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RU2008110949A - Соединения и композиции-иммуносупрессанты - Google Patents

Соединения и композиции-иммуносупрессанты Download PDF

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Publication number
RU2008110949A
RU2008110949A RU2008110949/04A RU2008110949A RU2008110949A RU 2008110949 A RU2008110949 A RU 2008110949A RU 2008110949/04 A RU2008110949/04 A RU 2008110949/04A RU 2008110949 A RU2008110949 A RU 2008110949A RU 2008110949 A RU2008110949 A RU 2008110949A
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RU
Russia
Prior art keywords
trifluoromethylbiphenyl
phenyl
yloxymethyl
fluoro
alkyl
Prior art date
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RU2008110949/04A
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English (en)
Inventor
Вэньци ГАО (US)
Вэньци Гао
Еньцинь ВАНЬ (US)
Еньцинь ВАНЬ
Цзицин ЦЗЯН (US)
Цзицин Цзян
И Фань (Us)
И Фань
Натанаэл С. ГРЕЙ (US)
Натанаэл С. Грей
Шифэн ПАНЬ (US)
Шифэн Пань
Original Assignee
Айрм Ллк (Bm)
Айрм Ллк
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Application filed by Айрм Ллк (Bm), Айрм Ллк filed Critical Айрм Ллк (Bm)
Publication of RU2008110949A publication Critical patent/RU2008110949A/ru

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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
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  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

1. Соединение, выбранное из формул Ia, Ib, Ic и Id ! ! ! в которых А выбирают из групп циано, -X1C(O)OR3, -X1OP(O)(OR3)2, -X1P(O)(OR3)2, ! -X1P(O)OR3, -X1S(O)2OR3, -X1P(O)(R3)OR3, -X1C(O)NR3R3, -X1C(O)NR3X1OR3, ! -X1C(O)NR3X1C(O)OR3, -X1C(O)X1C(O)OR3 и 1Н-тетразол-5-ил, где каждый X1 независимо выбирают из связи, C1-С3алкилена и С2-С3алкенилена, а каждый R3 независимо выбирают из водорода и C1-С6алкила; где R3 и водород алкена X1 в любой компоненте NR3X1 в А может образовывать циклическую группу; ! В выбирают из CR4=CR5-, -CR4=N-, -N=CR4-, -S- и -NR4-; где R4 и R5 независимо выбирают из водорода, галоида и C1-С6алкила; ! С выбирают из =CR4- и =N-; где R4 выбирают из водорода, галоида и C1-С6алкила; ! L выбирают из Х2OХ3-, -X2NR3X3-, -X2C(O)NR3X3-, -X2NR3C(O)X3- и -Х2S(O)0-2Х3-; где каждый Х2 и Х3 независимо выбирают из связи, C1-С3алкилена и С2-С3алкенилена, а R3 выбирают из водорода и C1-С6алкила; ! Y выбирают из связи, O-, -S-, -S(O)-, -S(O)2-, -NR3-, метилена и этилена; R3 выбирают из водорода и C1-С6алкила; ! n выбирают из 0, 1, 2 и 3; ! R1 выбирают из С6-С10арила и C1-С10гетероарила; при этом любой арил или гетероарил R1 необязательно замещен радикалом, выбранным из С6-С10арилС0-С4алкила, С5-С6гетероарилС0-С4алкила, С3-С8циклоалкилС0-С4алкила, С3-С8гетероциклоалкилС0-С4алкила и C1-С10алкила; где любая арильная, гетероарильная, циклоалкильная или гетероциклоалкильная группа R1 или заместителя R1 может быть необязательно замещена 1-5 радикалами, независимо выбранными из галоида, C1-С10алкила, C1-С10алкокси, галоидзамещенного С1-С10алкила и галоидзамещенной C1-С10алкокси; и любая алкильная группа R1 может необязательно иметь метиленовый фрагмент, замененный на атом или группу, выбранную из S(O)0-2-, -NR3- и -O-; где R3 выбирают из водорода и C1-С10алкила; ! R2 выбирают из галоида, циано, нитро, C1-С6алкокси и C1-С6алкила; ! и фенильное кольцо в фор�

Claims (9)

1. Соединение, выбранное из формул Ia, Ib, Ic и Id
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
в которых А выбирают из групп циано, -X1C(O)OR3, -X1OP(O)(OR3)2, -X1P(O)(OR3)2,
-X1P(O)OR3, -X1S(O)2OR3, -X1P(O)(R3)OR3, -X1C(O)NR3R3, -X1C(O)NR3X1OR3,
-X1C(O)NR3X1C(O)OR3, -X1C(O)X1C(O)OR3 и 1Н-тетразол-5-ил, где каждый X1 независимо выбирают из связи, C1-С3алкилена и С2-С3алкенилена, а каждый R3 независимо выбирают из водорода и C1-С6алкила; где R3 и водород алкена X1 в любой компоненте NR3X1 в А может образовывать циклическую группу;
В выбирают из CR4=CR5-, -CR4=N-, -N=CR4-, -S- и -NR4-; где R4 и R5 независимо выбирают из водорода, галоида и C1-С6алкила;
С выбирают из =CR4- и =N-; где R4 выбирают из водорода, галоида и C1-С6алкила;
L выбирают из Х2OХ3-, -X2NR3X3-, -X2C(O)NR3X3-, -X2NR3C(O)X3- и -Х2S(O)0-2Х3-; где каждый Х2 и Х3 независимо выбирают из связи, C1-С3алкилена и С2-С3алкенилена, а R3 выбирают из водорода и C1-С6алкила;
Y выбирают из связи, O-, -S-, -S(O)-, -S(O)2-, -NR3-, метилена и этилена; R3 выбирают из водорода и C1-С6алкила;
n выбирают из 0, 1, 2 и 3;
R1 выбирают из С6-С10арила и C1-С10гетероарила; при этом любой арил или гетероарил R1 необязательно замещен радикалом, выбранным из С6-С10арилС0-С4алкила, С5-С6гетероарилС0-С4алкила, С3-С8циклоалкилС0-С4алкила, С3-С8гетероциклоалкилС0-С4алкила и C1-С10алкила; где любая арильная, гетероарильная, циклоалкильная или гетероциклоалкильная группа R1 или заместителя R1 может быть необязательно замещена 1-5 радикалами, независимо выбранными из галоида, C1-С10алкила, C1-С10алкокси, галоидзамещенного С1-С10алкила и галоидзамещенной C1-С10алкокси; и любая алкильная группа R1 может необязательно иметь метиленовый фрагмент, замененный на атом или группу, выбранную из S(O)0-2-, -NR3- и -O-; где R3 выбирают из водорода и C1-С10алкила;
R2 выбирают из галоида, циано, нитро, C1-С6алкокси и C1-С6алкила;
и фенильное кольцо в формулах Iа и Ib может необязательно иметь до трех групп =С, замененных на азот;
а также их фармацевтически приемлемые соли.
2. Соединение по п.1, в котором:
А выбирают из групп циано, -X1C(O)OR3, -X1OP(O)(OR3)2, -X1P(O)(OR3)2, -X1P(O)OR3, -X1S(O)2OR3, -X1P(O)(R3)OR3, -X1C(O)NR3R3, -X1C(O)NR3X1OR3,
-X1C(O)NR3X1C(O)OR3, -X1C(O)X1C(O)OR3 и 1H-тетразол-5-ил; где каждый X1 независимо выбирают из связи, C1-С6алкилена и С2-С3алкенилена, а каждый R3 независимо выбирают из водорода и C1-Сбалкила; при этом R3 и алкиленовый водород X1 в любой компоненте NR3X1 в А может образовывать циклическую группу;
n выбирают из 0 и 1;
R1 выбирают из С6-С10арила и C1-С10гетероарила; где любой арил или гетероарил
R1 может быть необязательно замещен радикалом, выбранным из С6-С10арилС0-С4алкила, С5-С6гетероарилС0-С4алкила, С3-С8циклоалкилС0-C4алкила,
С3-С8гетероциклоалкилС0-С4алкила и C1-С10алкила; при этом любая арильная, гетероарильная, циклоалкильная или гетероциклоалкильная группа R1 или заместителя R1 может быть необязательно замещена 1-5 радикалами, независимо выбранными из галоида, C1-С10алкила, C1-С10алкокси, галозамещенного C1-С10алкила и галозамещенной C1-С10алкокси; и любая алкильная группа R1 может необязательно иметь метиленовый фрагмент, замененный на атом или группу, выбранную из -S(O)0-2-, -NR3- и -O-; где R3 выбирают из водорода и C1-С6алкила; и
R2 выбирают из галоида и C1-С6алкила.
3. Соединение по п.2, в котором А выбирают из циано, -СООН, -СН2С(O)ОН,
-(СН2)2С(O)ОН, -C(O)NH2, -C(O)NH(CH2)2OH, -C(O)NH(CH2)3OH,
C(O)NH(CH2)2C(O)OH, -C(O)(CH2)2C(O)OH, 3-гидроксиазетидин-1-карбонила и тетразолила.
4. Соединение по п.3, в котором R1 означает фенил, необязательно замещенный 1-2 радикалами, независимо выбранными из галоида, метила, трифторметила, тиазолила и фенила, необязательно замещенного галоидом или метилом; и R2 означает галоид.
5. Соединение по п.4, выбранное из
5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты;
5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты;
2-[4-(3'-метил-2-трифторметилбифенил-4-илоксиметил)фенил]-1Н-имидазол-4-карбоновой кислоты;
{5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-3-ил}уксусной кислоты;
5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]-2-(1Н-тетразол-5-ил)пиридина;
амида 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]-1Н-имидазол-2-карбоновой кислоты; 5-[4-(3'-метил-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[2-хлор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]никотиновой кислоты; 5-[2-фтор-4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[2-фтор-4-(4-тиазол-2-ил-3-трифторметилфеноксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2-трифторметилбифенил-4-илметокси)фенил]пиридин-2-карбоновой кислоты; 5-[4-(4-циклогексил-3-трифторметилфеноксиметил)-2-фторфенил]пиридин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбонитрила; 5-[2-хлор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]-1-оксипиридин-2-карбоновой кислоты; 4-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; {6-[4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-3-ил}уксусной кислоты; 3-{5-[4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-ил}пропионовой кислоты; 3-{5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-ил}пропионовой кислоты; 3-{5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-ил}пропионовой кислоты; 3-{5-[2-хлор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-ил}пропионовой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)-2-метилфенил]пиридин-2-карбоновой кислоты; 5-[3-фтор-4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[3-хлор-4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)-3-нитрофенил]пиридин-2-карбоновой кислоты; 3-фтор-5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 3-бром-5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенокси]пиридин-2-карбоновой кислоты; 4-(4-октилоксифенил)пиридин-2-карбоновой кислоты; 3-[4-(4-октилоксифенил)пиридин-2-ил]пропионовой кислоты; 3-(5-{2-[4-(5-фенилпентилокси)фенил]этил}пиридин-2-ил)пропионовой кислоты; 3-{4-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиразол-1-ил}пропионовой кислоты; {4-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиразол-1-ил}уксусной кислоты; {4-[4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиразол-1-ил}уксусной кислоты; {4-[2-фтор-4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиразол-1-ил}уксусной кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]тиазол-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиримидин-2-карбоновой кислоты; 5-[4-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиразин-2-карбоновой кислоты; 5-[3-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 4-[3-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 6-[3-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 5-[3-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]никотиновой кислоты; 5-[3-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-3-ил}уксусной кислоты; (2-гидроксиэтил)амида 5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; (3-гидроксипропил)амида 5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбоновой кислоты; 3-({5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-карбонил}амино)пропионовой кислоты; {5-[2-фтор-4-(2-трифторметилбифенил-4-илоксиметил)фенил]пиридин-2-ил}-(3-гидроксиазетидин-1-ил)метанона; 5-[2-(2-трифторметилбифенил-4-ил)бензоксазол-6-ил]пиридин-2-карбоновой кислоты; и 4-[5-(2'-фтор-2-трифторметилбифенил-4-илоксиметил)индол-1-ил]-4-оксомасляной кислоты.
6. Фармацевтическая композиция, включающая терапевтически эффективное количество соединения по п.1 в комбинации с фармацевтически приемлемым наполнителем.
7. Способ лечения заболевания у животного, при котором изменение сигнальной трансдукции, опосредованной EDG/S1P рецептором, может предотвращать, ингибировать или уменьшать патологию и/или симптоматику заболевания; данный способ включает введение животному терапевтически эффективного количества соединения по п.1.
8. Способ профилактики или лечения нарушений или заболеваний, опосредованных лимфоцитами, лечения острого или хронического отторжения трансплантата или опосредованных Т-клетками воспалительных или аутоиммунных заболеваний, ингибирования или контролирования нерегулируемого ангиогенеза или лечения заболеваний, опосредованных процессом неоангиогенеза или связанных с нерегулируемым ангиогенезом у субъекта, включающий введение субъекту в случае нужды эффективного количества соединения по п.1 или его фармацевтически приемлемой соли.
9. Применение соединения по п.1 в получении лекарства для лечения заболевания у животного, при котором альтерация сигнальной трансдукции, опосредованной EDG/S1P рецептором, вносит вклад в патологию и/или симптоматику заболевания.
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