EA200100806A1 - DERIVATIVES ALKINYL-CONTAINING HYDROXAMIC ACIDS, METHODS FOR THEIR RECOVERY AND APPLICATION OF SPECIFIED SUBSTANCES AS MATRIX METAL PROTEINASE INHIBITORS (MMP) AND FNO-ALPHA, the CFO-FRSHFREPTROF-FRTHTTLE; - Google Patents
DERIVATIVES ALKINYL-CONTAINING HYDROXAMIC ACIDS, METHODS FOR THEIR RECOVERY AND APPLICATION OF SPECIFIED SUBSTANCES AS MATRIX METAL PROTEINASE INHIBITORS (MMP) AND FNO-ALPHA, the CFO-FRSHFREPTROF-FRTHTTLE;Info
- Publication number
- EA200100806A1 EA200100806A1 EA200100806A EA200100806A EA200100806A1 EA 200100806 A1 EA200100806 A1 EA 200100806A1 EA 200100806 A EA200100806 A EA 200100806A EA 200100806 A EA200100806 A EA 200100806A EA 200100806 A1 EA200100806 A1 EA 200100806A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- carbon atoms
- atoms
- heteroaryl
- aryl
- alkyl
- Prior art date
Links
- NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical class C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 title 1
- 229940019748 antifibrinolytic proteinase inhibitors Drugs 0.000 title 1
- 239000011159 matrix material Substances 0.000 title 1
- 239000002184 metal Substances 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 238000011084 recovery Methods 0.000 title 1
- 239000000126 substance Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 12
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000004429 atom Chemical group 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 abstract 2
- 208000020084 Bone disease Diseases 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 102000004877 Insulin Human genes 0.000 abstract 1
- 108090001061 Insulin Proteins 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000025865 Ulcer Diseases 0.000 abstract 1
- 206010052428 Wound Diseases 0.000 abstract 1
- 208000027418 Wounds and injury Diseases 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 229940125396 insulin Drugs 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 201000001245 periodontitis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 210000001519 tissue Anatomy 0.000 abstract 1
- 230000036269 ulceration Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/60—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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
- C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrane Compounds (AREA)
Abstract
Соединения формулы (I), где Rозначает водород, арил, гетероарил, алкил с 1-8 атомами углерода, алкенил с 2-6 атомами углерода, алкинил с 2-6 атомами углерода, циклоалкил с 3-6 атомами углерода или -С-С-циклогетероалкил; Rи Rозначают водород, алкил с 1-6 атомами углерода, -CN или -ССН; R, R, Rи Rнезависимо означают водород, арил или гетероарил, циклоалкил с 3-6 атомами углерода, -С-С-циклогетероалкил, алкил с 1-18 атомами углерода, алкенил с 2-18 атомами углерода, алкинил с 2-18 атомами углерода; при условии, что одна из пар Rи R, Rи Rили Rи Rвместе с атомом углерода или атомами, к которым они присоединены, образуют циклоалкильное кольцо, содержащее 3-6 атомов углерода, или -С-С-циклогетероалкильное кольцо; Rозначает водород, арил или гетероарил, циклоалкил с 3-6 атомами углерода, -С-С-циклогетероалкил или алкил с 1-6 атомами углерода; А и Х означают О, S, SO, SO, NRили СН; Y означает арил или гетероарил при условии, что А и Х не присоединены к смежным атомам Y; и n равно 0-2; или их фармацевтически приемлемые соли, которые пригодны для лечения артрита, опухолевых метастазов, изъязвления тканей, патологических ран, периодонтита, заболевания костей, диабета (инсулинрезистентного) и ВИЧ-инфицирования.Международная заявка была опубликована вместе с отчетом о международном поиске.Compounds of formula (I) where R 2 is hydrogen, aryl, heteroaryl, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, alkynyl with 2-6 carbon atoms, cycloalkyl with 3-6 carbon atoms or -C — C -cycloheteroalkyl; R5 and R4 are hydrogen, alkyl with 1-6 carbon atoms, -CN or -CCH; R, R, R and R independently are hydrogen, aryl or heteroaryl, cycloalkyl with 3-6 carbon atoms, -C-C-cycloheteroalkyl, alkyl with 1-18 carbon atoms, alkenyl with 2-18 carbon atoms, alkynyl with 2-18 atoms carbon; with the proviso that one of the pairs R1 and R1, R1 and R8 or R1 and R4 together with the carbon atom or atoms to which they are attached form a cycloalkyl ring containing 3-6 carbon atoms, or a —C — C-cycloheteroalkyl ring; Rz is hydrogen, aryl or heteroaryl, cycloalkyl with 3-6 carbon atoms, -C-C-cycloheteroalkyl or alkyl with 1-6 carbon atoms; A and X mean O, S, SO, SO, NR or CH; Y is aryl or heteroaryl, with the proviso that A and X are not attached to adjacent Y atoms; and n is 0-2; or their pharmaceutically acceptable salts, which are suitable for the treatment of arthritis, tumor metastases, tissue ulceration, pathological wounds, periodontitis, bone diseases, diabetes (insulin-resistant) and HIV infection. The international application was published along with an international search report.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23803899A | 1999-01-27 | 1999-01-27 | |
| PCT/US2000/001864 WO2000044723A1 (en) | 1999-01-27 | 2000-01-27 | Alkynyl containing hydroxamic acid derivatives, their preparation and their use as matrix metalloproteinase (mmp) inhibitors/tnf-alpha converting enzyme (tace) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA200100806A1 true EA200100806A1 (en) | 2002-08-29 |
Family
ID=22896246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200100806A EA200100806A1 (en) | 1999-01-27 | 2000-01-27 | DERIVATIVES ALKINYL-CONTAINING HYDROXAMIC ACIDS, METHODS FOR THEIR RECOVERY AND APPLICATION OF SPECIFIED SUBSTANCES AS MATRIX METAL PROTEINASE INHIBITORS (MMP) AND FNO-ALPHA, the CFO-FRSHFREPTROF-FRTHTTLE; |
Country Status (13)
| Country | Link |
|---|---|
| JP (1) | JP2002535390A (en) |
| KR (1) | KR20010101732A (en) |
| AR (1) | AR035312A1 (en) |
| AT (1) | ATE309986T1 (en) |
| AU (1) | AU769418B2 (en) |
| CA (1) | CA2356313A1 (en) |
| CZ (1) | CZ20012711A3 (en) |
| DE (1) | DE60024056D1 (en) |
| EA (1) | EA200100806A1 (en) |
| HU (1) | HUP0200223A3 (en) |
| IL (1) | IL144345A0 (en) |
| NZ (1) | NZ512566A (en) |
| ZA (1) | ZA200105222B (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4566006B2 (en) * | 2002-12-26 | 2010-10-20 | カルナバイオサイエンス株式会社 | Alkynyl-substituted azasugar derivatives and drugs containing the same as active ingredients |
| JP2009542666A (en) * | 2006-06-30 | 2009-12-03 | シェーリング コーポレイション | Substituted piperidines that increase P53 activity and uses thereof |
| NZ589492A (en) * | 2008-06-02 | 2012-06-29 | Cipla Ltd | Processes for the synthesis of levocetirizine and intermediates for use therein |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| YU40999A (en) * | 1997-02-27 | 2002-06-19 | American Cyanamid Company | N-hydroxy-2-(alkyl,aryl,or heteroaryl sulfanyl,sulfinyl or sulfonyl)-3-substituted alkyl,aryl or heteroarylamides as matrix metalloproteinase inhibitors |
| PL342548A1 (en) * | 1998-02-19 | 2001-06-18 | American Cyanamid Co | N-hydroxy-2-(alkyl-, aryl- or heteroarylsulphanyl-, sulphinyl- or sulphonyl)-3-substituted alkyl-, aryl- or heteroarylamides as inhibitors of matrix metaloproteinases |
-
2000
- 2000-01-26 AR ARP000100327A patent/AR035312A1/en not_active Application Discontinuation
- 2000-01-27 AT AT00904569T patent/ATE309986T1/en not_active IP Right Cessation
- 2000-01-27 DE DE60024056T patent/DE60024056D1/en not_active Expired - Lifetime
- 2000-01-27 NZ NZ512566A patent/NZ512566A/en unknown
- 2000-01-27 KR KR1020017009432A patent/KR20010101732A/en not_active Application Discontinuation
- 2000-01-27 CA CA002356313A patent/CA2356313A1/en not_active Abandoned
- 2000-01-27 AU AU26305/00A patent/AU769418B2/en not_active Ceased
- 2000-01-27 CZ CZ20012711A patent/CZ20012711A3/en unknown
- 2000-01-27 JP JP2000595979A patent/JP2002535390A/en active Pending
- 2000-01-27 EA EA200100806A patent/EA200100806A1/en unknown
- 2000-01-27 HU HU0200223A patent/HUP0200223A3/en unknown
- 2000-01-27 IL IL14434500A patent/IL144345A0/en unknown
-
2001
- 2001-06-25 ZA ZA200105222A patent/ZA200105222B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CZ20012711A3 (en) | 2002-05-15 |
| JP2002535390A (en) | 2002-10-22 |
| HUP0200223A3 (en) | 2002-12-28 |
| KR20010101732A (en) | 2001-11-14 |
| CA2356313A1 (en) | 2000-08-03 |
| IL144345A0 (en) | 2002-05-23 |
| ZA200105222B (en) | 2002-09-25 |
| HUP0200223A2 (en) | 2002-06-29 |
| AR035312A1 (en) | 2004-05-12 |
| NZ512566A (en) | 2004-02-27 |
| ATE309986T1 (en) | 2005-12-15 |
| AU2630500A (en) | 2000-08-18 |
| DE60024056D1 (en) | 2005-12-22 |
| AU769418B2 (en) | 2004-01-29 |
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