ME02609B - TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE - Google Patents

TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE

Info

Publication number
ME02609B
ME02609B MEP-2017-44A MEP201744A ME02609B ME 02609 B ME02609 B ME 02609B ME P201744 A MEP201744 A ME P201744A ME 02609 B ME02609 B ME 02609B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
fumaric acid
compound
acceptable derivative
salt
Prior art date
Application number
MEP-2017-44A
Other languages
German (de)
English (en)
French (fr)
Inventor
Laykea Tafesse
Shigeru Ando
Noriyuki Kurose
Original Assignee
Purdue Pharma Lp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46513798&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02609(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Purdue Pharma Lp filed Critical Purdue Pharma Lp
Publication of ME02609B publication Critical patent/ME02609B/me

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (17)

1. Jedinjenje formule (I): ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što: R1 je -halo ili; R4 je -H; svaki R8 i R9 je nezavisno -H, -halo, -CH3 ili -CF3; svaki halo je nezavisno -F, -Cl, -Br, ili -I; i m je ceo broj 1; gde je metil grupa vezana za piperazinski prsten (S)-2-metil grupa; i ugljenikov atom na a poziciji a-b veze je u (S) konfiguraciji; pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf, pseudopolimorf, solvat, kokristal, radioobeleženi oblik, i/ili tautomer.
2. Jedinjenje iz zahteva 1, naznačeno time, što je farmaceutski prihvatljivi derivat farmaceutski prihvatljiva so, radioobeleženi oblik, ili kokristal hlorovodonične kiseline, tartarne kiseline, benzensulfonske kiseline, p-toluensulfonske kiseline ili fumarne kiseline.
3. Jedinjenje iz zahteva 2, naznačeno time, što je farmaceutski prihvatljivi derivat so fumarne kiseline, fumarno-kiselinski kokristal ili njihova kombinacija.
4. Jedinjenje iz zahteva 1, sa formulom (II): ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što: R4 je -H; R8 je -H, -F ili -CH3; R9 je -H, -halo, -CH3 ili -CF3; i svaki halo je nezavisno -F, -Cl, -Br, ili -I, gde je metil grupa vezana za piperazinski prsten (S)-2-metil grupa; i ugljenikov atom na a poziciji a-b veze je u (S) konfiguraciji; i pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf, pseudopolimorf, solvat, kokristal, radioobeleženi oblik, i/ili tautomer.
5. Jedinjenje iz zahteva 4, naznačeno time, što je farmaceutski prihvatljivi derivat (i) farmaceutski prihvatljiva so, ili fumarno-kiselinski kokristal; ili (ii) so fumarne kiseline, fumarno-kiselinski kokristal, ili njihova kombinacija.
6. Jedinjenje iz zahteva 5, opcija (i), naznačeno time, što je farmaceutski prihvatljivi derivat so hlorovodonične kiseline, natrijumova so, kalijumova so, so p-toluensulfonske kiseline, so fumarne kiseline ili fumarno-kiselinski kokristal.
7. Jedinjenje iz zahteva 4 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što su: pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf. pseudopolimorf, solvat, kokristal, radioobeleženi oblik i/ili tautomer.
8. Jedinjenje iz bilo kojeg od zahteva 1 ili 7, naznačeno time, što je (i) so fumarne kiseline, fumarno-kiselinski kokristal, ili njihova kombinacija, ili (ii) slobodna baza.
9. Jedinjenje iz bilo kojeg od zahteva 1-8 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što se koriste za lečenje bola, bola udruženog sa osteoartritisom, osteoartritisa, UI, ulcera, IBD ili IBS, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
10. Proizvod kombinovanja jedinjenja iz bilo kojeg od zahteva 1-8 sa fumarnom kiselinom, naznačen time, što u proizvodu, molarni odnos (Jedinjenje Formule (I) ili (II)):(fumarna kiselina) iznosi oko 1.0:0.5.
11. Smeša, naznačena time, što sadrži (i) jedinjenje iz bilo kojeg od zahteva 1-8 ili njegov farmaceutski prihvatljivi derivat: ili (ii) proizvod iz zahteva 10;i farmaceutski prihvatljivi nosač ili ekscipijnt, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
12. Proizvod iz zahteva 10 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što se koriste za lečenje bola, bola udruženog sa osteoartritisom, osteoartritisa, UI, ulcera, IBD ili IBS, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
13. Jedinjenje iz zahteva 4, naznačeno time, što ima strukturu ili je fumarno-kiselinski kristal istog.
14. Jedinjenje iz zahteva 13, naznačeno time, što je u obliku kokristala nastalog kombinovanjem sa fumarnom kiselinom, pri čemu u kokristalu, molarni odnos (Jedinjenje):(fumarna kiselina) iznosi oko 1.0:0.5.
15. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 12.5º ± 0.2º, 16.8º ± 0.2º, i 25.3º ± 0.2º.
16. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 8.6º ± 0.2º, 12.5º ± 0.2º, 14.0º ± 0.2º, 16.8º ± 0.2º, 18.7º± 0.2º, i 25.3º ± 0.2º.
17. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 8.6º ± 0.2º, 12.5º ± 0.2º, 14.0º ± 0.2º, 16.8º ± 0.2º, 18.7º± 0.2º, 20.4º ± 0.2º, 21.3º ± 0.2º, 22.0º ± 0.2º, 23.2º ± 0.2º, 25.3º ± 0.2º i 38.5º ± 0.2º.
MEP-2017-44A 2011-06-22 2012-06-21 TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE ME02609B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161499989P 2011-06-22 2011-06-22
PCT/IB2012/001252 WO2012176061A1 (en) 2011-06-22 2012-06-21 Trpv1 antagonists including dihydroxy substituent and uses thereof
EP12735333.2A EP2723732B1 (en) 2011-06-22 2012-06-21 Trpv1 antagonists including dihydroxy substituent and uses thereof

Publications (1)

Publication Number Publication Date
ME02609B true ME02609B (me) 2017-06-20

Family

ID=46513798

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2017-44A ME02609B (me) 2011-06-22 2012-06-21 TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE

Country Status (34)

Country Link
US (4) US9273043B2 (me)
EP (2) EP2723732B1 (me)
JP (1) JP5699251B2 (me)
KR (2) KR20150055094A (me)
CN (2) CN105693712A (me)
AR (1) AR086709A1 (me)
AU (1) AU2012273652B2 (me)
BR (1) BR112013032658A2 (me)
CA (1) CA2837178C (me)
CL (1) CL2013003550A1 (me)
CO (1) CO6852081A2 (me)
CY (1) CY1119111T1 (me)
DK (1) DK2723732T3 (me)
ES (1) ES2620528T3 (me)
HR (1) HRP20170507T1 (me)
HU (1) HUE031372T2 (me)
IL (1) IL229817A (me)
LT (1) LT2723732T (me)
ME (1) ME02609B (me)
MX (1) MX354015B (me)
MY (1) MY185061A (me)
PE (1) PE20141531A1 (me)
PH (1) PH12013502412B1 (me)
PL (1) PL2723732T3 (me)
PT (1) PT2723732T (me)
RS (1) RS55701B1 (me)
RU (1) RU2621708C2 (me)
SG (2) SG195136A1 (me)
SI (1) SI2723732T1 (me)
SM (1) SMT201700197T1 (me)
TW (1) TWI453205B (me)
UA (1) UA113288C2 (me)
WO (1) WO2012176061A1 (me)
ZA (1) ZA201400419B (me)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273043B2 (en) * 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
KR101933622B1 (ko) * 2012-10-09 2018-12-28 삼성전자주식회사 소포를 모니터링하기 위한 조성물, 키트 및 이를 이용하여 소포를 모니터링하는 방법
JP6528845B2 (ja) * 2015-07-31 2019-06-12 株式会社村田製作所 アンテナ整合回路、アンテナ回路、フロントエンド回路および通信装置
RU2755206C1 (ru) 2020-05-20 2021-09-14 Федеральное государственное бюджетное учреждение науки Тихоокеанский институт биоорганической химии им. Г.Б. Елякова Дальневосточного отделения Российской академии наук (ТИБОХ ДВО РАН) Средство пролонгированного анальгетического действия и лекарственный препарат на его основе
CN113077942B (zh) * 2021-04-12 2021-12-17 西北工业大学 一种基于功率超声制备智能柔性导电薄膜及其应用
CN120513091A (zh) 2022-10-31 2025-08-19 盐野义制药株式会社 作为trpv1拮抗剂的吡啶衍生物的用途

Family Cites Families (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4409229A (en) 1977-12-02 1983-10-11 Hoechst-Roussel Pharmaceuticals, Inc. Antidepressive and tranquilizing substituted 1,3-dihydrospiro[benzo(c)thiophene]s
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
JPH0680054B2 (ja) 1985-06-19 1994-10-12 吉富製薬株式会社 ピペリジン誘導体
JPS6289679U (me) 1985-11-22 1987-06-08
US4797419A (en) 1986-11-03 1989-01-10 Warner-Lambert Company Method of treating the symptoms of senile cognitive decline employing di- or trisubstituted urea cholinergic agents
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
DE3905364A1 (de) 1989-02-22 1990-08-23 Hoechst Ag Substituierte pyrimidin-derivate, verfahren zu ihrer herstellung und ihre verwendung als tool
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
KR100215627B1 (ko) 1990-06-07 1999-08-16 레슬리 제인 에드워즈 치료용 헤테로사이클 화합물
US5698155A (en) 1991-05-31 1997-12-16 Gs Technologies, Inc. Method for the manufacture of pharmaceutical cellulose capsules
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
JP3191429B2 (ja) 1992-09-02 2001-07-23 富士通テン株式会社 電子機器の挿排装置
NZ254550A (en) 1992-09-28 1997-08-22 Pfizer Use of nitrogen-substituted pyrimidines to prepare medicaments useful for treatment or prevention of diabetic complications
DE4234295A1 (de) 1992-10-12 1994-04-14 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
DE4302051A1 (de) 1993-01-26 1994-07-28 Thomae Gmbh Dr K 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
JP2606138Y2 (ja) 1993-04-20 2000-09-25 株式会社小松製作所 クラッチ作動圧力検出手段を備えたクラッチ油圧制御弁装置
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
DE19514313A1 (de) 1994-08-03 1996-02-08 Bayer Ag Benzoxazolyl- und Benzothiazolyloxazolidinone
WO1996041626A1 (en) 1995-06-12 1996-12-27 G.D. Searle & Co. Compositions comprising a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor
PL193686B1 (pl) 1995-09-07 2007-03-30 Hoffmann La Roche Pochodne piperydyny, środki lecznicze zawierającepochodne piperydyny, sposoby wytwarzania tych pochodnych oraz zastosowanie pochodnych
JP2001526625A (ja) 1995-11-13 2001-12-18 オールバニ メジカル カレッジ 鎮痛性化合物およびその使用
FR2744448B1 (fr) 1996-02-02 1998-04-24 Pf Medicament Nouvelles piperidines derivees d'aryl piperazine, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments
CA2249601A1 (en) 1996-04-03 1997-10-23 Thorsten E. Fisher Inhibitors of farnesyl-protein transferase
US5891889A (en) 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5948786A (en) 1996-04-12 1999-09-07 Sumitomo Pharmaceuticals Company, Limited Piperidinylpyrimidine derivatives
US5990107A (en) 1996-06-28 1999-11-23 Merck & Co., Inc. Fibrinogen receptor antagonist prodrugs
US5854245A (en) 1996-06-28 1998-12-29 Merck & Co., Inc. Fibrinogen receptor antagonists
US5798360A (en) 1996-08-01 1998-08-25 Isis Pharmaceuticals, Inc. N-(aminoalkyl)- and/or N-(amidoalkyl)- dinitrogen heterocyclic compositions
FR2758327B1 (fr) 1997-01-15 1999-04-02 Pf Medicament Nouvelles arylpiperazines derivees de piperidine
FR2758328B1 (fr) 1997-01-15 1999-04-02 Pf Medicament Nouvelles amines aromatiques derivees d'amines cycliques utiles comme medicaments
DE69819345T2 (de) 1997-08-20 2004-07-15 The Regents Of The University Of California, Oakland Für den capsaicin rezeptor kodierende nukleinsäuresequenzen und dem capsaicin rezeptor ähnliche polypeptide und ihre verwendung
JPH11199573A (ja) 1998-01-07 1999-07-27 Yamanouchi Pharmaceut Co Ltd ５ｈｔ３受容体作動薬及び新規ベンゾチアゾール誘導体
DE69934093T2 (de) 1998-01-27 2007-06-21 Aventis Pharmaceuticals Inc. SUBSTITUIERTE OXOAZAHETEROCYCLYL FAKTOR Xa HEMMER
EP0943683A1 (en) 1998-03-10 1999-09-22 Smithkline Beecham Plc Human vanilloid receptor homologue Vanilrep1
JP2002518386A (ja) 1998-06-19 2002-06-25 イーライ・リリー・アンド・カンパニー ヘテロアリール化合物の製造
AU4395399A (en) 1998-07-02 2000-01-24 Sankyo Company Limited Five-membered heteroaryl compounds
PL346795A1 (en) 1998-09-22 2002-02-25 Yamanouchi Pharma Co Ltd Cyanophenyl derivatives
WO2000042852A1 (en) 1999-01-25 2000-07-27 Smithkline Beecham Corporation Compounds and methods
GB9907097D0 (en) 1999-03-26 1999-05-19 Novartis Ag Organic compounds
CA2366858A1 (en) 1999-04-01 2000-10-12 Margaret Yuhua Chu-Moyer Sorbitol dehydrogenase inhibitors
EP1183238A1 (en) 1999-05-17 2002-03-06 Eli Lilly And Company Metabotropic glutamate receptor antagonists
GB9912411D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
DE19934799B4 (de) 1999-07-28 2008-01-24 Az Electronic Materials (Germany) Gmbh Chiral-smektische Flüssigkristallmischung und ihre Verwendung in Aktivmatrix-Displays mit hohen Kontrastwerten
WO2001017965A2 (en) 1999-09-07 2001-03-15 Syngenta Participations Ag Cyanopiperidines as pesticides
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
WO2001057008A1 (en) 2000-02-07 2001-08-09 Abbott Gesellschaft Mit Beschrankter Haftung & Company Kommanditgesellschaft 2-benzothiazolyl urea derivatives and their use as protein kinase inhibitors
NZ522928A (en) 2000-06-21 2005-05-27 F Benzothiazole derivatives
AR028782A1 (es) 2000-07-05 2003-05-21 Taisho Pharmaceutical Co Ltd Derivados heterociclicos tetrahidropiridino o piperidino
KR100849981B1 (ko) 2000-07-13 2008-08-01 메르크 파텐트 게엠베하 키랄 화합물 ｉ
WO2002008221A2 (en) 2000-07-20 2002-01-31 Neurogen Corporation Capsaicin receptor ligands
KR20040025874A (ko) 2000-10-18 2004-03-26 화이자 프로덕츠 인크. 스타틴 및 소르비톨 탈수소효소 억제제의 조합
IL155704A0 (en) 2000-11-30 2003-11-23 Pfizer Prod Inc Combination of gaba agonists and sorbitol dehydrogenase inhibitors
US7193113B2 (en) 2000-12-15 2007-03-20 Japan Science And Technology Corporation Arylbis(perfluoroalkylsulfonyl) methane and metallic salt thereof, and methods for producing the same
US20030232996A1 (en) 2001-04-20 2003-12-18 Brown David L Regioselective synthesis of 3,4-di{(carboclyl or heterocyclyl)thiophenes
DE60229059D1 (de) 2001-05-08 2008-11-06 Univ Yale Proteomimetische verbindungen und verfahren
US20040038982A1 (en) 2001-07-13 2004-02-26 Bondinell William E. Compounds and methods
JP2003095951A (ja) 2001-09-25 2003-04-03 Sumitomo Pharmaceut Co Ltd 慢性関節リウマチ治療剤
JPWO2003029199A1 (ja) 2001-09-28 2005-01-13 武田薬品工業株式会社 ベンゼン誘導体、その製造法および用途
EP1458385A4 (en) 2001-12-19 2005-12-21 Merck & Co Inc METABOTROPIC GLUTAMATE RECEPTOR 5-HETEROARYL-SUBSTITUTED IMIDAZOLE MODULATORS
US7390813B1 (en) 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
US20050119251A1 (en) 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
JP2003192673A (ja) 2001-12-27 2003-07-09 Bayer Ag ピペラジンカルボキシアミド誘導体
DK1472225T3 (da) 2002-02-01 2010-08-09 Euro Celtique Sa 2-Piperazinpyridiner, som er anvendelige til behandling af smerte
AR038420A1 (es) 2002-02-15 2005-01-12 Glaxo Group Ltd Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende
US6974818B2 (en) 2002-03-01 2005-12-13 Euro-Celtique S.A. 1,2,5-thiadiazol-3-YL-piperazine therapeutic agents useful for treating pain
AU2003218737B2 (en) 2002-03-13 2008-04-10 Janssen Pharmaceutica N.V. Inhibitors of histone deacetylase
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
CN1150176C (zh) 2002-05-22 2004-05-19 上海医药工业研究院 芳烷酮哌嗪衍生物及其应用
WO2003099266A2 (en) 2002-05-23 2003-12-04 Abbott Laboratories Acetamides and benzamides that are useful in treating sexual dysfunction
WO2004002531A1 (ja) 2002-06-26 2004-01-08 Ono Pharmaceutical Co., Ltd. 血管の収縮または拡張による疾患治療剤
ES2300613T3 (es) 2002-06-28 2008-06-16 Euro-Celtique S.A. Derivados terapeuticos de piperacina utiles para tratar el dolor.
EP1388538B1 (en) 2002-07-09 2010-09-01 Merck Patent GmbH Polymerisation Initiator
US7262194B2 (en) 2002-07-26 2007-08-28 Euro-Celtique S.A. Therapeutic agents useful for treating pain
WO2004010942A2 (en) 2002-07-31 2004-02-05 Smithkline Beecham Corporation Substituted heterocyclic compounds as modulators of the ccr5 receptor
US7157462B2 (en) 2002-09-24 2007-01-02 Euro-Celtique S.A. Therapeutic agents useful for treating pain
KR101111085B1 (ko) 2002-09-27 2012-04-12 다이닛본 스미토모 세이야꾸 가부시끼가이샤 신규 아데닌 화합물 및 그 용도
AU2003301436A1 (en) 2002-10-17 2004-05-04 Amgen Inc. Benzimidazole derivatives and their use as vanilloid receptor ligands
US7582635B2 (en) 2002-12-24 2009-09-01 Purdue Pharma, L.P. Therapeutic agents useful for treating pain
JP5069905B2 (ja) 2003-01-21 2012-11-07 アプテュイト （ウエスト ラファイエット）、エルエルシー 新規な共結晶化
US7223788B2 (en) 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
DE10311065A1 (de) 2003-03-13 2004-09-23 Abbott Gmbh & Co. Kg Pyrimidin-2-on-Verbindungen und ihre therapeutische Verwendung
ATE556067T1 (de) 2003-05-20 2012-05-15 Ajinomoto Kk Modulatoren des vanilloid rezeptors
MY142655A (en) 2003-06-12 2010-12-15 Euro Celtique Sa Therapeutic agents useful for treating pain
US7129235B2 (en) 2003-07-11 2006-10-31 Abbott Laboratories Amides useful for treating pain
US20050009841A1 (en) 2003-07-11 2005-01-13 Zheng Guo Zhu Novel amides useful for treating pain
EP2080757A1 (en) 2003-07-24 2009-07-22 Euro-Celtique S.A. Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain
BRPI0412808A (pt) 2003-07-24 2006-09-26 Euro Celtique Sa compostos de piperidina e composições farmacêuticas contendo os mesmos
PL1867644T3 (pl) 2003-07-24 2009-10-30 Euro Celtique Sa Związki heteroarylo-tetrahydropiperydylowe przydatne w leczeniu lub zapobieganiu bólu
ES2386354T3 (es) 2003-07-29 2012-08-17 Xenon Pharmaceuticals Inc. Derivados de piridilo y su uso como agentes terapéuticos
JP4782008B2 (ja) 2003-07-30 2011-09-28 ゼノン・ファーマシューティカルズ・インコーポレイテッド ピリジル誘導体および治療剤としてのその用途
US7759348B2 (en) 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7456180B2 (en) 2003-07-30 2008-11-25 Xenon Pharmaceuticals Inc. Piperazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
EP3042895A1 (en) 2003-07-30 2016-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
AU2004261249B2 (en) 2003-07-30 2008-09-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
SI1942106T1 (sl) 2003-08-01 2012-01-31 Euro Celtique Sa Terapevtska sredstva, uporabna za zdravljenje bolečine
US7632950B2 (en) 2003-08-18 2009-12-15 Fujifilm Finechemicals Co., Ltd Pyridyltetrahydropyridines and pyridylpiperidines and method of manufacturing them
DE602004017481D1 (de) 2003-09-22 2008-12-11 Euro Celtique Sa Zur behandlung von schmerzen geeignete therapeutische mittel
PT2017276E (pt) 2003-09-22 2011-04-05 Euro Celtique Sa Compostos de fenilcarboxamida úteis para o tratamento da dor
WO2005037284A1 (en) 2003-10-15 2005-04-28 Pfizer Products Inc. Sorbitol dehydrogenase inhibitor and hypertensive agent combinations
WO2005037845A1 (en) 2003-10-17 2005-04-28 Rigel Pharmaceuticals, Inc. Benzothiazole and thiazole[5,5-b] pyridine compositions and their use as ubiquitin ligase inhibitors
CN1902178A (zh) 2003-12-30 2007-01-24 欧洲凯尔特公司 用于治疗疼痛的哌嗪
US7355045B2 (en) 2004-01-05 2008-04-08 Applera Corporation Isotopically enriched N-substituted piperazine acetic acids and methods for the preparation thereof
DE102004039789A1 (de) 2004-08-16 2006-03-02 Sanofi-Aventis Deutschland Gmbh Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
JP4958786B2 (ja) 2004-09-20 2012-06-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体および治療薬としてのそれらの使用
US20080167321A1 (en) 2004-09-20 2008-07-10 Xenon Pharmaceuticals Inc. Pyridine Derivatives For Inhibiting Human Stearoyl-Coa-Desaturase
EP2269610A3 (en) 2004-09-20 2011-03-09 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP1799667B1 (en) 2004-09-20 2013-03-20 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
BRPI0517622A (pt) * 2004-11-09 2008-10-14 Ciba Sc Holding Ag imidas n-substituìdas como iniciadores de polimerização
US20060116368A1 (en) 2004-11-29 2006-06-01 Calvo Raul R 4-Piperidinecarboxamide modulators of vanilloid VR1 receptor
GT200600046A (es) 2005-02-09 2006-09-25 Terapia de combinacion
MX2007011234A (es) 2005-03-14 2007-11-12 Transtech Pharma Inc Derivados de benzazol, composiciones y metodos de uso en la forma de inhibidores de b-secretasa.
DE102005014904A1 (de) 2005-03-26 2007-02-01 Abbott Gmbh & Co. Kg Substituierte Oxindol-Derivate, diese enthaltende Arzneimittel und deren Verwendung
FR2884516B1 (fr) 2005-04-15 2007-06-22 Cerep Sa Antagonistes npy, preparation et utilisations
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
US8097610B2 (en) 2005-08-26 2012-01-17 Shionogi & Co., Ltd. Derivative having PPAR agonistic activity
WO2007037187A1 (ja) 2005-09-27 2007-04-05 Shionogi & Co., Ltd. Ｐｇｄ２受容体アンタゴニスト活性を有するスルホンアミド誘導体
US20070155707A1 (en) 2005-12-29 2007-07-05 Kadmus Pharmaceuticals, Inc. Ionizable inhibitors of fatty acid amide hydrolase
ATE460404T1 (de) 2006-01-18 2010-03-15 Siena Biotech Spa Modulatoren von alpha7-nikotin-acetylcholin- rezeptoren und therapeutische anwendungen davon
BRPI0708337A2 (pt) 2006-02-28 2011-05-24 Helicon Therapeutics Inc pipirazinas terapêutica como inibidores pde4
WO2007103719A2 (en) 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
TW200815426A (en) 2006-06-28 2008-04-01 Astrazeneca Ab New pyridine analogues II 333
US20080076924A1 (en) 2006-06-30 2008-03-27 Patrick Betschmann Piperazines as P2X7 antagonists
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
JP2010510201A (ja) 2006-11-20 2010-04-02 グレンマーク・ファーマシューティカルズ・エスエー ステアリン酸ＣｏＡ脱飽和酵素阻害剤としてのアセチレン誘導体
DE102006060598A1 (de) 2006-12-21 2008-06-26 Merck Patent Gmbh Tetrahydrobenzoisoxazole
CA2682733A1 (en) 2007-04-13 2008-10-23 Supergen, Inc. Axl kinase inhibitors
EP2604599A1 (en) 2007-04-27 2013-06-19 Purdue Pharma LP TRPV1 antagonists and uses thereof
EP2479173A1 (en) 2007-04-27 2012-07-25 Purdue Pharma LP Therapeutic agents useful for treating pain
US8058299B2 (en) 2007-05-22 2011-11-15 Via Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
WO2008147864A2 (en) 2007-05-22 2008-12-04 Xenon Pharmaceuticals Inc. Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions
KR20100031528A (ko) 2007-06-01 2010-03-22 더 트러스티즈 오브 프린스턴 유니버시티 숙주세포 대사경로의 조절을 통한 바이러스 감염 치료
EP2167074A2 (en) 2007-06-13 2010-03-31 NorthEastern University Antibiotic compounds
WO2009005645A1 (en) 2007-06-28 2009-01-08 Schering Corporation Substituted piperazines as cb1 antagonists
CN103058957A (zh) 2007-06-29 2013-04-24 埃莫里大学 用于神经保护的nmda受体拮抗剂
EP2178866A2 (en) 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
US7998982B2 (en) 2007-08-09 2011-08-16 Abbott Laboratories Amide derivatives as TRPV1 antagonists
US7994174B2 (en) 2007-09-19 2011-08-09 Vertex Pharmaceuticals Incorporated Pyridyl sulfonamides as modulators of ion channels
WO2009045382A1 (en) 2007-10-04 2009-04-09 Merck & Co., Inc. Substituted aryl sulfone derivatives as calcium channel blockers
KR20100102646A (ko) 2007-12-11 2010-09-24 가부시키가이샤 사이토파스파인더 카르복스아미드 화합물 및 케모카인 수용체 길항제로서의 이의 용도
US7935817B2 (en) 2008-03-31 2011-05-03 Apotex Pharmachem Inc. Salt form and cocrystals of adefovir dipivoxil and processes for preparation thereof
JP2009249346A (ja) 2008-04-08 2009-10-29 Fujifilm Corp ピリジン骨格を有する血液脳関門透過性化合物
WO2009155116A2 (en) 2008-05-30 2009-12-23 Georgetown University Methods of reducing pain and inflammation
HRP20120841T4 (hr) 2008-07-21 2015-07-03 Purdue Pharma L.P. Premošteni piperidinski spojevi substituiranog kinoksalin-tipa i njihova uporaba
US8546388B2 (en) 2008-10-24 2013-10-01 Purdue Pharma L.P. Heterocyclic TRPV1 receptor ligands
US8703962B2 (en) 2008-10-24 2014-04-22 Purdue Pharma L.P. Monocyclic compounds and their use as TRPV1 ligands
US8759362B2 (en) 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
WO2010114957A1 (en) 2009-04-03 2010-10-07 Schering Corporation Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders
BR112012030184A2 (pt) 2010-05-27 2015-12-29 Bayer Cropscience Ag derivados de ácido piridinilcarboxílico como fungicidas
JP5876423B2 (ja) 2010-06-22 2016-03-02 塩野義製薬株式会社 Ｔｒｐｖ１阻害活性を有する化合物とその使用
WO2012047764A1 (en) 2010-10-04 2012-04-12 Intermune, Inc. Therapeutic antiviral peptides
CA2813162C (en) 2010-10-20 2015-06-16 Pfizer Inc. Pyridine-2- derivatives as smoothened receptor modulators
US8921372B2 (en) 2010-11-04 2014-12-30 Theravance Biopharma R&D Ip, Llc Inhibitors of hepatitis C virus
UY33817A (es) 2010-12-21 2012-07-31 Boehringer Ingelheim Int ?nuevas oxindolpirimidinas bencílicas?.
US20120202794A1 (en) 2011-01-24 2012-08-09 Pharmasset, Inc. Compounds
CN102336720B (zh) 2011-03-02 2016-01-13 华中科技大学 2-氨基噻唑衍生物及制备方法和应用
WO2012117421A1 (en) 2011-03-02 2012-09-07 Orchid Research Laboratories Ltd Histone deacetylase inhibitors
WO2012158784A2 (en) 2011-05-16 2012-11-22 Theodore Mark Kamenecka Modulators of the nuclear hormone receptor ror
EP2709609B1 (en) 2011-05-17 2017-10-04 Shionogi & Co., Ltd. Heterocyclic compounds
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
US20140155419A1 (en) 2011-07-29 2014-06-05 Erkan Baloglu Compounds and methods
AU2012293417A1 (en) 2011-08-10 2013-05-02 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
WO2013066831A1 (en) 2011-10-31 2013-05-10 Glaxosmithkline Llc Compounds and methods
US8426450B1 (en) 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
US20150011565A1 (en) 2012-01-25 2015-01-08 Spinifex Pharmaceuticals Pty Ltd Heterocyclic Compounds and Methods For Their Use
WO2013142628A2 (en) 2012-03-20 2013-09-26 Fred Hutchinson Cancer Research Center Antibiotic compounds and compositions, and methods for identification thereof
WO2013153539A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. Tricyclic compounds as tec kinase inhibitors
WO2013170113A1 (en) 2012-05-11 2013-11-14 Abbvie Inc. Nampt inhibitors
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents

Also Published As

Publication number Publication date
KR20140022469A (ko) 2014-02-24
CN103717594B (zh) 2016-12-14
SG195136A1 (en) 2013-12-30
EP2723732B1 (en) 2017-01-18
BR112013032658A2 (pt) 2017-11-07
MX2014000344A (es) 2015-09-23
US9630959B2 (en) 2017-04-25
CN105693712A (zh) 2016-06-22
ES2620528T3 (es) 2017-06-28
US10450308B2 (en) 2019-10-22
EP2723732A1 (en) 2014-04-30
TWI453205B (zh) 2014-09-21
LT2723732T (lt) 2017-02-27
US20140329829A1 (en) 2014-11-06
TW201313707A (zh) 2013-04-01
AR086709A1 (es) 2014-01-15
CN103717594A (zh) 2014-04-09
PH12013502412B1 (en) 2022-03-23
IL229817A (en) 2016-04-21
HRP20170507T1 (hr) 2017-06-02
KR101589837B1 (ko) 2016-01-29
SI2723732T1 (sl) 2017-05-31
AU2012273652B2 (en) 2015-09-03
AU2012273652A1 (en) 2013-05-02
PL2723732T3 (pl) 2017-07-31
CL2013003550A1 (es) 2014-11-14
US20200239460A1 (en) 2020-07-30
JP2014520139A (ja) 2014-08-21
US9273043B2 (en) 2016-03-01
US20160222002A1 (en) 2016-08-04
JP5699251B2 (ja) 2015-04-08
EP3173411B1 (en) 2018-05-09
PT2723732T (pt) 2017-02-17
HUE031372T2 (en) 2017-07-28
WO2012176061A1 (en) 2012-12-27
US20170183337A1 (en) 2017-06-29
MY185061A (en) 2021-04-30
MX354015B (es) 2018-02-08
RS55701B1 (sr) 2017-07-31
SG10201605163PA (en) 2016-08-30
DK2723732T3 (en) 2017-04-03
PH12013502412A1 (en) 2014-01-06
ZA201400419B (en) 2015-04-29
SMT201700197T1 (it) 2017-05-08
CA2837178A1 (en) 2012-12-27
CO6852081A2 (es) 2014-01-30
PE20141531A1 (es) 2014-10-23
KR20150055094A (ko) 2015-05-20
CA2837178C (en) 2016-09-20
WO2012176061A9 (en) 2013-03-14
NZ618912A (en) 2015-07-31
WO2012176061A8 (en) 2013-08-08
RU2014101255A (ru) 2015-07-27
RU2621708C2 (ru) 2017-06-07
UA113288C2 (xx) 2017-01-10
EP3173411A1 (en) 2017-05-31
CY1119111T1 (el) 2018-02-14

Similar Documents

Publication Publication Date Title
JP7279057B2 (ja) Ｐｄ１／ｐｄ－ｌ１活性化の阻害剤としてのピリミジン誘導体
EA200901379A1 (ru) Производные никотиновой кислоты как модуляторы метаботропных глутаматных рецепторов 5 подтипа
ES2602972T3 (es) Derivados de indazol para su uso en el tratamiento de infección por virus de la gripe
PE20100256A1 (es) Compuestos de ester boronato y composiciones farmaceuticas de los mismos
HRP20171893T1 (hr) 1h-pirazolo[3,4-b]piridini i njihova terapeutska uporaba
HRP20170507T1 (hr) Trpv1 antagonisti uključujući dihidroksi supstituente i njihove uporabe
AR084222A1 (es) Derivados de amido-piridina como antagonistas del receptor ep4
HRP20160208T4 (hr) Polimorfi dasatiniba i postupak za njihovu pripremu
JP2021511374A (ja) ピリドン誘導体と、その組成物、並びにそれらが抗ウイルス薬物としての応用
EA201201052A1 (ru) Замещенные нафтиридины и их применение в качестве ингибиторов киназы syk
PE20071254A1 (es) Derivados de sulfonamidas como agentes moduladores de los receptores de orexina y su preparacion
HRP20170303T1 (hr) Derivat piridona
MY158648A (en) Compositions for modulating a kinase cascade and methods of use thereof
WO2008115098A3 (fr) 2,3,4,5-tétrahydro-1h-pyrido[4,3-b]indoles substitués ainsi que procédés de leur fabrication et leur utilisation
AR080878A1 (es) Derivados heterociclicos de ariletinilo, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de la esquizofrenia y trastornos cognitivos.
HRP20160462T1 (hr) Derivati 1-benzil-3-hidroksimetilindazola i njihova uporaba u liječenju bolesti baziranih na ekspresiji mcp-1, cx3cr1
GB201110390D0 (en) Compounds for use in stabilising p53 mutants
RU2012140021A (ru) КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 4-{[9-ХЛОР-7-(2-ФТОР-6-МЕТОКСИФЕНИЛ)-5Н-ПИРИМИДО[5,4-d][2]БЕНЗАЗЕПИН-2-ИЛ]АМИНО}-2-МЕТОКСИБЕНЗОАТА НАТРИЯ
AR066421A1 (es) Compuestos derivados de piridona
JP2011510972A5 (me)
DK2966079T1 (da) Pyridopyrimidin eller pyrimidopyrimidinforbindelse, fremstillingsmetode, pharmaceutisk præparat og anvendelse heraf
CN104402831B (zh) 含酰脲结构单元的-5-氰基嘧啶衍生物及其制备方法和用途
Fiorino et al. New 5-HT1A, 5HT2A and 5HT2C receptor ligands containing a picolinic nucleus: Synthesis, in vitro and in vivo pharmacological evaluation
EA200901375A1 (ru) Производные пиридазина, пиридина и пирана в качестве агонистов рецептора gpbar1
MX2012008147A (es) Derivados de pirrazolopiridina.