HRP20120006T1 - Derivat bicikloestera - Google Patents

Derivat bicikloestera Download PDF

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Publication number
HRP20120006T1
HRP20120006T1 HR20120006T HRP20120006T HRP20120006T1 HR P20120006 T1 HRP20120006 T1 HR P20120006T1 HR 20120006 T HR20120006 T HR 20120006T HR P20120006 T HRP20120006 T HR P20120006T HR P20120006 T1 HRP20120006 T1 HR P20120006T1
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Croatia
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group
substituted
unsubstituted
amino
pharmaceutically acceptable
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HR20120006T
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English (en)
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Fukuda Yasumichi
Asahina Yoshikazu
Ohata Kohei
Yokota Kazuya
Murakami Koji
Matsui Toshiyuki
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Kyorin Pharmaceutical Co.
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Publication of HRP20120006T1 publication Critical patent/HRP20120006T1/hr

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P3/06—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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

Derivat bicikloestera, naznačen time što ga prikazuje sljedeća opća formula (1): u kojoj R1 je supstituirana ili nesupstituirana C1 do C6 alkilna skupina, supstituirana ili nesupstituirana C3 do C6 cikloalkilna skupina, tetrahidropiranilna skupina, supstituirana ili nesupstituirana arilmetilna skupina, supstituirana ili nesupstituirana ariletilna skupina, supstituirana ili nesupstituirana aromatska ugljikovodična skupina, supstituirani ili nesupstituirani aromatski heterociklički prsten ili supstituirani ili nesupstituirani alifatski heterociklički prsten; X je CH2, CHF, CF2, CHOH, S, ili O; in je 1, 2 ili 3, ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 12 patentnih zahtjeva.

Claims (13)

1. Derivat bicikloestera, naznačen time što ga prikazuje sljedeća opća formula (1): [image] u kojoj R1 je supstituirana ili nesupstituirana C1 do C6 alkilna skupina, supstituirana ili nesupstituirana C3 do C6 cikloalkilna skupina, tetrahidropiranilna skupina, supstituirana ili nesupstituirana arilmetilna skupina, supstituirana ili nesupstituirana ariletilna skupina, supstituirana ili nesupstituirana aromatska ugljikovodična skupina, supstituirani ili nesupstituirani aromatski heterociklički prsten ili supstituirani ili nesupstituirani alifatski heterociklički prsten; X je CH2, CHF, CF2, CHOH, S, ili O; i n je 1, 2 ili 3, ili njegova farmaceutski prihvatljiva sol.
2. Derivat bicikloestera u skladu s patentnim zahtjevom 1, naznačen time što ga prikazuje sljedeća opća formula (1): [image] u kojoj R1 je supstituirana ili nesupstituirana C1 do C6 alkilna skupina, supstituirana ili nesupstituirana arilmetilna skupina, ili supstituirana ili nesupstituirana ariletilna skupina; X je CH2, CHF ili CF2; i n je 1 ili 2 ili njegova farmaceutski prihvatljiva sol.
3. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što X je CH2.
4. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što X je CHF.
5. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što n je 1.
6. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što n je 2.
7. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što R1 je C1 do C6 alkilna skupina, koja može imati 1 do 5 supstituenti, koje se bira iz skupine koju čine atom halogena, hidroksi skupina, cijano skupina, C1 do C6 alkoksi skupina, supstituirana ili nesupstituirana ariloksi skupina, C1 do C6 alkilkarbonilna skupina, C1 do C6 alkoksikarbonilna skupina, C1 do C6 alkiltio skupina, amino skupina, mono- ili disupstituirana C1 do C6 alkilamino skupina, 4- do 9-eročlana prstenasta amino skupina, koja može sadržavati 1 do 3 heteroatoma, formilamino skupina, C1 do C6 alkilkarbonilamino skupina, C1 do C6 alkoksikarbonilamino skupina, C1 do C6 alkilsulfonilamino skupina, te supstituirana ili nesupstituirana arilsulfonilamino skupina.
8. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što R1 je C1 do C6 alkilna skupina, koju se bira iz skupine koju čine metilna skupina, ciklopropilmetilna skupina, etilna skupina, propilna skupina, 1-metiletilna skupina, 1-metilpropilna skupina, 2-metilpropilna skupina, 1-etilpropilna skupina, 2-etilpropilna skupina, butilna skupina, t-butilna skupina, te heksilna skupina.
9. Derivat bicikloestera u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što derivat bicikloestera se bira iz skupine koju čine (2S,4S)-1-[[N-(4-etoksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]-4-fluorpirolidin-2-karbonitril, (2S)-1-[[N-(4-etoksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]pirolidin-2-karbonitril, (2S)-1-[[N-(4-t-butoksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]pirolidin-2-karbonitril, (2S,4S)-1-[[N-[4-(2-tetrahidropiranil)oksikarbonilbiciklo[2.2.2]okt-1-il]amino]acetil]-4-fluorpirolidin-2-karbonitril, (2S)-1-[[N-[4-(2-tetrahidropiranil)oksikarbonilbiciklo[2.2.2]okt-1-il]amino]acetil]pirolidin-2-karbonitril, (2S,4S)-1-[[N-(4-etoksikarbonilbiciklo[2.2.1]hept-1-il)amino]acetil]-4-fluorpirolidin-2-karbonitril, (2S)-1-[[N-(4-etoksikarbonilbiciklo[2.2.1]hept-1-il)amino]acetil]pirolidin-2-karbonitril, (2S,4S)-1-[[N-(4-benziloksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]-4-fluorpirolidin-2-karbonitril, (2S,4S)-1-[[N-(4-ciklopropilmetiloksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]-4-fluorpirolidin-2-karbonitril, (2S,4S)-4-fluor-1-[[N-(4-(4-trifluormetil)benziloksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]pirolidin-2-karbonitril, (2S,4S)-4-fluor-1-[[N-(4-izobutiloksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]pirolidin-2-karbonitril, te (2S,4S)-4-fluor-1-[[N-(4-izopropiloksikarbonilbiciklo[2.2.2]okt-1-il)amino]acetil]pirolidin-2-karbonitril.
10. Farmaceutski proizvod, naznačen time što kao aktivni sastojak sadrži derivat bicikloestera u skladu s patentnim zahtjevom 1 do 9, ili njegovu farmaceutski prihvatljivu sol.
11. Inhibitor DPP-IV, naznačen time što kao aktivni sastojak sadrži derivat bicikloestera u skladu s patentnim zahtjevom 1 do 9, ili njegovu farmaceutski prihvatljivu sol.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi in the liječenje i/ili sprječavanje medicinskog stanja, koje se bira iz skupine koju čine dijabetes, dijabetične komplikacije, hiperinzulinemija, hiperglikemija, abnormalni metabolizam lipida, pretilost, AIDS kao posljedica infekcije virusom HIV-1, odbacivanje presađenog organa ili tkiva, multipla skleroza, reumatoidni artritis, upala, alergije, osteoporoza, psorijaza i lišaj, dobroćudna hipertrofija prostate, metastaze raka dojke i prostate u plućima, hipertenzija i zarazne bolesti.
13. Spoj namijenjen upotrebi u liječenju i/ili sprječavanju medicinskog stanja u skladu s patentnim zahtjevom 12, naznačen time što medicinsko stanje je dijabetes ili dijabetične komplikacije.
HR20120006T 2004-02-05 2012-01-03 Derivat bicikloestera HRP20120006T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2004029856 2004-02-05
PCT/JP2005/001377 WO2005075421A1 (ja) 2004-02-05 2005-02-01 ビシクロエステル誘導体

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HRP20120006T1 true HRP20120006T1 (hr) 2012-01-31

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US (2) US7754757B2 (hr)
EP (1) EP1712547B1 (hr)
JP (1) JP3954626B2 (hr)
KR (1) KR101130433B1 (hr)
CN (2) CN1918119B (hr)
AT (1) ATE537141T1 (hr)
AU (1) AU2005210285B2 (hr)
BR (1) BRPI0506622A (hr)
CA (1) CA2554493C (hr)
CY (1) CY1112550T1 (hr)
DK (1) DK1712547T3 (hr)
ES (1) ES2375625T3 (hr)
HK (1) HK1100511A1 (hr)
HR (1) HRP20120006T1 (hr)
NO (1) NO20063486L (hr)
NZ (1) NZ548440A (hr)
PL (1) PL1712547T3 (hr)
PT (1) PT1712547E (hr)
RS (1) RS52163B (hr)
SI (1) SI1712547T1 (hr)
WO (1) WO2005075421A1 (hr)
ZA (1) ZA200606237B (hr)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101130433B1 (ko) * 2004-02-05 2012-03-27 교린 세이야꾸 가부시키 가이샤 비시클로에스테르 유도체
EP1719757B1 (en) * 2004-02-27 2013-10-09 Kyorin Pharmaceutical Co., Ltd. Bicyclo derivative
GB0526291D0 (en) 2005-12-23 2006-02-01 Prosidion Ltd Therapeutic method
CN101395131B (zh) * 2006-03-08 2012-11-14 杏林制药株式会社 氨基乙酰基吡咯烷甲腈衍生物的制备方法及其制备中间体
JP2010120851A (ja) * 2007-02-09 2010-06-03 Kyorin Pharmaceut Co Ltd 二量化シクロ誘導体
JPWO2008114857A1 (ja) 2007-03-22 2010-07-08 杏林製薬株式会社 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
EP2143443B1 (en) 2007-04-03 2014-11-19 Mitsubishi Tanabe Pharma Corporation A combination of dipeptidyl peptidase iv inhibitor and sweetener for use in the treatment of obesity
CL2008003653A1 (es) * 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
CA2732984A1 (en) * 2008-08-07 2010-02-11 Kyorin Pharmaceutical Co., Ltd. Process for production of bicyclo[2.2.2]octylamine derivative
WO2010018217A2 (en) 2008-08-15 2010-02-18 Boehringer Ingelheim International Gmbh Organic compounds for wound healing
CN102186474A (zh) * 2008-08-14 2011-09-14 杏林制药株式会社 稳定的医药组合物
US20110172444A1 (en) * 2008-09-16 2011-07-14 Futoshi Shiga Method for purifying aminoacetylpyrrolidinecarbonitrile derivative and salt thereof
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
KR101750420B1 (ko) * 2009-01-09 2017-06-26 오키드 파마 리미티드 디펩티딜 펩티다제 ｉｖ 억제제
TWI466672B (zh) 2009-01-29 2015-01-01 Boehringer Ingelheim Int 小兒科病人糖尿病之治療
EA029759B1 (ru) 2009-02-13 2018-05-31 Бёрингер Ингельхайм Интернациональ Гмбх Антидиабетические лекарственные средства, содержащие ингибитор dpp-4 (линаглиптин) необязательно в комбинации с другими антидиабетическими средствами
RU2011142829A (ru) * 2009-03-27 2013-05-10 Киорин Фармасьютикал Ко., Лтд. Препарат матричного типа с пролонгированным высвобождением, содержащий базисную добавку
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
EP3646859A1 (en) 2009-11-27 2020-05-06 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US20130109703A1 (en) 2010-03-18 2013-05-02 Boehringer Ingelheim International Gmbh Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions
CN102918027A (zh) 2010-04-06 2013-02-06 艾尼纳制药公司 Gpr119受体调节剂和对与所述受体有关的障碍的治疗
AU2011249722B2 (en) 2010-05-05 2015-09-17 Boehringer Ingelheim International Gmbh Combination therapy
BR112012032579B1 (pt) 2010-06-24 2021-05-11 Boehringer Ingelheim International Gmbh uso de linagliptina e composição farmacêutica compreendendo linagliptina e insulina basal de longa duração
JP2013216580A (ja) * 2010-08-06 2013-10-24 Kyorin Pharmaceutical Co Ltd ビシクロ［２．２．２］オクチルアミン誘導体の製造方法
AU2011305525B2 (en) 2010-09-22 2016-08-18 Arena Pharmaceuticals, 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
WO2012145603A1 (en) 2011-04-22 2012-10-26 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
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
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
WO2014159802A1 (en) * 2013-03-14 2014-10-02 Bristol-Myers Squibb Company Bicyclo [2.2.2] acid gpr120 modulators

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US20020006899A1 (en) 1998-10-06 2002-01-17 Pospisilik Andrew J. Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US5965764A (en) 1997-08-06 1999-10-12 Toray Industries, Inc. Process for producing a nitrile
US20030176357A1 (en) 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
MXPA01009410A (es) 1999-03-19 2003-06-06 Anormed Inc Composiciones farmaceuticas que comprenden complejos de metal.
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
US20040152745A1 (en) 1999-11-12 2004-08-05 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
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
US7064145B2 (en) 2000-02-25 2006-06-20 Novo Nordisk A/S Inhibition of beta cell degeneration
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
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
TW583185B (en) 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
TW540248B (en) 2000-07-19 2003-07-01 Koninkl Philips Electronics Nv Method and device for generating a multiplexed MPEG signal
EP1950199B1 (en) 2000-08-10 2009-12-02 Mitsubishi Tanabe Pharma Corporation Proline derivatives and use thereof as drugs
US20020037829A1 (en) 2000-08-23 2002-03-28 Aronson Peter S. Use of DPPIV inhibitors as diuretic and anti-hypertensive agents
KR100526091B1 (ko) 2000-10-06 2005-11-08 다나베 세이야꾸 가부시키가이샤 지방족 질소 함유 오원환 화합물
JP4329290B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 脂肪族含窒素五員環化合物
JP4329291B2 (ja) 2000-10-06 2009-09-09 田辺三菱製薬株式会社 含窒素五員環化合物
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
PL364221A1 (en) 2001-02-02 2004-12-13 Takeda Chemical Industries, Ltd. Fused heterocyclic compounds
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP4300108B2 (ja) 2001-06-27 2009-07-22 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ピロリジン類
IL158923A0 (en) 2001-06-27 2004-05-12 Smithkline Beecham Corp Fluoropyrrolidines as dipeptidyl peptidase inhibitors
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
US6869947B2 (en) 2001-07-03 2005-03-22 Novo Nordisk A/S Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
EP1404675B1 (en) 2001-07-03 2008-03-12 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
AU2002360732A1 (en) 2001-12-26 2003-07-24 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
WO2003080633A1 (en) 2002-03-25 2003-10-02 Nippon Kayaku Kabushiki Kaisha Novel $g(a)-amino-n-(diaminophosphinyl)lactam derivative
JP4329381B2 (ja) * 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
JP4329382B2 (ja) 2002-04-04 2009-09-09 田辺三菱製薬株式会社 医薬組成物
US20040106802A1 (en) 2002-04-08 2004-06-03 Torrent Pharmaceuticals Ltd. Novel compounds and therapeutic uses thereof
CN1633420A (zh) * 2002-04-08 2005-06-29 托伦脱药品有限公司 噻唑烷－4－腈和类似物以及它们作为二肽基－肽酶抑制剂的用途
JPWO2003095425A1 (ja) 2002-05-09 2005-09-15 大正製薬株式会社 シアノピロリジン誘導体
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
HUP0202001A2 (hu) 2002-06-14 2005-08-29 Sanofi-Aventis DDP-IV gátló hatású azabiciklooktán- és nonánszármazékok
GB0214344D0 (en) 2002-06-21 2002-07-31 Givaudan Sa New odorant Compounds
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
TW200401635A (en) 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
US20040121964A1 (en) 2002-09-19 2004-06-24 Madar David J. Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
KR101072236B1 (ko) 2002-09-19 2011-10-12 아보트 러보러터리즈 디펩티딜 펩티다제-ｉｖ(ｄｐｐ-ｉｖ)의 억제제로서의약제학적 조성물
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
PT1715893E (pt) 2004-01-20 2009-10-20 Novartis Pharma Ag Formulação para compressão directa e processos
KR101130433B1 (ko) * 2004-02-05 2012-03-27 교린 세이야꾸 가부시키 가이샤 비시클로에스테르 유도체
EP1717225A4 (en) * 2004-02-18 2009-10-21 Kyorin Seiyaku Kk BICYCLIC AMIDE DERIVATIVES
EP1719757B1 (en) 2004-02-27 2013-10-09 Kyorin Pharmaceutical Co., Ltd. Bicyclo derivative
TWI354569B (en) 2004-05-28 2011-12-21 Bristol Myers Squibb Co Coated tablet formulation and method
PE20060652A1 (es) 2004-08-27 2006-08-11 Novartis Ag Composiciones farmaceuticas de liberacion inmediata que comprenden granulos de fusion
EA013463B1 (ru) 2004-10-12 2010-04-30 ГЛЕНМАРК ФАРМАСЬЮТИКАЛС Эс.Эй. Новые ингибиторы дипептидилпептидазы iv, содержащие их фармацевтические композиции, способ их получения и способ лечения с их применением
JP2008019168A (ja) 2004-10-22 2008-01-31 Astellas Pharma Inc ２−シアノ−４−フルオロピロリジン誘導体の製造法
JP2006160733A (ja) 2004-11-15 2006-06-22 Taisho Pharmaceut Co Ltd シアノフルオロピロリジン誘導体を有効成分として含有する医薬
GT200600008A (es) 2005-01-18 2006-08-09 Formulacion de compresion directa y proceso
MY152185A (en) 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
CN101395131B (zh) 2006-03-08 2012-11-14 杏林制药株式会社 氨基乙酰基吡咯烷甲腈衍生物的制备方法及其制备中间体
JP2010120851A (ja) 2007-02-09 2010-06-03 Kyorin Pharmaceut Co Ltd 二量化シクロ誘導体
JPWO2008114857A1 (ja) 2007-03-22 2010-07-08 杏林製薬株式会社 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
JP2008239543A (ja) 2007-03-27 2008-10-09 Kyorin Pharmaceut Co Ltd ビシクロ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およびその製造中間体
JP2008290969A (ja) 2007-05-24 2008-12-04 Kyorin Pharmaceut Co Ltd アミノアセチルピロリジン誘導体の製造方法
JP2009114127A (ja) 2007-11-07 2009-05-28 Kyorin Pharmaceut 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

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