WO2012040279A1 - Modulators of the gpr119 receptor and the treatment of disorders related thereto - Google Patents

Modulators of the gpr119 receptor and the treatment of disorders related thereto Download PDF

Info

Publication number
WO2012040279A1
WO2012040279A1 PCT/US2011/052478 US2011052478W WO2012040279A1 WO 2012040279 A1 WO2012040279 A1 WO 2012040279A1 US 2011052478 W US2011052478 W US 2011052478W WO 2012040279 A1 WO2012040279 A1 WO 2012040279A1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical agent
increasing
individual
disorder
incretin
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.)
Ceased
Application number
PCT/US2011/052478
Other languages
English (en)
French (fr)
Inventor
Robert M. Jones
Juerg Lehmann
Weichao Chen
Jeffrey Edwards
Glen Marquez
Michael E. Morgan
Abu J.M. Sadeque
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.)
Arena Pharmaceuticals Inc
Original Assignee
Arena Pharmaceuticals Inc
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
Priority to EP11764056.5A priority Critical patent/EP2619198A1/en
Priority to CN201180056068.6A priority patent/CN103221410B/zh
Priority to US13/825,601 priority patent/US10894787B2/en
Priority to SG2013019070A priority patent/SG188548A1/en
Priority to JP2013529426A priority patent/JP5941916B2/ja
Priority to EA201390421A priority patent/EA201390421A1/ru
Priority to MX2013003184A priority patent/MX2013003184A/es
Priority to KR1020137009961A priority patent/KR101871011B1/ko
Priority to BR112013008100A priority patent/BR112013008100A2/pt
Application filed by Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Priority to PH1/2013/500547A priority patent/PH12013500547A1/en
Priority to AU2011305525A priority patent/AU2011305525B2/en
Priority to CA2812061A priority patent/CA2812061A1/en
Publication of WO2012040279A1 publication Critical patent/WO2012040279A1/en
Priority to CR20130145A priority patent/CR20130145A/es
Anticipated expiration legal-status Critical
Priority to US17/122,052 priority patent/US20210340133A1/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Definitions

  • the etiology of the different types of diabetes is not the same; however, everyone with diabetes has two things in common: overproduction of glucose by the liver and little or no ability to move glucose out of the blood into the cells where it becomes the body's primary fuel.
  • Obesity which is the result of an imbalance between caloric intake and energy expenditure, is highly correlated with insulin resistance and diabetes in experimental animals and human.
  • Atherosclerosis is a complex disease characterized by inflammation, lipid accumulation, cell death and fibrosis. Atherosclerosis is characterized by cholesterol deposition and monocyte infiltration into the subendothelial space, resulting in foam cell formation. Thrombosis subsequent to atherosclerosis leads to myocardial infarction and stroke. Atherosclerosis is the leading cause of mortality in many countries, including the United States. (See, e.g., Ruggeri, Nat Med (2002) 8: 1227-1234; Arehart et al, Circ Res, Circ. Res. (2008) 102:986-993.)
  • CD Crohn's disease
  • GPR119 has also been referred to as RUP3 (see, International Application WO 00/31258) and as Glucose-Dependent Insulinotropic Receptor GDIR (see, Jones, et. al. Expert Opin. Ther. Patents (2009), 19(10): 1339- 1359).
  • GPR119 agonists enhance incretin release and therefore can be used in treatment of disorders related to the incretins, such as, GIP, GLP-1, and PYY.
  • GIP and GLP-1 are substrates for the enzyme dipeptidyl peptidase-4 (DPP-IV). Jones and co-workers (Jones, et al, Ann. Rep. Med. Chem.
  • G. Glucose-dependent Insulinotropic Polypeptide GIP
  • GIP Glucose-dependent insulinotropic polypeptide
  • gastric inhibitory polypeptide is a peptide incretin hormone of 42 amino acids that is released from duodenal endocrine K cells after meal ingestion. The amount of GIP released is largely dependent on the amount of glucose consumed. GIP has been shown to stimulate glucose-dependent insulin secretion in pancreatic beta cells. GIP mediates its actions through a specific G protein-coupled receptor, namely GIPR.
  • PYY 3 _ 36 Peripheral administration of PYY 3 _ 36 has been reported to markedly reduce food intake and weight gain in rats, to decrease appetite and food intake in humans, and to decrease food intake in mice, but not in Y2R-null mice, which was said to suggest that the food intake effect requires the Y2R.
  • infusion of PYY 3 . 36 was found to significantly decrease appetite and reduce food intake by 33% over 24 hours.
  • One aspect of the present invention pertains to methods for modulating the activity of a GPR119 receptor, comprising prescribing to an individual in need thereof: a therapeutically effective amount of a compound of the present invention; a composition of the present invention; or a pharmaceutical product of the present invention.
  • One aspect of the present invention pertains to a compound of the present invention; a composition of the present invention; or a pharmaceutical product of the present invention; for use in a method of treatment of the human or animal body by therapy.
  • Figure 1 shows the effects of 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-l ,2,4- oxadiazol-5-yl)piperidin- 1 -yl)pyrinndin-4-ylamino)-N,N-dimethylbenzamide on glucose homeostasis in male diabetic ZDF rats (oral glucose tolerance test (oGTT)).
  • modulate or modulating refers to an increase or decrease in the amount, quality, response or effect of a particular activity, function or molecule.
  • composition refers to a compound, including but not limited to, a compound of the present invention and salts, solvates, and hydrates thereof, in combination with at least one additional component.
  • pharmaceutical composition refers to a composition comprising at least one active ingredient, such as a compound of the present invention; including but not limited to, a compound of the present invention and salts, solvates, and hydrates thereof, whereby the composition is amenable for treating and/or investigating a specified, efficacious outcome in a mammal (for example, without limitation, a human).
  • a mammal for example, without limitation, a human
  • the features reported herein can vary by plus or minus about 10 °C.
  • the features reported herein can also vary by plus or minus about 2% weight change due to, for example, sample variation.
  • One aspect of the present invention relates to an anhydrous form of 3-fluoro-4-(5- fluoro-6-(4-(3-(2-fluoropropan-2-yl)-l ,2,4-oxadiazol-5-yl)piperidin-l -yl)pyrinndin-4-ylamino)- N,N-dimethylbenzamide (Compound 1).
  • the physical properties of the crystalline form of Compound 1 anhydrous form are summarized in the following table.
  • thermogravimetric analysis profile showing ⁇ 0.05% weight loss up to about
  • One aspect of the present invention pertains to the use of a compound of the present invention in combination with a second pharmaceutical agent in the manufacture of a medicament for agonizing a GPRl 19 receptor in an individual.
  • a compound of the present invention can be formulated into pharmaceutical compositions using techniques well known to those in the art. Suitable pharmaceutically- acceptable carriers, outside those mentioned herein, are known in the art; for example, see
  • the pharmaceutical composition may be in the form of, for example, a tablet, capsule, suspension or liquid.
  • the pharmaceutical composition is preferably made in the form of a dosage unit containing a particular amount of the active ingredient.
  • dosage units are capsules, tablets, powders, granules or a suspension, with conventional additives such as lactose, mannitol, corn starch or potato starch; with binders such as crystalline cellulose, cellulose derivatives, acacia, corn starch or gelatins; with disintegrators such as corn starch, potato starch or sodium carboxymethyl-cellulose; and with lubricants such as talc or magnesium stearate.
  • the active ingredient may also be administered by injection as a composition wherein, for example, saline, dextrose or water may be used as a suitable pharmaceutically acceptable carrier.
  • DPP-IV inhibitors selected from the DPP-IV inhibitors found in Patent Publication Nos. EP 1517907, EP 1513808, EP 1492777, EP 1490335, EP 1489088, EP 1480961, EP 1476435, EP 1476429, EP 1469873, EP 1465891, EP 1463727, EP 1461337, EP 1450794, EP 1446116, EP 1442049, EP 1441719, EP 1426366, EP 1412357, EP1406873, EP 1406872, EP 1406622, EP 1404675, EP 1399420, EP 1399471, EP 1399470, EP 1399469, EP 1399433, EP 1399154, EP 1385508, EP 1377288, EP 1355886, EP 1354882, EP 1338592, EP 1333025, EP 1304327, EP 1301187, EP 1296974, EP 1280797, EP 1282600, EP 1261586, EP 1258476, EP 1254113,
  • the compound, 4(5)-fluoro-l -[2-[(lR,35)-3-(lH-l ,2,4-triazol-l - ylmethyl)cyclopentylamino]acetyl]pyrrolidine-2(5)-carbonitrile, is disclosed in international patent publication WO2006/040625.
  • Some embodiments of the present invention include every combination of one or more compounds selected from compounds disclosed in WO2006/040625 and pharmaceutically acceptable salts, solvates, and hydrates thereof.
  • the biguanides are a class of drugs that stimulate anaerobic glycolysis, increase the sensitivity to insulin in the peripheral tissues, inhibit glucose absorption from the intestine, suppress of hepatic gluconeogenesis, and inhibit fatty acid oxidation.
  • biguanides include phenformin ((phenylethyl) biguanide), metformin (dimethylbiguanide), buformin
  • the sulfonylureas are drugs which promote secretion of insulin from pancreatic beta cells by transmitting signals of insulin secretion via receptors in the cell membranes.
  • Examples of a sulfonylurea include tolbutamide (Orinase, N-(butylcarbamoyl)-4- methylbenzenesulfonamide); acetohexamide (Dymelor, 4-acetyl-N- (cyclohexylcarbamoyl)benzenesulfonamide); tolazamide (Tolinase, N-(azepan-l-ylcarbamoyl)- 4-methylbenzenesulfonamide); chlorpropamide (Diabinese, 4-chloro-N- (propylcarbamoyl)benzenesulfonamide); glipizide (Glucotrol, N-(4-(N-
  • the pharmaceutical agent or the second pharmaceutical agent is a sulfonylurea selected from N-(butylcarbamoyl)-4-methylbenzenesulfonamide (chemical structure shown below) and pharmaceutically acceptable salts, solvates, and hydrates thereof:
  • the pharmaceutical agent or the second pharmaceutical agent is a sulfonylurea selected from the following sulfonylureas and pharmaceutically acceptable salts, solvates, and hydrates thereof: glipizide, glimepiride, and glibenclamide.
  • the pharmaceutical agent or the second pharmaceutical agent is tolbutamide.
  • the pharmaceutical agent or the second pharmaceutical agent is acetohexamide.
  • the pharmaceutical agent or the second pharmaceutical agent is tolazamide.
  • the pharmaceutical agent or the second pharmaceutical agent is chlorpropamide.
  • the pharmaceutical agent or the second pharmaceutical agent is glipizide.
  • the pharmaceutical agent or the second pharmaceutical agent is glyburide.
  • Astellas and Kotobuki disclosed a series of SGLT2 inhibitors in international patent publication WO2004/080990. Some embodiments of the present invention include every combination of one or more compounds selected from compounds disclosed in WO2004/080990 and pharmaceutically acceptable salts, solvates, and hydrates thereof.
  • the pharmaceutical agent or the second pharmaceutical agent is 5-(4-(2-(5-ethylpyridin-2-yl)ethoxy)benzyl)thiazolidine-2,4-dione (chemical structure shown below) and pharmaceutica thereof:
  • Synthetic methods for incorporating radio-isotopes into organic compounds are applicable to compounds of the invention and are well known in the art. These synthetic methods, for example, incorporating activity levels of tritium into target molecules, are as follows:
  • GPRl 19 receptor directly correlates to its binding affinity.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PCT/US2011/052478 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto Ceased WO2012040279A1 (en)

Priority Applications (14)

Application Number Priority Date Filing Date Title
BR112013008100A BR112013008100A2 (pt) 2010-09-22 2011-09-21 "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles."
US13/825,601 US10894787B2 (en) 2010-09-22 2011-09-21 Modulators of the GPR119 receptor and the treatment of disorders related thereto
SG2013019070A SG188548A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto
JP2013529426A JP5941916B2 (ja) 2010-09-22 2011-09-21 Ｇｐｒ１１９レセプターのモジュレーターおよびそれに関連する障害の処置
EA201390421A EA201390421A1 (ru) 2010-09-22 2011-09-21 Модуляторы рецептора gpr119 и лечение связанных с ним нарушений
MX2013003184A MX2013003184A (es) 2010-09-22 2011-09-21 Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo.
KR1020137009961A KR101871011B1 (ko) 2010-09-22 2011-09-21 Ｇｐｒ１１９ 수용체의 조절제 및 그와 관련된 장애의 치료
EP11764056.5A EP2619198A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto
PH1/2013/500547A PH12013500547A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto
CN201180056068.6A CN103221410B (zh) 2010-09-22 2011-09-21 Gpr119受体调节剂和对与其相关的障碍的治疗
AU2011305525A AU2011305525B2 (en) 2010-09-22 2011-09-21 Modulators of the GPR119 receptor and the treatment of disorders related thereto
CA2812061A CA2812061A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto
CR20130145A CR20130145A (es) 2010-09-22 2013-03-22 Moduladores del receptor gpr119 y el tratamieto de trastornos relacionados con este
US17/122,052 US20210340133A1 (en) 2010-09-22 2020-12-15 Modulators of the gpr119 receptor and the treatment of disorders related thereto

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US38541010P 2010-09-22 2010-09-22
US61/385,410 2010-09-22
US201161478262P 2011-04-22 2011-04-22
US61/478,262 2011-04-22

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/825,601 A-371-Of-International US10894787B2 (en) 2010-09-22 2011-09-21 Modulators of the GPR119 receptor and the treatment of disorders related thereto
US17/122,052 Continuation US20210340133A1 (en) 2010-09-22 2020-12-15 Modulators of the gpr119 receptor and the treatment of disorders related thereto

Publications (1)

Publication Number Publication Date
WO2012040279A1 true WO2012040279A1 (en) 2012-03-29

Family

ID=44721104

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/052478 Ceased WO2012040279A1 (en) 2010-09-22 2011-09-21 Modulators of the gpr119 receptor and the treatment of disorders related thereto

Country Status (22)

Country Link
US (2) US10894787B2 (https=)
EP (2) EP2619198A1 (https=)
JP (1) JP5941916B2 (https=)
KR (1) KR101871011B1 (https=)
CN (2) CN103539791B (https=)
AU (2) AU2011305525B2 (https=)
BR (1) BR112013008100A2 (https=)
CA (1) CA2812061A1 (https=)
CL (1) CL2013000785A1 (https=)
CO (1) CO6700841A2 (https=)
CR (1) CR20130145A (https=)
DO (1) DOP2013000061A (https=)
EA (1) EA201390421A1 (https=)
EC (1) ECSP13012704A (https=)
GT (1) GT201300075A (https=)
HK (1) HK1254745A1 (https=)
MX (1) MX2013003184A (https=)
NI (1) NI201300030A (https=)
PE (1) PE20131371A1 (https=)
PH (1) PH12013500547A1 (https=)
SG (1) SG188548A1 (https=)
WO (1) WO2012040279A1 (https=)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012170867A1 (en) 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
WO2014011926A1 (en) 2012-07-11 2014-01-16 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2020250123A1 (en) 2019-06-10 2020-12-17 Lupin Limited Prmt5 inhibitors
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201906876PA (en) 2010-01-27 2019-09-27 Arena Pharm Inc Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
NL2026511B1 (en) * 2020-09-21 2022-05-24 Sulfateq Bv Compounds for treatment of heart failure

Citations (240)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991016339A1 (en) 1990-04-14 1991-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
DD296075A5 (de) 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
WO1993008259A2 (en) 1991-10-22 1993-04-29 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
WO1993010127A1 (en) 1991-11-22 1993-05-27 Boehringer Ingelheim Pharmaceuticals, Inc. Method for making a prolineboronate ester
WO1995015309A1 (en) 1993-12-03 1995-06-08 Ferring B.V. Dp-iv-serine protease inhibitors
WO1995029691A1 (en) 1994-04-28 1995-11-09 Georgia Tech Research Corporation Proline phosphonate derivatives
DE19616486A1 (de) 1996-04-25 1997-10-30 Knoell Hans Forschung Ev Verfahren zur Senkung des Blutglukosespiegels in Säugern
JPH1081666A (ja) 1996-06-12 1998-03-31 Ishihara Sangyo Kaisha Ltd フタルイミド誘導体又はその塩、それらの製造方法及びそれらを含有する医薬組成物
WO1998018763A1 (en) 1996-10-25 1998-05-07 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
WO1998019998A2 (en) 1996-11-07 1998-05-14 Novartis Ag N-substituted 2-cyanopyrrolidines
JPH10182613A (ja) 1996-10-25 1998-07-07 Tanabe Seiyaku Co Ltd テトラヒドロイソキノリン誘導体
WO1998050046A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Use of cd26 inhibitor for the manufacture of a medicament for the treatment of hiv
WO1998050066A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Potentiation of the immune response through delivery of compounds binding a cytoplasmic dipeptidase
WO1999016864A1 (en) 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
WO1999025719A1 (en) 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
WO1999056753A1 (en) 1998-05-04 1999-11-11 Point Therapeutics, Inc. Hematopoietic stimulation
WO1999061431A1 (de) 1998-05-28 1999-12-02 Probiodrug Gesellschaft für Arzneimittelforschung mbH Neue effektoren von dipeptidylpeptidase iv
WO1999062914A1 (en) 1998-06-05 1999-12-09 Point Therapeutics, Inc. Cyclic boroproline compounds
WO1999067278A1 (de) 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Prodrugs von dp iv-inhibitoren
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
WO2000010549A1 (en) 1998-08-21 2000-03-02 Point Therapeutics, Inc. Regulation of substrate activity
WO2000023421A1 (en) 1998-10-22 2000-04-27 Idun Pharmaceuticals, Inc. (SUBSTITUTED)ACYL DIPEPTIDYL INHIBITORS OF THE ICE/ced-3 FAMILY OF CYSTEINE PROTEASES
WO2000031258A2 (en) 1998-11-20 2000-06-02 Arena Pharmaceuticals, Inc. Human orphan g protein-coupled receptors
WO2000034241A1 (en) 1998-12-10 2000-06-15 Novartis Ag N-substituted 2-cyanopyrrolidines
JP2000191616A (ja) 1998-12-24 2000-07-11 Senju Pharmaceut Co Ltd 新規ジペプチジルアルデヒド誘導体およびそれを含有する医薬
WO2000056296A2 (en) 1999-03-23 2000-09-28 Ferring Bv Compositions for improving fertility
WO2000056297A2 (en) 1999-03-23 2000-09-28 Ferring B.V. Pharmaceutical compositions comprising dipeptidy peptidase iv inhibitors for the promotion of growth
WO2000069868A1 (en) 1999-05-17 2000-11-23 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Sulphostin analogues and processes for the preparation of sulphostin and analogues thereof
WO2000071135A1 (en) 1999-05-25 2000-11-30 Point Therapeutics, Inc. Anti-tumor comprising boroproline compounds
WO2001034594A1 (en) 1999-11-12 2001-05-17 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
WO2001052825A2 (en) 2000-01-21 2001-07-26 Novartis Ag Combinations comprising dipeptidylpeptidase-iv inhibitors and antidiabetic agents
WO2001055105A1 (en) 2000-01-24 2001-08-02 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
WO2001068603A2 (en) 2000-03-10 2001-09-20 Bristol-Myers Squibb Co. Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use
WO2001081304A1 (en) 2000-04-26 2001-11-01 Ferring Bv Inhibitors of dipeptidyl peptidase iv
WO2001081337A1 (en) 2000-04-26 2001-11-01 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
WO2001096295A2 (en) 2000-06-13 2001-12-20 Novartis Ag 2-cyanopyrrolidine derivatives and their use as medicaments
WO2001097808A1 (en) 2000-06-19 2001-12-27 Smithkline Beecham Plc Combinations of depeptidyl peptidase iv inhibitors and other antidiabetic agents for the treatment of diabete mellitus
WO2002002560A2 (en) 2000-07-04 2002-01-10 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv)
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
WO2002014271A1 (en) 2000-08-10 2002-02-21 Mitsubishi Pharma Corporation Proline derivatives and use thereof as drugs
WO2002030891A1 (en) 2000-10-06 2002-04-18 Tanabe Seiyaku Co., Ltd. Aliphatic nitrogenous five-membered ring compounds
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
WO2002034900A1 (en) 2000-10-27 2002-05-02 The University Of Sydney Dipeptidyl peptidases
WO2002038541A1 (en) 2000-11-10 2002-05-16 Taisho Pharmaceutical Co., Ltd. Cyanopyrrolidine derivatives
US6410508B1 (en) 1998-10-07 2002-06-25 Med College Georgia Res Inst Glucose-dependent insulinotropic peptide for use as an osteotropic hormone
CA2433090A1 (en) 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
WO2002055088A1 (en) 2001-01-16 2002-07-18 Nippon Kayaku Kabushiki Kaisha Remedies for bone marrow suppression and infectious diseases and white blood cell count elevating agents
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
WO2002062764A1 (en) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Fused heterocyclic compounds
WO2002068420A1 (de) 2001-02-24 2002-09-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
JP2002265439A (ja) 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
EP1245568A1 (fr) 2001-03-28 2002-10-02 Les Laboratoires Servier Dérives sulfonyles d'-aminoacides et leur utilisation en tant qu'inhibiteurs de dipeptidyl-peptidase IV ( DPP IV)
WO2002076450A1 (en) 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2002083128A1 (en) 2001-04-12 2002-10-24 Bristol-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase iv and method
WO2002083109A1 (en) 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv
EP1258476A1 (fr) 2001-05-15 2002-11-20 Les Laboratoires Servier Dérivés d'alpha-amino-acides, leur procédé de préparation ainsi que leur utilisation en tant qu'inhibiteurs de dipeptidyl-peptidase IV (DPP IV)
JP2002356472A (ja) 2000-10-06 2002-12-13 Tanabe Seiyaku Co Ltd 含窒素五員環化合物
JP2002356471A (ja) 2000-10-06 2002-12-13 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000250A1 (en) 2001-06-25 2003-01-03 Ferring Bv 3-fluoro-pyrrolidines as antidiabetic agents
WO2003002593A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
WO2003002553A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
WO2003002531A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
WO2003002595A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
WO2003004496A1 (en) 2001-07-03 2003-01-16 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
WO2003004498A1 (en) 2001-07-06 2003-01-16 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2003022871A2 (en) 2001-09-06 2003-03-20 Probiodrug Ag Peptides having a c- terminal hydroxylamino group as inhibitors of dipeptidyl peptidase i
WO2003024942A1 (en) 2001-09-14 2003-03-27 Mitsubishi Pharma Corporation Thiazolidine derivative and medicinal use thereof
WO2003024965A2 (en) 2001-09-19 2003-03-27 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
WO2003035057A1 (en) 2001-10-23 2003-05-01 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
WO2003035067A1 (en) 2001-10-23 2003-05-01 Ferring B.V. Novel dipeptidyl peptidase iv (dp-iv) inhibitors as anti-diabetic agents
WO2003037327A1 (en) 2001-10-26 2003-05-08 F. Hoffmann-La-Roche Ag N-substituted pyrrolidin derivatives as dipeptidyl peptidase iv inhibitors
WO2003038123A2 (en) 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
WO2003040174A2 (en) 2001-11-09 2003-05-15 Probiodrug Ag Substituted amino ketone compounds
WO2003045228A2 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
US20030105077A1 (en) 2001-07-03 2003-06-05 Kanstrup Anders Bendtz Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
US20030119750A1 (en) 2001-06-27 2003-06-26 Hans-Ulrich Demuth Use of dipeptidyl peptidase IV inhibitors
US20030119738A1 (en) 2001-09-06 2003-06-26 Andre Niestroj Novel inhibitors of dipeptidyl peptidase I
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
WO2003055881A1 (en) 2001-12-27 2003-07-10 F. Hoffmann-La Roche Ag Pyrido(2,1-a)isoquinoline derivatives as dpp-iv inhibitors
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
WO2003068757A1 (en) 2002-02-13 2003-08-21 F. Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
WO2003068748A1 (en) 2002-02-13 2003-08-21 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
EP1338651A1 (en) 2000-12-01 2003-08-27 Yamanouchi Pharmaceutical Co. Ltd. Method of screening remedy for diabetes
EP1338592A1 (en) 2002-02-22 2003-08-27 Nippon Zoki Pharmaceutical Co., Ltd. Novel 2-phenylpiperazine derivatives
JP2003238566A (ja) 2001-02-02 2003-08-27 Takeda Chem Ind Ltd 縮合複素環化合物
US20030162820A1 (en) 2002-02-28 2003-08-28 Hans-Ulrich Demuth Glutaminyl based DPIV inhibitors
WO2003072528A2 (en) 2002-02-08 2003-09-04 Idun Pharmaceuticals, Inc. (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
WO2003074500A2 (en) 2002-03-06 2003-09-12 Sanofi-Aventis N-aminoacetyl-pyrrolidine-2-carbonitriles and their use as ddp-iv inhibitors
WO2003080633A1 (fr) 2002-03-25 2003-10-02 Nippon Kayaku Kabushiki Kaisha Nouveau derive d'$g(a)-amino-n-(diaminophosphinyl)lactame
WO2003082817A2 (en) 2002-03-25 2003-10-09 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2003084940A1 (en) 2002-04-08 2003-10-16 Alangudi Sankaranarayanan Thiazolidine-4-carbonitriles and analogues and their use as dipeptidyl-peptidas inhibitors
JP2003300977A (ja) 2002-04-10 2003-10-21 Sumitomo Pharmaceut Co Ltd キサンチン誘導体
JP2003327532A (ja) 2002-05-10 2003-11-19 Takeda Chem Ind Ltd ペプチダーゼ阻害剤
WO2003095425A1 (en) 2002-05-09 2003-11-20 Taisho Pharmaceutical Co.,Ltd. Cyanopyrrolidine derivatives
WO2003099279A1 (en) 2002-05-29 2003-12-04 Novartis Ag Combination of a dpp iv inhibitor and a cardiovascular compound
WO2003101448A1 (en) 2002-06-03 2003-12-11 Novartis Ag The use of substituted cyanopyrrolidines and combination preparations containing them for treating hyperlipidemia and associated diseases
WO2003101958A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
WO2003104229A1 (ja) 2002-06-06 2003-12-18 エーザイ株式会社 新規縮合イミダゾール誘導体
WO2003105763A2 (en) 2002-06-14 2003-12-24 Amylin Pharmaceuticals, Inc. Prevention and/or treatment of inflammatory bowel disease using pyy or agonists thereof
WO2003106456A2 (en) 2002-06-14 2003-12-24 Sanofi-Synthelabo New compounds
WO2004000327A1 (ja) 2002-06-24 2003-12-31 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai ２型糖尿病治療剤
JP2004002367A (ja) 2002-04-04 2004-01-08 Tanabe Seiyaku Co Ltd 医薬組成物
JP2004002368A (ja) 2002-04-04 2004-01-08 Tanabe Seiyaku Co Ltd 医薬組成物
WO2004004661A2 (en) 2002-07-09 2004-01-15 Point Therapeutics, Inc. Boroproline compound combination therapy
WO2004007517A1 (de) 2002-07-11 2004-01-22 Aventis Pharma Deutschland Gmbh Neue thiophenglycosidderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2004007468A1 (en) 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2004007446A1 (ja) 2002-07-10 2004-01-22 Yamanouchi Pharmaceutical Co., Ltd. 新規なアゼチジン誘導体又はその塩
WO2004009544A1 (ja) 2002-07-23 2004-01-29 Yamanouchi Pharmaceutical Co., Ltd. 2-シアノ−４−フルオロピロリジン誘導体又はその塩
JP2004026820A (ja) 2002-05-09 2004-01-29 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼｉｖ阻害剤
JP2004035574A (ja) 2000-10-06 2004-02-05 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
JP2004043429A (ja) 2002-02-25 2004-02-12 Eisai Co Ltd 新規キサンチン誘導体およびｄｐｐｉｖ阻害剤
WO2004014860A2 (en) 2002-08-08 2004-02-19 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds as peptidase inhibitors
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004018468A2 (de) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthine, deren herstellung und deren verwendung als arzneimittel
DE10238243A1 (de) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004020407A1 (ja) 2002-08-29 2004-03-11 Taisho Pharmaceutical Co.,Ltd. ４−フルオロ−２−シアノピロリジン誘導体ベンゼンスルホン酸塩
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
WO2004026822A2 (en) 2002-09-19 2004-04-01 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
WO2004032836A2 (en) 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
US20040082570A1 (en) 2002-02-25 2004-04-29 Eisai Co., Ltd. Xanthine derivative and DPPIV inhibitor
WO2004037169A2 (en) 2002-10-18 2004-05-06 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004037181A2 (en) 2002-10-23 2004-05-06 Bristol-Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase iv and methods
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US20040097510A1 (en) 2002-08-21 2004-05-20 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
WO2004041795A1 (en) 2002-10-30 2004-05-21 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
WO2004043940A1 (en) 2002-11-07 2004-05-27 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004046106A1 (en) 2002-11-18 2004-06-03 Pfizer Products Inc. Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides
WO2004048379A1 (ja) 2002-11-01 2004-06-10 Sumitomo Pharmaceuticals Co., Ltd. キサンチン化合物
WO2004050658A1 (de) 2002-12-03 2004-06-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte imidazo-pyridinone und imidazo-pyridazinone, ihre herstellung und ihre verwendung als arzneimittel
WO2004050022A2 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004052362A1 (en) 2002-12-10 2004-06-24 Novartis Ag Combination of an dpp-iv inhibitor and a ppar-alpha compound
WO2004052850A2 (en) 2002-12-09 2004-06-24 Bristol-Myers Squibb Company Methods and compounds producing dipeptidyl peptidase iv inhibitors and intermediates thereof
DE10256264A1 (de) 2002-12-03 2004-06-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US20040138214A1 (en) 2002-11-08 2004-07-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
WO2004058266A1 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004065380A1 (en) 2003-01-14 2004-08-05 Arena Pharmaceuticals Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2004064778A2 (en) 2003-01-17 2004-08-05 Merck & Co. Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004067509A1 (ja) 2003-01-31 2004-08-12 Sanwa Kagaku Kenkyusho Co., Ltd. ジペプチジルペプチダーゼivを阻害する化合物
WO2004069162A2 (en) 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
JP2004244412A (ja) 2003-01-20 2004-09-02 Kotobuki Seiyaku Kk ４位に置換基を有する２−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤
WO2004076433A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004076413A2 (en) 2003-02-24 2004-09-10 Arena Pharmaceuticals, Inc. Phenyl- and pyridylpiperidine-derivatives as modulators of glucose metabolism
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004080990A1 (ja) 2003-03-14 2004-09-23 Astellas Pharma Inc. Ｃ－グリコシド誘導体又はその塩
WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
WO2004085378A1 (en) 2003-03-19 2004-10-07 Merck & Co. Inc. Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
US6803357B1 (en) 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
WO2004087650A2 (en) 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
WO2004087053A2 (en) 2003-03-25 2004-10-14 Syrrx, Inc. Dipeptidyl peptidase inhibitors
EP1469873A2 (en) 2001-11-26 2004-10-27 Trustees of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
WO2004092128A1 (en) 2003-04-10 2004-10-28 Smithkline Beecham Corporation Anhydrous crystalline forms of (2s, 4s)-1-{(2r)-2-amino-3-‘4-methoxybenzyl)sulfonyl!-3-methylbutanoyl}-4-fluoropyrrolindine-2-carbonitrile
US6812350B2 (en) 2002-06-04 2004-11-02 Pfizer Inc. Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
JP2004315496A (ja) 2002-08-08 2004-11-11 Takeda Chem Ind Ltd 縮合複素環化合物
WO2004096806A1 (ja) 2003-04-30 2004-11-11 Sumitomo Pharmaceuticals Co. Ltd. 縮合イミダゾール誘導体
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
WO2004103276A2 (en) 2003-05-14 2004-12-02 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004104215A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
WO2004104216A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4)
WO2004103993A1 (en) 2003-05-14 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004108730A1 (en) 2003-06-05 2004-12-16 Fujisawa Pharmaceutical Co., Ltd. 1h-imidazo`4,5-d!pyridazines as dpp-iv inhibitors for the treatment of niddm
US20040259902A1 (en) 2003-06-20 2004-12-23 Markus Boehringer Pyrido [2,1-a] isoquinoline derivatives
US20040259903A1 (en) 2003-06-20 2004-12-23 Markus Boehringer Pyrido [2,1-a] isoquinoline derivatives
WO2004111041A1 (en) 2003-06-12 2004-12-23 Fujisawa Pharmaceutical Co., Ltd. Pyrrolidine, thiazolidine and oxazolidine compounds which inhibit dipeptidyl peptidase-iv (dpp)
WO2004111051A1 (de) 2003-06-18 2004-12-23 Boehringer Ingelheim International Gmbh Imidazopyridazinon- und imidazopyridonderivate, deren herstellung und deren verwendung als arzneimittel
WO2004110436A1 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004110375A2 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Combination therapy for the treatment of diabetes
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2005003135A1 (en) 2003-06-24 2005-01-13 Merck & Co., Inc. Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
JP2005023038A (ja) 2003-07-04 2005-01-27 Taisho Pharmaceut Co Ltd 慢性腎疾患治療薬
WO2005007647A1 (en) 2003-07-11 2005-01-27 Arena Pharmaceuticals, Inc. Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2005009956A1 (en) 2003-07-21 2005-02-03 Smithkline Beecham Corporation (2s,4s)-4-fluoro-1-[4-fluoro-beta-(4-fluorophenyl)-l-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
WO2005011581A2 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2005012308A1 (de) 2003-07-25 2005-02-10 Sanofi-Aventis Deutschland Gmbh Neue cyanopyrrolidide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2005012312A1 (de) 2003-07-25 2005-02-10 Sanofi-Aventis Deutschland Gmbh Neue cyanothiazolide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2005012249A2 (en) 2003-08-01 2005-02-10 Bristol-Myers Squibb Company Adamantyglycine- based inhibitors of dipeptidyl peptidase iv for the treatment of diabetes
WO2005012326A1 (en) 2003-08-01 2005-02-10 Tanabe Seiyaku Co., Ltd. Novel compounds having inhibitory activity against sodium-dependant transporter
US20050043292A1 (en) 2003-08-20 2005-02-24 Pfizer Inc Fluorinated lysine derivatives as dipeptidyl peptidase IV inhibitors
WO2005020920A2 (en) 2003-09-02 2005-03-10 Merck & Co., Inc. Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
US20050059716A1 (en) 2003-07-25 2005-03-17 Aventis Pharma Deutschland Gmbh Novel bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
US20050059724A1 (en) 2003-07-25 2005-03-17 Aventis Pharma Deutschland Gmbh Novel cyanopyrrolidides, process for their preparation and their use as medicaments
WO2005025554A2 (en) 2003-09-09 2005-03-24 Japan Tobacco Inc. Dipeptidyl peptidase iv inhibitor
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2005030127A2 (en) 2003-09-23 2005-04-07 Merck & Co., Inc. Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2005030751A2 (en) 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005032590A1 (ja) 2003-10-03 2005-04-14 Takeda Pharmaceutical Company Limited 糖尿病治療剤
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
WO2005034940A2 (de) 2003-10-15 2005-04-21 Imtm Gmbh Duale alanyl-aminopeptidase- und dipeptidylpeptidase iv-inhibitoren zur funktionellen beeinflussung unterschiedlicher zellen und zur behandlung immunologischer, entzündlicher, neuronaler und anderer erkrankungen
WO2005037828A1 (en) 2003-10-20 2005-04-28 Lg Life Sciences Ltd. Novel inhibitors of dpp-iv, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
WO2005037779A2 (de) 2003-10-15 2005-04-28 Imtm Gmbh Neue dipeptidylpeptidase iv-inhibitoren zur funktionellen beeinflussung unterschiedlicher zellen und zur behandlung immunologischer, entzündlicher, neuronaler und anderer erkrankungen
WO2005040095A1 (en) 2003-10-16 2005-05-06 Astrazeneca Ab Inhibitors of dipeptidyl peptidase iv
WO2005042488A1 (en) 2003-10-31 2005-05-12 Takeda Pharmaceutical Company Limited Pyridine compounds as inhibitors of dipeptidyl peptidase iv
WO2005044195A2 (en) 2003-11-04 2005-05-19 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2005047297A1 (en) 2003-11-12 2005-05-26 Phenomix Corporation Heterocyclic boronic acid compounds
WO2005049022A2 (en) 2003-11-17 2005-06-02 Novartis Ag Use of dipeptidyl peptidase iv inhibitors
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
WO2005063750A1 (de) 2003-12-23 2005-07-14 Boehringer Ingelheim International Gmbh Bicyclische imidazolverbindungen, deren herstellung und deren verwendung als arzneimittel
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
WO2005079795A2 (en) 2004-02-20 2005-09-01 Novartis Ag Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders
WO2005082849A1 (en) 2004-02-23 2005-09-09 Trustees Of Tufts College Lactams as conformationally constrained peptidomimetic inhibitors
WO2005082348A2 (en) 2004-02-23 2005-09-09 Trustees Of Tufts College Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism
WO2005087235A1 (en) 2004-03-09 2005-09-22 National Health Research Institutes Pyrrolidine compounds
WO2005092877A1 (de) 2004-03-16 2005-10-06 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituierte benzol-derivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2005095381A1 (en) 2004-03-15 2005-10-13 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005116014A1 (en) 2004-05-12 2005-12-08 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
WO2006040625A1 (en) 2004-10-12 2006-04-20 Glenmark Pharmaceuticals S.A. Novel dipeptidyl peptidase iv inhibitors, pharmaceutical compositions containing them, and process for their preparation
WO2006068163A1 (ja) 2004-12-24 2006-06-29 Dainippon Sumitomo Pharma Co., Ltd. 二環性ピロール誘導体
WO2006076231A2 (en) 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
WO2006080421A1 (ja) 2005-01-28 2006-08-03 Chugai Seiyaku Kabushiki Kaisha スピロケタール誘導体、およびその糖尿病治療薬としての使用
WO2006088129A1 (ja) 2005-02-18 2006-08-24 Mitsubishi Pharma Corporation プロリン誘導体の塩、またはその溶媒和物、及びその製造方法
WO2006100181A2 (en) 2005-03-22 2006-09-28 F. Hoffmann-La Roche Ag New salt and polymorphs of a dpp-iv inhibitor
WO2006116157A2 (en) 2005-04-22 2006-11-02 Alantos Pharmaceuticals Holding, Inc. Dipeptidyl peptidase-iv inhibitors
WO2007019255A2 (en) 2005-08-04 2007-02-15 Novartis Ag Salts of vildagliptin
WO2007027651A2 (en) 2005-08-30 2007-03-08 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
WO2007035372A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Polymorphs of benzoate salt of 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
WO2007071576A1 (en) 2005-12-21 2007-06-28 F. Hoffmann-La Roche Ag New salt and polymorph of dpp-iv inhibitor
US20070167468A1 (en) 2004-08-06 2007-07-19 Sanofi-Aventis Deutschland Gmbh Substituted bicyclic 8-pyrr0lidinoxanthines, methods for their production, pharmaceutical formulations and their use
WO2007120702A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Use of gpr119 receptor agonists for increasing bone mass and for treating osteoporosis, and combination therapy relating thereto
WO2007120689A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual
WO2007128721A1 (de) 2006-05-04 2007-11-15 Boehringer Ingelheim Internationalgmbh Polymorphe
WO2007148185A2 (en) 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
WO2008027273A2 (en) 2006-08-30 2008-03-06 Phenomix Corporation Solid citrate and tartrate salts of dpp-iv inhibitors
EP1902730A1 (en) 2005-06-09 2008-03-26 Banyu Pharmaceutical Co., Ltd. Npy y2 agonist for use as therapeutic agent for disease accompanied by diarrhea
WO2008067465A1 (en) 2006-11-29 2008-06-05 Takeda Pharmaceutical Company Limited Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US20080146818A1 (en) 2004-02-05 2008-06-19 Yasumichi Fukuda Bicycloester Derivative
WO2008109591A1 (en) 2007-03-08 2008-09-12 Lexicon Pharmaceuticals, Inc. Phlorizin analogs as inhibitors of sodium glucose co-transporter 2
WO2008114857A1 (ja) 2007-03-22 2008-09-25 Kyorin Pharmaceutical Co., Ltd. アミノアセチルピロリジンカルボニトリル誘導体の製造方法
US20090036434A1 (en) * 2004-06-04 2009-02-05 Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2009084497A1 (ja) 2007-12-28 2009-07-09 Dainippon Sumitomo Pharma Co., Ltd. メチル置換ピペリジン誘導体
WO2009126245A1 (en) 2008-04-07 2009-10-15 Arena Pharmaceuticals, Inc. Methods of using a g protein-coupled receptor to identify peptide yy (pyy) secretagogues and compounds useful in the treatment of conditions modulated by pyy
WO2010075273A1 (en) * 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof

Family Cites Families (318)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH389134A (de) 1960-03-15 1965-03-15 Ciba Geigy Verfahren zur Herstellung neuer Anthrachinonküpenfarbstoffe
CH478817A (de) 1965-10-22 1969-09-30 Ciba Geigy Verfahren zur Herstellung neuer N,N'-Di-(pyrimidyl-(4)-aminoalkyl)-diazacycloalkanen
CH480410A (de) 1967-01-09 1969-10-31 Geigy Ag J R Verfahren zur Herstellung von wasserlöslichen Azopyrimidinfarbstoffen
CA961052A (en) 1967-01-12 1975-01-14 Max Schellenbaum N-2-ethylhexyl-n'-aryl ureas and preparation containing them
FR1593586A (https=) 1967-10-17 1970-06-01
US3608087A (en) 1968-06-21 1971-09-21 Merck & Co Inc Feed compositions
US3887329A (en) 1969-05-05 1975-06-03 Ciba Geigy Ag Hexamethyl phosphotriamide-dye compositions
BE756953A (fr) 1969-10-02 1971-04-01 Merck & Co Inc Potentialisation d'antibiotiques
US3686238A (en) 1970-01-19 1972-08-22 Syntex Corp Glycerol esterified with 2-naphthyl-acetic acids and fatty acids
US3852434A (en) 1970-09-11 1974-12-03 Merck & Co Inc Potentiation of ({31 ) cis-1,2-epoxypropyl)phosphonic acid and analogues thereof
US3690834A (en) 1971-01-11 1972-09-12 Syva Co Ligand determination with spin labeled compounds by receptor displacement
US3966744A (en) 1971-01-11 1976-06-29 Syva Company Spin labeled compounds
DE2106585A1 (de) 1971-02-11 1972-08-24 Farbenfabriken Bayer Ag, 5090 Leverkusen Aminothiodiazole und Thiodiazol-Azofarbstoffe
CH558137A (de) 1971-05-17 1975-01-31 Ciba Geigy Ag Mittel zur beeinflussung des pflanzenwachstums.
CH560197A5 (en) 1971-05-17 1975-03-27 Ciba Geigy Ag 2-alkylthio-4,6-bis (subst amino)-5-nitropyrimidines - - herbicides
US3966764A (en) 1972-07-10 1976-06-29 Syva Company Ligand determination of spin labeled compounds by receptor displacement-amphetamine analogs
US3849420A (en) 1972-10-20 1974-11-19 Dow Chemical Co Bis-(alkylthio-and alkylsulfonyl)-pentachloroquinolines
CH574206A5 (https=) 1972-11-16 1976-04-15 Ciba Geigy Ag
DE2340569C2 (de) 1973-08-10 1982-12-02 Bayer Ag, 5090 Leverkusen Azofarbstoffe
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
US4101541A (en) 1973-12-21 1978-07-18 Ciba-Geigy Corporation 3-Cyano-1,2,4-thiadiazolyl-5-czo dyestuffs
CH584739A5 (https=) 1973-12-21 1977-02-15 Ciba Geigy Ag
FR2258841B1 (https=) 1974-01-29 1977-11-04 Ugine Kuhlmann
AT327605B (de) 1974-05-06 1976-02-10 Ciba Geigy Ag Mittel zur hemmung des pflanzenwachstums
AU492126B2 (en) 1974-05-14 1975-11-20 Ciba-Geigy Ag Nitropyrimidine derivatives
FR2306697A1 (fr) 1975-04-10 1976-11-05 Sogeras Nouvelles pyrimidines utilisables comme medicaments antidiabetiques et hypocholesterolemiants
US4189579A (en) 1977-05-20 1980-02-19 The Dow Chemical Company Aminoalkylthiopurines
US4139705A (en) 1977-05-20 1979-02-13 The Dow Chemical Company Pyrazolopyrimidines
DE2731264A1 (de) 1977-07-11 1979-02-01 Boehringer Mannheim Gmbh Neue 1-acyl-2-cyanaziridine, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen
JPS6038696B2 (ja) 1977-12-09 1985-09-02 コニカ株式会社 ハロゲン化銀カラ−写真感光材料
US4242507A (en) 1978-02-23 1980-12-30 Fujisawa Pharmaceutical Co., Ltd. Sulfonic acid esters
DE2831580C2 (de) 1978-07-18 1980-09-18 Boehringer Mannheim Gmbh, 6800 Mannheim Verfahren und Reagens zur Bestimmung von Glycerin
DE2831850A1 (de) 1978-07-20 1980-02-07 Basf Ag N-arylsulfonylpyrrole, ihre herstellung und diese enthaltende therapeutische mittel
DE2906603A1 (de) 1979-02-21 1980-09-04 Boehringer Mannheim Gmbh N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel
US4343804A (en) 1979-03-26 1982-08-10 A. H. Robins Company, Inc. 4-Amino-3-quinolinecarboxylic acids and esters-antisecretory anti-ulcer compounds
DE3070304D1 (en) 1980-04-28 1985-04-25 Teijin Ltd Thiazolo(3,2-a)pyrimidine derivatives, process for preparing same, and drug containing same
EP0053678A1 (de) 1980-12-05 1982-06-16 BASF Aktiengesellschaft 5-Amino-1-phenyl-4-cyanpyrazole, diese enthaltende herbizide Mittel, Verfahren zu ihrer Herstellung und ihre Anwendung als Herbizide
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
DE3334455A1 (de) 1983-03-04 1984-09-06 Bayer Ag, 5090 Leverkusen Guanidin - derivate
US4612376A (en) 1983-03-25 1986-09-16 Fujisawa Pharmaceutical Co., Ltd. Substituted-3,4-dihydro-4-(2,4,6-trimethoxyphenylimino)-2(1H)-pyrimidones useful as cardiotonic, antihypertensive, cerebrovascular vasodilator and anti-platelet agent
ZA848275B (en) 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
DE3406329A1 (de) 1984-02-22 1985-08-22 Merck Patent Gmbh, 6100 Darmstadt Pyridone
JPS6157587A (ja) 1984-08-29 1986-03-24 Shionogi & Co Ltd 縮合複素環誘導体および抗潰瘍剤
PH22302A (en) 1985-02-11 1988-07-22 Fujisawa Pharmaceutical Co Piperidine compounds
AU601145B2 (en) 1985-03-01 1990-09-06 Duphar International Research B.V. Benzoyl urea derivatives having anti-tumor activity
DE3601196A1 (de) 1986-01-17 1987-07-23 Merck Patent Gmbh 1,4-dihydropyridine
CA1340284C (en) 1987-03-19 1998-12-22 Zeneca Inc. Herbicidal substituted cyclic diones
EP0324426B1 (en) 1988-01-11 1996-06-19 Fuji Photo Film Co., Ltd. Process for forming super high contrast negative images
NZ238863A (en) 1990-07-19 1993-03-26 Janssen Pharmaceutica Nv Substituted thiazolyl and pyridinyl derivatives
EP0567643A4 (en) 1991-01-16 1995-07-19 Yoshitomi Pharmaceutical NEW PYRIDE DERIVATIVE AND ITS USE AS A SELECTIVE MEDICINAL PRODUCT.
CA2070978A1 (en) 1991-06-11 1992-12-12 William J. Greenlee Cyclic renin inhibitors
GB9114760D0 (en) 1991-07-09 1991-08-28 Pfizer Ltd Therapeutic agents
JPH0533359A (ja) 1991-08-02 1993-02-09 Kubota Corp 全旋回型の小型バツクホウ
EP0556889A1 (en) 1992-02-18 1993-08-25 Duphar International Research B.V Method of preparing aryl(homo)piperazines
DE4208254A1 (de) 1992-03-14 1993-09-16 Hoechst Ag Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid
TW237456B (https=) 1992-04-09 1995-01-01 Ciba Geigy
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
NZ314207A (en) 1992-09-28 2000-12-22 Vertex Pharma 1-(2-Oxoacetyl)-piperidine-2-carboxylic acid derivatives as multi drug resistant cancer cell sensitizers
DE4241632A1 (de) 1992-12-10 1994-06-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
JPH0753546A (ja) 1993-08-09 1995-02-28 Kuraray Co Ltd ジアリール置換複素環化合物およびその医薬用途
PL313973A1 (en) 1993-10-12 1996-08-05 Du Pont Merck Pharma 1 n-alkyl-n-arylopyrimidin amines and their derivatives
GB9400889D0 (en) 1994-01-18 1994-03-16 Sandoz Ltd Novel compounds
TW530047B (en) 1994-06-08 2003-05-01 Pfizer Corticotropin releasing factor antagonists
FI970967A7 (fi) 1994-09-09 1997-03-07 Nippon Shinyaku Co Ltd Heterosyklinen johdannainen ja lääkeaine
NZ295749A (en) 1994-11-29 1998-05-27 Dainippon Pharmaceutical Co Indole derivatives; preparation and medicaments for treating obesity and diabetes mellitus
ATE251141T1 (de) 1995-03-10 2003-10-15 Berlex Lab Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
US5691364A (en) 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
WO1996033994A1 (en) 1995-04-28 1996-10-31 Nippon Soda Co., Ltd. Amino-substituted derivatives, process for the preparation thereof, and herbicide
US6020492A (en) 1995-05-12 2000-02-01 Neurogen Corporation Deazapurine derivatives; a new class of CRF1 specific ligands
WO1996036613A1 (en) 1995-05-19 1996-11-21 Nippon Soda Co., Ltd. Substituted benzoic acid derivatives, process for the production thereof, and herbicides
US6956047B1 (en) 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
TWI238064B (en) 1995-06-20 2005-08-21 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
KR0169813B1 (ko) 1995-07-12 1999-01-15 김종인 4-아미노-3-아실나프티리딘 유도체
ATE197150T1 (de) 1995-08-31 2000-11-15 Lonza Ag Verfahren zur herstellung von dihydroxypyrimidin- derivaten
CZ126598A3 (cs) 1995-10-26 1998-09-16 Mitsubishi-Tokyo Pharmaceuticals, Inc. Fenylethanolaminové sloučeniny, způsob jejich výroby a farmaceutické prostředky s jejich obsahem
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
DE19602095A1 (de) 1996-01-22 1997-07-24 Bayer Ag Halogenpyrimidine
DE69720429T9 (de) 1996-02-02 2004-09-23 Merck & Co., Inc. Heterocyclische verbindungen als antidiabetische mittel und für die behandlung von fettleibigkeit
JP3356291B2 (ja) 1996-02-07 2002-12-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｃｒｆレセプター拮抗薬としてのピラゾロピリミジン類
US5948786A (en) 1996-04-12 1999-09-07 Sumitomo Pharmaceuticals Company, Limited Piperidinylpyrimidine derivatives
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
IL127566A0 (en) 1996-08-28 1999-10-28 Pfizer Substituted 6,5-hetero- bicyclic derivatives
ATE228513T1 (de) 1996-09-12 2002-12-15 Schering Ag Durch cyclische aminosäuren oder cyclische hydroxysäuren substituierte benzamidinderivate und deren verwendung als antikoagulantien
US6008234A (en) 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
CA2229123A1 (en) 1997-02-11 1998-08-11 Mitchell Irvin Steinberg Pharmaceutical agents
JP2001511813A (ja) 1997-02-18 2001-08-14 ニューロクライン バイオサイエンシーズ，インコーポレイテッド Ｃｒｆレセプターアンタゴニストおよびそれらに関連する方法
JP2002501493A (ja) 1997-04-22 2002-01-15 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｃｒｆアンタゴニストのチオフェノピリジン類
ES2207834T3 (es) 1997-04-22 2004-06-01 Janssen Pharmaceutica N.V. Quino- y quinazolinas antagonistas del crf.
JPH11193277A (ja) 1997-05-14 1999-07-21 Nippon Soda Co Ltd ピリミジン誘導体、その製法および有害生物防除剤
DE19737723A1 (de) 1997-08-14 1999-02-18 Bayer Ag Methoximinomethyloxadiazine
JP2001515076A (ja) 1997-08-14 2001-09-18 バイエル・アクチエンゲゼルシヤフト 有害生物防除剤として使用されるメトキシイミノメチルオキサジアジン
NL1010018C2 (nl) 1997-09-09 1999-03-10 Duphar Int Res Chinoline en chinazoline derivaten met corticotropine releasing factor (CRF) antagonistische werking.
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
JP2002510687A (ja) 1998-04-02 2002-04-09 ニューロゲン コーポレイション アミノアルキル置換ピロロ［２，３−ｂ］ピリジンおよびピロロ［２，３−ｄ］ピリミジン誘導体：ｃｒｆ１レセプタのモジュレータ
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
CA2339188A1 (en) 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
HRP20080359B1 (hr) 1998-11-10 2016-01-01 Janssen Pharmaceutica N.V. PIRIMIDINI KOJI INHIBIRAJU REPLIKACIJU HIV-a
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6239126B1 (en) 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
EP1140831A1 (en) 1998-12-17 2001-10-10 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine urea derivatives having 5ht1a receptor activity
WO2000035886A2 (en) 1998-12-18 2000-06-22 Axys Pharmaceuticals, Inc. (hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
RU2260007C2 (ru) 1999-03-17 2005-09-10 Астразенека Аб Производные амида, способ их получения (варианты), фармацевтическая композиция, способ ингибирования
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
EP1074549B1 (en) 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
CA2385747A1 (en) 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
JP2001089452A (ja) 1999-09-22 2001-04-03 Sankyo Co Ltd ピリミジン誘導体
CA2384188C (en) 1999-09-24 2008-06-17 Janssen Pharmaceutica N.V. Antiviral compositions
EP1218381B1 (en) 1999-09-30 2006-12-06 Neurogen Corporation AMINO SUBSTITUTED PYRAZOLO¬1,5-a|-1,5-PYRIMIDINES AND PYRAZOLO¬1,5-a|-1,3,5-TRIAZINES
JP2003510325A (ja) 1999-09-30 2003-03-18 ニューロジェン・コーポレーション ある種のアルキレンジアミン−置換ピラゾロ［１，５−ａ］−１，５−ピリミジン及びピラゾロ［１，５−ａ］−１，３，５−トリアジン
IL148903A0 (en) 1999-09-30 2002-09-12 Neurogen Corp Certain alkylene diamine-substituted heterocycles
DE19947154A1 (de) 1999-10-01 2001-10-04 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
GR990100388A (el) 1999-11-09 2001-07-31 Φαρμακευτικος συνδυασμος αποτελουμενος απο χωριστες δοσολογικες μορφες σε συσκευασια συμμορφωσης (compliance package) ενος αναστολεα της αναγωγασης του υδροξυ-μεθυλο-γλουταρυλο συνενζυμου α (στατινης, statin) και ενος παραγωγου του φιμπρικου οξεος....
WO2001046204A1 (en) 1999-12-22 2001-06-28 Merck Frosst Canada & Co. Aromatic phosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors
DE19962936A1 (de) 1999-12-24 2001-06-28 Bayer Ag Neue beta-Aminosäureverbindungen als Integrinantagonisten
DE60009154D1 (de) 1999-12-30 2004-04-22 Lundbeck & Co As H Phenylpiperazinyl-derivate
HRP20020599A2 (en) 2000-01-18 2004-08-31 Pfizer Prod Inc Corticotropin releasing factor antagonists
IL150841A0 (en) 2000-02-09 2003-02-12 Hokuriku Pharmaceutical 1h-imidazopyridine derivatives
AU2001236948A1 (en) 2000-02-15 2001-08-27 Foster-Miller Inc. No voc radiation curable resin compositions
AU784722B2 (en) 2000-02-18 2006-06-01 Merck & Co., Inc. Aryloxyacetic acids for diabetes and lipid disorders
US6569879B2 (en) 2000-02-18 2003-05-27 Merck & Co., Inc. Aryloxyacetic acids for diabetes and lipid disorders
JP4064671B2 (ja) 2000-02-25 2008-03-19 エフ．ホフマン−ラ ロシュ アーゲー アデノシン受容体モジュレーター
RU2298418C2 (ru) 2000-04-12 2007-05-10 Новартис Аг Комбинация по меньшей мере двух соединений, выбранных из групп антагонистов at1-рецептора или ингибиторов асе (ангиотензинпревращающий фермент), или ингибиторов hmg-coa-редуктазы (бета-гидрокси-бета-метилглутарил-кофермент-а-редуктаза)
JP4969010B2 (ja) 2000-05-08 2012-07-04 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｉｖ複製阻害性ピリミジンのプロドラッグ
DE10024319A1 (de) 2000-05-17 2001-11-22 Merck Patent Gmbh Bisacylguanidine
ATE348162T1 (de) 2000-05-18 2007-01-15 Bayer Healthcare Ag Regulation eines menschlichen dopamine-ähnlichen g-protein gekoppelten rezeptor.
WO2001087892A1 (en) 2000-05-18 2001-11-22 Neurocrine Biosciences, Inc. Crf receptor antagonists
WO2001090082A1 (en) 2000-05-25 2001-11-29 F. Hoffmann-La Roche Ag Substituted 1-aminoalkyl-lactams and their use as muscarinic receptor antagonists
US6620821B2 (en) 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
JP2004501191A (ja) 2000-06-28 2004-01-15 テバ　ファーマシューティカル　インダストリーズ　リミティド カルベジロール
NZ523445A (en) 2000-06-29 2004-10-29 Abbott Lab Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
AR028782A1 (es) 2000-07-05 2003-05-21 Taisho Pharmaceutical Co Ltd Derivados heterociclicos tetrahidropiridino o piperidino
US6444685B1 (en) 2000-07-17 2002-09-03 Wyeth N-(4-sulfonylaryl)Cyclylamine 2-hydroxyethylamines as beta-3 adrenergic receptor agonists
US20030232860A1 (en) 2000-07-18 2003-12-18 Hironori Harada Medicine comprising dicyanopyridine derivative
WO2002008188A1 (en) 2000-07-25 2002-01-31 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
WO2002019975A1 (fr) 2000-09-05 2002-03-14 Taisho Pharmaceutical Co., Ltd. Stimulants de la croissance des cheveux
AU6294501A (en) 2000-09-20 2002-04-02 Rtp Pharma Inc Spray drying process and compositions of fenofibrate
US20030224058A1 (en) 2002-05-24 2003-12-04 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
US7276249B2 (en) 2002-05-24 2007-10-02 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
PE20020507A1 (es) 2000-10-17 2002-06-25 Schering Corp Compuestos no-imidazoles como antagonistas del receptor histamina h3
AU2002223626A1 (en) 2000-10-20 2002-04-29 Novartis Ag Combinations of a thyromimetic compound and a statin
ATE521353T1 (de) 2000-10-23 2011-09-15 Glaxosmithkline Llc Neues trisubstitutiertes 8h-pyridoä2,3- düpyrimidin-7-onderivat zur behandlung von durch csbp/p38kinase vermittelten krankheiten
JP4350946B2 (ja) 2000-10-31 2009-10-28 メルク エンド カムパニー インコーポレーテッド 糖尿病及び脂質異常症の治療のためのベンゾピランカルボン酸誘導体
KR20030060927A (ko) 2000-11-03 2003-07-16 뉴로크린 바이오사이언시즈 인코퍼레이티드 Ｃｒｆ 수용체 길항제 및 이와 관련된 방법
US20020058026A1 (en) 2000-11-13 2002-05-16 Milton Hammerly HMG CoA reductase inhibitor medications combined wih CoEnzyme Q-10
UA77165C2 (en) 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition
CA2429426A1 (en) 2000-11-17 2002-05-23 Takeda Chemical Industries, Ltd. Isoxazole derivatives
BR0115400A (pt) 2000-11-20 2003-09-30 Biovitrum Ab Compostos de piperazinilpirazina atuando como agonistas ou antagonistas do receptor 5ht-2 de serotonina
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US6545017B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Urea substituted imidazopyridines
US6525064B1 (en) 2000-12-08 2003-02-25 3M Innovative Properties Company Sulfonamido substituted imidazopyridines
US20020107262A1 (en) 2000-12-08 2002-08-08 3M Innovative Properties Company Substituted imidazopyridines
US6545016B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Amide substituted imidazopyridines
CA2433018A1 (en) 2000-12-21 2002-06-27 Joel C. Barrish Thiazolyl inhibitors of tec family tyrosine kinases
AR035533A1 (es) 2001-01-26 2004-06-02 Schering Corp Uso de por lo menos un inhibidor de la absorcion de los esteroles o sus sales, solvatos, prodrogas farmaceuticamente aceptables o mezclas de los mismos para la preparacion de un medicamento para el tratamiento de la sitosterolemia, composiciones farmaceuticas, el uso de dichas composiciones para la
WO2002060388A2 (en) 2001-01-30 2002-08-08 Merck & Co., Inc. Acyl sulfamides for treatment of obesity, diabetes and lipid disorders
MXPA03007134A (es) 2001-02-08 2004-10-15 Memory Pharm Corp Trifluorometilpurinas como inhibidores de fosfodiesterasa 4.
AU2002251978B2 (en) 2001-02-09 2007-07-19 Merck & Co., Inc. 2-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders
DE10110754A1 (de) 2001-03-07 2002-09-19 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
WO2002072101A1 (en) 2001-03-13 2002-09-19 Bristol-Myers Squibb Pharma Company A corticotropin releasing factor receptor ligand, its enantiomer and pharmaceutically acceptable salts
WO2002081454A1 (en) 2001-04-09 2002-10-17 Dr. Reddy's Laboratories Ltd. Derivatives of aryl acids, their use in medicine, process for their preparation and pharmaceutical compositions containing them
CA2444095A1 (en) 2001-04-20 2002-10-31 Wyeth Heterocyclyloxy-, -thioxy- and -aminobenzazole derivatives as 5-hydroxytryptamine-6 ligands
PT1397351E (pt) 2001-06-01 2010-01-04 Hoffmann La Roche Derivados de pirimidina, triazina e pirazina como receptores de glutamato
WO2002102560A1 (en) 2001-06-15 2002-12-27 The University Of Melbourne Boron-based wood preservatives and treatment of wood with boron-based preservatives
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ　スクイブ　カンパニー ホスホジエステラーゼ７に対するピリミジン阻害剤
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
US20030139435A1 (en) 2001-06-26 2003-07-24 Gulzar Ahmed N-heterocyclic inhibitors of TNF-alpha expression
GB0117899D0 (en) 2001-07-23 2001-09-12 Astrazeneca Ab Chemical compounds
WO2003026661A1 (fr) 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
EP1438048A1 (en) 2001-10-18 2004-07-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
SE0104334D0 (sv) 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
GB0229931D0 (en) 2002-12-21 2003-01-29 Astrazeneca Ab Therapeutic agents
JP2005518408A (ja) 2001-12-29 2005-06-23 ノボ　ノルディスク　アクティーゼルスカブ 異常脂肪血症を治療するための、ｇｌｐ−１化合物と他の薬物との組み合わせ使用
US20050043315A1 (en) 2002-01-02 2005-02-24 Hideo Tsutsumi Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
US20070225351A1 (en) 2002-01-11 2007-09-27 Lippa Arnold S Methods and compositions for controlling body weight and appetite
GB0201850D0 (en) 2002-01-26 2002-03-13 Astrazeneca Ab Therapeutic treatment
ES2361403T3 (es) 2002-03-07 2011-06-16 X-Ceptor Therapeutics, Inc. Moduladores de quinazolinona de receptores nucleares.
AU2003214110A1 (en) 2002-03-15 2003-09-29 Ciba Specialty Chemicals Holding Inc. 4-aminopyrimidines and their use for the antimicrobial treatment of surfaces
TW200810743A (en) 2002-03-22 2008-03-01 Novartis Ag Combination of organic compounds
WO2003088962A1 (en) 2002-04-16 2003-10-30 Merck & Co., Inc. Combination therapy using a ppar alpha/gamma agonist
EP1499598A1 (en) 2002-04-18 2005-01-26 Ucb, S.A. Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions
DE10219435A1 (de) 2002-05-02 2003-11-13 Bayer Cropscience Ag Substituierte Pyrazolo-pyrimidin-4-one
WO2003094845A2 (en) 2002-05-08 2003-11-20 Bristol-Myers Squibb Company Pyridine-based thyroid receptor ligands
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
AU2003245313A1 (en) 2002-06-10 2003-12-22 Elan Pharma International, Ltd Nanoparticulate formulations comprising hmg coa reductase inhibitor derivatives (statins), novel combinations thereof as well as manufacturing of these pharmaceutical compositions
JP4533134B2 (ja) 2002-06-10 2010-09-01 エラン ファーマ インターナショナル，リミティド ナノ粒子ポリコサノール製剤および新規なポリコサノールの組合せ
CA2488617A1 (en) 2002-06-10 2003-12-18 Eugene R. Cooper Nanoparticulate sterol formulations and sterol combinations
DE10226943A1 (de) 2002-06-17 2004-01-08 Bayer Ag Phenylaminopyrimidine und ihre Verwendung
GB0214254D0 (en) 2002-06-20 2002-07-31 Glaxo Group Ltd Chemical compounds
SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201976D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
DK1531832T3 (da) 2002-06-28 2009-07-27 Glykos Finland Oy Terapeutiske sammensætninger til anvendelse ved profylakse eller behandling af diarré
US20040053842A1 (en) 2002-07-02 2004-03-18 Pfizer Inc. Methods of treatment with CETP inhibitors and antihypertensive agents
US7071210B2 (en) 2002-07-02 2006-07-04 Pfizer Inc. CETP inhibitors in combination with antihypertensive agents and uses thereof
JP2006514918A (ja) 2002-07-23 2006-05-18 スミスクライン ビーチャム コーポレーション キナーゼインヒビターとしてのピラゾロピリミジン
WO2004009597A2 (en) 2002-07-23 2004-01-29 Smithkline Beecham Corporation Pyrazolopyrimidines as protein kinase inhibitors
JP2005536517A (ja) 2002-07-23 2005-12-02 スミスクライン ビーチャム コーポレーション キナーゼインヒビターとしてのピラゾロピリミジン
US20060105445A1 (en) 2002-07-29 2006-05-18 Klaus Godl Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins
US7297715B2 (en) 2002-07-30 2007-11-20 Merck & Co., Inc. PPAR alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
CA2491733A1 (en) 2002-07-30 2004-02-05 Merck & Co., Inc. Ppar alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
JP2004067575A (ja) 2002-08-06 2004-03-04 Yaizu Suisankagaku Industry Co Ltd 糖尿病治療薬効果促進剤
BR0313255A (pt) 2002-08-08 2005-07-12 Amgen Inc Composto, composição farmacêutica, uso de um composto e métodos de fabricar um medicamento e de preparar um composto
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
AU2003256419A1 (en) 2002-08-21 2004-03-11 Merck & Co., Inc. Combination therapy using a dual ppar alpha/gamma agonist and an angiotensin ii type i receptor antagonist
WO2004019869A2 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
WO2004020408A1 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
AU2003262042A1 (en) 2002-09-11 2004-04-30 Yamanouchi Pharmaceutical Co., Ltd. Method of screening insulin content enhancer
JP2006510597A (ja) 2002-09-27 2006-03-30 メルク　エンド　カムパニー　インコーポレーテッド 置換ピリミジン類
US7067658B2 (en) 2002-09-30 2006-06-27 Bristol-Myers Squibb Company Pyridino and pyrimidino pyrazinones
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
WO2004033710A2 (en) 2002-10-09 2004-04-22 Genaissance Pharmaceuticals, Inc. Itgb3 gene haplotypes and atorvastatin dose effects on hdl cholesterol
EP1551842A1 (en) 2002-10-15 2005-07-13 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
CA2503715A1 (en) 2002-10-30 2004-05-21 Merck & Co., Inc. Kinase inhibitors
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
US20040110241A1 (en) 2002-12-06 2004-06-10 Segal Mark S. Materials and methods for monitoring vascular endothelial function
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
AU2003299790A1 (en) 2002-12-20 2004-07-22 Bayer Pharmaceuticals Corporation Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
WO2004058727A1 (en) 2002-12-20 2004-07-15 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
GB0230020D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
GB0230021D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
DE602004005960T2 (de) 2003-01-16 2008-01-17 Sb Pharmco Puerto Rico Inc. Heteroaryl-substituierte pyrrolä2, 3- büpyridin-derivate als crf-rezeptor-antagonisten
JP2007504285A (ja) 2003-01-17 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド Ｎ−シクロヘキシルアミノカルボニルベンゼンスルホンアミド誘導体
TW200418829A (en) 2003-02-14 2004-10-01 Avanir Pharmaceutics Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
JP2004269468A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
JP2004269469A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
KR100729883B1 (ko) 2003-03-28 2007-06-18 화이자 프로덕츠 인코포레이티드 죽상경화증 및 비만증을 치료하기 위한 ｃｅｔｐ억제제로서의 1,2,4-치환된 1,2,3,4-테트라하이드로- 및1,2-디하이드로-퀴놀린 및1,2,3,4-테트라하이드로-퀴녹살린 유도체
TWI494102B (zh) 2003-05-02 2015-08-01 Japan Tobacco Inc 包含ｓ-〔２（〔〔１-（２-乙基丁基）環己基〕羰基〕胺基）苯基〕２-甲基丙烷硫酯及ｈｍｇ輔酶ａ還原酶抑制劑之組合
DE60333546D1 (de) 2003-05-06 2010-09-09 Univ Palackeho PyrazoloÄ4,3-DÜpyrimidines, verfahren zur ihre herstellung und deren verwendung
SE0301368D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
US7083933B1 (en) 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
US6987118B2 (en) 2003-05-21 2006-01-17 Pfizer Inc. Tetrahydroisoquinoline derivatives as PPAR-alpha activators
WO2004110368A2 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Combination therapy for the treatment of hypertension
AU2003902882A0 (en) 2003-06-10 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Piperidyl derivatives
US20050005717A1 (en) 2003-07-10 2005-01-13 Pfizer Inc Probe holder
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
NZ585188A (en) 2003-08-15 2011-09-30 Novartis Ag 2,4-Pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders
US20050043327A1 (en) 2003-08-21 2005-02-24 Pfizer Inc Pharmaceutical composition for the prevention and treatment of addiction in a mammal
UY28500A1 (es) 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
AU2004275719B2 (en) 2003-09-23 2010-08-19 Merck Sharp & Dohme Corp. Quinoline potassium channel inhibitors
WO2005037215A2 (en) 2003-10-14 2005-04-28 Massachusetts Institute Of Technology Compositions and methods for enhancing cognitive function and synaptic plasticity
AU2004289304A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Pyridine compounds
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005058315A1 (en) 2003-12-12 2005-06-30 Ribapharm, Inc. Novel heterocyclic compounds as ikk2 inhibitors with anti-hbv activity
JP4958560B2 (ja) 2003-12-24 2012-06-20 プロシディオン・リミテッド Ｇｐｃｒ受容体作動薬としてのヘテロ環誘導体
JP2007522233A (ja) 2004-02-11 2007-08-09 アムジエン・インコーポレーテツド バニロイド受容体リガンド及び治療におけるそれらの使用
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
AU2005233437A1 (en) 2004-04-12 2005-10-27 Sankyo Company, Limited Thienopyridine derivatives
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
EP1827438B2 (en) 2004-09-20 2014-12-10 Xenon Pharmaceuticals Inc. Piperazin derivatives for inhibiting human stearoyl-coa-desaturase
AU2005292134B2 (en) 2004-10-01 2010-12-23 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
EP1806347A4 (en) 2004-10-08 2009-07-01 Astellas Pharma Inc PYRIMIDINE DERIVATIVES FUSED WITH AN AROMATIC RING
TW200621257A (en) 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
AU2005305083B2 (en) 2004-11-03 2012-02-02 Arena Pharmaceuticals, Inc. GPR41 and modulators thereof for the treatment of insulin-related disorders
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
WO2006064744A1 (ja) * 2004-12-13 2006-06-22 Daiichi Sankyo Company, Limited 糖尿病の治療のための医薬組成物
JP5065908B2 (ja) 2004-12-24 2012-11-07 プロシディオン・リミテッド Ｇタンパク質結合受容体作動薬
EP1838311A1 (en) 2004-12-24 2007-10-03 Prosidion Limited G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
DOP2006000010A (es) 2005-01-10 2006-07-31 Arena Pharm Inc Procedimiento para preparar eteres aromáticos
DOP2006000009A (es) 2005-01-13 2006-08-15 Arena Pharm Inc Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina
JP2008528506A (ja) 2005-01-19 2008-07-31 ニューロジェン・コーポレーション ヘテロアリール置換ピペラジニル−ピリジン類縁体
BRPI0612599A2 (pt) 2005-06-30 2010-11-23 Prosidion Ltd composto, composição farmacêutica compreendendo o mesmo, método de tratamento e uso do mesmo
PL1899329T3 (pl) 2005-07-01 2012-03-30 Irm Llc Pirymidyno-podstawione pochodne benzimidazolu jako inhibitory kinaz białkowych
BRPI0616245A2 (pt) 2005-09-16 2011-06-14 Arena Pharm Inc modulador de metabolismo, seus usos, composiÇço farmaceutica compreendendo o mesmo, bem como mÉtodo para produÇço da referida composiÇço
TW200745055A (en) 2005-09-23 2007-12-16 Organon Nv 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives
DK1984344T3 (da) 2005-12-29 2013-01-14 Lexicon Pharmaceuticals Inc Multicykliske aminosyrederivater og fremgangsmåder til anvendelse heraf
AU2006335967B2 (en) 2006-01-19 2012-01-19 Orchid Chemicals & Pharmaceuticals Limited Novel heterocycles
TW200811147A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
TW200811140A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
EP2043744A2 (en) 2006-07-13 2009-04-08 SmithKline Beecham Corporation Chemical compounds
US20080103123A1 (en) 2006-08-30 2008-05-01 Biovitrum New compounds
ATE528300T1 (de) 2006-12-06 2011-10-15 Glaxosmithkline Llc Bizyklische verbindungen und ihre verwendung als antidiabetika
EP2112880A4 (en) 2006-12-14 2011-12-21 Merck Sharp & Dohme ACYLBIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND TREATMENT METHOD
WO2008128832A1 (en) 2007-04-18 2008-10-30 Nicox S.A. Nitroderivatives of non-peptidic renin inhibitors for the treatment of cardiovascular, renal and chronic liver disease, inflammations and metabolic syndrome
CN101668756A (zh) 2007-05-04 2010-03-10 百时美施贵宝公司 [6,6]和[6,7]-双环gpr119 g蛋白偶合受体激动剂
AU2008279447A1 (en) * 2007-07-19 2009-01-29 Metabolex, Inc. N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders
RU2443699C2 (ru) 2007-09-20 2012-02-27 Айрм Ллк Соединения и композиции в качестве модуляторов активности gpr119
EA018703B1 (ru) 2008-04-07 2013-10-30 Айрм Ллк Соединения и композиции в качестве модуляторов активности gpr119
WO2009125434A2 (en) 2008-04-07 2009-10-15 Cadila Healthcare Limited Oxime derivatives
MX2010013876A (es) * 2008-06-20 2011-03-04 Metabolex Inc Agonistas de arilo grpr119 y sus usos .
WO2010075271A1 (en) 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
WO2010074271A1 (ja) 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤
US20120016119A1 (en) 2009-01-22 2012-01-19 Yasunori Tsuboi NOVEL PYRROLO(2,3-d)PYRIMIDINE COMPOUND
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
AR077638A1 (es) 2009-07-15 2011-09-14 Lilly Co Eli Compuesto de (metanosulfonil -piperidin )-( alcoxi-aril) -tetrahidro- piridina , composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento de diabetes u obesidad
WO2011030139A1 (en) 2009-09-11 2011-03-17 Astrazeneca Ab 4- (pyrimidin-2-yl) -piperazine and 4- (pyrimidin-2-yl) -piperidine derivatives as gpr119 modulators
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
AU2011237775A1 (en) 2010-04-06 2012-11-22 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
PH12013500547A1 (en) * 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140066369A1 (en) 2011-04-19 2014-03-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140038889A1 (en) 2011-04-22 2014-02-06 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto

Patent Citations (409)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD296075A5 (de) 1989-08-07 1991-11-21 Martin-Luther-Universitaet Halle-Wittenberg,De Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv
WO1991016339A1 (en) 1990-04-14 1991-10-31 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
EP0528858A1 (en) 1990-04-14 1993-03-03 New England Medical Center Inc DIPEPTIDYL-AMINOPEPTIDASE TYPE IV INHIBITORS.
JPH05508624A (ja) 1990-04-14 1993-12-02 ニュー　イングランド　メデカル　センター　ホスピタルズ　インク ジペプチジル―アミノベプチダーゼ・４型の阻害剤
WO1993008259A2 (en) 1991-10-22 1993-04-29 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type iv
EP0610317A1 (en) 1991-10-22 1994-08-17 New England Medical Center Inhibitors of dipeptidyl-aminopeptidase type iv
EP1050540A2 (en) 1991-10-22 2000-11-08 New England Medical Center Hospitals, Inc. Inhibitors of dipeptidyl-aminopeptidase type IV
WO1993010127A1 (en) 1991-11-22 1993-05-27 Boehringer Ingelheim Pharmaceuticals, Inc. Method for making a prolineboronate ester
CA2123128A1 (en) 1991-11-22 1993-05-27 Roger Snow Method for making a prolineboronate ester
JPH07501078A (ja) 1991-11-22 1995-02-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド プロリンボロネートエステルの製法
EP0641347A1 (en) 1991-11-22 1995-03-08 Boehringer Ingelheim Pharmaceuticals Inc. Method for making a prolineboronate ester
EP0731789A1 (en) 1993-12-03 1996-09-18 Ferring B.V. Dp-iv-serine protease inhibitors
JPH09509921A (ja) 1993-12-03 1997-10-07 フェーリング ベスローテン フェンノートシャップ 酵素インヒビター
WO1995015309A1 (en) 1993-12-03 1995-06-08 Ferring B.V. Dp-iv-serine protease inhibitors
WO1995029691A1 (en) 1994-04-28 1995-11-09 Georgia Tech Research Corporation Proline phosphonate derivatives
DE19616486A1 (de) 1996-04-25 1997-10-30 Knoell Hans Forschung Ev Verfahren zur Senkung des Blutglukosespiegels in Säugern
WO1997040832A1 (de) 1996-04-25 1997-11-06 Probiodrug Gesellschaft für Arzneimittelforschung mbH Verwendung von dipeptidyl peptidase iv effektoren zur senkung des blutglukosespiegels in säugern
JP2001510442A (ja) 1996-04-25 2001-07-31 プロビオドラッグ ゲゼルシャフト フュル アルツナイミッテルフォルシュング エムベーハー 哺乳動物の血糖値低下のためのジペプチジルペプチダーゼ▲ｉｖ▼エフェクターの使用
US6303661B1 (en) 1996-04-25 2001-10-16 Probiodrug Use of dipeptidyl peptidase IV effectors for lowering the blood glucose level in mammals
JPH1081666A (ja) 1996-06-12 1998-03-31 Ishihara Sangyo Kaisha Ltd フタルイミド誘導体又はその塩、それらの製造方法及びそれらを含有する医薬組成物
WO1998018763A1 (en) 1996-10-25 1998-05-07 Tanabe Seiyaku Co., Ltd. Tetrahydroisoquinoline derivatives
JPH10182613A (ja) 1996-10-25 1998-07-07 Tanabe Seiyaku Co Ltd テトラヒドロイソキノリン誘導体
WO1998019998A2 (en) 1996-11-07 1998-05-14 Novartis Ag N-substituted 2-cyanopyrrolidines
JP2000511559A (ja) 1996-11-07 2000-09-05 ノバルティス アクチエンゲゼルシャフト Ｎ―置換２―シアノピロリジン
CA2289125A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Potentiation of the immune response through delivery of compounds binding a cytoplasmic dipeptidase
US6040145A (en) 1997-05-07 2000-03-21 Tufts University Potentiation of the immune response
US6100234A (en) 1997-05-07 2000-08-08 Tufts University Treatment of HIV
WO1998050046A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Use of cd26 inhibitor for the manufacture of a medicament for the treatment of hiv
WO1998050066A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Potentiation of the immune response through delivery of compounds binding a cytoplasmic dipeptidase
EP0975359A1 (en) 1997-05-07 2000-02-02 Trustees Of Tufts College Potentiation of the immune response through delivery of compounds binding a cytoplasmic dipeptidase
CA2289124A1 (en) 1997-05-07 1998-11-12 Trustees Of Tufts College Use of cd26 inhibitor for the manufacture of a medicament for the treatment of hiv
EP0980249A1 (en) 1997-05-07 2000-02-23 Trustees Of Tufts College Use of cd26 inhibitor for the manufacture of a medicament for the treatment of hiv
WO1999016864A1 (en) 1997-09-29 1999-04-08 Point Therapeutics, Inc. Stimulation of hematopoietic cells in vitro
EP1043328A1 (en) 1997-11-18 2000-10-11 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
WO1999025719A1 (en) 1997-11-18 1999-05-27 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Novel physiologically active substance sulphostin, process for producing the same, and use thereof
US6803357B1 (en) 1998-02-02 2004-10-12 New England Medical Center Hospitals, Inc. Method of regulating glucose metabolism, and reagents related thereto
WO1999056753A1 (en) 1998-05-04 1999-11-11 Point Therapeutics, Inc. Hematopoietic stimulation
EP1304327A2 (de) 1998-05-28 2003-04-23 Probiodrug AG Glutamin-Thiazolidide und -Pyrrolidide sowie ihre Verwendung als Dipeptidylpeptidase IV Inhibitoren
JP2002516318A (ja) 1998-05-28 2002-06-04 プロバイオドラッグ ゲゼルシャフト フュア アルツナイミッテルフォルシュンク エムベーハー ジペプチジル・ペプチダーゼｉｖの新規エフェクター
EP1215207A2 (de) 1998-05-28 2002-06-19 Probiodrug AG Salze von Isoleucyl-Thiazolidin und -Pyrrolidin und ihre Verwendung als Dipeptidylpeptidase-Inhibitoren
EP1082314A1 (de) 1998-05-28 2001-03-14 Probiodrug Gesellschaft für Arzneimittelforschung mbH Neue effektoren von dipeptidylpeptidase iv
US20030134802A1 (en) 1998-05-28 2003-07-17 Hans-Ulrich Demuth Novel effectors of dipepetidyl peptidase IV
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
WO1999061431A1 (de) 1998-05-28 1999-12-02 Probiodrug Gesellschaft für Arzneimittelforschung mbH Neue effektoren von dipeptidylpeptidase iv
JP2002517401A (ja) 1998-06-05 2002-06-18 ポイント セラピューティクス， インコーポレイテッド 環状ボロプロリン化合物
WO1999062914A1 (en) 1998-06-05 1999-12-09 Point Therapeutics, Inc. Cyclic boroproline compounds
US20020049164A1 (en) 1998-06-24 2002-04-25 Hans-Ulrich Demuth Prodrugs of DP IV-inhibitors
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
JP2003524591A (ja) 1998-06-24 2003-08-19 プロバイオドラッグ ゲゼルシャフト フュア アルツナイミッテルフォルシュンク エムベーハー Ｄｐｉｖ阻害剤のプロドラッグ
WO1999067278A1 (de) 1998-06-24 1999-12-29 Probiodrug Gesellschaft für Arzneimittelforschung mbH Prodrugs von dp iv-inhibitoren
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
EP0995440A1 (de) 1998-07-31 2000-04-26 Probiodrug Gesellschaft für Arzneimittelforschung mbH Verfahren zur Stiegerung des Blutglukosespiegels in Säugern
EP1104293A1 (en) 1998-08-21 2001-06-06 Point Therapeutics, Inc. Regulation of substrate activity
WO2000010549A1 (en) 1998-08-21 2000-03-02 Point Therapeutics, Inc. Regulation of substrate activity
CA2339537A1 (en) 1998-08-21 2000-03-02 Barbara Wallner Regulation of substrate activity
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
US6410508B1 (en) 1998-10-07 2002-06-25 Med College Georgia Res Inst Glucose-dependent insulinotropic peptide for use as an osteotropic hormone
JP2002527504A (ja) 1998-10-22 2002-08-27 アイドゥン ファーマシューティカルズ， インコーポレイテッド システインプロテアーゼのＩＣＥ／ｃｅｄ−３系の置換アシルジペプチジル抑制剤
WO2000023421A1 (en) 1998-10-22 2000-04-27 Idun Pharmaceuticals, Inc. (SUBSTITUTED)ACYL DIPEPTIDYL INHIBITORS OF THE ICE/ced-3 FAMILY OF CYSTEINE PROTEASES
EP1123272A1 (en) 1998-10-22 2001-08-16 Idun Pharmaceuticals, Inc. (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
WO2000031258A2 (en) 1998-11-20 2000-06-02 Arena Pharmaceuticals, Inc. Human orphan g protein-coupled receptors
US6166063A (en) 1998-12-10 2000-12-26 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
EP1137635A1 (en) 1998-12-10 2001-10-04 Novartis AG N-substituted 2-cyanopyrrolidines
WO2000034241A1 (en) 1998-12-10 2000-06-15 Novartis Ag N-substituted 2-cyanopyrrolidines
JP2002531547A (ja) 1998-12-10 2002-09-24 ノバルティス アクチエンゲゼルシャフト Ｎ置換されている２−シアノピロリジン
JP2000191616A (ja) 1998-12-24 2000-07-11 Senju Pharmaceut Co Ltd 新規ジペプチジルアルデヒド誘導体およびそれを含有する医薬
WO2000056296A2 (en) 1999-03-23 2000-09-28 Ferring Bv Compositions for improving fertility
WO2000056297A2 (en) 1999-03-23 2000-09-28 Ferring B.V. Pharmaceutical compositions comprising dipeptidy peptidase iv inhibitors for the promotion of growth
JP2000327689A (ja) 1999-05-17 2000-11-28 Microbial Chem Res Found スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法
WO2000069868A1 (en) 1999-05-17 2000-11-23 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Sulphostin analogues and processes for the preparation of sulphostin and analogues thereof
WO2000071135A1 (en) 1999-05-25 2000-11-30 Point Therapeutics, Inc. Anti-tumor comprising boroproline compounds
US6617340B1 (en) 1999-07-29 2003-09-09 Novartis Ag N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
WO2001034594A1 (en) 1999-11-12 2001-05-17 Guilford Pharmaceuticals, Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
JP2003535034A (ja) 1999-11-12 2003-11-25 ギルフォード ファーマシューティカルズ インコーポレイテッド ジペプチジルペプチダーゼｉｖ阻害剤並びにジペプチジルペプチダーゼｉｖ阻害剤の製造及び使用法
EP1228061A1 (en) 1999-11-12 2002-08-07 Guilford Pharmaceuticals Inc. Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors
US6380398B2 (en) 2000-01-04 2002-04-30 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1248604A2 (en) 2000-01-21 2002-10-16 Novartis AG Combinations comprising dipeptidylpeptidase-iv inhibitors and antidiabetic agents
WO2001052825A2 (en) 2000-01-21 2001-07-26 Novartis Ag Combinations comprising dipeptidylpeptidase-iv inhibitors and antidiabetic agents
WO2001055105A1 (en) 2000-01-24 2001-08-02 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
US6645995B2 (en) 2000-01-24 2003-11-11 Novo Nordisk A/S Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1254113A1 (en) 2000-01-24 2002-11-06 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
JP2003520849A (ja) 2000-01-24 2003-07-08 ノボ ノルディスク アクティーゼルスカブ 酵素ｄｐｐ−ｉｖの阻害剤であるｎ−置換２−シアノピロールおよび−ピロリン
US20020103384A1 (en) 2000-01-24 2002-08-01 Anders Kanstrup Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
WO2001068603A2 (en) 2000-03-10 2001-09-20 Bristol-Myers Squibb Co. Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use
JP2003531118A (ja) 2000-03-10 2003-10-21 ブリストル−マイヤーズ スクイブ カンパニー シクロプロピル縮合ピロリジン骨格を有するジペプチジルペプチダーゼｉｖの阻害剤及び方法
EP1261586A2 (en) 2000-03-10 2002-12-04 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase iv, processes for their preparation, and their use
JP2003531204A (ja) 2000-04-26 2003-10-21 フェリング ベスローテン フェンノートシャップ ジペプチジルペプチダーゼｉｖの阻害剤
EP1282600A1 (en) 2000-04-26 2003-02-12 Ferring BV Inhibitors of dipeptidyl peptidase iv
EP1280797A1 (en) 2000-04-26 2003-02-05 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
JP2003531191A (ja) 2000-04-26 2003-10-21 フェリング ベスローテン フェンノートシャップ ジペプチジル・ペプチダーゼｉｖの阻害剤
WO2001081337A1 (en) 2000-04-26 2001-11-01 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
WO2001081304A1 (en) 2000-04-26 2001-11-01 Ferring Bv Inhibitors of dipeptidyl peptidase iv
US20030216450A1 (en) 2000-04-26 2003-11-20 Evans David Michael Inhibitors of dipeptidyl peptidase IV
US6432969B1 (en) 2000-06-13 2002-08-13 Novartis Ag N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
EP1296974A2 (en) 2000-06-13 2003-04-02 Novartis AG 2-cyanopyrrolidine derivatives and their use as medicaments
WO2001096295A2 (en) 2000-06-13 2001-12-20 Novartis Ag 2-cyanopyrrolidine derivatives and their use as medicaments
JP2004503531A (ja) 2000-06-13 2004-02-05 ノバルティス　アクチエンゲゼルシャフト ２−シアノピロリジン誘導体および薬剤としてのそれらの使用
WO2001097808A1 (en) 2000-06-19 2001-12-27 Smithkline Beecham Plc Combinations of depeptidyl peptidase iv inhibitors and other antidiabetic agents for the treatment of diabete mellitus
JP2003535898A (ja) 2000-06-19 2003-12-02 スミスクライン ビーチャム パブリック リミテッド カンパニー 真性糖尿病の治療用のジペプチジルペプチダーゼｉｖ阻害剤および他の抗糖尿病剤の組み合わせ
US20040034014A1 (en) 2000-07-04 2004-02-19 Kanstrup Anders Bendtz Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV
EP1301187A2 (en) 2000-07-04 2003-04-16 Novo Nordisk A/S Heterocyclic compounds, which are inhibitors of the enzyme dpp-iv
WO2002002560A2 (en) 2000-07-04 2002-01-10 Novo Nordisk A/S Purine-2,6-diones which are inhibitors of the enzyme dipeptidyl peptidase iv (dpp-iv)
WO2002014271A1 (en) 2000-08-10 2002-02-21 Mitsubishi Pharma Corporation Proline derivatives and use thereof as drugs
US6849622B2 (en) 2000-10-06 2005-02-01 Tanabe Seiyaku Co., Ltd. Aliphatic nitrogenous five-membered ring compounds
US20040063935A1 (en) 2000-10-06 2004-04-01 Kosuke Yasuda Aliphatic nitrogenous five-membered ring compounds
WO2002030890A1 (en) 2000-10-06 2002-04-18 Tanabe Seiyaku Co., Ltd. Nitrogenous five-membered ring compounds
WO2002030891A1 (en) 2000-10-06 2002-04-18 Tanabe Seiyaku Co., Ltd. Aliphatic nitrogenous five-membered ring compounds
US20040229926A1 (en) 2000-10-06 2004-11-18 Tanabe Seiyaku Co., Ltd. Aliphatic nitrogen - containing 5 - membered ring compound
JP2004035574A (ja) 2000-10-06 2004-02-05 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
JP2002356471A (ja) 2000-10-06 2002-12-13 Tanabe Seiyaku Co Ltd 脂肪族含窒素五員環化合物
JP2002356472A (ja) 2000-10-06 2002-12-13 Tanabe Seiyaku Co Ltd 含窒素五員環化合物
WO2002034900A1 (en) 2000-10-27 2002-05-02 The University Of Sydney Dipeptidyl peptidases
US20040072892A1 (en) 2000-11-10 2004-04-15 Hiroshi Fukushima Cyanopyrrolidine derivatives
WO2002038541A1 (en) 2000-11-10 2002-05-16 Taisho Pharmaceutical Co., Ltd. Cyanopyrrolidine derivatives
US20070112059A1 (en) 2000-11-10 2007-05-17 Taisho Pharmaceutical Co., Ltd. Cyanopyrrolidine derivatives
EP1333025A1 (en) 2000-11-10 2003-08-06 Taisho Pharmaceutical Co., Ltd Cyanopyrrolidine derivatives
EP1338651A1 (en) 2000-12-01 2003-08-27 Yamanouchi Pharmaceutical Co. Ltd. Method of screening remedy for diabetes
US20040180925A1 (en) 2000-12-27 2004-09-16 Kenji Matsuno Dipeptidylpeptidase-IV inhibitor
WO2002051836A1 (en) 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
EP1354882A1 (en) 2000-12-27 2003-10-22 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
CA2433090A1 (en) 2000-12-27 2002-07-04 Kyowa Hakko Kogyo Co., Ltd. Dipeptidyl peptidase iv inhibitor
WO2002055088A1 (en) 2001-01-16 2002-07-18 Nippon Kayaku Kabushiki Kaisha Remedies for bone marrow suppression and infectious diseases and white blood cell count elevating agents
WO2002062764A1 (en) 2001-02-02 2002-08-15 Takeda Chemical Industries, Ltd. Fused heterocyclic compounds
EP1355886A1 (en) 2001-02-02 2003-10-29 Takeda Chemical Industries, Ltd. Fused heterocyclic compounds
JP2003238566A (ja) 2001-02-02 2003-08-27 Takeda Chem Ind Ltd 縮合複素環化合物
US20040087587A1 (en) 2001-02-24 2004-05-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
US20040077645A1 (en) 2001-02-24 2004-04-22 Frank Himmelsbach Xanthine derivatives,production and use thereof as medicament
WO2002068420A1 (de) 2001-02-24 2002-09-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthinderivate, deren herstellung und deren verwendung als arzneimittel
US20020198205A1 (en) 2001-02-24 2002-12-26 Frank Himmelsbach Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
JP2004522786A (ja) 2001-02-24 2004-07-29 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト キサンチン誘導体、それらの調製及び医薬組成物としてのそれらの使用
JP2002265439A (ja) 2001-03-08 2002-09-18 Mitsubishi Pharma Corp シアノピロリジン誘導体およびその医薬用途
JP2004525929A (ja) 2001-03-27 2004-08-26 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病の治療または予防用のジペプチジルペプチダーゼ阻害薬
EP1385508A1 (en) 2001-03-27 2004-02-04 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2002076450A1 (en) 2001-03-27 2002-10-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040106656A1 (en) 2001-03-27 2004-06-03 Ashton Wallace T Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1245568A1 (fr) 2001-03-28 2002-10-02 Les Laboratoires Servier Dérives sulfonyles d'-aminoacides et leur utilisation en tant qu'inhibiteurs de dipeptidyl-peptidase IV ( DPP IV)
US6716843B2 (en) 2001-03-28 2004-04-06 Les Laboratoires Servier Alpha-amino acid sulphonyl compounds
US20030087950A1 (en) 2001-03-28 2003-05-08 Denanteuil Guillaume New alpha-amino acid sulphonyl compounds
FR2822826A1 (fr) 2001-03-28 2002-10-04 Servier Lab Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2002083109A1 (en) 2001-04-11 2002-10-24 Ferring Bv Treatment of type 2 diabetes with inhibitors of dipeptidyl peptidase iv
JP2004525179A (ja) 2001-04-11 2004-08-19 フェリング ベスローテン フェンノートシャップ ジペプチジルペプチダーゼｉｖ阻害剤でのｉｉ型糖尿病の処置
US20020183367A1 (en) 2001-04-12 2002-12-05 Sulsky Richard B. 2,1-Oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
JP2004532220A (ja) 2001-04-12 2004-10-21 ブリストル−マイヤーズ　スクイブ　カンパニー ジペプチジル・ペプチダーゼｉｖの２，１−オキサゾリンおよび１，２−ピラゾリンに基づくインヒビターおよび方法
EP1377288A1 (en) 2001-04-12 2004-01-07 Bristol-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase iv and method
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
WO2002083128A1 (en) 2001-04-12 2002-10-24 Bristol-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase iv and method
FR2824825A1 (fr) 2001-05-15 2002-11-22 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP2002363157A (ja) 2001-05-15 2002-12-18 Lab Servier 新規α−アミノ酸化合物、その調製方法及びそれを含有する医薬組成物
US20030078247A1 (en) 2001-05-15 2003-04-24 De Nanteuil Guillaume Alpha-amino-acid compounds
EP1258476A1 (fr) 2001-05-15 2002-11-20 Les Laboratoires Servier Dérivés d'alpha-amino-acides, leur procédé de préparation ainsi que leur utilisation en tant qu'inhibiteurs de dipeptidyl-peptidase IV (DPP IV)
US6706742B2 (en) 2001-05-15 2004-03-16 Les Laboratories Servier Alpha-amino-acid compounds
JP2004535433A (ja) 2001-06-20 2004-11-25 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病治療用のジペプチジルペプチダーゼ阻害薬
JP2005500308A (ja) 2001-06-20 2005-01-06 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病を治療するためのジペプチジルペプチダーゼ阻害剤
EP1406622A2 (en) 2001-06-20 2004-04-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000181A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
EP1406872A2 (en) 2001-06-20 2004-04-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004534815A (ja) 2001-06-25 2004-11-18 フェリング ベスローテン フェンノートシャップ 抗糖尿病薬としての３−フルオロ−ピロリジン
WO2003000250A1 (en) 2001-06-25 2003-01-03 Ferring Bv 3-fluoro-pyrrolidines as antidiabetic agents
EP1399154A1 (en) 2001-06-25 2004-03-24 Ferring BV 3-fluoro-pyrrolidines as antidiabetic agents
JP2004530729A (ja) 2001-06-27 2004-10-07 プロバイオドラッグ アーゲー ジペプチジルペプチダーゼｉｖ触媒作用の拮抗調節に有用なペプチド構造
US20030130199A1 (en) 2001-06-27 2003-07-10 Von Hoersten Stephan Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
EP1399420A2 (en) 2001-06-27 2004-03-24 SmithKline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
WO2003072556A1 (en) 2001-06-27 2003-09-04 Prosidion Ltd. Glutaminyl based dpiv inhibitors
EP1406873A2 (en) 2001-06-27 2004-04-14 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
EP1399471A2 (en) 2001-06-27 2004-03-24 Probiodrug AG Use of dipeptidyl peptidase iv inhibitors as therapeutics for neurological disorders
EP1399469A2 (en) 2001-06-27 2004-03-24 Probiodrug AG Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
JP2004534836A (ja) 2001-06-27 2004-11-18 プロバイオドラッグ アーゲー ジペプチジルぺプチダ−ゼｉｖ阻害剤の新規な使用
JP2004535445A (ja) 2001-06-27 2004-11-25 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
EP1399470A2 (en) 2001-06-27 2004-03-24 Probiodrug AG Dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
JP2004521149A (ja) 2001-06-27 2004-07-15 プロバイオドラッグ アーゲー 新規なジペプチジルぺプチダ−ゼｉｖ阻害剤およびそれらの抗癌剤としての使用
EP1399433A2 (en) 2001-06-27 2004-03-24 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
WO2003002593A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
WO2003002596A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Use of dipeptidyl peptidase iv inhibitors as therapeutics for neurological disorders
WO2003002595A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents
JP2005500321A (ja) 2001-06-27 2005-01-06 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類
WO2003002531A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US20030119750A1 (en) 2001-06-27 2003-06-26 Hans-Ulrich Demuth Use of dipeptidyl peptidase IV inhibitors
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
WO2003002553A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
JP2005502624A (ja) 2001-07-03 2005-01-27 ノボ　ノルディスク　アクティーゼルスカブ 糖尿病を治療するための、ｄｐｐ−ｉｖを阻害するプリン誘導体
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
WO2003004496A1 (en) 2001-07-03 2003-01-16 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
US20030105077A1 (en) 2001-07-03 2003-06-05 Kanstrup Anders Bendtz Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1404675A1 (en) 2001-07-03 2004-04-07 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
WO2003004498A1 (en) 2001-07-06 2003-01-16 Merck & Co., Inc. Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2004536115A (ja) 2001-07-06 2004-12-02 メルク　エンド　カムパニー　インコーポレーテッド 糖尿病を治療又は予防するためのジペプチジルペプチダーゼ阻害薬としてのβ−アミノテトラヒドロイミダゾ（１，２−Ａ）ピラジン類及びテトラヒドロトリアゾロ（４，３−Ａ）ピラジン類
EP1412357A1 (en) 2001-07-06 2004-04-28 Merck & Co., Inc. Beta-amino tetrahydroimidazo(1,2-a)pyrazines and tetrahydrotriazolo(4,3-a)pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20030100563A1 (en) 2001-07-06 2003-05-29 Edmondson Scott D. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US6699871B2 (en) 2001-07-06 2004-03-02 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2005505531A (ja) 2001-08-17 2005-02-24 プロビオドルグ アーゲー 新規ジペプチジルペプチダーゼｉｖ阻害剤および血圧レベルを低下させるためのそれらの使用
WO2003015775A1 (en) 2001-08-17 2003-02-27 Probiodrug Ag New dipeptidyl peptidase iv inhibitors and their uses for lowering blood pressure levels
WO2003022871A2 (en) 2001-09-06 2003-03-20 Probiodrug Ag Peptides having a c- terminal hydroxylamino group as inhibitors of dipeptidyl peptidase i
US20030119738A1 (en) 2001-09-06 2003-06-26 Andre Niestroj Novel inhibitors of dipeptidyl peptidase I
DE10143840A1 (de) 2001-09-06 2003-03-27 Probiodrug Ag Neue Inhibitoren der Dipeptidylpeptidase I
EP1426366A1 (en) 2001-09-14 2004-06-09 Mitsubishi Pharma Corporation Thiazolidine derivative and medicinal use thereof
US20040259883A1 (en) 2001-09-14 2004-12-23 Hiroshi Sakashita Thiazolidine derivative and medicinal use thereof
WO2003024942A1 (en) 2001-09-14 2003-03-27 Mitsubishi Pharma Corporation Thiazolidine derivative and medicinal use thereof
WO2003024965A2 (en) 2001-09-19 2003-03-27 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
EP1463727A2 (en) 2001-09-19 2004-10-06 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme dpp-iv
US20030199528A1 (en) 2001-09-19 2003-10-23 Kanstrup Anders B. Hetrocyclic compounds that are inhibitors of the enzyme DPP-IV
WO2003035057A1 (en) 2001-10-23 2003-05-01 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
EP1446116A1 (en) 2001-10-23 2004-08-18 Ferring B.V. Inhibitors of dipeptidyl peptidase iv
US20050004205A1 (en) 2001-10-23 2005-01-06 Evans David M Novel dipeptidyl peptidase iv (dp-iv) inhibitors as anti-diabetic agents
EP1450794A1 (en) 2001-10-23 2004-09-01 Ferring B.V. Novel dipeptidyl peptidase iv (dp-iv) inhibitors as anti-diabetic agents
WO2003035067A1 (en) 2001-10-23 2003-05-01 Ferring B.V. Novel dipeptidyl peptidase iv (dp-iv) inhibitors as anti-diabetic agents
WO2003037327A1 (en) 2001-10-26 2003-05-08 F. Hoffmann-La-Roche Ag N-substituted pyrrolidin derivatives as dipeptidyl peptidase iv inhibitors
US20030130281A1 (en) 2001-10-26 2003-07-10 Markus Boehringer DPP IV inhibitors
EP1441719A1 (en) 2001-10-26 2004-08-04 F. Hoffmann-La Roche Ag N-substituted pyrrolidin derivatives as dipeptidyl peptidase iv inhibitors
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
JP2005507261A (ja) 2001-10-31 2005-03-17 ノバルティス アクチエンゲゼルシャフト Ｔｃｆ１遺伝子における多型に基づく糖尿病および関連状態の治療方法
WO2003038123A2 (en) 2001-10-31 2003-05-08 Novartis Ag Methods to treat diabetes and related conditions based on polymorphisms in the tcf1 gene
EP1442049A2 (en) 2001-11-09 2004-08-04 Probiodrug AG Substituted amino ketone compounds
WO2003040174A2 (en) 2001-11-09 2003-05-15 Probiodrug Ag Substituted amino ketone compounds
US20030125304A1 (en) 2001-11-09 2003-07-03 Hans-Ulrich Demuth Substituted amino ketone compounds
WO2003045228A2 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
EP1469873A2 (en) 2001-11-26 2004-10-27 Trustees of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
CA2466870A1 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
EP1465891A2 (en) 2001-12-26 2004-10-13 Guilford Pharmaceuticals Inc. Inhibitors of dipeptidyl peptidase iv
WO2003057144A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
WO2003057666A2 (en) 2001-12-26 2003-07-17 Guilford Pharmaceuticals Inhibitors of dipeptidyl peptidase iv
US20030149071A1 (en) 2001-12-27 2003-08-07 Gobbi Luca Claudio Pyrido [2,1-a] isoquinoline derivatives
EP1461337A1 (en) 2001-12-27 2004-09-29 F. Hoffmann-La Roche Ag Pyrido[2,1-a]isoquinoline derivatives as dpp-iv inhibitors
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
WO2003055881A1 (en) 2001-12-27 2003-07-10 F. Hoffmann-La Roche Ag Pyrido(2,1-a)isoquinoline derivatives as dpp-iv inhibitors
US20040176406A1 (en) 2001-12-27 2004-09-09 Gobbi Luca Claudio Pyrido [2,1-a] isoquinoline derivatives
US20030232788A1 (en) 2002-02-08 2003-12-18 Idun Pharmaceuticals, Inc. (Substituted)acyl dipeptidyl inhibitors of the ICE/ced-3 family of cysteine proteases
WO2003072528A2 (en) 2002-02-08 2003-09-04 Idun Pharmaceuticals, Inc. (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
WO2003068748A1 (en) 2002-02-13 2003-08-21 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
US6800650B2 (en) 2002-02-13 2004-10-05 Hoffmann-La Roche Inc. Pyridine and quinoline derivatives
US6867205B2 (en) 2002-02-13 2005-03-15 Hoffman-La Roche Inc. Pyridine and pyrimidine derivatives
WO2003068757A1 (en) 2002-02-13 2003-08-21 F. Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
US20030195188A1 (en) 2002-02-13 2003-10-16 Markus Boehringer Pyridine and quinoline derivatives
US20030216382A1 (en) 2002-02-13 2003-11-20 Markus Boehringer Pyridine and pyrimidine derivatives
EP1476435A1 (en) 2002-02-13 2004-11-17 F. Hoffmann-La Roche Ag Novel pyridin- and pyrimidin-derivatives
EP1476429A1 (en) 2002-02-13 2004-11-17 F. Hoffmann-La Roche Ag Novel pyridine- and quinoline-derivatives
EP1338592A1 (en) 2002-02-22 2003-08-27 Nippon Zoki Pharmaceutical Co., Ltd. Novel 2-phenylpiperazine derivatives
JP2004043429A (ja) 2002-02-25 2004-02-12 Eisai Co Ltd 新規キサンチン誘導体およびｄｐｐｉｖ阻害剤
US20040082570A1 (en) 2002-02-25 2004-04-29 Eisai Co., Ltd. Xanthine derivative and DPPIV inhibitor
EP1480961A1 (en) 2002-02-28 2004-12-01 Prosidion Limited Glutaminyl based dpiv inhibitors
US20030162820A1 (en) 2002-02-28 2003-08-28 Hans-Ulrich Demuth Glutaminyl based DPIV inhibitors
WO2003074500A2 (en) 2002-03-06 2003-09-12 Sanofi-Aventis N-aminoacetyl-pyrrolidine-2-carbonitriles and their use as ddp-iv inhibitors
EP1490335A2 (en) 2002-03-25 2004-12-29 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2003080633A1 (fr) 2002-03-25 2003-10-02 Nippon Kayaku Kabushiki Kaisha Nouveau derive d'$g(a)-amino-n-(diaminophosphinyl)lactame
WO2003082817A2 (en) 2002-03-25 2003-10-09 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1489088A1 (en) 2002-03-25 2004-12-22 Nippon Kayaku Kabushiki Kaisha Novel alpha-amino-n-(diaminophosphinyl)lactam derivative
JP2004002368A (ja) 2002-04-04 2004-01-08 Tanabe Seiyaku Co Ltd 医薬組成物
JP2004002367A (ja) 2002-04-04 2004-01-08 Tanabe Seiyaku Co Ltd 医薬組成物
US20030225102A1 (en) 2002-04-08 2003-12-04 Torrent Pharmaceuticals Ltd. Novel compounds and therapeutic uses thereof
WO2003084940A1 (en) 2002-04-08 2003-10-16 Alangudi Sankaranarayanan Thiazolidine-4-carbonitriles and analogues and their use as dipeptidyl-peptidas inhibitors
EP1492777A1 (en) 2002-04-08 2005-01-05 Torrent Pharmaceuticals Ltd Thiazolidine-4-carbonitriles and analogues and their use as dipeptidyl-peptidase inhibitors
JP2003300977A (ja) 2002-04-10 2003-10-21 Sumitomo Pharmaceut Co Ltd キサンチン誘導体
WO2003095425A1 (en) 2002-05-09 2003-11-20 Taisho Pharmaceutical Co.,Ltd. Cyanopyrrolidine derivatives
JP2004026820A (ja) 2002-05-09 2004-01-29 Taisho Pharmaceut Co Ltd ジペプチジルペプチダーゼｉｖ阻害剤
JP2003327532A (ja) 2002-05-10 2003-11-19 Takeda Chem Ind Ltd ペプチダーゼ阻害剤
WO2003099279A1 (en) 2002-05-29 2003-12-04 Novartis Ag Combination of a dpp iv inhibitor and a cardiovascular compound
WO2003101448A1 (en) 2002-06-03 2003-12-11 Novartis Ag The use of substituted cyanopyrrolidines and combination preparations containing them for treating hyperlipidemia and associated diseases
US6812350B2 (en) 2002-06-04 2004-11-02 Pfizer Inc. Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
US20040242898A1 (en) 2002-06-04 2004-12-02 Pfizer Inc Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
EP1513808A2 (en) 2002-06-04 2005-03-16 Pfizer Products Inc. Fluorinated cyclic amides as dipeptidyl peptidase iv inhibitors
WO2003101958A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors
US6710040B1 (en) 2002-06-04 2004-03-23 Pfizer Inc. Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors
US20040116328A1 (en) 2002-06-06 2004-06-17 Eisai Co., Ltd. Condensed imidazole derivatives
WO2003104229A1 (ja) 2002-06-06 2003-12-18 エーザイ株式会社 新規縮合イミダゾール誘導体
WO2003105763A2 (en) 2002-06-14 2003-12-24 Amylin Pharmaceuticals, Inc. Prevention and/or treatment of inflammatory bowel disease using pyy or agonists thereof
EP1517907A2 (en) 2002-06-14 2005-03-30 Sanofi-Aventis Azabicyclo-octane and nonane derivatives with ddp-iv inhibiting activity
WO2003106456A2 (en) 2002-06-14 2003-12-24 Sanofi-Synthelabo New compounds
JP2004026678A (ja) 2002-06-24 2004-01-29 Microbial Chem Res Found ２型糖尿病治療剤
WO2004000327A1 (ja) 2002-06-24 2003-12-31 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai ２型糖尿病治療剤
WO2004004661A2 (en) 2002-07-09 2004-01-15 Point Therapeutics, Inc. Boroproline compound combination therapy
WO2004007446A1 (ja) 2002-07-10 2004-01-22 Yamanouchi Pharmaceutical Co., Ltd. 新規なアゼチジン誘導体又はその塩
WO2004007517A1 (de) 2002-07-11 2004-01-22 Aventis Pharma Deutschland Gmbh Neue thiophenglycosidderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2004007468A1 (en) 2002-07-15 2004-01-22 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2004009544A1 (ja) 2002-07-23 2004-01-29 Yamanouchi Pharmaceutical Co., Ltd. 2-シアノ−４−フルオロピロリジン誘導体又はその塩
WO2004014860A2 (en) 2002-08-08 2004-02-19 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds as peptidase inhibitors
JP2004315496A (ja) 2002-08-08 2004-11-11 Takeda Chem Ind Ltd 縮合複素環化合物
DE10238243A1 (de) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-Amino-piperidin-1-yl]-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
WO2004018468A2 (de) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthine, deren herstellung und deren verwendung als arzneimittel
US20040097510A1 (en) 2002-08-21 2004-05-20 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004018469A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue purinderivate, deren herstelllung und deren verwendung als arzneimittel
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004018467A2 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Phenacylxanthinderivate als dpp-iv-hemmer
WO2004020407A1 (ja) 2002-08-29 2004-03-11 Taisho Pharmaceutical Co.,Ltd. ４−フルオロ−２−シアノピロリジン誘導体ベンゼンスルホン酸塩
WO2004026822A2 (en) 2002-09-19 2004-04-01 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
WO2004032836A2 (en) 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
WO2004037169A2 (en) 2002-10-18 2004-05-06 Merck & Co., Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004037181A2 (en) 2002-10-23 2004-05-06 Bristol-Myers Squibb Company Glycinenitrile-based inhibitors of dipeptidyl peptidase iv and methods
WO2004041795A1 (en) 2002-10-30 2004-05-21 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
WO2004048379A1 (ja) 2002-11-01 2004-06-10 Sumitomo Pharmaceuticals Co., Ltd. キサンチン化合物
WO2004043940A1 (en) 2002-11-07 2004-05-27 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
US20040138214A1 (en) 2002-11-08 2004-07-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
WO2004041820A1 (de) 2002-11-08 2004-05-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue xanthinderivate, deren herstellung und deren verwendung als arzneimittel
DE10251927A1 (de) 2002-11-08 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
US20040110817A1 (en) 2002-11-18 2004-06-10 Pfizer Inc Dipeptidyl peptidase IV inhibiting fluorinated cyclic amides
WO2004046106A1 (en) 2002-11-18 2004-06-03 Pfizer Products Inc. Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides
DE10256264A1 (de) 2002-12-03 2004-06-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Imidazo-pyridinone und Imidazo-pyridazinone, ihre Herstellung und ihre Verwendung als Arzneimittel
WO2004050658A1 (de) 2002-12-03 2004-06-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte imidazo-pyridinone und imidazo-pyridazinone, ihre herstellung und ihre verwendung als arzneimittel
WO2004050022A2 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004052850A2 (en) 2002-12-09 2004-06-24 Bristol-Myers Squibb Company Methods and compounds producing dipeptidyl peptidase iv inhibitors and intermediates thereof
WO2004052362A1 (en) 2002-12-10 2004-06-24 Novartis Ag Combination of an dpp-iv inhibitor and a ppar-alpha compound
WO2004058266A1 (en) 2002-12-20 2004-07-15 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004065380A1 (en) 2003-01-14 2004-08-05 Arena Pharmaceuticals Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2004064778A2 (en) 2003-01-17 2004-08-05 Merck & Co. Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2004244412A (ja) 2003-01-20 2004-09-02 Kotobuki Seiyaku Kk ４位に置換基を有する２−シアノピロリジン誘導体及びその製造方法並びにそれを含有する薬剤
WO2004069162A2 (en) 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004067509A1 (ja) 2003-01-31 2004-08-12 Sanwa Kagaku Kenkyusho Co., Ltd. ジペプチジルペプチダーゼivを阻害する化合物
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
WO2004076413A2 (en) 2003-02-24 2004-09-10 Arena Pharmaceuticals, Inc. Phenyl- and pyridylpiperidine-derivatives as modulators of glucose metabolism
WO2004076433A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
WO2004080990A1 (ja) 2003-03-14 2004-09-23 Astellas Pharma Inc. Ｃ－グリコシド誘導体又はその塩
WO2004085378A1 (en) 2003-03-19 2004-10-07 Merck & Co. Inc. Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
WO2004085661A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
WO2004087053A2 (en) 2003-03-25 2004-10-14 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004087650A2 (en) 2003-03-27 2004-10-14 Merck & Co. Inc. Process and intermediates for the preparation of beta-amino acid amide dipeptidyl peptidase-iv inhibitors
WO2004092128A1 (en) 2003-04-10 2004-10-28 Smithkline Beecham Corporation Anhydrous crystalline forms of (2s, 4s)-1-{(2r)-2-amino-3-‘4-methoxybenzyl)sulfonyl!-3-methylbutanoyl}-4-fluoropyrrolindine-2-carbonitrile
WO2004096806A1 (ja) 2003-04-30 2004-11-11 Sumitomo Pharmaceuticals Co. Ltd. 縮合イミダゾール誘導体
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
US20040254226A1 (en) 2003-05-14 2004-12-16 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004103276A2 (en) 2003-05-14 2004-12-02 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004103993A1 (en) 2003-05-14 2004-12-02 Syrrx, Inc. Dipeptidyl peptidase inhibitors
WO2004104215A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase 7 (dpp7)
WO2004104216A2 (en) 2003-05-21 2004-12-02 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4)
WO2004108730A1 (en) 2003-06-05 2004-12-16 Fujisawa Pharmaceutical Co., Ltd. 1h-imidazo`4,5-d!pyridazines as dpp-iv inhibitors for the treatment of niddm
WO2004110375A2 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Combination therapy for the treatment of diabetes
WO2004110436A1 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004111041A1 (en) 2003-06-12 2004-12-23 Fujisawa Pharmaceutical Co., Ltd. Pyrrolidine, thiazolidine and oxazolidine compounds which inhibit dipeptidyl peptidase-iv (dpp)
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE10327439A1 (de) 2003-06-18 2005-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2004111051A1 (de) 2003-06-18 2004-12-23 Boehringer Ingelheim International Gmbh Imidazopyridazinon- und imidazopyridonderivate, deren herstellung und deren verwendung als arzneimittel
US20040259903A1 (en) 2003-06-20 2004-12-23 Markus Boehringer Pyrido [2,1-a] isoquinoline derivatives
WO2005000848A1 (en) 2003-06-20 2005-01-06 F. Hoffmann-La Roche Ag Pyrido` 2, 1-a - isoquinoline derivatives as dpp-iv inhibitors
WO2005000846A1 (en) 2003-06-20 2005-01-06 F.Hoffmann-La Roche Ag Hexahydropyridoisoqinolines as dpp-iv inhibitors
US20040259902A1 (en) 2003-06-20 2004-12-23 Markus Boehringer Pyrido [2,1-a] isoquinoline derivatives
US20050032804A1 (en) 2003-06-24 2005-02-10 Cypes Stephen Howard Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
WO2005003135A1 (en) 2003-06-24 2005-01-13 Merck & Co., Inc. Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
JP2005023038A (ja) 2003-07-04 2005-01-27 Taisho Pharmaceut Co Ltd 慢性腎疾患治療薬
WO2005007647A1 (en) 2003-07-11 2005-01-27 Arena Pharmaceuticals, Inc. Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2005009956A1 (en) 2003-07-21 2005-02-03 Smithkline Beecham Corporation (2s,4s)-4-fluoro-1-[4-fluoro-beta-(4-fluorophenyl)-l-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt and anhydrous crystalline forms thereof
US20050059716A1 (en) 2003-07-25 2005-03-17 Aventis Pharma Deutschland Gmbh Novel bicyclic cyanoheterocycles, process for their preparation and their use as medicaments
WO2005012312A1 (de) 2003-07-25 2005-02-10 Sanofi-Aventis Deutschland Gmbh Neue cyanothiazolide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE10333935A1 (de) 2003-07-25 2005-02-24 Aventis Pharma Deutschland Gmbh Neue bicyclische Cyanoheterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US20050059724A1 (en) 2003-07-25 2005-03-17 Aventis Pharma Deutschland Gmbh Novel cyanopyrrolidides, process for their preparation and their use as medicaments
WO2005012308A1 (de) 2003-07-25 2005-02-10 Sanofi-Aventis Deutschland Gmbh Neue cyanopyrrolidide, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
WO2005011581A2 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2005012249A2 (en) 2003-08-01 2005-02-10 Bristol-Myers Squibb Company Adamantyglycine- based inhibitors of dipeptidyl peptidase iv for the treatment of diabetes
US20050038020A1 (en) 2003-08-01 2005-02-17 Hamann Lawrence G. Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods
WO2005012326A1 (en) 2003-08-01 2005-02-10 Tanabe Seiyaku Co., Ltd. Novel compounds having inhibitory activity against sodium-dependant transporter
US20050043292A1 (en) 2003-08-20 2005-02-24 Pfizer Inc Fluorinated lysine derivatives as dipeptidyl peptidase IV inhibitors
WO2005019168A2 (en) 2003-08-20 2005-03-03 Pfizer Products Inc. Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors
WO2005020920A2 (en) 2003-09-02 2005-03-10 Merck & Co., Inc. Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2005030751A2 (en) 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005025554A2 (en) 2003-09-09 2005-03-24 Japan Tobacco Inc. Dipeptidyl peptidase iv inhibitor
WO2005030127A2 (en) 2003-09-23 2005-04-07 Merck & Co., Inc. Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
WO2005032590A1 (ja) 2003-10-03 2005-04-14 Takeda Pharmaceutical Company Limited 糖尿病治療剤
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
WO2005037779A2 (de) 2003-10-15 2005-04-28 Imtm Gmbh Neue dipeptidylpeptidase iv-inhibitoren zur funktionellen beeinflussung unterschiedlicher zellen und zur behandlung immunologischer, entzündlicher, neuronaler und anderer erkrankungen
WO2005034940A2 (de) 2003-10-15 2005-04-21 Imtm Gmbh Duale alanyl-aminopeptidase- und dipeptidylpeptidase iv-inhibitoren zur funktionellen beeinflussung unterschiedlicher zellen und zur behandlung immunologischer, entzündlicher, neuronaler und anderer erkrankungen
WO2005040095A1 (en) 2003-10-16 2005-05-06 Astrazeneca Ab Inhibitors of dipeptidyl peptidase iv
WO2005037828A1 (en) 2003-10-20 2005-04-28 Lg Life Sciences Ltd. Novel inhibitors of dpp-iv, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
WO2005042488A1 (en) 2003-10-31 2005-05-12 Takeda Pharmaceutical Company Limited Pyridine compounds as inhibitors of dipeptidyl peptidase iv
WO2005044195A2 (en) 2003-11-04 2005-05-19 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2005047297A1 (en) 2003-11-12 2005-05-26 Phenomix Corporation Heterocyclic boronic acid compounds
WO2005049022A2 (en) 2003-11-17 2005-06-02 Novartis Ag Use of dipeptidyl peptidase iv inhibitors
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
WO2005063750A1 (de) 2003-12-23 2005-07-14 Boehringer Ingelheim International Gmbh Bicyclische imidazolverbindungen, deren herstellung und deren verwendung als arzneimittel
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
US20080146818A1 (en) 2004-02-05 2008-06-19 Yasumichi Fukuda Bicycloester Derivative
WO2005079795A2 (en) 2004-02-20 2005-09-01 Novartis Ag Dpp-iv inhibitors for treating neurodegeneration and cognitive disorders
WO2005082849A1 (en) 2004-02-23 2005-09-09 Trustees Of Tufts College Lactams as conformationally constrained peptidomimetic inhibitors
WO2005082348A2 (en) 2004-02-23 2005-09-09 Trustees Of Tufts College Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism
WO2005087235A1 (en) 2004-03-09 2005-09-22 National Health Research Institutes Pyrrolidine compounds
WO2005095381A1 (en) 2004-03-15 2005-10-13 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005092877A1 (de) 2004-03-16 2005-10-06 Boehringer Ingelheim International Gmbh Glucopyranosyl-substituierte benzol-derivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2005116014A1 (en) 2004-05-12 2005-12-08 Pfizer Products Inc. Proline derivatives and their use as dipeptidyl peptidase iv inhibitors
US20090036434A1 (en) * 2004-06-04 2009-02-05 Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US20070167468A1 (en) 2004-08-06 2007-07-19 Sanofi-Aventis Deutschland Gmbh Substituted bicyclic 8-pyrr0lidinoxanthines, methods for their production, pharmaceutical formulations and their use
WO2006040625A1 (en) 2004-10-12 2006-04-20 Glenmark Pharmaceuticals S.A. Novel dipeptidyl peptidase iv inhibitors, pharmaceutical compositions containing them, and process for their preparation
US20090192129A1 (en) 2004-12-12 2009-07-30 Dainippon Sumitomo Pharma Co., Ltd. Bicyclic pyrrole derivatives
WO2006068163A1 (ja) 2004-12-24 2006-06-29 Dainippon Sumitomo Pharma Co., Ltd. 二環性ピロール誘導体
WO2006076231A2 (en) 2005-01-10 2006-07-20 Arena Pharmaceuticals, Inc. Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood glp-1 level
WO2006080421A1 (ja) 2005-01-28 2006-08-03 Chugai Seiyaku Kabushiki Kaisha スピロケタール誘導体、およびその糖尿病治療薬としての使用
WO2006088129A1 (ja) 2005-02-18 2006-08-24 Mitsubishi Pharma Corporation プロリン誘導体の塩、またはその溶媒和物、及びその製造方法
US20090216016A1 (en) 2005-02-18 2009-08-27 Mitsubishi Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
WO2006100181A2 (en) 2005-03-22 2006-09-28 F. Hoffmann-La Roche Ag New salt and polymorphs of a dpp-iv inhibitor
WO2006116157A2 (en) 2005-04-22 2006-11-02 Alantos Pharmaceuticals Holding, Inc. Dipeptidyl peptidase-iv inhibitors
EP1902730A1 (en) 2005-06-09 2008-03-26 Banyu Pharmaceutical Co., Ltd. Npy y2 agonist for use as therapeutic agent for disease accompanied by diarrhea
WO2007019255A2 (en) 2005-08-04 2007-02-15 Novartis Ag Salts of vildagliptin
WO2007027651A2 (en) 2005-08-30 2007-03-08 Abbott Laboratories Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
WO2007035372A2 (en) 2005-09-16 2007-03-29 Takeda Pharmaceutical Company Limited Polymorphs of benzoate salt of 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2h)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor
WO2007071576A1 (en) 2005-12-21 2007-06-28 F. Hoffmann-La Roche Ag New salt and polymorph of dpp-iv inhibitor
WO2007120702A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Use of gpr119 receptor agonists for increasing bone mass and for treating osteoporosis, and combination therapy relating thereto
WO2007120689A2 (en) 2006-04-11 2007-10-25 Arena Pharmaceuticals, Inc. Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual
WO2007128721A1 (de) 2006-05-04 2007-11-15 Boehringer Ingelheim Internationalgmbh Polymorphe
WO2007148185A2 (en) 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
WO2008027273A2 (en) 2006-08-30 2008-03-06 Phenomix Corporation Solid citrate and tartrate salts of dpp-iv inhibitors
WO2008067465A1 (en) 2006-11-29 2008-06-05 Takeda Pharmaceutical Company Limited Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2h-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008109591A1 (en) 2007-03-08 2008-09-12 Lexicon Pharmaceuticals, Inc. Phlorizin analogs as inhibitors of sodium glucose co-transporter 2
WO2008114857A1 (ja) 2007-03-22 2008-09-25 Kyorin Pharmaceutical Co., Ltd. アミノアセチルピロリジンカルボニトリル誘導体の製造方法
WO2009084497A1 (ja) 2007-12-28 2009-07-09 Dainippon Sumitomo Pharma Co., Ltd. メチル置換ピペリジン誘導体
WO2009126245A1 (en) 2008-04-07 2009-10-15 Arena Pharmaceuticals, Inc. Methods of using a g protein-coupled receptor to identify peptide yy (pyy) secretagogues and compounds useful in the treatment of conditions modulated by pyy
WO2010075273A1 (en) * 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof

Non-Patent Citations (124)

* Cited by examiner, † Cited by third party
Title
"World Health Organization Technical Report Series", PREVENTION AND MANAGEMENT OF OSTEOPOROSIS, vol. 921, 2003
ABBOTT ET AL., BRAIN RES, vol. 1043, 2005, pages 139 - 144
ABE ET AL., J. NA.T PROD., vol. 67, 2004, pages 999 - 1004
ADRIAN ET AL., GASTRUENTERUL, vol. 89, 1985, pages 1070 - 1077
AHREN ET AL., DIABETES CARE, vol. 25, 2002, pages 869 - 875
AHREN ET AL., ENDOCRINOLOGY, vol. 146, 2005, pages 2055 - 2059
AHREN ET AL., J. CLIN. ENDOCRINOL. METAB., vol. 89, 2004, pages 2078 - 2084
AREHART ET AL., CIRC RES, CIRC. RES., vol. 102, 2008, pages 986 - 993
ATIK ET AL., CLIN. ORTHOP. RELAT. RES., vol. 443, 2006, pages 19 - 24
BALASUBRAMANIAM ET AL., J. MED. CHEM., vol. 43, 2000, pages 3420 - 3427
BALASUBRAMANIAM ET AL., PEPTIDES, vol. 28, 2007, pages 235 - 240
BATTERHAM ET AL., NATURE, vol. 418, 2002, pages 650 - 654
BEHRE, SCAND J CLIN LAB INVEST, vol. 67, 2007, pages 449 - 458
BERGE ET AL., JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 66, 1977, pages 1 - 19
BILCHIK ET AL., GASTROENTEROL, vol. 105, 1993, pages 1441 - 1448
BOEY ET AL., DIABETOLOGIA, vol. 49, 2006, pages 1360 - 1370
BOEY ET AL., NEUROPEPTIDES, vol. 42, 2008, pages 19 - 30
BOLLAG ET AL., ENDOCRINOLOGY, vol. 141, 2000, pages 1228 - 1235
BOLLAG ET AL., MOL CELL ENDOCRINOL, vol. 177, 2001, pages 35 - 41
BOSE ET AL., DIABETES, vol. 54, 2005, pages 146 - 151
BRADLEY, 1 PATHOL, vol. 214, 2008, pages 149 - 160
BRANCATI, F. L. ET AL., ARCH. INTERN. MED., vol. 159, 1999, pages 957 - 963
CALDWELL ET AL., BIOORG. MED.CHEM. LETT., vol. 14, 2004, pages 1265 - 1268
CHAUDHRI, ANNU REV PHYSIOL, vol. 70, 2008, pages 239 - 255
COLLIER, T. L., J. LABELLED COMPD. RADIOPHARM., vol. 42, 1999, pages S264 - S266
COX, PEPTIDES, vol. 28, 2007, pages 345 - 351
CRUZE ET AL., PEPTIDES, vol. 28, 2007, pages 269 - 280
DEACON ET AL., J CLIN ENDOCRINOL METAB, vol. 85, 2000, pages 3575 - 3581
DEACON, REGUL PEPT, vol. 128, 2005, pages 117 - 124
DRUCKER, CELL METAB, vol. 3, 2006, pages 153 - 165
DURING ET AL., NAT. MED., vol. 9, 2003, pages 1173 - 1179
EBERLEIN ET AL., PEPTIDES, vol. 10, 1989, pages 797 - 803
EDMONDSON ET AL., BIOORG. MED. CHEM. LETT., vol. 14, 2004, pages 5151 - 5155
EKBLAD ET AL., PEPTIDES, vol. 23, 2002, pages 251 - 261
EKSTRAND ET AL., PNAS USA, vol. 100, 2003, pages 6033 - 6038
EL BAHH ET AL., EUR..1. NEUROSCI., vol. 22, 2005, pages 1417 - 1430
G. P. STAHLY, CRYSTAL GROWTH & DESIGN, vol. 7, no. 6, 2007, pages 1007 - 1026
GOMEZ ET AL., AM. J. PHYSIOL., vol. 268, 1995, pages G71 - G81
GONON ET AL., CARDIOVASC RES., vol. 78, 2008, pages 116 - 122
GRANDT ET AL., REGUL. PEPT., vol. 51, 1994, pages 151 - 159
GREENE, T. W., WUTS, P. G. M.: "Protecting Groups in Organic Synthesis", 1999, WILEY
GREIG ET AL., ANN N Y ACAD SCI, vol. 1035, 2004, pages 290 - 315
GRISE ET AL., J. SURG. RES., vol. 82, 1999, pages 151 - 155
GUERRE-MILLO, DIABETES & METABOLISM, vol. 34, 2008, pages 12 - 18
H.-U. DEMUTH ET AL.: "Type 2 diabetes-therapy with DPP-IV inhibitors", BIOCHIM. BIOPHYS. ACTA, vol. 1751, 2005, pages 33 - 44
HANSMANN ET AL., CIRCULATION, vol. 115, 2007, pages 1275 - 1284
HARA ET AL., DIABETES CARE, vol. 29, 2006, pages 1357 - 1362
HAY ET AL., J. CLIN. GASTROENTEROL., vol. 14, 1992, pages 309 - 317
HILL, J. O. ET AL., SCIENCE, vol. 280, 1998, pages 1371 - 1374
JONES ET AL., ANN. REP. MED. CHEM, vol. 44, 2009, pages 149 - 170
JONES ET AL., ANN. REP. MED. CHEM., vol. 44, 2009, pages 149 - 170
JONES, EXPERT OPIN. THER. PATENTS, vol. 19, no. 10, 2009, pages 1339 - 1359
K. AUGUSTYNS ET AL.: "Inhibitors of proline-specific dipeptidyl peptidases: DPP-IV inhibitors as a novel approach for the treatment of type 2 diabetes", EXPERT OPIN. THER. PATENTS, vol. 15, 2005, pages 1387 - 1407, XP002453370, DOI: doi:10.1517/13543776.15.10.1387
K.J. GUILLORY: "Polymorphism in Pharmaceutical Solids", vol. 95, 1999, MARCEL DEKKER, INC., article "Generation of Polymorphs, Hydrates, Solvates, and Amorphous Solids", pages: 202 - 209
KEIGHLEY ET AL., AILMENT PHARMACOL. THER., vol. 18, 2003, pages 66 - 70
KEIRE ET AL., AM. J. PHYSIOL. GASTROINTEST. LIVER PHYSIOL., vol. 279, 2000, pages G126 - G131
KUBOTA, J. BIOL. CHEM., vol. 277, 2002, pages 25863 - 25866
LAMB ET AL., J. MED. CHEM., vol. 50, 2007, pages 2264 - 2268
LE BAS, M.-D., J. LABELLED COMPD. RADIOPHARM., vol. 44, 2001, pages S280 - S282
LE STUNFF ET AL., DIABETES, vol. 43, 1989, pages 696 - 702
LEE ET AL., J. CLIN. INVEST., vol. 111, 2003, pages 1853 - 1862
LEE ET AL., PEPTIDES, vol. 24, 2003, pages 99 - 106
LIU ET AL., AM SURG, vol. 62, 1996, pages 232 - 236
LIU ET AL., J. SURG. RES., vol. 58, 1995, pages 6 - 11
LIU ET AL., J. SURG. RES., vol. 58, 1995, pages 707 - 712
LIU ET AL., SURGERY, vol. 118, 1995, pages 229 - 236
LUNDBERG ET AL., PNAS USA, vol. 79, 1982, pages 4471 - 4475
MAEDA ET AL., NUT. MED., vol. 8, 2002, pages 731 - 737
MARSO ET AL., DIABETES CARE, vol. 31, 2008, pages 989 - 994
MATSUDA ET AL., J BIOL CHEM, vol. 277, 2002, pages 37487 - 37491
MCINTOSH ET AL., REGUL PEPT, vol. 128, 2005, pages 159 - 165
MCPADDEN ET AL., AM. J. SURG., vol. 188, 2004, pages 516 - 519
MENTLEIN, EXPERT OPIN INVESTIG DRUGS, vol. 14, 2005, pages 57 - 64
MORLEY ET AL., LIFE SCIENCES, vol. 41, 1987, pages 2157 - 2165
NAUCK ET AL., DIABETES, vol. 53, no. 3, 2004, pages 190 - 196
NAUCK ET AL., DRUG NEWS PERSPECT, vol. 16, 2003, pages 413 - 422
NIGHTINGALE ET AL., GUT, vol. 39, 1996, pages 267 - 272
NISHIMURA ET AL., CIRCULATION, vol. 117, 2008, pages 216 - 223
O'BRIEN, M., DAILY, B., SCHURRIA, M.: "Assay for DPPIV activity using a homogeneous, luminescent method", CELL NOTES, no. 11, 2005
OHASHI ET AL., HYPERTENSION, vol. 47, 2006, pages 1108 - 1116
OKADA ET AL., ENDOCRINOLOGY SUPPLEMENT, 1993, pages 180
OKU ET AL., FEBS LETTERS, vol. 581, 2007, pages 5029 - 5033
ORTIZ ET AL., IPET, vol. 323, 2007, pages 692 - 700
ORTIZ ET AL., JPET, vol. 323, 2007, pages 692 - 700
OUCHI ET AL., CIRCULATION, vol. 100, 1999, pages 2473 - 2476
OUCHI ET AL., CLIN CHIM ACTA, vol. 380, 2007, pages 24 - 30
PARKER ET AL., BR. J. PHARMACOL., vol. 153, 2008, pages 420 - 431
PARKER ET AL., BR.J. PHARMACOL., vol. 153, 2008, pages 420 - 431
PEARSON, NURSING TIMES, vol. 100, 2004, pages 86 - 90
PEDERSON, P., DIAB. METAB. REV., vol. 5, 1989, pages 505 - 509
PERRY, I. J. ET AL., BMJ, vol. 310, 1995, pages 560 - 564
PETERS ET AL., BIOORG. MED. CHEM. LETT., vol. 14, 2004, pages 1491 - 1493
PITTNER ET AL., INT. J. OBES. RELAT. METAB. DISORD., vol. 28, 2004, pages 963 - 971
RAISZ, J. CLIN. INVEST., vol. 115, 2005, pages 3318 - 3325
REMINGTON: "The Science and Practice of Pharmacy", 2000, LIPPINCOTT WILLIAMS & WILKINS
RENSHAW ET AL., CURRENT DRUG TARGETS, vol. 6, 2005, pages 171 - 179
RIMOIN, D. L.: "Emery and Rimoin's Principles and Practice of Medical Genetics", vol. 1, 1996, pages: 1401 - 1402
ROTWEIN, R. ET AL., N. ENGL. J. MED., vol. 308, 1983, pages 65 - 71
RUGGERI, NAT MED, vol. 8, 2002, pages 1227 - 1234
SCHWARTZ, CELL METABOLISM, vol. 11, 2010, pages 445 - 447
SHAH, CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT, vol. 12, 2009, pages 519 - 532
SHIBATA ET AL., J. BIOL. CHEM., vol. 279, 2004, pages 28670 - 28674
SHIBATA ET AL., J. MOL. CELL CARDIOL., vol. 42, 2007, pages 1065 - 1074
SHIBATA ET AL., NAT MED, vol. 11, 2005, pages 1096 - 1103
SHORE ET AL., J. ALLERGY CLIN. IMMUNOL, vol. 118, 2006, pages 389 - 395
SUMMER ET AL., AM J. PHYSIOL. LUNG CELL MOL. PHYSIOL, 7 March 2008 (2008-03-07)
T. IIIGUCHI, V. STELLA: "Pro-drugs as Novel Delivery Systems", vol. 14, A.C.S. SYMPOSIUM SERIES
TAO ET AL., CIRCULATION, vol. 115, 2007, pages 1408 - 1416
TATEMOTO ET AL., NATURE, vol. 285, 1980, pages 417 - 418
TILG ET AL., NAT. REV. IMMUNOL., vol. 6, 2006, pages 772 - 783
TSENG ET AL., PEPTIDES, vol. 23, 2002, pages 389 - 395
TSUKIYAMA ET AL., MOL ENDOCRINOL, vol. 20, 2006, pages 1644 - 1651
UENO ET AL., REGUL PEPT, vol. 145, 2008, pages 12 - 16
VILLHAUER ET AL., J. MED. CHEM., vol. 45, 2002, pages 2362 - 2365
VILLHAUER ET AL., J. MED. CHEM., vol. 46, 2003, pages 2774 - 2789
VONA-DAVIS ET AL., PEPTIDES, vol. 28, 2007, pages 334 - 338
WOLDBYE ET AL., NEUROBIOLOGY OF DISEASE, vol. 20, 2005, pages 760 - 772
WORTLEY ET AL., GASTROENTEROL, vol. 133, 2007, pages 1534 - 1543
XIE ET AL., BONE, vol. 37, 2005, pages 759 - 769
YAMAMOTO ET AL., CLINICAL SCIENCE, vol. 103, 2002, pages 137 - 142
YOKOTA, BLOOD, vol. 96, 2000, pages 1723 - 1732
ZANDER ET AL., LANCET, vol. 359, 2002, pages 824 - 830
ZHONG ET AL., AM J PHYSIOL ENDOCRINOL METAB, vol. 292, 2007, pages E543 - E548
ZHU, G-D., 1. ORG. CHEM., vol. 67, 2002, pages 943 - 948

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8933083B2 (en) 2003-01-14 2015-01-13 Arena Pharmaceuticals, Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
WO2012170867A1 (en) 2011-06-09 2012-12-13 Rhizen Pharmaceuticals Sa Novel compounds as modulators of gpr-119
WO2014011926A1 (en) 2012-07-11 2014-01-16 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US11884626B2 (en) 2015-06-22 2024-01-30 Arena Pharmaceuticals, Inc. Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1P1 receptor-associated disorders
US11534424B2 (en) 2017-02-16 2022-12-27 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
US12156866B2 (en) 2018-06-06 2024-12-03 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
WO2020250123A1 (en) 2019-06-10 2020-12-17 Lupin Limited Prmt5 inhibitors
US12391695B2 (en) 2019-06-10 2025-08-19 Lupin Limited PRMT5 inhibitors

Also Published As

Publication number Publication date
EP3323818A1 (en) 2018-05-23
CO6700841A2 (es) 2013-06-28
CN103221410A (zh) 2013-07-24
US20140051629A1 (en) 2014-02-20
EA201390421A1 (ru) 2013-09-30
PH12013500547A1 (en) 2013-06-10
CN103221410B (zh) 2017-09-15
AU2011305525B2 (en) 2016-08-18
AU2011305525A1 (en) 2013-05-09
MX2013003184A (es) 2013-06-07
US20210340133A1 (en) 2021-11-04
AU2011305525A8 (en) 2013-05-23
BR112013008100A2 (pt) 2016-08-09
JP5941916B2 (ja) 2016-06-29
DOP2013000061A (es) 2013-07-31
JP2013537242A (ja) 2013-09-30
CN103539791B (zh) 2017-01-11
NI201300030A (es) 2013-05-06
CR20130145A (es) 2013-07-09
GT201300075A (es) 2014-08-26
CN103539791A (zh) 2014-01-29
ECSP13012704A (es) 2013-08-30
CL2013000785A1 (es) 2013-11-15
US10894787B2 (en) 2021-01-19
KR101871011B1 (ko) 2018-06-25
AU2016259322A1 (en) 2016-12-01
PE20131371A1 (es) 2013-11-25
EP2619198A1 (en) 2013-07-31
HK1254745A1 (en) 2019-07-26
CA2812061A1 (en) 2012-03-29
SG188548A1 (en) 2013-04-30
KR20130119921A (ko) 2013-11-01

Similar Documents

Publication Publication Date Title
US20210340133A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20130023494A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140051714A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2011005929A1 (en) Piperidine derivative and its use for the treatment of diabets and obesity
US20140038889A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
US20140066369A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140018371A1 (en) Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2013055910A1 (en) Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20100160359A1 (en) Modulators of Metabolism and the Treatment of Disorders Related Thereto
JP2009542702A (ja) 代謝の調節因子および代謝に関連する障害の処置
JP2009542699A (ja) 代謝の調節因子および代謝に関連する障害の処置
WO2014074668A1 (en) Modulators of gpr119 and the treatment of disorders related thereto
EA040124B1 (ru) Модуляторы рецептора gpr119 и лечение связанных с ним нарушений

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 11764056

Country of ref document: EP

Kind code of ref document: A1

DPE1 Request for preliminary examination filed after expiration of 19th month from priority date (pct application filed from 20040101)
WWE Wipo information: entry into national phase

Ref document number: 225065

Country of ref document: IL

ENP Entry into the national phase

Ref document number: 2812061

Country of ref document: CA

ENP Entry into the national phase

Ref document number: 2013529426

Country of ref document: JP

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: MX/A/2013/003184

Country of ref document: MX

WWE Wipo information: entry into national phase

Ref document number: 2013000785

Country of ref document: CL

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 13057520

Country of ref document: CO

Ref document number: 000624-2013

Country of ref document: PE

Ref document number: 12013500547

Country of ref document: PH

Ref document number: CR2013-000145

Country of ref document: CR

WWE Wipo information: entry into national phase

Ref document number: 13062

Country of ref document: GE

ENP Entry into the national phase

Ref document number: 20137009961

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: A201305118

Country of ref document: UA

Ref document number: 201390421

Country of ref document: EA

WWE Wipo information: entry into national phase

Ref document number: 2011764056

Country of ref document: EP

ENP Entry into the national phase

Ref document number: 2011305525

Country of ref document: AU

Date of ref document: 20110921

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 13825601

Country of ref document: US

REG Reference to national code

Ref country code: BR

Ref legal event code: B01A

Ref document number: 112013008100

Country of ref document: BR

ENP Entry into the national phase

Ref document number: 112013008100

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20130321