994,578 priority patent/US9493462B2/en
Priority to US15/285,871 priority patent/US9815837B2/en
Priority to US15/725,426 priority patent/US10301313B2/en
Priority to US16/373,971 priority patent/US20190233423A1/en
Priority to US16/662,406 priority patent/US11084819B2/en
Priority to US17/363,441 priority patent/US11919903B2/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Definitions

  • the invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
  • the enzyme DPP-IV also known by the name CD26, is a serine protease which promotes the cleaving of dipeptides in proteins with a proline or alanine group at the N-terminal end. DPP-IV inhibitors thereby influence the plasma level of bioactive peptides including the peptide GLP-1.
  • Compounds of this type are useful for the prevention or treatment of illnesses or conditions which are associated with an increased DPP-IV activity or which can be prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, prediabetes, or reduced glucose tolerance.
  • WO 2004/018468 describes DPP-IV inhibitors with valuable pharmacological properties.
  • One example of the inhibitors disclosed therein is 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine.
  • FIG. 1 shows the thermoanalysis of the anhydrous form A/B.
  • FIG. 2 shows a cyclic DSC diagram, in which the phase transition from ⁇ 40° C. to 120° C. and vice versa has been run through a total of 3 times.
  • FIG. 3 shows an X-ray powder diagram of the anhydrous form A.
  • FIG. 4 shows an X-ray powder diagram of the anhydrous form B.
  • FIG. 5 shows an X-ray powder diagram of polymorph C.
  • FIG. 6 shows the thermoanalysis of form C.
  • polymorph A The pure high temperature form (polymorph A), which can be obtained by heating the mixture to temperatures >40° C., melts at 206 ⁇ 3° C.
  • this form shows characteristic reflexes at the following d values: 11.49 ⁇ , 7.60 ⁇ , 7.15 ⁇ , 3.86 ⁇ , 3.54 ⁇ and 3.47 ⁇ (cf. also Table 1 and 2).
  • Anhydrous polymorph A may be prepared by
  • the low temperature form (polymorph B) is obtained by cooling to temperatures ⁇ 10° C.
  • this form shows characteristic reflexes at the following d values: 11.25 ⁇ , 9.32 ⁇ , 7.46 ⁇ , 6.98 ⁇ and 3.77 ⁇ (cf. also Table 3 and 4).
  • Anhydrous polymorph B may be prepared by
  • polymorph C shows characteristic reflexes in the X-ray powder diagram (see FIG. 5 ) at the following d values: 12.90 ⁇ , 11.10 ⁇ , 6.44 ⁇ , 3.93 ⁇ and 3.74 ⁇ (cf. also Table 5).
  • polymorph D melts at 150 ⁇ 3° C. This polymorph is obtained if polymorph C is heated to a temperature of 30-100° C. or dried at this temperature.
  • polymorph E which melts at a temperature of 175 ⁇ 3° C. Anhydrous polymorph E is formed if polymorph D is melted. On further heating, polymorph E crystallises out of the melt.
  • the polymorphs thus obtained may be used in the same way as the mixture of the two polymorphs A and B described in WO 2004/018468 for preparing a pharmaceutical composition which is suitable for treating patients with type I and type II diabetes mellitus, prediabetes or reduced glucose tolerance, with rheumatoid arthritis, obesity, or calcitonin-induced osteoporosis, as well as patients in whom an allograft transplant has been carried out.
  • These medicaments contain in addition to one or more inert carriers at least 0.1% to 0.5%, preferably at least 0.5% to 1.5% and particularly preferably at least 1% to 3% of one of the polymorphs A, B, or C.
  • FIG. 1 shows the thermoanalysis of the anhydrous form A/B.
  • Plymorph A melts at 206 ⁇ 3° C. In the DSC diagram another slightly endothermic signal can be seen at approx. 25° C. This is a fully reversible solid-solid phase transition between the two enantiotropic crystal modifications A and B.
  • the form A is the thermodynamically stable modification above this transformation temperature
  • form B is the thermodynamically stable modification below this transformation temperature.
  • FIG. 2 shows a cyclic DSC diagram, in which the phase transition from ⁇ 40° C. to 120° C. and vice versa has been run through a total of 3 times.
  • the phase transition is observed as an endothermic signal and, correspondingly, during cooling it is observed as an exothermic signal.
  • the phase transition may also be observed as an endothermic double signal or as a very broad signal while in all the other cycles the signal occurs as a very sharp endothermic or exothermic signal, depending on whether heating or cooling is taking place.
  • FIG. 3 shows an X-ray powder diagram of the anhydrous form A
  • Polymorph B is obtained by cooling form A from Example 1 to temperatures ⁇ 10° C.
  • FIG. 4 shows an X-ray powder diagram of the anhydrous form B
  • a further 78 l tert. butylmethylether are added to the suspension over 30 minutes and then it is stirred again for a further 60 minutes at 45-55° C. It is diluted to four times the volume. The suspension is slowly cooled to 15-25° C. and stirred overnight at this temperature. After the suspension has been cooled to 0-5° C. the crystals are suction filtered, washed with 2 batches tert.-butylmethylether and dried at 70° C. in the vacuum dryer.
  • FIG. 5 shows an X-ray powder diagram of polymorph C
  • Polymorph D is obtained if polymorph C from Example 3 is heated to a temperature of 30-100° C. or dried at this temperature.
  • Anhydrous polymorph E is obtained if polymorph D is melted. On further heating, polymorph E crystallises out of the melt.
  • FIG. 6 shows a thermoanalysis of form C
  • An X-ray powder diagram taken of a sample maintained at a temperature of 100° C. shows different X-ray reflexes from the starting material, suggesting that form C is a hydrate phase with stoichiometry somewhere in the region of a hemihydrate or monohydrate.
  • the temperature-controlled sample is another anhydrous modification D, which only stable under anhydrous conditions.
  • the D form melts at approx. 150° C.
  • Another anhydrous crystal modification E crystallises from the melt, and when heated further melts at approx. 175° C.
  • form A crystallises from the melt of form E is also a metastable crystal modification which occurs only at high temperatures.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
US11/744,700 2006-05-04 2007-05-04 Polymorphs Abandoned US20070259900A1 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
US13/563,767 US20120296091A1 (en) 2006-05-04 2012-08-01 Polymorphs
US14/462,654 US9266888B2 (en) 2006-05-04 2014-08-19 Polymorphs
US14/994,578 US9493462B2 (en) 2006-05-04 2016-01-13 Polymorphs
US15/285,871 US9815837B2 (en) 2006-05-04 2016-10-05 Polymorphs
US15/725,426 US10301313B2 (en) 2006-05-04 2017-10-05 Polymorphs
US16/373,971 US20190233423A1 (en) 2006-05-04 2019-04-03 Polymorphs
US16/662,406 US11084819B2 (en) 2006-05-04 2019-10-24 Polymorphs
US17/363,441 US11919903B2 (en) 2006-05-04 2021-06-30 Polymorphs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06009202 2006-05-04
EP06009202 2006-05-04

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/563,767 Continuation US20120296091A1 (en) 2006-05-04 2012-08-01 Polymorphs

Publications (1)

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US20070259900A1 true US20070259900A1 (en) 2007-11-08

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Family Applications (9)

Application Number Title Priority Date Filing Date
US11/744,700 Abandoned US20070259900A1 (en) 2006-05-04 2007-05-04 Polymorphs
US13/563,767 Abandoned US20120296091A1 (en) 2006-05-04 2012-08-01 Polymorphs
US14/462,654 Active 2027-05-25 US9266888B2 (en) 2006-05-04 2014-08-19 Polymorphs
US14/994,578 Active 2027-05-06 US9493462B2 (en) 2006-05-04 2016-01-13 Polymorphs
US15/285,871 Active US9815837B2 (en) 2006-05-04 2016-10-05 Polymorphs
US15/725,426 Active US10301313B2 (en) 2006-05-04 2017-10-05 Polymorphs
US16/373,971 Abandoned US20190233423A1 (en) 2006-05-04 2019-04-03 Polymorphs
US16/662,406 Active US11084819B2 (en) 2006-05-04 2019-10-24 Polymorphs
US17/363,441 Active 2027-05-20 US11919903B2 (en) 2006-05-04 2021-06-30 Polymorphs

Family Applications After (8)

Application Number Title Priority Date Filing Date
US13/563,767 Abandoned US20120296091A1 (en) 2006-05-04 2012-08-01 Polymorphs
US14/462,654 Active 2027-05-25 US9266888B2 (en) 2006-05-04 2014-08-19 Polymorphs
US14/994,578 Active 2027-05-06 US9493462B2 (en) 2006-05-04 2016-01-13 Polymorphs
US15/285,871 Active US9815837B2 (en) 2006-05-04 2016-10-05 Polymorphs
US15/725,426 Active US10301313B2 (en) 2006-05-04 2017-10-05 Polymorphs
US16/373,971 Abandoned US20190233423A1 (en) 2006-05-04 2019-04-03 Polymorphs
US16/662,406 Active US11084819B2 (en) 2006-05-04 2019-10-24 Polymorphs
US17/363,441 Active 2027-05-20 US11919903B2 (en) 2006-05-04 2021-06-30 Polymorphs

Country Status (24)

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US (9) US20070259900A1 (fr)
EP (2) EP2016079A1 (fr)
JP (5) JP5323684B2 (fr)
KR (2) KR101452915B1 (fr)
CN (5) CN102838599A (fr)
AR (1) AR060756A1 (fr)
AU (1) AU2007247190A1 (fr)
BR (1) BRPI0711558A2 (fr)
CA (5) CA2651089C (fr)
EA (2) EA015687B1 (fr)
EC (1) ECSP088794A (fr)
HK (3) HK1200132A1 (fr)
IL (1) IL195029A (fr)
MX (1) MX2008014024A (fr)
MY (1) MY158107A (fr)
NO (2) NO347644B1 (fr)
NZ (3) NZ573360A (fr)
PE (1) PE20080088A1 (fr)
SG (1) SG174054A1 (fr)
TW (2) TWI534147B (fr)
UA (1) UA97244C2 (fr)
UY (1) UY30320A1 (fr)
WO (1) WO2007128721A1 (fr)
ZA (1) ZA200808224B (fr)

Cited By (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060058323A1 (en) * 2004-09-11 2006-03-16 Boehringer Ingelheim International Gmbh New 8-(3-amino-piperidin-1-yl)-7-(but-2-ynyl)-xanthines, the preparation thereof and their use as pharmaceutical compositions
US20060142310A1 (en) * 2004-11-05 2006-06-29 Boehringer Ingelheim International Gmbh Process for the preparation of chiral 8-(-3-aminopiperidin-1-yl) xanthines
US20080249089A1 (en) * 2002-08-21 2008-10-09 Boehringer Ingelheim Pharma Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US20080312243A1 (en) * 2004-06-24 2008-12-18 Matthias Eckhardt Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions
WO2009021740A2 (fr) 2007-08-15 2009-02-19 Sanofis-Aventis Nouvelles tétrahydronaphtalines substituées, leurs procédés de préparation et leur utilisation comme médicaments
US7495002B2 (en) 2004-09-14 2009-02-24 Boehringer Ingelheim International Gmbh 3-methyl-7-butinyl-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7495005B2 (en) 2002-08-22 2009-02-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, their preparation and their use in pharmaceutical compositions
US20090088569A1 (en) * 2004-04-10 2009-04-02 Matthias Eckhardt 2-amino-imidazo[4,5-d]pyridazin-4-ones, their preparation, and their use as pharmaceutical compositions
US20090137801A1 (en) * 2004-02-18 2009-05-28 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
US7560450B2 (en) 2002-11-21 2009-07-14 Boehringer Ingelheim Pharma Gmbh & Co., Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
US7645763B2 (en) 2004-02-23 2010-01-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical composition
US7667035B2 (en) 2004-05-10 2010-02-23 Boehringer Ingelheim International Gmbh Imidazole derivatives, their preparation and their use as intermediates for the preparation of pharmaceutical compositions and pesticides
US7696212B2 (en) 2002-11-08 2010-04-13 Boehringer Ingelheim Pharma Gmbh And Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
WO2010086411A1 (fr) * 2009-01-29 2010-08-05 Boehringer Ingelheim International Gmbh Traitement du diabète chez des patients pédiatriques
US20110178134A1 (en) * 2008-02-07 2011-07-21 Sanofi-Aventis Novel phenyl-substituted imidazolidines, process for preparation thereof, medicaments comprising said compounds and use thereof
US20110195917A1 (en) * 2007-08-16 2011-08-11 Boehringer Ingelheim International Gmbh Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivate
WO2011107494A1 (fr) 2010-03-03 2011-09-09 Sanofi Nouveaux dérivés aromatiques de glycoside, médicaments contenants ces composés, et leur utilisation
WO2011113947A1 (fr) * 2010-03-18 2011-09-22 Boehringer Ingelheim International Gmbh Combinaisons d'agonistes de gpr119 et d'inhibiteurs de dpp-iv, linagliptine, pour le traitement du diabète et d'états apparentés
US8071583B2 (en) 2006-08-08 2011-12-06 Boehringer Ingelheim International Gmbh Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of diabetes mellitus
WO2011157827A1 (fr) 2010-06-18 2011-12-22 Sanofi Dérivés d'azolopyridin-3-one en tant qu'inhibiteurs de lipases et de phospholipases
WO2011161030A1 (fr) 2010-06-21 2011-12-29 Sanofi Dérivés de méthoxyphényle à substitution hétérocyclique par un groupe oxo, leur procédé de production et leur utilisation comme modulateurs du récepteur gpr40
WO2012004269A1 (fr) 2010-07-05 2012-01-12 Sanofi Dérivés d'acide ( 2 -aryloxy -acétylamino) - phényl - propionique, procédé de production et utilisation comme médicament
WO2012004270A1 (fr) 2010-07-05 2012-01-12 Sanofi Dérivés 1,3-propanedioxyde à substitution spirocyclique, procédé de préparation et utilisation comme médicament
WO2012010413A1 (fr) 2010-07-05 2012-01-26 Sanofi Acides hydroxy-phényl-hexiniques substitués par aryloxy-alkylène, procédé de production et utilisation comme médicament
US8106060B2 (en) 2005-07-30 2012-01-31 Boehringer Ingelheim International Gmbh 8-(3-amino-piperidin-1-yl)-xanthines, their preparation, and their use as pharmaceuticals
US8232281B2 (en) 2006-05-04 2012-07-31 Boehringer Ingelheim International Gmbh Uses of DPP-IV inhibitors
WO2012120053A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine ramifiés, procédé pour leur préparation, utilisation en tant que médicament, agents pharmaceutiques contenant ces dérivés et leur utilisation
WO2012120052A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés d'oxathiazine substitués par des carbocycles ou des hétérocycles, leur procédé de préparation, médicaments contenant ces composés et leur utilisation
WO2012120054A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine di- et tri-substitués, procédé pour leur préparation, utilisation en tant que médicament, agent pharmaceutique contenant ces dérivés et utilisation
WO2012120056A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine tétra-substitués, procédé pour leur préparation, utilisation en tant que médicament, agent pharmaceutique contenant ces dérivés et utilisation
WO2012120055A1 (fr) 2011-03-08 2012-09-13 Sanofi Dérivés oxathiazine di- et tri-substitués, procédé pour leur préparation, utilisation en tant que médicament, agent pharmaceutique contenant ces dérivés et utilisation
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