AR064198A1 - Piperidinilamino piridazinas como antagonistas del receptor de dopamina 2 de rapida disociacion. procesos de obtencion y composiciones farmaceuticas - Google Patents
Piperidinilamino piridazinas como antagonistas del receptor de dopamina 2 de rapida disociacion. procesos de obtencion y composiciones farmaceuticasInfo
- Publication number
- AR064198A1 AR064198A1 ARP070105498A ARP070105498A AR064198A1 AR 064198 A1 AR064198 A1 AR 064198A1 AR P070105498 A ARP070105498 A AR P070105498A AR P070105498 A ARP070105498 A AR P070105498A AR 064198 A1 AR064198 A1 AR 064198A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- halo
- compounds
- processes
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
La presente se refiere a 6-(piperidin-4-ilamino) piridazin-3-carbonitrilos que son antagonistas del receptor de dopamina 2 de rápida disociacion, a procesos para preparar estos compuestos, a composiciones farmacéuticas que comprenden estos compuestos como principio activo. Los compuestos encuentran utilidad como medicamentos para tratar o prevenir trastornos del sistema nervioso central, por ejemplo la esquizofrenia, al ejercer un efecto antipsicotico sin efectos colaterales motores. Reivindicacion 1: Un compuesto de formula (1) o una de sus sales o solvatos aceptables desde el punto de vista farmacéutico, o una de sus (orinas estereoisoméricas, en el cual R es hidrogeno o alquilo C1-6; R1 es fenilo; fenilo sustituido con 1, 2 o 3 sustituyentes seleccionados cada uno en forma independiente del grupo formado por hidrogeno, halo, ciano, alquilo C1-4, alcoxi C1-4, perfluoroalquilo C1-4, y trifluorometoxi; tienilo; tienilo sustituido con 1 o 2 sustituyentes seleccionados del grupo formado por halo y alquilo C1-4; alquilo C1-4; alquilo C1-4 sustituido con hidroxilo, cicloalquilo C3-8 o cicloalquenilo C5-7; cicloalquilo C3-8 o cicloalquenilo C5-7; R2 es hidrogeno o alquilo C1-6; R3 y R4 son cada uno en forma independiente hidrogeno, alquilo C1-4 o halo, o R3 y R4 juntos forman un anillo carbocíclico de 5, 6 o 7 miembros o un anillo heterocíclico de 5, 6 o 7 miembros que comprende por lo menos un átomo de oxigeno, nitrogeno o azufre.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06125685 | 2006-12-08 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR064198A1 true AR064198A1 (es) | 2009-03-18 |
Family
ID=37964744
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070105498A AR064198A1 (es) | 2006-12-08 | 2007-12-07 | Piperidinilamino piridazinas como antagonistas del receptor de dopamina 2 de rapida disociacion. procesos de obtencion y composiciones farmaceuticas |
Country Status (29)
Country | Link |
---|---|
US (1) | US8466153B2 (es) |
EP (1) | EP2091938B1 (es) |
JP (1) | JP5255568B2 (es) |
KR (1) | KR101468384B1 (es) |
CN (1) | CN101547915B (es) |
AR (1) | AR064198A1 (es) |
AT (1) | ATE486070T1 (es) |
AU (1) | AU2007328897B2 (es) |
BR (1) | BRPI0720247A2 (es) |
CA (1) | CA2665924C (es) |
CL (1) | CL2007003556A1 (es) |
CY (1) | CY1112227T1 (es) |
DE (1) | DE602007010179D1 (es) |
DK (1) | DK2091938T3 (es) |
EA (1) | EA016654B1 (es) |
ES (1) | ES2354756T3 (es) |
HK (1) | HK1137434A1 (es) |
IL (1) | IL199076A (es) |
JO (1) | JO2642B1 (es) |
MX (1) | MX2009005983A (es) |
MY (1) | MY148772A (es) |
NO (1) | NO20092574L (es) |
NZ (1) | NZ576484A (es) |
PL (1) | PL2091938T3 (es) |
PT (1) | PT2091938E (es) |
SI (1) | SI2091938T1 (es) |
TW (1) | TWI433676B (es) |
UA (1) | UA98940C2 (es) |
WO (1) | WO2008068277A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JO2769B1 (en) | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
JO2849B1 (en) * | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
WO2008128996A1 (en) * | 2007-04-23 | 2008-10-30 | Janssen Pharmaceutica N.V. | Thia(dia)zoles as fast dissociating dopamine 2 receptor antagonists |
KR20100016498A (ko) * | 2007-04-23 | 2010-02-12 | 얀센 파마슈티카 엔.브이. | 속해리성 도파민 2 수용체 길항제로서의 피리딘 유도체 |
JP5431305B2 (ja) * | 2007-04-23 | 2014-03-05 | 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 | 高速解離性ドパミン2受容体アンタゴニストとしての4−アルコキシピリダジン誘導体 |
CA2729313C (en) * | 2008-07-03 | 2016-08-30 | Janssen Pharmaceutica Nv | Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists |
EP2307374B1 (en) * | 2008-07-31 | 2017-01-25 | Janssen Pharmaceutica NV | Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists |
Family Cites Families (37)
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DE2341965C3 (de) | 1973-08-20 | 1979-01-25 | C.H. Boehringer Sohn, 6507 Ingelheim | 4- [N- (o-PyridyD- N-acyl] -aminolphenäthylpiperidine, Verfahren zu deren Herstellung sowie deren Verwendung bei der Bekämpfung von Schmerzzuständen |
US4197304A (en) | 1975-09-23 | 1980-04-08 | Janssen Pharmaceutica N.V. | N-Aryl-N-(1-L-4-piperidinyl)-arylacetamides |
NO147672C (no) | 1975-09-23 | 1983-05-25 | Janssen Pharmaceutica Nv | Analogifremgangsmaate for fremstilling av n-aryl-n-(1-l1-4-piperidinyl)-arylacetamider |
EG12406A (en) | 1976-08-12 | 1979-03-31 | Janssen Pharmaceutica Nv | Process for preparing of novel n-aryl-n-(1-l-4-piperidinyl)-arylacetamides |
DE3218482A1 (de) | 1982-05-15 | 1983-11-17 | Bayer Ag, 5090 Leverkusen | Substituierte 5-trifluormethyl-1,3,4-thiadiazol-2-yloxyessigsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
MX173362B (es) | 1987-03-02 | 1994-02-23 | Pfizer | Compuestos de piperazinil heterociclicos y procedimiento para su preparacion |
GB9216298D0 (en) | 1991-08-15 | 1992-09-16 | Ici Plc | Piperidine derivatives |
TW406075B (en) | 1994-12-13 | 2000-09-21 | Upjohn Co | Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds |
US5753679A (en) | 1995-05-10 | 1998-05-19 | Hoffmann-La Roche Inc. | Benzyl-piperidine derivatives |
MY116093A (en) | 1996-02-26 | 2003-11-28 | Upjohn Co | Azolyl piperazinyl phenyl oxazolidinone antimicrobials |
TW504510B (en) * | 1996-05-10 | 2002-10-01 | Janssen Pharmaceutica Nv | 2,4-diaminopyrimidine derivatives |
ID23803A (id) * | 1997-08-15 | 2000-05-11 | Pfizer Prod Inc | Turunan-turunan 2-(4-aril atau heteroaril-piperazin-1-ilmetil)-1h-indola |
KR100261139B1 (ko) | 1998-01-16 | 2000-08-01 | 황준수 | 신규한 알릴티오피리다진 유도체 및 그의 제조방법 |
AR028948A1 (es) | 2000-06-20 | 2003-05-28 | Astrazeneca Ab | Compuestos novedosos |
US7217716B2 (en) | 2001-02-23 | 2007-05-15 | Merck & Co., Inc. | N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists |
JP4009251B2 (ja) | 2001-10-09 | 2007-11-14 | 杏林製薬株式会社 | 新規な4−(2−フロイル)アミノピペリジン、その合成中間体、その製造方法および医薬としてのその用途 |
AU2002360561A1 (en) | 2001-12-11 | 2003-06-23 | Sepracor, Inc. | 4-substituted piperidines, and methods of use thereof |
EP1467981A1 (en) | 2002-01-25 | 2004-10-20 | Kylix Pharmaceuticals B.V. | 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2 |
CA2474214A1 (en) | 2002-02-05 | 2003-08-14 | Novo Nordisk A/S | Novel aryl- and heteroarylpiperazines |
AU2003211385A1 (en) | 2002-02-28 | 2003-09-09 | Takeda Chemical Industries, Ltd. | Azole compounds |
SE0201544D0 (sv) | 2002-05-17 | 2002-05-17 | Biovitrum Ab | Novel compounds and thier use |
WO2004028520A1 (ja) | 2002-09-26 | 2004-04-08 | Mandom Corporation | 防腐殺菌剤並びに該防腐殺菌剤を配合した化粧料、医薬品及び食品 |
US7601843B2 (en) | 2003-05-08 | 2009-10-13 | Kyorin Pharmaceutical Co., Ltd | 4-(2-furoyl)aminopiperidine compound useful as therapeutic agent for itching |
WO2005005779A2 (en) | 2003-07-14 | 2005-01-20 | Genesis Mining Technologies (Pty) Ltd | Dual retention cutting arrangement |
JP4680903B2 (ja) | 2003-07-29 | 2011-05-11 | ハイ・ポイント・ファーマスーティカルズ、エルエルシー | ピリダジニル−ピペラジンおよびそれらのヒスタミンh3受容体リガンドとしての使用 |
JP2007501801A (ja) | 2003-08-07 | 2007-02-01 | 日本たばこ産業株式会社 | ピロロ[1,2−b]ピリダジン誘導体 |
EP1742932A1 (en) | 2004-04-28 | 2007-01-17 | Pfizer Limited | 3-heterocyclyl-4-phenyl-triazole derivatives as inhibitors of the vasopressin v1a receptor |
US7820817B2 (en) | 2004-05-28 | 2010-10-26 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
WO2006034440A2 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
DK1805158T3 (en) | 2004-10-29 | 2018-08-06 | Kalypsys Inc | SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR |
JP2008546784A (ja) | 2005-06-20 | 2008-12-25 | シェーリング コーポレイション | ヒスタミンh3アンタゴニストとして有用なピペリジン誘導体 |
JO2769B1 (en) * | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
WO2007130383A2 (en) | 2006-04-28 | 2007-11-15 | Northwestern University | Compositions and treatments using pyridazine compounds and secretases |
BRPI0715967A2 (pt) | 2006-08-15 | 2013-08-06 | Hoffmann La Roche | compostos, processo para a sua manufatura, composiÇÕes farmacÊuticas que os compreendem, mÉtodos para o tratamento e/ou prevenÇço de enfermidades que estço associadas com a modulaÇço de receptores de sst do subtipo 5, e uso destes compostos |
US8058243B2 (en) | 2006-10-13 | 2011-11-15 | Hsc Research And Development Limited Partnership | Method for treating a brain cancer with ifenprodil |
JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
EP2307374B1 (en) | 2008-07-31 | 2017-01-25 | Janssen Pharmaceutica NV | Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists |
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2007
- 2007-11-19 JO JO2007479A patent/JO2642B1/en active
- 2007-12-05 BR BRPI0720247-4A patent/BRPI0720247A2/pt active Search and Examination
- 2007-12-05 MY MYPI20092235A patent/MY148772A/en unknown
- 2007-12-05 ES ES07847833T patent/ES2354756T3/es active Active
- 2007-12-05 AT AT07847833T patent/ATE486070T1/de active
- 2007-12-05 NZ NZ576484A patent/NZ576484A/en not_active IP Right Cessation
- 2007-12-05 AU AU2007328897A patent/AU2007328897B2/en not_active Ceased
- 2007-12-05 CA CA2665924A patent/CA2665924C/en active Active
- 2007-12-05 PT PT07847833T patent/PT2091938E/pt unknown
- 2007-12-05 WO PCT/EP2007/063338 patent/WO2008068277A1/en active Application Filing
- 2007-12-05 JP JP2009539743A patent/JP5255568B2/ja active Active
- 2007-12-05 MX MX2009005983A patent/MX2009005983A/es active IP Right Grant
- 2007-12-05 SI SI200730472T patent/SI2091938T1/sl unknown
- 2007-12-05 EP EP07847833A patent/EP2091938B1/en active Active
- 2007-12-05 UA UAA200903503A patent/UA98940C2/ru unknown
- 2007-12-05 PL PL07847833T patent/PL2091938T3/pl unknown
- 2007-12-05 US US12/516,645 patent/US8466153B2/en active Active
- 2007-12-05 DK DK07847833.6T patent/DK2091938T3/da active
- 2007-12-05 KR KR1020097010872A patent/KR101468384B1/ko active IP Right Grant
- 2007-12-05 CN CN2007800446538A patent/CN101547915B/zh active Active
- 2007-12-05 EA EA200970553A patent/EA016654B1/ru not_active IP Right Cessation
- 2007-12-05 DE DE602007010179T patent/DE602007010179D1/de active Active
- 2007-12-07 AR ARP070105498A patent/AR064198A1/es unknown
- 2007-12-07 TW TW096146645A patent/TWI433676B/zh not_active IP Right Cessation
- 2007-12-07 CL CL200703556A patent/CL2007003556A1/es unknown
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2009
- 2009-06-02 IL IL199076A patent/IL199076A/en active IP Right Grant
- 2009-07-07 NO NO20092574A patent/NO20092574L/no not_active Application Discontinuation
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2010
- 2010-02-02 HK HK10101123.6A patent/HK1137434A1/xx not_active IP Right Cessation
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2011
- 2011-01-27 CY CY20111100088T patent/CY1112227T1/el unknown
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